CA1196865A - Lubricating suppository and method for making and using same - Google Patents
Lubricating suppository and method for making and using sameInfo
- Publication number
- CA1196865A CA1196865A CA000410297A CA410297A CA1196865A CA 1196865 A CA1196865 A CA 1196865A CA 000410297 A CA000410297 A CA 000410297A CA 410297 A CA410297 A CA 410297A CA 1196865 A CA1196865 A CA 1196865A
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- suppository
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- polyoxyethylene
- melt
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Abstract
Abstract of the Disclosure The disclosed lubricating suppository is formulated to have properties advantageous for coital use, including extraordinary water washability.
The ingredients and phase relationships of the suppository composition provide a high degree of compatibility with water and with naturally-occurring vaginal moisture. The suppository composition contains a glyceride lubricant and can be lubricious with or without the presence of moisture, The suppository, which is solid at room temperature but melts in a short time at body temperature, is made by dissolving, for example, 10-30 parts by weight of high-HLB (e.g.
> 14) nonionic surfactant in 50-70 parts by weight of a molten, water-soluble polyoxyethylene glycol component and by dispersing or emulsifying 10-20 parts by weight of the glyceride (e.g. a triglyceride of C6-C18 aliphatic carboxylic acids) included in the composition. In use, the suppository can be inserted prior to coitus and permitted to melt to a liquid, which is lubricious even in the absence of moisture, but still has the aforementioned extraordinary water washability.
The ingredients and phase relationships of the suppository composition provide a high degree of compatibility with water and with naturally-occurring vaginal moisture. The suppository composition contains a glyceride lubricant and can be lubricious with or without the presence of moisture, The suppository, which is solid at room temperature but melts in a short time at body temperature, is made by dissolving, for example, 10-30 parts by weight of high-HLB (e.g.
> 14) nonionic surfactant in 50-70 parts by weight of a molten, water-soluble polyoxyethylene glycol component and by dispersing or emulsifying 10-20 parts by weight of the glyceride (e.g. a triglyceride of C6-C18 aliphatic carboxylic acids) included in the composition. In use, the suppository can be inserted prior to coitus and permitted to melt to a liquid, which is lubricious even in the absence of moisture, but still has the aforementioned extraordinary water washability.
Description
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LUL3R:[CArll:rN(; StJl:'l'O';T'rORY ~ND
ME~ IOD ~or~ ~IAT~ [~J~: ~\;\lD US:LN(~ 1'111~ S~ E, This invention relates to a lubricant in the form of a suppository, which ]ubr:icant is designed speciEically for the human vagina. An aspec-t of -this inver-tion relates to a pre~coital lubricant in suppository form. Still anothex aspect of -this lnvention relates -to a method for lubricatiny the human vagina by inser-tion of a solid suppository which melts to form a lubricant a-t human body temperature. Still ano-ther aspect of this invention relates to a me-thod Eor making a lubriea-ting suppository from a plurality of generally solid materials, at leas-t one of whieh is lubricious !-at normal ambient temperatures. ¦-Deseription of the Prior Art A variety of materials have been sugges-ted as lubrieants for human body eanals, partieularly -the vaginal and anal eanals. The requirements of sueh lubriean-ts vary depending upon the reason for lubrieating the inside surfaees of the canal. Prior to or during eoitus, the human body itself provides some na-tural lubrieation. However, there is a well-established market for materials whieh supplement the funetion of the natural lubrieant.
Theoretically, any lubricious material ~Ihich is not harmful to skin eould be a pre-coital :
lubricant, and petroleum jelly, mineral or triglyeeride oils, and similar biologieally inert, oleophilie materials have been used for this purpose Ir 1..
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iS ~ , ~c I.i}~e any olcopl~ ic mate:ria:ls, however, tlley are capahle of stain;.ng fabl^i.c, are rc.l,at:ively incornpafible ~7i.th natural vagillal. moisture, and rnay resist rernoval from -the skin or the interior oE the vayi.nal canal when plain water rinses are used. The pharmaceutical, cosmetic, and personal care industries have accordin~],y --made an effor-t to formulate lubri.can-ts which are better suited for pre-coital use and other vaginal canal lubrica-tiny purposes. A composition known as "K Y Jelly" is an example of a sterile, yeneral purpose lubricant with label instructions for use as a lubricant in obstetrical and gynecoloyical procedures and to aid in the insertion of thermometers and other instruments into the vagina or rectum. "Ortho 15 Personal Lubricant", on the o-ther hand, is an example ~, of a composition],abel],ed for use specifically for sexual in~ercourse. Nevertheless, the latter produc-t is somewhat similar in its composition to the sterile, general purpose jelly. Both products contain a major amount of water combined wi-th a cellulose derivative and are packag-ed in collapsible tuhes. The predominantly a~ueous nature of these products can provide advantages over oleaginous materials for the reasons already indica-ted, but because the water portion of both of these formu].ations appears to play - an important role in making the product lubricious,,.
upon evaporation the lubricity may be lost. Such ~, evaporation can occur even during coitus.
When insertion of any material into a human : .
- 30 body canal (particularly the vagina or anus) is -desirable, suppositories have advantages and are -often preferred by pa-tients, doc-tors, and o-ther users.
The suppository ar-t is a highly de~e].oped one, particularly with respect to suppositories which .
35 provide a matrix for releasi.ng some medicament. ~, 6~
...~ i,~) Sucn supposltor:i.e.c; can be m~lcle l.ub:r iC':i-lUS; SeC!, for example, U.S. Patent 3,776,001 (~-lallke), isswcd December ~, 1973. ~lecli.cators, -tampons, and the like have also been made lubr:icious, at least on S their surfaces. The following reEerences are helieved to be reasonabl.y representative o:E this art. .
U.S. Patent No. Issue Da-te Paten-tee 3,756,238 September 4, 1973 Hanke 3,~15,600 June 1.1, 1974 Groves 3,884,233 May 20, 1975 Summey 3,836,940 June 3, 1975 Hunger 4,026,292 May 31, 1977 ~lutchins et al 4,140,756 February 20, 1979 Gallian Summary of the Invention It has now been found that a pre-coital lubricant can be formulated such that it is suitable for formation into suppositories and is no-t dependent upon a high level of water content Qr moisture to be lubricious, but yet is water-washable to a far greater degree than any of -the common oleagi.nous lubricants. Indeed, lubricants of this invention have a high level of compatibility with plain water and can easily be solvated or uniformly distributed (dissolved and/or dispersed and~or suspended) in -water. Suppositories of this inven-tion are solid at - normal ambien-t temperatures bu-t melt a-t human body temperature to form a substantially homogeneous - liquid having the appearance of a single liquid phase, even though a glyceride of an aliphatic carboxylic acid is distributed through this homogeneous liquid.
In either the liquid or solid state, suppositories of this invention comprise: -(a) a continuous phase comprising a -.
polyoxyalkylene polyol component consisting essen-tially of polyethylene glycols having -j .- .!; --a molecular weight within the range of 400 to 5,000, so that this component w:LIl have a rnelting range 1O~J
enough for the purposes of this invention;
tb) about 10-60 par-ts, per 100 parts by weight of S the aforementioned polyol componen-t (and typically 10-30% by weight of the supposi-tory), of a nonionic surfactant having an HLB value greater than 12 (typically -this surfac-tant dissolves in the polyol component); and (c) about 10-40 parts per hundred, based on the weight of the polyol component, of a C6-C12 aliphatic carboxylic acid glyceride, which glyceride is uniformly dis-tributed throughout the continuous phase with the aid of the nonionic surfactant.
In the invention described, the continuous phase may further comprise a lower aliphatic monomeric hydrophilic polyol dissolved in -the continuous phase.
The nonionic surfactant may comprise a blend of oxyethylene chain-containing esters or ethers, the blend having an HLB value above about 1~, the es-ter or e-ther functional groups of the esters or ethers comprising a higher aliphatic residue.
