WO1986006632A1 - Compositions antiacides a action prolongee - Google Patents

Compositions antiacides a action prolongee Download PDF

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Publication number
WO1986006632A1
WO1986006632A1 PCT/US1986/001018 US8601018W WO8606632A1 WO 1986006632 A1 WO1986006632 A1 WO 1986006632A1 US 8601018 W US8601018 W US 8601018W WO 8606632 A1 WO8606632 A1 WO 8606632A1
Authority
WO
WIPO (PCT)
Prior art keywords
long
antacid
acting
grams
dosage unit
Prior art date
Application number
PCT/US1986/001018
Other languages
English (en)
Inventor
Max A. Tesler
John D. Flanagan
Original Assignee
Pharmacontrol Corp.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pharmacontrol Corp. filed Critical Pharmacontrol Corp.
Publication of WO1986006632A1 publication Critical patent/WO1986006632A1/fr
Priority to DK010387A priority Critical patent/DK10387A/da
Priority to NO870092A priority patent/NO870092D0/no

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/10—Carbonates; Bicarbonates
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/16—Inorganic salts, minerals or trace elements
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/20—Reducing nutritive value; Dietetic products with reduced nutritive value
    • A23L33/21—Addition of substantially indigestible substances, e.g. dietary fibres
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/08—Oxides; Hydroxides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/286—Carthamus (distaff thistle)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/899—Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane

