CN105007949A - Coating composition, coated preparation and method for producing same - Google Patents
Coating composition, coated preparation and method for producing same Download PDFInfo
- Publication number
- CN105007949A CN105007949A CN201480012829.1A CN201480012829A CN105007949A CN 105007949 A CN105007949 A CN 105007949A CN 201480012829 A CN201480012829 A CN 201480012829A CN 105007949 A CN105007949 A CN 105007949A
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- CN
- China
- Prior art keywords
- coating
- coated
- composition
- alginate
- coated composition
- Prior art date
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- 239000003795 chemical substances by application Substances 0.000 description 1
- 229910052802 copper Inorganic materials 0.000 description 1
- 239000010949 copper Substances 0.000 description 1
- 229910001431 copper ion Inorganic materials 0.000 description 1
- 239000012228 culture supernatant Substances 0.000 description 1
- 229960003067 cystine Drugs 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 1
- 238000003618 dip coating Methods 0.000 description 1
- 238000009826 distribution Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 235000012732 erythrosine Nutrition 0.000 description 1
- 235000019441 ethanol Nutrition 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 235000021433 fructose syrup Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 229910052737 gold Inorganic materials 0.000 description 1
- 239000010931 gold Substances 0.000 description 1
- 235000009569 green tea Nutrition 0.000 description 1
- 229920000591 gum Polymers 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N iron oxide Inorganic materials [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 1
- WTFXARWRTYJXII-UHFFFAOYSA-N iron(2+);iron(3+);oxygen(2-) Chemical compound [O-2].[O-2].[O-2].[O-2].[Fe+2].[Fe+3].[Fe+3] WTFXARWRTYJXII-UHFFFAOYSA-N 0.000 description 1
- SZVJSHCCFOBDDC-UHFFFAOYSA-N iron(II,III) oxide Inorganic materials O=[Fe]O[Fe]O[Fe]=O SZVJSHCCFOBDDC-UHFFFAOYSA-N 0.000 description 1
- JEIPFZHSYJVQDO-UHFFFAOYSA-N iron(III) oxide Inorganic materials O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 1
- YOBAEOGBNPPUQV-UHFFFAOYSA-N iron;trihydrate Chemical compound O.O.O.[Fe].[Fe] YOBAEOGBNPPUQV-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000010410 layer Substances 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 229940105082 medicinal charcoal Drugs 0.000 description 1
- 150000002711 medium chain fatty acid esters Chemical class 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 239000011859 microparticle Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 235000014593 oils and fats Nutrition 0.000 description 1
- NDLPOXTZKUMGOV-UHFFFAOYSA-N oxo(oxoferriooxy)iron hydrate Chemical compound O.O=[Fe]O[Fe]=O NDLPOXTZKUMGOV-UHFFFAOYSA-N 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 210000000229 preadipocyte Anatomy 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- 229920002414 procyanidin Polymers 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 229950001574 riboflavin phosphate Drugs 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000013049 sediment Substances 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 235000012751 sunset yellow FCF Nutrition 0.000 description 1
- 239000004173 sunset yellow FCF Substances 0.000 description 1
- 229940087291 tridecyl alcohol Drugs 0.000 description 1
- 230000009278 visceral effect Effects 0.000 description 1
- NCYCYZXNIZJOKI-UHFFFAOYSA-N vitamin A aldehyde Natural products O=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-UHFFFAOYSA-N 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- OENHQHLEOONYIE-JLTXGRSLSA-N β-Carotene Chemical compound CC=1CCCC(C)(C)C=1\C=C\C(\C)=C\C=C\C(\C)=C\C=C\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C OENHQHLEOONYIE-JLTXGRSLSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
Abstract
Provided is a coating composition which contains (A) an alginic acid salt and (B) a plasticizer, and which is capable of delivering a coated material such as a coated active ingredient to the intestine since the coating composition does not dissolve in the stomach but dissolves in the intestine. This coating composition has excellent coating properties and is capable of providing a uniform coating without chipping or peeling. Also provided is a coated preparation which is coated with this coating composition.
Description
Technical field
The present invention relates to the coated composition, coated preparation and the manufacture method thereof that use in the coating of food, pharmaceuticals etc.
Background technology
Need following Enteric formulations: have as the functional component of the protein such as lactobacillus and enzyme, by preventing from keeping its structure in the decomposition of gastric, it is made to arrive intestinal thus the effective ingredient of performance high functionality, said preparation does not dissolve at gastric and dissolves in intestinal, and effective ingredient is arrived in intestinal.