According to ano-ther aspect of the invention there is provided a solid, pre-coital, vaginal lubricant suppository which melts at 37C., the suppository having been cas-t and solidified from a generally homogeneous molten mass cornprising a continuous phase. This continuous phase consists essentially of:
(a) 50-70% by weight, based on the weight of the suppository, of a blend of glycols consis-ting essentially of (1) a polyoxyethylene glycol having an average molecular weight of 900-1100, and (2) a polyoxyethylene glycol having an average molecular weight of 1200-1700, the ratio of glycol (2) to glycol (1) ranging from about 1:1 to about 4:1.
(b) 5-20% by weight, based on the weight of the suppository, of glycerin;
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-- 4a -(c) 10-30% by weight, based on the weight of the suppository, of a combination of nonionic surfac-tan-ts having a weighted-average HLB value of about 14 to about 18, this combination comprising polyoxyethylene lauryl e-ther and polyoxyethy~Lene stearate; and (d) as a discontinuous phase emulsified in and distributed uniformly throuyhout the con-tinuous phase, a triglyceride of coconut origin containing caprylic and capric acid residues.
The human vagina can be pre-coitally lubricated with a suppository of this invention by inserting -the solid suppository and permit-ting it to melt within the vaginal canal prior to coitus. The melting is generally complete within a very few minutes. If desired, the insertion can take place up to a few hours before coitus.
Suppositories of this invention are made by melting the polyethylene glycols at a moderately elevated -temperature, thereby obtaining a homogeneous melt. The preferred nonionic surfactant (including surfactant combinations) can be dissolved in the melt. The resul-ting ho-t mixture is a suitable medium for distribu-ting the glyceride, which is the primary lubricating substance. When a suitable blend has been formed, it can be cast into the form of suppositories using molds or a suppository packaging material that serves as both mold and package.
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~ 5 --Detai1tl_Desc~lpt1~n ~s will be apparent frorn the Eoregoing h~ie~ j summary, t}liS invention is tai]o~ed specifical1y -to the requirements of pre-coi-tal lubrication, althouyh suppositor:ies oE -this invent:ion may incidentally faci]itate insertion of rnedical instruments or the like into human body canals. I
For coital lubrication, compa-tibili-ty with ~later11' or moisture is desirable not only to provide water washa~ility, but also to facilltate combination with na-tural vaginal moisture and ulliEorm spreadiny throughout the surfaces of the vaginal canal. A
relatively low viscosity in -the molten state also improves the pre-coital lubricating function of this invention. Such low viscosi-ty may have one drawback, however: the lubrican-t can easily pass from the vaginal canal onto clothing or other fabric~
To overcome this drawbac]c, it has been found that an extremely high level of water compatibility can be provlded without losing any of the other advantages of this invention. A solid residue or stain (e.g. on fabric) from such leakage can be removed with plain water because of the e~traordinarily high level of dispersion of the oleaginous phase or phases of the lubricant and the compatibility of the nonionic surfactants with the polyoxyethylene -- glycol base. Compositions of this inven-tion need not and preferably do not contain any solid material which will not readily disperse or become suspended in water. Eyen the cellulosic materials of the prior art are more difficult to suspend or disperse in water than compositions of this inyention The !i polyoxyalkylene polyol component, since it consists essentially of polyethylene glycols is essentially soluble in water. The nonionic surfactant component ~':
-. . ;
is essentially soLuble in the po:Lyethy],ene ylycols, thereby simp]ifying the phase relationship be-tween -the glycols and -the glyceride Lubricant. 'r'he concentration of nonionic surfactan-t is high enough to insure that -the glyceride will be well emulsified and can be re-emulsified if a spot or s-tain on fabric results from -the use of this invention.
Even in the absence of na-tural vaginal moisture, a fully or partially melted suppository or vaginal insert of this invention has lubricating properties. rhe unique combination of ingredients of this invention further allows the melted lubricating substance to become miscible with the vaginal moisture present even in small amounts. As the insert or suppository melts and mixes with any vaginal moisture, it spreads readily throughout the vagina. In addition, -the lubricity of the invention is not reduced due to evaporation of moisture during coitus.
In addition to the glycol, glyceride lubricant, and surfactant components of a composition of this invention, -the composition can be further modified with a lower aliphatic monomeric hydrophilic polyol which will dissolve in -the glycol phase. A preferred monomeric polyol is glycerin. Pigments, fillers, extenders, preservatives, and antioxidants can also be included in the compositi,on, but it is ordinarily preferred to avoid the use of any filler, extender, or pigmen-t which will leave a visible solid residue. For antioxidant or preservative effects, various FDA-approved compounds are suitable, including the conventional alkylated hydroxy aromatic compounds such as BHT (butylated hydroxytoluene) or BHA (butylated hydroxyanisole).
Typical compositions of this invention will now be described in greater detail.
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The ma,jor amount of the col~t-,i.nuous phase co~pr:i.sns one or more (prc~erably a bLerld) of polyo~.~ethylene or polyethylerle ~Jlycolc. These g1.ycols contain an ox~e-thylene chaln wi-th an extraordilla,ry compatik,i.l.:ity with water and with a hyclroscopicity of at leas-t 0.1%, preferably at leas-t 1~ of glyceri.n~ secause these polyet~ylene glycols make up such a ].arge proportion of -the lubri,cating suppository, it is prefer.red that a single such glycol (if used a,lone) or any combination of such ylycols be solid at normal ambien-t temperatures (20~25D C.) and preferably a-t moderately elevated temperatures which may inadvertantly be reached duriny storage, e.g. 30 or 35 C. On the other hand, it is desira~le tha-t -the glycol component be capable oE melting at temperatures c].ose to human body temperature (e.g. 37 C.~. The melting point of -the glycol component can of course be depressed by blending into it compatible liquids or low-melting solids. Nevertheless, it is preferable that, in the absence of such liquids or low-melting solids, the glycol component have a melting poin-t or melting range low enough to insure the formation of a clear mol-ten li~ui.d at less than about 75 C., more preferably at less than abo~t 55 or 60 C~
Among the low-melting solids and liquids which can ~~ provide the aforementioned melting point depressant effect are low molecular weight polyo~yethylene t~
glycols which are avallable in molecular weights well below 1,000 (equivalent weights well below 5001.
It is preferred however to keep the molecular weigh-t of the lowest-melting glycol above about 400. A '~
polyethylene glycol having an average ~olecu].ar weight of about 500 could be a solid at 20 C. but --may have the consistency of low-melting petrolatum.
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? ~ ;3 ~ 'olyoxyeLlly~Lene gLycols are c-y.lilclble in mOIC`C~Ulclr weiclhts above I,000,000, but rnost o~ the molecular weicll~t ral,cJe above 5,000 is of limi~ d utility in the colltext of this invent:ion because of the relatively high melting points or solidification ranges of such ma-terials. The optimum averaye molecular weiyht range :Eor ylycols useful in this invention is above about 900 and below about 2,000, thereby assuring a solidifica-tion range below 60 C~
A blend of such glycols within this molecular weight range will generally begin to melt at temperatures no higher than about 50 C. With "fine tuniny" of the blend, it can be formulated to beyin to mel-t ~, at 36-3~ or 39 C., which is approximately the ideal melting range, absent any melting point depressant other than a low molecular weight polyoxyethylene glycol. ~ith a melting point depressant, this range can be extended to 40~ C. and higherr as explained previously. It is desirable in any event that the glycol component be~in -to melt at 36-38~ C'. within a few minutes.
A particularly effective way to provide the water-washability of lubricating compositions of this invention is to insure that the glyceride (e.g. the glyceryl trialkanoate~ is well distributed with a surfactan-t component which is compatible with the, polyethylene glycols in the con-tinuous phase and, perhaps equally important, that these glycols have a measurable degree of water solubility, e.g. more than 10% hy weight. A remarkable Eeature of the polyethylene glycols is that even relatively high polymers of ethylene oxide have water ~~~~~~ solubility. At relatively low molecular weights, these hydroxy-terminated polymers will dissolve to the extent oE about 70% by weight (or more) in water.