Definitions

  • This invention relates to compositions that- can reduce gastric acidity for relatively long periods of time after administration. More particularly, the invention relates to novel combinations of acid-neutralizing compounds, dietary fiber and prostaglandin biosynthetic precursors. These compositions are in a highly palatable form and are useful ⁇ for the treatment or prevention of gastric hyperacidity and the discomfort and disease conditions that it can produce.
  • Antacid drugs are an important palliative in the treatment of duodenal and gastric ulcer.
  • antacids consist of a simple acid-neutralizing composition such as calcium carbonate, sodium bicarbonate or aluminum-magnesium hydroxide.
  • These simple antacids are deficient, however, in that the period of time during which they can reduce gastric acidity is relatively short, typically well under an hour from the time of administration.
  • some of the simple acid-neutralizing compounds such as calcium carbonate when administered alone cause a delayed gastric hypersecretion called acid rebound [Fordtran, New Eng. J. Med. 279:900 (1968)]
  • 4,369,172 used hydroxypropylmethyl cellulose or a mixture of that polymer and ethylcellulose and/or sodium carboxymethyl cellulose as a base to prolong the release of various active medicaments in lozenges, tablets, suppositories and other solid dosage forms. 10
  • Sheth et al. [D.S. Patent 4,140,755] used a hydrocolloid selected from a group of derivatized celluloses that produced a sustained release tablet 0 formulation in combination with a medicament. The formulation when taken orally became buoyant in gastric juice, thereby resisting passage through the pylorus.
  • Watanabe et al. [U.S. Patent 4,127,622] prepared hollow particulates containing ethyl cellulose, a lower chlorinated
  • erythro 15, 16-dioxyprostanoic acids and esters [Weiss, U.S. Patent 4,113,967], 11 ⁇ -homo-prostanoic acid derivatives [Floyd, Jr. et al , ., U.S. Patent 3,985,798], 16,16-ethylene derivatives of prostaglandin E, and its homologues [Walker, U.S. Patent 4,039,654], and arachidonic acid [Konture et al., J. Physiol. 286;15 (1979); Conolly et al., Gut 1 :429 (1977)] have been shown to inhibit gastric acid secretion.
  • Arachidonic acid has been shown by Tarnawski et al. [J.
  • the present invention provides novel compositions for the prolonged reduction: of gastric acidity. This reduction
  • in gastric acidity is useful for the treatment or prevention o of a number of disorders caused by such acidity such as heartburn, epigastric buring pain, sour stomach, -indigestion, esophagitis, peptic ulcers and gastritis-duodenitis.
  • the prolonged gastric acid-reducing effects of the invention are achieved by novel combinations of one or more antacid compounds, a source of prostaglandin precursors and t dietary fiber. These components act in concert to counter gastric acidity: the antacid compound (or compounds) acts to neutralize the acidity, while the prostaglandin precursors and dietary fiber serve to delay gastric emptying, thereby prolonging the antacid action.
  • compositions of the invention can be added to alleviate or reduce distress due to symptoms that often accompany gastric hyperacidity.
  • an antiflatulent may be added to alleviate or reduce symptoms of gas.
  • a laxative ingredient may be added to correct for constipation that might be caused by the antacid.
  • an analgesic ingredient may also be added to the compositions of the invention.
  • compositions of the invention may be added to the compositions of the invention.
  • mouth feel may be optimized by manipulation of the granularity of the ingredients of the compositions, particularly the dietary fiber component.
  • the compositons of the invention are incorporated into a solid wafer or cookie form. These dosage forms are
  • This invention relates to novel compositions containing one or more antacid compounds, a source of prostaglandin biosynthetic precursors and dietary fiber. Acting together, these components of the invention when administered orally produce a prolonged reduction in gastric acidity.
  • the invention further relates to compositions having other active components that can alleviate or reduce sources of discomfort that may accompany gastric hyperacidity or antacid treatment such as gas, constipation or generalized or 0 local pain.
  • the invention still further relates to compositions having coloring and/or flavoring agents that enhance palatability.
  • the antacid ingredients of the invention may be any nontoxic antacid compounds commonly used to neutralize gastric fluids.
  • Such compounds include but are not limited to aluminum carbonate; aluminum hydroxide; dihydroxyaluminum 0 aminoacetate; aluminum phosphate; dihydroxyaluminum sodium carbonate; sodium bicarbonate; bismuth aluminate, carbonate, subcarbonate, subgallate or subnitrate; calcium carbonate or phosphate; citric acid or its salts; magnesium aluminosilicates, carbonate, glycinate, hydroxide, oxide or trisilicate; mono-, di-' or tribasic calcium phosphate; potassium bicarbonate; sodium potassium tartrate; magnesium o hydroxyaluminates and aluminum oxyhydroxide or combinations thereof.
  • aluminum hydroxide and/or calcium carbonate are employed.
  • the quantity of antacid used per dosage unit may range from about 25 to about 95 milliequivalents ( Eq) of acid neutralizing capacity per dosage unit, with a preferred range of from about 60 to about 90 Eq.
  • the amount of calcium carbonate used per dosage unit may range from about 0.5 to about 4.0 grams, but preferably is in the range of from about 0.5 to about 2.0 grams.
  • aluminum hydroxide is the antacid a range of from about 0.6 to about
  • the acid neutralizing capacity of a sample can be determined by grinding the sample to a fine powder, mixing 10 grams of the power with 70 ml of deionized water, pipetting 25 mi of 1.0 N HCl into the solution and mixing for 15 minutes, and titrating the mixture with 1.0 N NaOH to pH 3.5.
  • the overall acid neutralizing capacity of a dosage unit is of course the product of the above value and the total weight of the dosage unit in grams.
  • a convenient dosage unit weights from about 26 to 31 grams, although of course other dosage sizes could be used instead.
  • the prostaglandin precursor source for the invention may be any material containing the polyunsaturated fatty acids that can be metabolized to the prostaglandins.