As the protecting film in order to make effective ingredient arrive intestinal; do not dissolve under generally having pH condition (acidity) under one's belt and the composition of dissolving under the pH condition (neutral ~ alkalescence) of small intestinal, such as metha crylic macromolecular compound, Lac, zein etc.
But metha crylic macromolecular compound is only limitted to pharmaceuticals purposes, food can not be used for.On the other hand, although Lac, zein also may be used for food applications, generally with an organic solvent spray.Even in food applications, also expect to utilize consider environment, available water carries out the water solublity membrane of coating.
Prior art document
Patent documentation
Patent documentation 1: Japanese Patent Laid-Open 2002-193792 publication
Summary of the invention
The problem that invention will solve
The object of the present invention is to provide a kind of coated composition, by the coated preparation of this coated composition coating and manufacture method thereof, described coated composition does not dissolve at gastric and dissolves in intestinal, can make to be arrived intestinal by the effective ingredient of coating etc. by coating thing, defect does not occur and comes off and can carry out coating equably, coating is excellent.
The means of dealing with problems
The present inventor finds: the coated composition containing alginate and plasticizer does not dissolve at gastric and dissolves in intestinal, effective ingredient etc. can be made to be arrived intestinal by coating thing, and coating is excellent, thus completes the present invention.
Therefore, the invention provides following invention.
[1]. a kind of coated composition, it contains (A) alginate and (B) plasticizer.
[2]. the coated composition as described in [1], wherein (A) composition is the alginate being selected from alginic acid sodium salt, alginic acid potassium salt and alginic acid ammonium salt.
[3]. the coated composition as described in [1] or [2], wherein (A) composition is the alginate (A-1) of the viscosity of 1 quality % aqueous solution at 20 DEG C more than 50mPas.
[4]. the coated composition as described in [1] or [2], the wherein alginate (A-2) of (A) composition to be the viscosity of 1 quality % aqueous solution at 20 DEG C more than the alginate (A-1) of 50mPas and the viscosity of 1 quality % aqueous solution at 20 DEG C be below 50mPas.
[5]. as the coated composition according to any one of [1] ~ [4], it is selected from the composition of gelatin, pectin, curdlan, pulullan polysaccharide, arabic gum, xanthan gum, gellan gum, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose and hydroxypropyl cellulose further containing (C).
[6]. as the coated composition according to any one of [1] ~ [5], it is further containing (D) microgranule.
[7]. as the coated composition according to any one of [1] ~ [6], wherein (B) composition is glycerol and/or sucrose fatty acid ester.
[8]. as the coated composition according to any one of [1] ~ [7], wherein with (A): what (C) represented is 1:10 ~ 20:1 containing mass ratio.
[9]. a kind of coated preparation, it has the coating membrane that the coated composition according to any one of [1] ~ [8] is formed.
[10]. the enteric coatings preparation as described in [9], the enteric coatings preparation of its to be coating membrane be enteric solubility.
[11]. a kind of manufacture method of coated preparation, it comprises following operation: to also dry by the Coating Solution of coating thing spraying containing the coated composition according to any one of [1] ~ [8] and water, thus formed coating membrane by the surface of coating thing.
The effect of invention
The present invention can provide coated composition, by the coated preparation of this coated composition coating and manufacture method thereof, described coated composition does not dissolve at gastric and dissolves in intestinal, can make to be arrived intestinal by the effective ingredient of coating, and coating is excellent.
Accompanying drawing explanation
Fig. 1 is the chart providing test example result.
Detailed description of the invention
Below, the present invention is described in detail.
(I) coated composition
Coated composition of the present invention contains (A) alginate and (B) plasticizer.
(A) alginate
Monovalence alginate, the alginic acid water soluble salts such as alginate particular certain cancers, potassium salt, ammonium salt.Can enumerate the viscosity of (A-1) 1 quality % aqueous solution at 20 DEG C more than the alginate of 50mPas, the viscosity of (A-2) 1 quality % aqueous solution at 20 DEG C as alginate is the alginate of below 50mPas, can be used alone a kind of or appropriately combined two or more use.
(A-1) viscosity of 1 quality % aqueous solution at 20 DEG C more than the alginate of 50mPas preferably greater than 50mPas and the alginate of below 600mPas, more preferably above 50mPas and the alginate of below 400mPas.