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. 9 ~s the mole(u1.clr weig1~t ir~creasec; :into tile thousands, the water sol~1b:iLity ~ecl:ines }~lt no-t drac:tic;1lly.
Polyoxyetllylerle c~.lycol.s used i.n this ;nvention, either indivic1ua].ly or in cor.lbination, ty~i.cally have a wa-te.r solubili-ty in excess of 50% on a 1ei~ht/
weigllt basis. For thi.s reason, mixtures of oxyethylene polymers with oxypropylene or te-trarne-thy]eneoxy polymers are no-t preferred. ~mong non-onic polymers, it is difficult to improve upon the water solubili-ty of the oxyethylene (i.e. ethylene oxide) polymers, and certainly the water eompatibili.ty of propylene oxide or other oxya]kylene polymers is meager in comparison to the polyoxye-thylenes. In short, the oxyalkylene chains obtained from two-earbon oxyal~ylene units are unique among this elass of strue-tures, partieularly in terms of their compatibility with wa-ter. Absent modification with pendant or reeurring oxyethylene units, other hydrophilie solids sueh as eellulose also laek this extraordinarily high degree of water eompatibility. Relatively hydrophobie or oleophilie eompounds which may detraet from the water eompatibility of the glyeol eomponent of this invention are preferably excludecl from this component. With the exeeption of very minor amounts of antioxiclants, preservatives, or the like, it will ordinarily be the ease that the least hydrophilie ~ ingredient of a eomposition of this invention will be the glyeeride, which is substantially insoluble in water.
In typiea]. suppository eompositions of this invention, 50--70% by weight of the eomposition is made up of this glyeol component. The total eomposition eontains a nonionic surfaetant eomponent whieh can be uniformly distributed tdissolved, dispersed, or suspended) through the eon-tinuous phase.
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~t is ord,irlari~y preferrc~cl t-haL kh;s surEclctant comL)onen~ be sll~Eicicrlt'ly comE~at-il~L-e ~7;L-h the continuous phase to ~crln a part o,E it, the~ehy simplifying the phasc relationsh:,,ps wi,thin the composition. I-t is also preEerrecl that the surEactant have a significant declree of compatibi]ity with wa-ter, which can be provided by selecting surfac-t~nt compoundc, or compositions havincJ an ~ILB value grea-ter than 12, more preferably greater -than 1~. (The IILB
value is the hydrophile-lipophile ba]ance and is determined in accordance with well-known procedures published in the scientific and trade literature;
~ILB values below 9 are considered cJenerally lipophilic, values of 9-11 are considered intermecliate or borderline, and values above 12 are clearly hydrophilic.) Although HLB values of 20 or 30 or more have been reported, it is generally unnecessary to use nonionic surfactants having values significantly above 18.~~When ,a combina-tion of surfactan-ts is 20 used (as is particularly preferred in this invention), -the overall HLB ~alue can be determined on a weighted-average basis, as is conventional in the detergent art. Some nonionic emulsifiers and other surfactan~s will actually dissolve in molten polyoxyethylene glycols, forernos-t among these surfactants being those containing oxyethylene chains ~ such as the poly(oxyethylene) polyol esters, poly(oxyethylene) polyol ethers, and mix-tures of these esters and ethers. Some of these compound's, such as polyoxyethylene(20) sorbitan mono-oleate are also water soluble. Several series of polyoxyethylene ethers of higher aliphatic alcohols are commercially availab]e, as are the polyoxye-thylene deriva-tives of higher aliphatic carboxyli,c acids, e.g. the polyoxyethylene polyol alkanoates.
S
~' l] ~ 'r Unsa~ura~ed aliphcltic carboxy:L:ic acicls and alco~lols can also be used to forrn-the desJ.red polyo~yethylene deri.vcltives. A sigrliEicarlt c1ecJree of higher aliphatic character can be obtai.ned with ac:icls and alcohols con-t~ining at least 6 carbons, preferably at least 10 carbons. ~t ~2~ and higher, the aliphatic charac-ter may become e~cessive and may even be somewha~ excessive at C20 or C22. Relatively hydrophilic nucl.ei such as sorbitan and other lower aliphatic monomeric polyols can help to counterbalan-e the aliphatic character of càrbon chains in the C12-C20 range. An example of a thus-balanced compound is polyoxyethylene (20) sorbitan mono-oleate. ~.
There can be distinct advantages in addi.ng a lower aliphatic monomeric hydrophilic polyol to the continuous phase. Glycerin, for example, is of interest because of its extraordinary affinity for water - about 10-100 times as much hygroscopicity as the preferred polyoxyethylene glycols. Glycerin, in fact, is commonly used as a humectant as well as a solvent, a plastici~er, and an emollient. It is a common ingredient of anal suppositories and is considered safe and effective for a variety of medical uses. (Surfactants generally used in this invention are also considered to be safe materials, the particularly preferred ones having been cleared for - food or drug use.) Although glycerin is -an optional ingredient in the supposi`tories of this invention, it is ordinarily preferred to include about 5 to about 20% by weight of this compound, based on the total weight of the suppository composition.
The Emulsified Phase The most important ingredient of the phase which is emulsified in the continuous phase is a lubricitous glyeeride, preferably a triglyceride generally ... . . . ,, . _ _ ___ ,_,.. ., . ,.. . .. , . _.. _. " .. _, i5 considered -to be safe and effec-tive for lubricating or plasticizing human skin. rrhe glyceryl lower alkanoates such as triacetin and tribu-tyrin tend -to be high boiling liquids which may have plasticizing properties but are less effective as lubricants as compared to -triglycerides of the aliphatic carboxylic acids having 6 or more carbon atoms.
Some of the most preferred lubricants for skin are of coconut origin and contain -triglycerides of C6 through C18 carboxylic acids, particularly the saturated aliphatic acids (e.g. capric, caprylic, lauric, palmitic, and stearic acids). These triglycerides can be fractiona-ted to shift the content toward either the C6-C12 -triglycerides or the C12-C18 triglycerides, as may be desired. Unfortunately, all of these triglycerides are subs-tantially insoluble in wa-ter. Even glyceryl tributyrate (the C4 analog of the coconut-origin triglycerides) is reported to have a solubility in water of only 0.01%. However, the highly effective emulsifier or surfactant component of this invention provides excellent water washability and the prospect of virtually total removal of any triglyceride residue from clothing or other fabric with an essentially plain water rinse. In addition, this emulsifier system helps to provide a clear, apparently homogeneous melt within and above the melting range of the suppository of this invention. Although this invention is not bound by any theory, it is believed -that the triglyceride is extremely well dispersed in the composition to the point where the composition approaches the nature of a true solution.
Method of Manufacture The oxyethylene glycols are normally -the first ingredients charged to a hea-ted mixer since they is - .13 normally make ~p ~he major amourlt o:E the suppos:Ltory COTllpOSi tiOIl . rrhe teml?~ra tu.re Wi th:i rl the miY~er i S
ma;.lltained at a suffici.ently high leve]. to keeE~-the glycols in -the mo].ten state without approaching the flash point o:E any co-mponent oE the composition.
Ordinarily, it is no-t necessary to exceed a temperature o:E about 75 C. in the mixer. The ylycols form a clear melt, to which the nonionic sur-Eactant system can be added and, preferably, dissolved with stirriny.
The glyceride is also added under constant s-tirring, and 15-20 minutes will -typically be a sufficien-t period oE agitation to thoroughly disperse or suspend this component. The result will be a uniform P-distribution of all componen-ts oE the composition.
15 The glycerin or other hydrophi.lic polyol can be .-added to the composition at any suitable stage during manufactu~e.
The heated mass can be poured from the mixer -into molds, demolded, and then individually wrapped in foil~laminate packaging material. Cooling of the mold is particularly desired for the purpose of obtaining rapid and complete solidification of the portion of molten material which has been poured - into the mold. Alternatively, the heated mass can 25 be cast i.nto a preformed suppository packaging ---- ma-terial that serves as both mold and package.