(A-2) viscosity of 1 quality % aqueous solution at 20 DEG C is the alginate of the preferred 5 ~ 50mPas of alginate of below 50mPas, the more preferably alginate of 10 ~ 50mPas.(A-2) the preferred alginic acid sodium salt of alginate.
Relative to coated composition, the combined amount of (A) composition preferably 5 ~ 85 quality % (solids: when being denoted as solids is below the ratio relative to the composition total amount after desolventizing, identical with the ratio in coating membrane.)。More preferably the scope of 10 ~ 80 quality % (solids), the further scope of preferred 10 ~ 70 quality % (solids), further preferred 10 ~ 60 quality % (solids).
When mixing (A-1) alginate, relative to coated composition, combined amount is 5 ~ 85 quality % (solids) preferably, more preferably 10 ~ 60 quality % (solids), further the scope of preferred 20 ~ 50 quality % (solids).By more than above-mentioned scope, better enteric solubility can be obtained.By below above-mentioned scope, adhesion when can prevent coating and come off and obtain good coating performance.
When mixing (A-2) alginate, relative to coated composition, combined amount preferably 85 quality % (solids) below, more preferably 5 ~ 50 quality % (solids), the further scope of preferred 10 ~ 40 quality % (solids).By more than above-mentioned scope, enteric solubility improves, and coating is good.
In the present invention, (A) alginate preferably uses (A-1) alginate.By using the alginate of so certain above length, coating is good, can give the coating membrane of formation with highly-acidproof.In addition, by also with (A-1) alginate and (A-2) alginate, while maintenance enteric solubility, more coating performance can be improved.
The alginate of two kinds of different viscosities as above-mentioned (A-1) alginate and (A-2) alginate is used not to be only from the viewpoint of regulating coating solution viscosity but selecting two kinds of alginates from enteric solubility and coating.Its mass ratio (A-1): (A-2) ((A-1)/(A-2)) be 1:5 ~ 10:1 (0.2 ~ 10) preferably, more preferably 1:3 ~ 5:1 (0.33 ~ 5), further preferred 1:1.8 ~ 3:1 (0.56 ~ 3).By more than lower limit, the epithelium performance under acidify is higher, and therefore stripping property is not good.By below the upper limit, coating is better.
In addition, in the present invention, the viscosimetric analysis of alginate uses rotary viscosimeter (BM type) to carry out.Use rotor No.1 less than the viscosity of 200mPas, more than 200mPas and use rotor No.2 less than the viscosity of 1,000mPas, 20 DEG C, measure 1 quality % aqueous solution under the condition of 30rpm, get the value after 60 seconds as measured value.
The viscosity of alginate is roughly directly proportional to the molecular weight of alginate.The weight average molecular weight (Mw) of such as above-mentioned (A-1) is more than 800,000, preferably 80 ~ less than 3,000,000, more preferably molecular weight 80 ~ less than 1,900,000.(A-2) weight average molecular weight (Mw) is more than 200,000 and less than 800,000, preferably more than 300,000 and less than 800,000.In addition, the gel chromatography assay method of the weight average molecular weight (Mw) of alginate of the present invention is as follows.
(1) preparation of sample
Alginate is dissolved in mobile phase (0.1M (mol/L) NaNO
3aqueous solution) in, make alginate concentration be 0.1 quality %, in this, as sample.
The standard substance of various molecular weight (pulullan polysaccharide: Mw=166 ten thousand, Mw=38 ten thousand, Mw=10 ten thousand, Mw=1.22 ten thousand dissolve with 0.1 quality % concentration in mobile phase) are used to make standard curve.
(2) GPC condition determination
Chromatographic column: Shodex OHpak SB-806M HQ (8mmI.D. × 300mmL., 13 μm)
Mobile phase: 0.1M (mol/L) NaNO
3aqueous solution
Flow: 0.5mL/min
Temperature: 40 DEG C
Sample size: 200 μ L (in mobile phase 0.1%)
Detector: differential refraction rate (RI) detector
(3) analytical method
Try to achieve standard curve formula by standard curve sample, gpc analysis result per sample, try to achieve the weight average molecular weight (Mw) being converted into pulullan polysaccharide.
(B) plasticizer
Plasticizer can enumerate the surfactants such as sucrose fatty acid ester, fatty acid glyceride, fatty acid monoglyceride, polyoxyethylene sorbitan fatty acid ester; The polyhydric alcohol such as glycerol, propylene glycol, Polyethylene Glycol; The sugar such as glucose, high fructose syrup, sucrose; The sugar alcohols such as Sorbitol, maltose alcohol, mannitol, erythritol, xylitol; The higher alcohol of dodecanol, tridecyl alcohol, tetradecanol, pentadecanol, hexadecanol, heptadecanol, octadecanol, hexadecanol, isooctadecanol, 2-octyldodecanol etc. (suitable is carbon number 6 ~ 22); The oils and fatss such as medium chain fatty acid ester (suitable is carbon number 6 ~ 12).They can one be used alone or appropriately combined two or more use.Wherein, from the viewpoint of the plasticization effect of coating membrane, preferably glycerine, from the viewpoint of enteric solubility, preferred surfactant, more preferably glycerol and/or sucrose fatty acid ester.
Relative to coated composition, combined amount preferably 0.1 ~ 70 quality % (solids) of (B) component, more preferably 2 ~ 50 quality % (solids).By more than above-mentioned scope, film during coating more can be suppressed to come off, by below above-mentioned scope, viscosity during coating can be suppressed, the while that Cotton seeds becoming easier, good enteric solubility can be obtained.
The mass ratio represented with (B)/(A) preferably 0.05 ~ 3.0 scope, more preferably 0.1 ~ 2.0, further preferably 0.15 ~ 1.5, particularly preferably 0.15 ~ 1.1.By in above-mentioned scope, the epithelium performance under acidify is higher, and by below the upper limit, coating is better.
Also the epithelium forming component beyond (A) can be mixed in coated composition of the present invention.(C) epithelium forms that component can enumerate gelatin, pectin, curdlan, pulullan polysaccharide, arabic gum, xanthan gum, gellan gum, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, agar, chitosan, tamarind gum, locust bean gum, polyvinyl alcohol, aqueous ethylcellulose fall apart liquid etc.They can be used alone a kind of or appropriately combined two or more use.Wherein, consider from coating and with the angle that (A) composition combines, be preferably selected from the composition of gelatin, pectin, curdlan, pulullan polysaccharide, arabic gum, xanthan gum, gellan gum, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose and hydroxypropyl cellulose.
Now, with (A): the preferred 1:10 ~ 20:1 of mass ratio (0.1 ~ 20) that (C) ((A)/(C)) represents, more preferably 1:5 ~ 20:1 (0.2 ~ 20), further preferred 1:1 ~ 10:1 (1 ~ 10).By within the scope of this, can obtain on the basis keeping coating and appearance looks elegant, the tablet of the enteric excellent performance that the epithelium performance particularly under acidity is higher.
Relative to coated composition, combined amount preferably 1 ~ 90 quality % (solids) of (C) component, more preferably 5 ~ 80 quality % (solids), further preferred 10 ~ 80 quality % (solids).By more than above-mentioned scope, the effect of mixing (C) composition can be obtained better, mix if exceed above-mentioned scope, then likely enteric solubility is had an impact.
Also (D) microgranule can be mixed in coated composition.By hybrid fine particles, can prevent the coating membrane caused owing to mutually adhering between tablet during Cotton seeds from coming off.(D) component can exemplify Pulvis Talci, calcium stearate, silicon dioxide, titanium oxide etc., can be used alone a kind of or appropriately combined two or more use.The particle diameter of microgranule is 0.01 ~ 50 μm, preferably 0.1 ~ 20 μm.In addition, the mensuration of particle diameter uses laser diffraction formula particle size distribution device (dry type mensuration) to carry out.
Relative to coated composition, combined amount preferably 1 ~ 80 quality % (solids) of (D) composition, more preferably 3 ~ 60 quality % (solids), further preferred 5 ~ 40 quality % (solids).By more than above-mentioned scope, the effect of mixing above-mentioned (D) composition can be obtained better, mix if exceed above-mentioned scope, then likely film property is had an impact.
In addition, preferably the bivalent metal ions such as copper ion, barium ions, calcium ion are not comprised in coated composition.Because alginate occurs to be cross-linked and gelation by these ions, coating is deteriorated.That is, when making monovalence alginate and bivalent cation react to make it crosslinked, although the film of drying is water-insoluble, owing to becoming too high because of gelation viscosity, therefore the spraying of fine liquid and the ductility on tablet become difficult.As a result, be difficult to form uniform epithelium, degraded appearance, in addition, stripping property is unstable sometimes.Relative to the monomer 1 mole of alginate, the allowed band of bivalent metal ion preferably less than 0.25 mole, more preferably less than 0.1 mole.