- The preferred me-thod of use is to insert the suppository into the vagina at least about 5 minutes prior -to sexual intercourse. If this procedure is not convenient, the suppository can be inser-ted as much as an hour or two before intercourse, and a sufficient amount of liquid lubricant will still be present in the vayinal canal when intercourse is commenced. After -thorough mel-ting of the suppository, --leakage of the molten lubricant from the vaginal .
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carlal w.ill. not vitiate ~he e~fEectiveness oE ~his invention, becclu~se o.~ tlle compatih.i.lity o:~ tile trig]yceride with nat:urcll luhri.cànts, the ease of blend;rlcj of the lub.ricant ~J:ith natur,lL moistur~
wllich may be present, -the spreadincJ of -the lubricant throughout the canal, and -the efEectiveness of very small residual amounts o:~ -the lubricant.
The invention is illustrated in more detail in the following non-llmi-ting Example.
. Exam? e A solid suppository was cast from the following formulation.
Ingred.ient Parts by l~Jeight ~=.
Polye-thylene . glycol, 25 average molecular weicJh-t 1300-1600, solidifying range 40-509 C., soft, white waxy solid, sol-~bility in water at 2Q C., approximate]y 70% (weight/weight), pEI
of a 5O aqueous solution about 6.5 ~CARBOWAX~ 1540) Polyet~ylene glycol, 25 average molecular weight 950-1050, solidifyi.ng -- range 35-40 C., solubility in water at 20 CO about 70% on a weight/weight basis (CARBOWAX~`? 1000) Glycerin 10 Polyoxyethylene t23) lauryl 10 ether (BRIJ3 351 Polyoxyethylene (20) sorbitan 5* .`
mono-oleate (TWEEN~ 80) ~-Polyoxyethylene (40) s-tearate 5 ;-(''MYRJI' 52-5 [trademark]) *Alternatively, can be replaced with more BRIJ or MYRJ.
~36~
Fract:iondtecl-tri~lyccricle 20 of COCOIlUt oric~in (caprylic/capric tri-c~lyceride, "N~O~E~
~I-5" [trademark]) The ~ILB value of the polyoxyethy]ene lauryl e-ther and the polyoxye-thylene s-tearate is normally within the ranye of 16.5 to 17. The HLB value of the polyoxyethylene sorbitan mono-o:Lea-te is normally 15. Accordinyly, the average HLB value of the nonionic surfactant system of this invention is above 16. The glycol component was melted and main-tained within the temperature range of 55-70 C.
during manufacture of the suppository composi-tion.
Manufacture was carried out on a batch basis, but can also be done continuously.
One ~art of antioxidant, B~IT (butylated hydroxy toluene) was added to 10,000 parts of the composition described above. A suppository cast from this composition was 30 ~m in length and 13 mm wide at its widest point. (Suppositories 10-50 mm in length and 2-20 mm in width can easily be cast and molded.) Although not ordinarily preferred, medicaments related to coitus such as spermicides and bactericides may be added to suppository compositions of -this ~ invention.
Throughout this applicatlon, the terms "polyethylene glycol" and "polyoxyethylene glycol"
are used synonymously.
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LUL3R:[CArll:rN(; StJl:'l'O';T'rORY ~ND
ME~ IOD ~or~ ~IAT~ [~J~: ~\;\lD US:LN(~ 1'111~ S~ E, This invention relates to a lubricant in the form of a suppository, which ]ubr:icant is designed speciEically for the human vagina. An aspec-t of -this inver-tion relates to a pre~coital lubricant in suppository form. Still anothex aspect of -this lnvention relates -to a method for lubricatiny the human vagina by inser-tion of a solid suppository which melts to form a lubricant a-t human body temperature. Still ano-ther aspect of this invention relates to a me-thod Eor making a lubriea-ting suppository from a plurality of generally solid materials, at leas-t one of whieh is lubricious !-at normal ambient temperatures. ¦-Deseription of the Prior Art A variety of materials have been sugges-ted as lubrieants for human body eanals, partieularly -the vaginal and anal eanals. The requirements of sueh lubriean-ts vary depending upon the reason for lubrieating the inside surfaees of the canal. Prior to or during eoitus, the human body itself provides some na-tural lubrieation. However, there is a well-established market for materials whieh supplement the funetion of the natural lubrieant.
Theoretically, any lubricious material ~Ihich is not harmful to skin eould be a pre-coital :
lubricant, and petroleum jelly, mineral or triglyeeride oils, and similar biologieally inert, oleophilie materials have been used for this purpose Ir 1..
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-.
.', * ~
iS ~ , ~c I.i}~e any olcopl~ ic mate:ria:ls, however, tlley are capahle of stain;.ng fabl^i.c, are rc.l,at:ively incornpafible ~7i.th natural vagillal. moisture, and rnay resist rernoval from -the skin or the interior oE the vayi.nal canal when plain water rinses are used. The pharmaceutical, cosmetic, and personal care industries have accordin~],y --made an effor-t to formulate lubri.can-ts which are better suited for pre-coital use and other vaginal canal lubrica-tiny purposes. A composition known as "K Y Jelly" is an example of a sterile, yeneral purpose lubricant with label instructions for use as a lubricant in obstetrical and gynecoloyical procedures and to aid in the insertion of thermometers and other instruments into the vagina or rectum. "Ortho 15 Personal Lubricant", on the o-ther hand, is an example ~, of a composition],abel],ed for use specifically for sexual in~ercourse. Nevertheless, the latter produc-t is somewhat similar in its composition to the sterile, general purpose jelly. Both products contain a major amount of water combined wi-th a cellulose derivative and are packag-ed in collapsible tuhes. The predominantly a~ueous nature of these products can provide advantages over oleaginous materials for the reasons already indica-ted, but because the water portion of both of these formu].ations appears to play - an important role in making the product lubricious,,.
upon evaporation the lubricity may be lost. Such ~, evaporation can occur even during coitus.
When insertion of any material into a human : .
- 30 body canal (particularly the vagina or anus) is -desirable, suppositories have advantages and are -often preferred by pa-tients, doc-tors, and o-ther users.
The suppository ar-t is a highly de~e].oped one, particularly with respect to suppositories which .
35 provide a matrix for releasi.ng some medicament. ~, 6~
...~ i,~) Sucn supposltor:i.e.c; can be m~lcle l.ub:r iC':i-lUS; SeC!, for example, U.S. Patent 3,776,001 (~-lallke), isswcd December ~, 1973. ~lecli.cators, -tampons, and the like have also been made lubr:icious, at least on S their surfaces. The following reEerences are helieved to be reasonabl.y representative o:E this art. .
U.S. Patent No. Issue Da-te Paten-tee 3,756,238 September 4, 1973 Hanke 3,~15,600 June 1.1, 1974 Groves 3,884,233 May 20, 1975 Summey 3,836,940 June 3, 1975 Hunger 4,026,292 May 31, 1977 ~lutchins et al 4,140,756 February 20, 1979 Gallian Summary of the Invention It has now been found that a pre-coital lubricant can be formulated such that it is suitable for formation into suppositories and is no-t dependent upon a high level of water content Qr moisture to be lubricious, but yet is water-washable to a far greater degree than any of -the common oleagi.nous lubricants. Indeed, lubricants of this invention have a high level of compatibility with plain water and can easily be solvated or uniformly distributed (dissolved and/or dispersed and~or suspended) in -water. Suppositories of this inven-tion are solid at - normal ambien-t temperatures bu-t melt a-t human body temperature to form a substantially homogeneous - liquid having the appearance of a single liquid phase, even though a glyceride of an aliphatic carboxylic acid is distributed through this homogeneous liquid.