In coated composition of the present invention, except above-mentioned (A) ~ (D) composition, normally used composition in the two or more coated composition of a kind of or appropriate mixing can also be used alone.Any conduct like this can enumerate defoamer, coloring agent etc.
Defoamer include, for example fatty acid glyceride, dimethyl polysiloxane, dimethyl polysiloxane silica mixture, aqueous silicon dioxide, silicon dioxide etc., can be used alone a kind of or appropriately combined two or more use.
Coloring agent can enumerate such as catechutannic acid powder, Rhizoma Curcumae Longae extracting solution, Yellow ferric oxide, citrusreticulata oil elite, brown iron oxide, white carbon black, caramel, carmine, carotene liquid, beta-carotene, Radix Glycyrrhizae extract, native gold, black iron oxide, light silicon anhydride, titanium oxide, iron sesquioxide, edible blue No. 1, edible yellow No. 4, edible yellow No. 4 aluminum colors form sediment, edible Sunset Yellow FCF, edible Amaranth, edible red No. 3, edible red No. 102, sodium hydroxide, chlorophyll copper sodium, copper chlorophyll, Fructus Hordei Vulgaris greenery extract, medicinal charcoal, Riboflavine Tertrabutyrate, riboflavin, green tea powder, riboflavin sodium phosphate etc.
In the scope not damaging effect of the present invention, coated composition of the present invention can contain the organic solvent such as water, ethanol.Relative to whole coated composition, the solvent combined amount in coated composition is suitable in the scope of 1 ~ 98 quality % selected, preferably 50 ~ 98 quality %, more preferably 70 ~ 96 quality %.
(II) coated preparation
Using above-mentioned coated composition, coating thing being formed the coating membrane formed by coated composition, coated preparation can be obtained.
The coating membrane formed by coated composition of the present invention contains above-mentioned (A) composition, but as described later alginic acid aqueous solution convection drying is formed water miscible film.This water miscible film has following characteristic: under acidity, and monovalent cation and hydrion are replaced, and become alginic acid and form insoluble film, dissolve further under neutrality ~ alkalescence.
Coated composition of the present invention and the coating membrane formed by this coated composition have enteric solubility, namely have the character of " do not dissolve at gastric and dissolve in intestinal, can make to be arrived intestinal by coating thing ".Obtain the enteric coatings preparation that coating membrane is enteric solubility.
" enteric solubility " in the present invention is the preparation of instigating functional components to arrive intestinal.Refer to that the method for the dissolution test method according to Japanese Pharmacopoeia is tested, in the dissolution test liquid (pH1.2) being equivalent to gastric juice, 2 hours dissolution rates are less than 50% (suitable is less than 30%), and in the dissolution test liquid (pH6.8) being equivalent to intestinal juice, the dissolution rate of 2 hours is more than 70%.
Be not particularly limited by the shape of coating thing, dosage form, be not particularly limited in tablet, powder, fine grained agent, granule etc.Tablet can be monolayer also can be more than two layers.Wherein, consider from the angle playing enteric solubility better, preferred tablet.The size of tablet is not particularly limited, and easily processes and the property swallowed from the viewpoint of tablet, and the diameter of tablet is preferred
more preferably
in addition, the quality of every sheet tablet is suitably for about 150 ~ 700mg.
The thickness of coating membrane is not particularly limited, preferably 5 μm ~ 1mm, more preferably 10 ~ 500 μm.In addition, when tablet, relative to coated preparation, coating membrane is 0.5 ~ 20 quality % preferably, more preferably 1 ~ 15 quality %.When granule, powder, powder, preferably 10 ~ 60 quality %, more preferably 15 ~ 50 quality %.In addition, in coating membrane, the content (solids) of above-mentioned each composition is identical with above-mentioned coated composition.
Be not particularly limited by coating thing, the effective ingredient such as food, pharmaceuticals etc. can be enumerated.Include, for example the protein such as lactobacillus, cystine, ferrum, antibody and lactoferrin, peptide, ATP-2Na etc., they can be used alone a kind of or appropriately combined two or more use.Wherein be advisable with the high molecular weight components such as protein and water insoluble active ingredient.