In either the liquid or solid state, suppositories of this invention comprise: -(a) a continuous phase comprising a -.
polyoxyalkylene polyol component consisting essen-tially of polyethylene glycols having -j .- .!; --a molecular weight within the range of 400 to 5,000, so that this component w:LIl have a rnelting range 1O~J
enough for the purposes of this invention;
tb) about 10-60 par-ts, per 100 parts by weight of S the aforementioned polyol componen-t (and typically 10-30% by weight of the supposi-tory), of a nonionic surfactant having an HLB value greater than 12 (typically -this surfac-tant dissolves in the polyol component); and (c) about 10-40 parts per hundred, based on the weight of the polyol component, of a C6-C12 aliphatic carboxylic acid glyceride, which glyceride is uniformly dis-tributed throughout the continuous phase with the aid of the nonionic surfactant.
In the invention described, the continuous phase may further comprise a lower aliphatic monomeric hydrophilic polyol dissolved in -the continuous phase.
The nonionic surfactant may comprise a blend of oxyethylene chain-containing esters or ethers, the blend having an HLB value above about 1~, the es-ter or e-ther functional groups of the esters or ethers comprising a higher aliphatic residue.
According to ano-ther aspect of the invention there is provided a solid, pre-coital, vaginal lubricant suppository which melts at 37C., the suppository having been cas-t and solidified from a generally homogeneous molten mass cornprising a continuous phase. This continuous phase consists essentially of:
(a) 50-70% by weight, based on the weight of the suppository, of a blend of glycols consis-ting essentially of (1) a polyoxyethylene glycol having an average molecular weight of 900-1100, and (2) a polyoxyethylene glycol having an average molecular weight of 1200-1700, the ratio of glycol (2) to glycol (1) ranging from about 1:1 to about 4:1.
(b) 5-20% by weight, based on the weight of the suppository, of glycerin;
6~
-- 4a -(c) 10-30% by weight, based on the weight of the suppository, of a combination of nonionic surfac-tan-ts having a weighted-average HLB value of about 14 to about 18, this combination comprising polyoxyethylene lauryl e-ther and polyoxyethy~Lene stearate; and (d) as a discontinuous phase emulsified in and distributed uniformly throuyhout the con-tinuous phase, a triglyceride of coconut origin containing caprylic and capric acid residues.
The human vagina can be pre-coitally lubricated with a suppository of this invention by inserting -the solid suppository and permit-ting it to melt within the vaginal canal prior to coitus. The melting is generally complete within a very few minutes. If desired, the insertion can take place up to a few hours before coitus.
Suppositories of this invention are made by melting the polyethylene glycols at a moderately elevated -temperature, thereby obtaining a homogeneous melt. The preferred nonionic surfactant (including surfactant combinations) can be dissolved in the melt. The resul-ting ho-t mixture is a suitable medium for distribu-ting the glyceride, which is the primary lubricating substance. When a suitable blend has been formed, it can be cast into the form of suppositories using molds or a suppository packaging material that serves as both mold and package.
~6~
~ 5 --Detai1tl_Desc~lpt1~n ~s will be apparent frorn the Eoregoing h~ie~ j summary, t}liS invention is tai]o~ed specifical1y -to the requirements of pre-coi-tal lubrication, althouyh suppositor:ies oE -this invent:ion may incidentally faci]itate insertion of rnedical instruments or the like into human body canals. I
For coital lubrication, compa-tibili-ty with ~later11' or moisture is desirable not only to provide water washa~ility, but also to facilltate combination with na-tural vaginal moisture and ulliEorm spreadiny throughout the surfaces of the vaginal canal. A
relatively low viscosity in -the molten state also improves the pre-coital lubricating function of this invention. Such low viscosi-ty may have one drawback, however: the lubrican-t can easily pass from the vaginal canal onto clothing or other fabric~
To overcome this drawbac]c, it has been found that an extremely high level of water compatibility can be provlded without losing any of the other advantages of this invention. A solid residue or stain (e.g. on fabric) from such leakage can be removed with plain water because of the e~traordinarily high level of dispersion of the oleaginous phase or phases of the lubricant and the compatibility of the nonionic surfactants with the polyoxyethylene -- glycol base. Compositions of this inven-tion need not and preferably do not contain any solid material which will not readily disperse or become suspended in water. Eyen the cellulosic materials of the prior art are more difficult to suspend or disperse in water than compositions of this inyention The !i polyoxyalkylene polyol component, since it consists essentially of polyethylene glycols is essentially soluble in water. The nonionic surfactant component ~':
-. . ;
is essentially soLuble in the po:Lyethy],ene ylycols, thereby simp]ifying the phase relationship be-tween -the glycols and -the glyceride Lubricant. 'r'he concentration of nonionic surfactan-t is high enough to insure that -the glyceride will be well emulsified and can be re-emulsified if a spot or s-tain on fabric results from -the use of this invention.
Even in the absence of na-tural vaginal moisture, a fully or partially melted suppository or vaginal insert of this invention has lubricating properties. rhe unique combination of ingredients of this invention further allows the melted lubricating substance to become miscible with the vaginal moisture present even in small amounts. As the insert or suppository melts and mixes with any vaginal moisture, it spreads readily throughout the vagina. In addition, -the lubricity of the invention is not reduced due to evaporation of moisture during coitus.
In addition to the glycol, glyceride lubricant, and surfactant components of a composition of this invention, -the composition can be further modified with a lower aliphatic monomeric hydrophilic polyol which will dissolve in -the glycol phase. A preferred monomeric polyol is glycerin. Pigments, fillers, extenders, preservatives, and antioxidants can also be included in the compositi,on, but it is ordinarily preferred to avoid the use of any filler, extender, or pigmen-t which will leave a visible solid residue. For antioxidant or preservative effects, various FDA-approved compounds are suitable, including the conventional alkylated hydroxy aromatic compounds such as BHT (butylated hydroxytoluene) or BHA (butylated hydroxyanisole).
Typical compositions of this invention will now be described in greater detail.
tir~ ~7 t .. , ..................... ,., I' rL'~-r~ C'orlti~ u~
The ma,jor amount of the col~t-,i.nuous phase co~pr:i.sns one or more (prc~erably a bLerld) of polyo~.~ethylene or polyethylerle ~Jlycolc. These g1.ycols contain an ox~e-thylene chaln wi-th an extraordilla,ry compatik,i.l.:ity with water and with a hyclroscopicity of at leas-t 0.1%, preferably at leas-t 1~ of glyceri.n~ secause these polyet~ylene glycols make up such a ].arge proportion of -the lubri,cating suppository, it is prefer.red that a single such glycol (if used a,lone) or any combination of such ylycols be solid at normal ambien-t temperatures (20~25D C.) and preferably a-t moderately elevated temperatures which may inadvertantly be reached duriny storage, e.g. 30 or 35 C. On the other hand, it is desira~le tha-t -the glycol component be capable oE melting at temperatures c].ose to human body temperature (e.g. 37 C.~. The melting point of -the glycol component can of course be depressed by blending into it compatible liquids or low-melting solids. Nevertheless, it is preferable that, in the absence of such liquids or low-melting solids, the glycol component have a melting poin-t or melting range low enough to insure the formation of a clear mol-ten li~ui.d at less than about 75 C., more preferably at less than abo~t 55 or 60 C~
Among the low-melting solids and liquids which can ~~ provide the aforementioned melting point depressant effect are low molecular weight polyo~yethylene t~
glycols which are avallable in molecular weights well below 1,000 (equivalent weights well below 5001.
It is preferred however to keep the molecular weigh-t of the lowest-melting glycol above about 400. A '~
polyethylene glycol having an average ~olecu].ar weight of about 500 could be a solid at 20 C. but --may have the consistency of low-melting petrolatum.
, . .