(III) manufacture method of coated preparation
Coated composition can by mixing is above-mentioned must component and obtaining, coated preparation can obtain by the following method: to by coating thing direct spraying coated composition, or spraying has added the Coating Solution of water, and dry and formed coating membrane by the surface of coating thing.Coated composition of the present invention is aqueous, and water therefore can be used to carry out coating, forms water-solubility membrane.
Coating Solution contains coated composition and water, water quantities preferably 50 ~ 98 quality % of Coating Solution, more preferably 70 ~ 96 quality %.In addition, in the scope not damaging effect of the present invention, the organic solvents such as all right mixed ethanol.
Seed-coating machine is not particularly limited, and can use pan coater (パ ン コ ー テ ィ ン グ Machine), fluidized-bed coating machine, drum type coating machine etc.
Coating method is not particularly limited, and include, for example by by coating thing spraying Coating Solution and heat drying and making by the method for the surperficial membranization of coating thing.Coating Solution can suitably heat, temperature preferably 30 ~ 80 DEG C, baking temperature preferably 40 ~ 80 DEG C.Relative to dry air quantity 1m
3/ min, the interpolation speed preferably 1 ~ 5g/min of Coating Solution.In addition, also can use and will be impregnated into dip-coating method dry after in Coating Solution by coating thing.Preferably the water quantities in coated preparation is dried to 0.1 ~ 20 quality %.
Embodiment
Below, provide embodiment and comparative example illustrates the present invention, but the present invention is not restricted to following embodiment.In addition, in following example if no special instructions, " % " of composition represents quality %, and ratio represents mass ratio.
Embodiment 1 ~ 78, comparative example 1 ~ 4
The plain sheet that preparation is following, prepares the Coating Solution of composition shown in following table 1 ~ 22, and coating element sheet, prepares coated tablet by the following method.
[plain sheet]
Mix following raw material, use tablet machine be pressed into tablet (300mg,
thickness 5mm).
< element sheet composition >
Lactoferrin: 1,156g
Piper longum (ヒ Ha Star) extract powder: 500g
Lactose: 492.5g
Microcrystalline Cellulose: 731.5g
Sodium carboxymethyl cellulose: 60g
Sucrose fatty acid ester: 30g
Silicon dioxide microparticle: 30g
[preparation of Coating Solution]
By (A) and (C) composition in the Coating Solution composition described in table 1 ~ 22, uniform dissolution is in hot water respectively, and the liquid after mixed dissolution, adds other composition, further mix and blend.In addition, the right hurdle in table represents solids (%).
[coating]
(POWREX (パ ウ レ ッ Network) makes to use seed-coating machine, POWREX COATER-PRC-05), with average 2g/min, plain sheet 200g is sprayed with Coating Solution (60 DEG C) 100g, at product temperature about 50 DEG C, implement coating.After spraying at about 45 DEG C dry 2 minutes, obtain coating materials (tablet).The thickness of coating membrane is in the scope of 10 ~ 200 μm.
[acid pH not stripping property test]
Use Japanese Pharmacopoeia 1 liquid (pH 1.2), carry out dissolution test according to Japanese Pharmacopoeia ordinary test method (paddle method).
The stripping property of ◎: 2 hours is below 10%
The stripping property of zero: 2 hour is more than 10% and below 30%
The stripping property of △: 2 hours is more than 30% and less than 50%
×: the stripping property of 2 hours is below 50%
[neutrality ~ alkaline pH stripping property test]
Use Japanese Pharmacopoeia 2 liquid (pH6.8), carry out dissolution test according to Japanese Pharmacopoeia ordinary test method (paddle method).
The stripping property of zero: 2 hour is more than 70%
The stripping property of △: 2 hours is more than 30% and less than 70%
×: the stripping property of 2 hours is less than 30%
In addition, in above-mentioned [test of acid pH stripping property], be " △ ", "○" or " ◎ " and be decided to be " enteric solubility " for when "○" in above-mentioned [neutrality ~ alkaline pH stripping property test].
[coating]
Based on following metewand, assessment coating.
◎: evenly coating, do not see defect, come off, coating surface is glossy.
Zero: evenly coating, almost do not see defect, come off, but coating surface is slightly chapped.
△: the defect of visible coating on a part of tablet.
×: on nearly all tablet all visible coating defect or come off.
[table 1]
[table 2]
[table 3]
[table 4]
[table 5]
[table 6]
[table 7]
[table 8]
[table 9]
[table 10]
[table 11]
[table 12]
[table 13]
[table 14]
[table 15]
[table 16]
[table 17]
[table 18]
[table 19]
[table 20]
[table 21]
[table 22]
As follows relative to the calcium ion molal quantity of the alginate monomer 1 mole of embodiment 75 ~ 78.
Embodiment 75:0.014mol
Embodiment 76:0.027mol
Embodiment 77:0.041mol
Embodiment 78:0.054mol
< test example 1>
Coated tablet 6 prepared by embodiment 38 and embodiment 53, comparative example 1,2 is put into 37 DEG C, the liquid of the pH1.2 (Japanese Pharmacopoeia 1 liquid+pepsin dissolution test liquid) of 100mL, stir 2 hours with vibrating machine.Then, at 100 DEG C, 20 points are processed to make pepsin inactivation.After being cooled to 37 DEG C, add the sodium bicarbonate aqueous solution 110mL of the pH 8.5 of 37 DEG C, regulate pH to about 6.0, further jolting stirs 2 hours.With this liquid of the metre filter of 0.45 μm, as assess sample.
To be diluted to concentration with visceral adipocytes division culture medium (primary cell company limited, Tokyo) is 3.0 × 10
5cell/cm
2people's Preadipocyte In Vitro be seeded in 24 orifice plates, at 5% concentration C O
2under environment, 37 DEG C cultivate 6 days.Then, assess sample is diluted the liquid 1mL of 10 times by interpolation culture medium, cultivates 24 hours.Then the glycerol concentration in culture supernatant is measured.Compare with comparative example 1 with matched group, can confirm, the glycerol concentration produced by promoting the steatolysis that caused by lactoferrin in embodiment rises, and the coated tablet of embodiment is enteric solubility.Result as shown in Figure 1.
The raw material used when preparation embodiment and comparative example is as follows.In addition, each component amount is provided in table.
[table 23]
[table 24]
Claims (11)
1. a coated composition, it contains (A) alginate and (B) plasticizer.
2. coated composition as claimed in claim 1, wherein (A) composition is the alginate being selected from alginic acid sodium salt, alginic acid potassium salt and alginic acid ammonium salt.
3. coated composition as claimed in claim 1 or 2, wherein (A) composition is the alginate (A-1) of the viscosity of 1 quality % aqueous solution at 20 DEG C more than 50mPas.
4. coated composition as claimed in claim 1 or 2, the wherein alginate (A-2) of (A) composition to be the viscosity of 1 quality % aqueous solution at 20 DEG C more than the alginate (A-1) of 50mPas and the viscosity of 1 quality % aqueous solution at 20 DEG C be below 50mPas.
5. the coated composition according to any one of Claims 1 to 4, it is selected from the composition of gelatin, pectin, curdlan, pulullan polysaccharide, arabic gum, xanthan gum, gellan gum, hydroxypropyl emthylcellulose, sodium carboxymethyl cellulose and hydroxypropyl cellulose further containing (C).
6. the coated composition according to any one of Claims 1 to 5, it is further containing (D) microgranule.
7. the coated composition according to any one of claim 1 ~ 6, wherein (B) composition is glycerol and/or sucrose fatty acid ester.
8. the coated composition according to any one of claim 1 ~ 7, wherein with (A): what (C) represented is 1:10 ~ 20:1 containing mass ratio.
9. a coated preparation, it has the coating membrane that the coated composition according to any one of claim 1 ~ 8 is formed.
10. coated preparation as claimed in claim 9, the enteric coatings preparation of its to be coating membrane be enteric solubility.
The manufacture method of 11. 1 kinds of coated preparations, it comprises following operation: to also dry by the Coating Solution of coating thing spraying containing the coated composition according to any one of claim 1 ~ 8 and water, thus formed coating membrane by the surface of coating thing.