? ~ ;3 ~ 'olyoxyeLlly~Lene gLycols are c-y.lilclble in mOIC`C~Ulclr weiclhts above I,000,000, but rnost o~ the molecular weicll~t ral,cJe above 5,000 is of limi~ d utility in the colltext of this invent:ion because of the relatively high melting points or solidification ranges of such ma-terials. The optimum averaye molecular weiyht range :Eor ylycols useful in this invention is above about 900 and below about 2,000, thereby assuring a solidifica-tion range below 60 C~
A blend of such glycols within this molecular weight range will generally begin to melt at temperatures no higher than about 50 C. With "fine tuniny" of the blend, it can be formulated to beyin to mel-t ~, at 36-3~ or 39 C., which is approximately the ideal melting range, absent any melting point depressant other than a low molecular weight polyoxyethylene glycol. ~ith a melting point depressant, this range can be extended to 40~ C. and higherr as explained previously. It is desirable in any event that the glycol component be~in -to melt at 36-38~ C'. within a few minutes.
A particularly effective way to provide the water-washability of lubricating compositions of this invention is to insure that the glyceride (e.g. the glyceryl trialkanoate~ is well distributed with a surfactan-t component which is compatible with the, polyethylene glycols in the con-tinuous phase and, perhaps equally important, that these glycols have a measurable degree of water solubility, e.g. more than 10% hy weight. A remarkable Eeature of the polyethylene glycols is that even relatively high polymers of ethylene oxide have water ~~~~~~ solubility. At relatively low molecular weights, these hydroxy-terminated polymers will dissolve to the extent oE about 70% by weight (or more) in water.
- :
. 9 ~s the mole(u1.clr weig1~t ir~creasec; :into tile thousands, the water sol~1b:iLity ~ecl:ines }~lt no-t drac:tic;1lly.
Polyoxyetllylerle c~.lycol.s used i.n this ;nvention, either indivic1ua].ly or in cor.lbination, ty~i.cally have a wa-te.r solubili-ty in excess of 50% on a 1ei~ht/
weigllt basis. For thi.s reason, mixtures of oxyethylene polymers with oxypropylene or te-trarne-thy]eneoxy polymers are no-t preferred. ~mong non-onic polymers, it is difficult to improve upon the water solubili-ty of the oxyethylene (i.e. ethylene oxide) polymers, and certainly the water eompatibili.ty of propylene oxide or other oxya]kylene polymers is meager in comparison to the polyoxye-thylenes. In short, the oxyalkylene chains obtained from two-earbon oxyal~ylene units are unique among this elass of strue-tures, partieularly in terms of their compatibility with wa-ter. Absent modification with pendant or reeurring oxyethylene units, other hydrophilie solids sueh as eellulose also laek this extraordinarily high degree of water eompatibility. Relatively hydrophobie or oleophilie eompounds which may detraet from the water eompatibility of the glyeol eomponent of this invention are preferably excludecl from this component. With the exeeption of very minor amounts of antioxiclants, preservatives, or the like, it will ordinarily be the ease that the least hydrophilie ~ ingredient of a eomposition of this invention will be the glyeeride, which is substantially insoluble in water.
In typiea]. suppository eompositions of this invention, 50--70% by weight of the eomposition is made up of this glyeol component. The total eomposition eontains a nonionic surfaetant eomponent whieh can be uniformly distributed tdissolved, dispersed, or suspended) through the eon-tinuous phase.
_ ~.
~t is ord,irlari~y preferrc~cl t-haL kh;s surEclctant comL)onen~ be sll~Eicicrlt'ly comE~at-il~L-e ~7;L-h the continuous phase to ~crln a part o,E it, the~ehy simplifying the phasc relationsh:,,ps wi,thin the composition. I-t is also preEerrecl that the surEactant have a significant declree of compatibi]ity with wa-ter, which can be provided by selecting surfac-t~nt compoundc, or compositions havincJ an ~ILB value grea-ter than 12, more preferably greater -than 1~. (The IILB
value is the hydrophile-lipophile ba]ance and is determined in accordance with well-known procedures published in the scientific and trade literature;
~ILB values below 9 are considered cJenerally lipophilic, values of 9-11 are considered intermecliate or borderline, and values above 12 are clearly hydrophilic.) Although HLB values of 20 or 30 or more have been reported, it is generally unnecessary to use nonionic surfactants having values significantly above 18.~~When ,a combina-tion of surfactan-ts is 20 used (as is particularly preferred in this invention), -the overall HLB ~alue can be determined on a weighted-average basis, as is conventional in the detergent art. Some nonionic emulsifiers and other surfactan~s will actually dissolve in molten polyoxyethylene glycols, forernos-t among these surfactants being those containing oxyethylene chains ~ such as the poly(oxyethylene) polyol esters, poly(oxyethylene) polyol ethers, and mix-tures of these esters and ethers. Some of these compound's, such as polyoxyethylene(20) sorbitan mono-oleate are also water soluble. Several series of polyoxyethylene ethers of higher aliphatic alcohols are commercially availab]e, as are the polyoxye-thylene deriva-tives of higher aliphatic carboxyli,c acids, e.g. the polyoxyethylene polyol alkanoates.
S
~' l] ~ 'r Unsa~ura~ed aliphcltic carboxy:L:ic acicls and alco~lols can also be used to forrn-the desJ.red polyo~yethylene deri.vcltives. A sigrliEicarlt c1ecJree of higher aliphatic character can be obtai.ned with ac:icls and alcohols con-t~ining at least 6 carbons, preferably at least 10 carbons. ~t ~2~ and higher, the aliphatic charac-ter may become e~cessive and may even be somewha~ excessive at C20 or C22. Relatively hydrophilic nucl.ei such as sorbitan and other lower aliphatic monomeric polyols can help to counterbalan-e the aliphatic character of càrbon chains in the C12-C20 range. An example of a thus-balanced compound is polyoxyethylene (20) sorbitan mono-oleate. ~.
There can be distinct advantages in addi.ng a lower aliphatic monomeric hydrophilic polyol to the continuous phase. Glycerin, for example, is of interest because of its extraordinary affinity for water - about 10-100 times as much hygroscopicity as the preferred polyoxyethylene glycols. Glycerin, in fact, is commonly used as a humectant as well as a solvent, a plastici~er, and an emollient. It is a common ingredient of anal suppositories and is considered safe and effective for a variety of medical uses. (Surfactants generally used in this invention are also considered to be safe materials, the particularly preferred ones having been cleared for - food or drug use.) Although glycerin is -an optional ingredient in the supposi`tories of this invention, it is ordinarily preferred to include about 5 to about 20% by weight of this compound, based on the total weight of the suppository composition.
The Emulsified Phase The most important ingredient of the phase which is emulsified in the continuous phase is a lubricitous glyeeride, preferably a triglyceride generally ... . . . ,, . _ _ ___ ,_,.. ., . ,.. . .. , . _.. _. " .. _, i5 considered -to be safe and effec-tive for lubricating or plasticizing human skin. rrhe glyceryl lower alkanoates such as triacetin and tribu-tyrin tend -to be high boiling liquids which may have plasticizing properties but are less effective as lubricants as compared to -triglycerides of the aliphatic carboxylic acids having 6 or more carbon atoms.
Some of the most preferred lubricants for skin are of coconut origin and contain -triglycerides of C6 through C18 carboxylic acids, particularly the saturated aliphatic acids (e.g. capric, caprylic, lauric, palmitic, and stearic acids). These triglycerides can be fractiona-ted to shift the content toward either the C6-C12 -triglycerides or the C12-C18 triglycerides, as may be desired. Unfortunately, all of these triglycerides are subs-tantially insoluble in wa-ter. Even glyceryl tributyrate (the C4 analog of the coconut-origin triglycerides) is reported to have a solubility in water of only 0.01%. However, the highly effective emulsifier or surfactant component of this invention provides excellent water washability and the prospect of virtually total removal of any triglyceride residue from clothing or other fabric with an essentially plain water rinse. In addition, this emulsifier system helps to provide a clear, apparently homogeneous melt within and above the melting range of the suppository of this invention. Although this invention is not bound by any theory, it is believed -that the triglyceride is extremely well dispersed in the composition to the point where the composition approaches the nature of a true solution.