Applications Claiming Priority (3)
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| JP2013046697 | 2013-03-08 | ||
| JP2013-046697 | 2013-03-08 | ||
| PCT/JP2014/055707 WO2014136857A1 (en) | 2013-03-08 | 2014-03-06 | Coating composition, coated preparation and method for producing same |
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| JP (1) | JP6304234B2 (en) |
| KR (1) | KR102201077B1 (en) |
| CN (1) | CN105007949B (en) |
| HK (1) | HK1214753A1 (en) |
| WO (1) | WO2014136857A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108543072A (en) * | 2018-04-09 | 2018-09-18 | 鲍引健 | A kind of composition for coating and its associated uses |
| CN109414411A (en) * | 2016-04-29 | 2019-03-01 | 中央兰开夏大学 | Solid dosage forms |
| CN110997005A (en) * | 2017-08-09 | 2020-04-10 | 狮王株式会社 | Coating composition, coating film, coated preparation and process for producing the same |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6642438B2 (en) * | 2014-09-03 | 2020-02-05 | ライオン株式会社 | Coating preparation and method for producing the same |
| BR112017013598A2 (en) * | 2014-12-23 | 2018-03-06 | Fmc Corp | enteric film coating compositions, coating method, and coated forms |
| CN104857520B (en) * | 2015-04-29 | 2017-12-29 | 南京圣诺生物科技实业有限公司 | A kind of sodium alginate coating solution composition and coating method |
| JP6801203B2 (en) * | 2016-03-18 | 2020-12-16 | 日油株式会社 | pH Response Elution Coated Granules and Foods |
| CN108740371B (en) * | 2018-04-04 | 2021-07-30 | 广州智特奇生物科技股份有限公司 | Enteric coating material, zinc oxide coated by coating material and preparation method thereof |
| KR102031515B1 (en) * | 2019-04-09 | 2019-10-11 | 나누리영농조합법인 | Egg surface coating composition and preparing method thereof |
| WO2021263230A1 (en) * | 2020-06-26 | 2021-12-30 | Sensient Colors Llc | Enteric coating composition and method of making and using the same |
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| US20070071821A1 (en) * | 2003-08-27 | 2007-03-29 | Vic Young | Formulation for providing an enteric coating material |
| JP2011504171A (en) * | 2007-11-13 | 2011-02-03 | ハーキュリーズ・インコーポレーテッド | Water dispersible enteric coating formulations for dietary supplements and pharmaceutical dosage forms |
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| KR19990072826A (en) * | 1998-02-26 | 1999-09-27 | 우재영 | A process for producing enteric-coated pancreatin granules |
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| JP5353159B2 (en) * | 2008-09-26 | 2013-11-27 | 東洋紡株式会社 | Method for producing medical material and medical material |
| RU2574018C2 (en) * | 2010-03-31 | 2016-01-27 | Мотида Фармасьютикал Ко., Лтд. | Easily dosed solid medicinal preparation |
-
2014
- 2014-03-06 KR KR1020157024322A patent/KR102201077B1/en active IP Right Grant
- 2014-03-06 WO PCT/JP2014/055707 patent/WO2014136857A1/en active Application Filing
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- 2014-03-06 CN CN201480012829.1A patent/CN105007949B/en active Active
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|---|---|---|---|---|
| US20070071821A1 (en) * | 2003-08-27 | 2007-03-29 | Vic Young | Formulation for providing an enteric coating material |
| WO2005025609A1 (en) * | 2003-09-10 | 2005-03-24 | Nrl Pharma, Inc. | Lactoferrin material composition |
| JP2011504171A (en) * | 2007-11-13 | 2011-02-03 | ハーキュリーズ・インコーポレーテッド | Water dispersible enteric coating formulations for dietary supplements and pharmaceutical dosage forms |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109414411A (en) * | 2016-04-29 | 2019-03-01 | 中央兰开夏大学 | Solid dosage forms |
| CN110997005A (en) * | 2017-08-09 | 2020-04-10 | 狮王株式会社 | Coating composition, coating film, coated preparation and process for producing the same |
| CN110997005B (en) * | 2017-08-09 | 2023-10-20 | 狮王株式会社 | Coating composition, coating film, coating preparation and manufacturing method thereof |
| CN108543072A (en) * | 2018-04-09 | 2018-09-18 | 鲍引健 | A kind of composition for coating and its associated uses |
Also Published As
| Publication number | Publication date |
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| JP6304234B2 (en) | 2018-04-04 |
| KR20150126613A (en) | 2015-11-12 |
| CN105007949B (en) | 2018-07-06 |
| KR102201077B1 (en) | 2021-01-11 |
| WO2014136857A1 (en) | 2014-09-12 |
| JPWO2014136857A1 (en) | 2017-02-16 |
| HK1214753A1 (en) | 2016-08-05 |
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