Method of Manufacture The oxyethylene glycols are normally -the first ingredients charged to a hea-ted mixer since they is - .13 normally make ~p ~he major amourlt o:E the suppos:Ltory COTllpOSi tiOIl . rrhe teml?~ra tu.re Wi th:i rl the miY~er i S
ma;.lltained at a suffici.ently high leve]. to keeE~-the glycols in -the mo].ten state without approaching the flash point o:E any co-mponent oE the composition.
Ordinarily, it is no-t necessary to exceed a temperature o:E about 75 C. in the mixer. The ylycols form a clear melt, to which the nonionic sur-Eactant system can be added and, preferably, dissolved with stirriny.
The glyceride is also added under constant s-tirring, and 15-20 minutes will -typically be a sufficien-t period oE agitation to thoroughly disperse or suspend this component. The result will be a uniform P-distribution of all componen-ts oE the composition.
15 The glycerin or other hydrophi.lic polyol can be .-added to the composition at any suitable stage during manufactu~e.
The heated mass can be poured from the mixer -into molds, demolded, and then individually wrapped in foil~laminate packaging material. Cooling of the mold is particularly desired for the purpose of obtaining rapid and complete solidification of the portion of molten material which has been poured - into the mold. Alternatively, the heated mass can 25 be cast i.nto a preformed suppository packaging ---- ma-terial that serves as both mold and package.
- The preferred me-thod of use is to insert the suppository into the vagina at least about 5 minutes prior -to sexual intercourse. If this procedure is not convenient, the suppository can be inser-ted as much as an hour or two before intercourse, and a sufficient amount of liquid lubricant will still be present in the vayinal canal when intercourse is commenced. After -thorough mel-ting of the suppository, --leakage of the molten lubricant from the vaginal .
.
carlal w.ill. not vitiate ~he e~fEectiveness oE ~his invention, becclu~se o.~ tlle compatih.i.lity o:~ tile trig]yceride with nat:urcll luhri.cànts, the ease of blend;rlcj of the lub.ricant ~J:ith natur,lL moistur~
wllich may be present, -the spreadincJ of -the lubricant throughout the canal, and -the efEectiveness of very small residual amounts o:~ -the lubricant.
The invention is illustrated in more detail in the following non-llmi-ting Example.
. Exam? e A solid suppository was cast from the following formulation.
Ingred.ient Parts by l~Jeight ~=.
Polye-thylene . glycol, 25 average molecular weicJh-t 1300-1600, solidifying range 40-509 C., soft, white waxy solid, sol-~bility in water at 2Q C., approximate]y 70% (weight/weight), pEI
of a 5O aqueous solution about 6.5 ~CARBOWAX~ 1540) Polyet~ylene glycol, 25 average molecular weight 950-1050, solidifyi.ng -- range 35-40 C., solubility in water at 20 CO about 70% on a weight/weight basis (CARBOWAX~`? 1000) Glycerin 10 Polyoxyethylene t23) lauryl 10 ether (BRIJ3 351 Polyoxyethylene (20) sorbitan 5* .`
mono-oleate (TWEEN~ 80) ~-Polyoxyethylene (40) s-tearate 5 ;-(''MYRJI' 52-5 [trademark]) *Alternatively, can be replaced with more BRIJ or MYRJ.
~36~
Fract:iondtecl-tri~lyccricle 20 of COCOIlUt oric~in (caprylic/capric tri-c~lyceride, "N~O~E~
~I-5" [trademark]) The ~ILB value of the polyoxyethy]ene lauryl e-ther and the polyoxye-thylene s-tearate is normally within the ranye of 16.5 to 17. The HLB value of the polyoxyethylene sorbitan mono-o:Lea-te is normally 15. Accordinyly, the average HLB value of the nonionic surfactant system of this invention is above 16. The glycol component was melted and main-tained within the temperature range of 55-70 C.
during manufacture of the suppository composi-tion.
Manufacture was carried out on a batch basis, but can also be done continuously.
One ~art of antioxidant, B~IT (butylated hydroxy toluene) was added to 10,000 parts of the composition described above. A suppository cast from this composition was 30 ~m in length and 13 mm wide at its widest point. (Suppositories 10-50 mm in length and 2-20 mm in width can easily be cast and molded.) Although not ordinarily preferred, medicaments related to coitus such as spermicides and bactericides may be added to suppository compositions of -this ~ invention.
Throughout this applicatlon, the terms "polyethylene glycol" and "polyoxyethylene glycol"
are used synonymously.
~-.
.
Claims (11)
1. A lubricating suppository for the human vaginal canal, which suppository is solid at normal ambient temperatures but melts at human body temperature to form a substantially homogeneous liquid having the appearance of a single liquid phase, said suppository comprising:
(a) a continuous phase comprising a water soluble polyoxy-alkylene polyol component consisting essentially of polyoxyethylene glycol having a molecular weight within the range of 400 to 5000, said component being formulated to have a melting range low enough to ensure the formation of a clear molten liquid at less than about 75°C.;
(b) about 10-60 parts per one hundred parts by weight of said polyoxyalkylene polyol component, of a nonionic surfactant having an HLB value greater than 12, said nonionic surfactant being uniformly distributed through said continuous phase;
(c) about 10-40 parts per hundred, based on the weight of said polyoxyalkylene polyol component, of a C6-C12 aliphatic carboxylic acid glyceride said glyceride being uniformly distri-buted throughout said continuous phase with the aid of said non-ionic surfactant;
said lubricating suppository, in either the solid or molten state, having sufficient compatibility with water to be readily uniformly distributable in water.
- Page one of Claims -
(a) a continuous phase comprising a water soluble polyoxy-alkylene polyol component consisting essentially of polyoxyethylene glycol having a molecular weight within the range of 400 to 5000, said component being formulated to have a melting range low enough to ensure the formation of a clear molten liquid at less than about 75°C.;
(b) about 10-60 parts per one hundred parts by weight of said polyoxyalkylene polyol component, of a nonionic surfactant having an HLB value greater than 12, said nonionic surfactant being uniformly distributed through said continuous phase;
(c) about 10-40 parts per hundred, based on the weight of said polyoxyalkylene polyol component, of a C6-C12 aliphatic carboxylic acid glyceride said glyceride being uniformly distri-buted throughout said continuous phase with the aid of said non-ionic surfactant;
said lubricating suppository, in either the solid or molten state, having sufficient compatibility with water to be readily uniformly distributable in water.
- Page one of Claims -
2. A suppository according to claim 1 wherein said continuous phase further comprises a lower aliphatic monomeric hydrophi1ic polyol dissolved in said continuous phase.
3. A suppository according to claim 2 wherein said hydro-philic polyol is glycerin.
4. A suppository according to claim 1 wherein said nonionic surfactant comprises a blend of oxyethylene chain-containing esters or ethers, said blend having an HLB value above about 14, the ester or ether functional groups of said esters or ethers comprising a higher aliphatic residue.
5. A suppository according to claim 4 wherein said HLB
value is less than about 18.
value is less than about 18.
6. A suppository according to claim 1 consisting essentially of:
(a) 50-70% by weight of a blend of polyoxyethylene glycols with a molecular weight within the range of about 900 to about 2000, which blend at least begins to melt at temperatures no higher than about 50 C.;
(b) dispersed in said blend of polyoxyethylene glycols, 10-20% by weight of a triglyceride of at least one C6-C12 saturated aliphatic carboxylic acids;
(c) dissolved in said blend of polyethylene glycols, 10-30% by weight of a blend of nonionic surfactants selected from the group consisting of poly(oxyethylene) polyol esters, - Page two of Claims -poly(oxyethylene) polyol ethers, and mixtures thereof, said blend having a weight-average HLB value of at least about 14; and (d) 0-20% by weight of glycerin dissolved in said blend of polyoxyethylene glycols.
(a) 50-70% by weight of a blend of polyoxyethylene glycols with a molecular weight within the range of about 900 to about 2000, which blend at least begins to melt at temperatures no higher than about 50 C.;
(b) dispersed in said blend of polyoxyethylene glycols, 10-20% by weight of a triglyceride of at least one C6-C12 saturated aliphatic carboxylic acids;
(c) dissolved in said blend of polyethylene glycols, 10-30% by weight of a blend of nonionic surfactants selected from the group consisting of poly(oxyethylene) polyol esters, - Page two of Claims -poly(oxyethylene) polyol ethers, and mixtures thereof, said blend having a weight-average HLB value of at least about 14; and (d) 0-20% by weight of glycerin dissolved in said blend of polyoxyethylene glycols.
7. A suppository according to claim 6 which further includes an effective amount of an antioxidant.
8. A solid, pre-coital, vaginal lubricant suppository which melts at 37°C., said suppository having been cast and soli-dified from a generally homogeneous molten mass comprising:
a continuous phase consisting essentially of:
(a) 50-70% by weight, based on the weight of the suppository, of a blend of glycols consisting essentially of:
(1) a polyoxyethylene glycol having an average molecular weight of 900-1100, and (2) a polyoxyethylene glycol having an average molecular weight of 1200-1700, the ratio of glycol (2) to glycol (1) ranging from about 1:1 to about 4:1;
(b) 5-20% by weight, based on the weight of the suppository, of glycerin;
(c) 10-30% by weight, based on the weight of the suppository, of a combination of nonionic surfactants having a weighted-average HLB value of about 14 to about 18, said combination comprising polyoxyethylene lauryl ether and polyoxyethylene stearate; and (d) as a discontinuous phase emulsified in and distributed uniformly throughout said continuous phase, a triglyceride of coconut origin containing caprylic and capric acid residues.
- Page three of Claims -
a continuous phase consisting essentially of:
(a) 50-70% by weight, based on the weight of the suppository, of a blend of glycols consisting essentially of:
(1) a polyoxyethylene glycol having an average molecular weight of 900-1100, and (2) a polyoxyethylene glycol having an average molecular weight of 1200-1700, the ratio of glycol (2) to glycol (1) ranging from about 1:1 to about 4:1;
(b) 5-20% by weight, based on the weight of the suppository, of glycerin;
(c) 10-30% by weight, based on the weight of the suppository, of a combination of nonionic surfactants having a weighted-average HLB value of about 14 to about 18, said combination comprising polyoxyethylene lauryl ether and polyoxyethylene stearate; and (d) as a discontinuous phase emulsified in and distributed uniformly throughout said continuous phase, a triglyceride of coconut origin containing caprylic and capric acid residues.
- Page three of Claims -
9. A suppository according to claim 8 comprising:
50% by weight of said glycol blend, 20% by weight of said triglyceride, 10% by weight of glycerin, 10-15% by weight of a polyoxyethylene lauryl ether having an HLB value of about 16.5 to about 17, 0-5% by weight of a polyoxyethylene sorbitan mono-oleate having an HLB value of about 15, 5-10% by weight of a polyoxyethylene stearate having an HLB value of about 16.5 to about 17, and an effective amount of an alkylated hydroxyaromatic antioxidant.
50% by weight of said glycol blend, 20% by weight of said triglyceride, 10% by weight of glycerin, 10-15% by weight of a polyoxyethylene lauryl ether having an HLB value of about 16.5 to about 17, 0-5% by weight of a polyoxyethylene sorbitan mono-oleate having an HLB value of about 15, 5-10% by weight of a polyoxyethylene stearate having an HLB value of about 16.5 to about 17, and an effective amount of an alkylated hydroxyaromatic antioxidant.
10. A method for pre-coitally lubricating the human vagina with a liquid lubricant comprising the step of:
(a) inserting a solid suppository of claim 1 into the vagina, and (b) permitting said suppository to melt within the vagina prior to coitus to form a water-compatible, lubricitous liquid coital lubricant.
(a) inserting a solid suppository of claim 1 into the vagina, and (b) permitting said suppository to melt within the vagina prior to coitus to form a water-compatible, lubricitous liquid coital lubricant.
11. A method for making a lubricating suppository which is solid at room temperature but melts at human body temperature, comprising the following steps:
(a) melting a blend of solid polyoxyethylene glycols at a temperature above normal ambient temperatures but below about 75°C., thereby obtaining a homogeneous melt;
(b) dissolving in the melt about 10-60 parts by weight, per 100 parts by weight of said polyoxyethylene glycols, of nonionic - Page four of Claims -surfactant having an HLB value above 12, while maintaining the melt at a temperature above normal ambient;
(c) distributing throughout the melt produced by step (b) about 10-40 parts by weight, per 100 parts by weight of said polyoxyethylene glycols a solid glyceride of at least one C6-C12 aliphatic carboxylic acid, until said solid glyceride forms a discontinuous phase uniformly distributed through the melt produced by step (b) and emulsified in said melt, while maintaining the resulting emulsified, two-phase melt at a temperature above normal ambient; and (d) casting portions of the resulting two-phase melt into the form of suppositories and solidifying the thus-cast portions.
- Page five of Claims -
(a) melting a blend of solid polyoxyethylene glycols at a temperature above normal ambient temperatures but below about 75°C., thereby obtaining a homogeneous melt;
(b) dissolving in the melt about 10-60 parts by weight, per 100 parts by weight of said polyoxyethylene glycols, of nonionic - Page four of Claims -surfactant having an HLB value above 12, while maintaining the melt at a temperature above normal ambient;
(c) distributing throughout the melt produced by step (b) about 10-40 parts by weight, per 100 parts by weight of said polyoxyethylene glycols a solid glyceride of at least one C6-C12 aliphatic carboxylic acid, until said solid glyceride forms a discontinuous phase uniformly distributed through the melt produced by step (b) and emulsified in said melt, while maintaining the resulting emulsified, two-phase melt at a temperature above normal ambient; and (d) casting portions of the resulting two-phase melt into the form of suppositories and solidifying the thus-cast portions.
- Page five of Claims -
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000410297A CA1196865A (en) | 1982-08-27 | 1982-08-27 | Lubricating suppository and method for making and using same |
| JP1635485A JPS61176522A (en) | 1982-08-27 | 1985-01-30 | Suppository for lubrication |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000410297A CA1196865A (en) | 1982-08-27 | 1982-08-27 | Lubricating suppository and method for making and using same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1196865A true CA1196865A (en) | 1985-11-19 |
Family
ID=4123488
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000410297A Expired CA1196865A (en) | 1982-08-27 | 1982-08-27 | Lubricating suppository and method for making and using same |
Country Status (2)
| Country | Link |
|---|---|
| JP (1) | JPS61176522A (en) |
| CA (1) | CA1196865A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0940138A1 (en) * | 1996-07-04 | 1999-09-08 | Seiken Chemical Co., Ltd. | Lubrication assistant and process for the preparation of ethyl stearate used therein |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4912089B2 (en) * | 2006-08-30 | 2012-04-04 | 京セラ株式会社 | Optical printer head |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6030650B2 (en) * | 1979-10-26 | 1985-07-17 | 日本油脂株式会社 | Suppository base composition |
| JPS5770824A (en) * | 1980-10-20 | 1982-05-01 | Nippon Saafuakutanto Kogyo Kk | Vehicle for medicine |
| JPS57131727A (en) * | 1981-02-09 | 1982-08-14 | Sumitomo Chem Co Ltd | Suppository base |
-
1982
- 1982-08-27 CA CA000410297A patent/CA1196865A/en not_active Expired
-
1985
- 1985-01-30 JP JP1635485A patent/JPS61176522A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0940138A1 (en) * | 1996-07-04 | 1999-09-08 | Seiken Chemical Co., Ltd. | Lubrication assistant and process for the preparation of ethyl stearate used therein |
| EP0940138A4 (en) * | 1996-07-04 | 2001-03-21 | Kimiko Yoshimizu | Lubrication assistant and process for the preparation of ethyl stearate used therein |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS61176522A (en) | 1986-08-08 |
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