  • the principal fatty acids are arachidonic acid, which is metabolized to prostaglandins E., P 2 ⁇ - and G 2 , and eicosatrienoic acid, which is converted in the body to prostaglandin G1. Of these fatty acids, arachidonic acid is more important.
  • arachidonic acid either chemically synthesized or from natural sources, could be used. More economical and thus preferable sources are commercial lecithin, soybean oil or safflower oil. Safflower oil contains a mixture of fatty acids with varying chain lengths esterified to glycerol, as does soybean oil. In soybean oil there may also be up to 1% of free fatty acids not esterified to glycerol. Lecithin, which most often is produced commercially as a by-product in the manufacture of soybean oil is another good source of arachidonic acid.
  • the prostaglandin precursor is present as part of a mixture of the diglycerids of stearic, palmitic, oleic and longer chain fatty acids linked to the choline ester of phosphoric acid.
  • Commercial grade soybean lecithin contains about 5.5% C 20 to C 22 fatty acids, in which fraction arachidonic acid is found, and is a preferred source.
  • the quantity of lecithin per dosage unit may range from about 0.5 to about 3.0 grams, with from about 0.8 to about 1.3 grams preferred for a 26 to 31 gram dosage unit.
  • Soybean oil may be used as a source of prostaglandin precursors in a range from about 0.5 to about 3.0 grams, with from about 0.8 to about 1.3 grams preferred for a 26 to 31 gram dosage unit. Where safflower oil is used as the source of prostaglandin precursors, it may be present in an amount of from about 0.5 to about 3.0 grams, and preferably from about 0.8 to about 1.3 grams for a 26 to 31 gram dosage unit.
  • the fiber component of the invention is preferably of plant origin, although synthetic polymers having similar physicochemical properties could be used instead.
  • Potentially useful dietary fibers include hemicelluloses, pectins and lignin.
  • Convenient sources of fiber are wheat and corn bran, with corn bran being preferred.
  • the quantity of corn bran for a 26 to 31 gram dosage unit may range from about 6.0 to about 9.0 grams, with about 7.5 grams preferred.
  • the bran may comprise a mixture of two or more grind sizes, as may be seen in the example below.
  • two 26 to 31 gram dosage units are given containing together 170 mEq buffering capacity of a suitable antacid as described above,
  • an antiflatulent such as simethicone could be incorporated to combat gas that is often associated with heartburn, sour stomach or acid indigestion. Headache pain and the general discomfort from acid indigestion etc. may be relieved or reduced by the incorporation into the compositions of the invention of any pharmaceutically acceptable analgesic compound that would not cause further irritation of the gastric lining. Because antacid compounds may in some cases cause constipation, the incorporation of a safe and effective laxative compound into 5 the compositions may also prove beneficial.
  • compositions of the invention may be incorporated into the compositions of the invention to produce a dosage form that is appealing to the eye and taste.
  • sweetening agents such as sucrose, fructose, lactose, aspartame (L-asartyl-L- phenylalanine methyl ester), annitol, sorbitol or xylitol may be added.
  • nontoxic food coloring agents may be added, as may flavoring agents such as oil of orange or lemon, lemon-lime, raspberry, cola, vanilla, mint, cinnamon, ginger, liquid butter or butterscotch flavoring or combinations thereof.
  • the dosage form of the compositions of the invention may be powdered or granular, taken either dry or as a suspension in an appropriate carrier liquid such as water or milk.
  • compositions are incorporated into a convenient bakery product which will provide stability during storage and optimal appearance and palatability.
  • Cupcake or biscuit dosage forms may be used, but a cookie dosage form is preferred since it provides enhanced stability of the active components of the invention * uring storage.
  • the dosage form is a bakery product, the ingredients characteristic of such products such as molasses, flour, baking powder or soda, animal or vegetable, shortening etc. will also be added to the compositions of the invention.
  • Formulations for a cookie dosage form of the present invention may be seen in Table 1.
  • the formulations are expressed as the quantities of ingredients in an amount of dough sufficient to make a single cookie.
  • ammonium bicarbonate was dissolved in the water in a separate container and then added to the above mixed ingredients over a period of one minute while mixing at speed one.
  • the blended dough mixture was then formed into cookies in a (make and model) rotary machine and the cookies were baked at 400 * F for 10 to 11 minutes.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Botany (AREA)
  • Nutrition Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Biotechnology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Des compositions à action prolongée de réduction de l'acidité gastrique comprennent un ou plusieurs composés antiacides, une source de précurseurs de prostaglandine et des fibres alimentaires.
PCT/US1986/001018 1985-05-10 1986-05-09 Compositions antiacides a action prolongee WO1986006632A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
DK010387A DK10387A (da) 1985-05-10 1987-01-09 Langvarigt virkende antacidt praeparat
NO870092A NO870092D0 (no) 1985-05-10 1987-01-09 Antisyrepreparater med langvarig virkning.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73278485A 1985-05-10 1985-05-10
US732,784 1985-05-10

Publications (1)

Publication Number Publication Date
WO1986006632A1 true WO1986006632A1 (fr) 1986-11-20

Family

ID=24944944

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1986/001018 WO1986006632A1 (fr) 1985-05-10 1986-05-09 Compositions antiacides a action prolongee

Country Status (3)

Country Link
EP (1) EP0222881A4 (fr)
DK (1) DK10387A (fr)
WO (1) WO1986006632A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2342292A (en) * 1998-10-06 2000-04-12 Mars Uk Ltd Composition for the treatment of animal stereotypy comprises fat, fibre and optionally, a stomach antacid
WO2001051064A1 (fr) * 2000-01-15 2001-07-19 Demontfort University Stereotypies buccales
US20110195130A1 (en) * 2010-02-09 2011-08-11 Sanford Siegal Edible compositions

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB190826894A (en) * 1908-12-11 1909-08-19 Thomson Bennett Ltd Improvements relating to Electric Ignition Apparatus for Internal Combustion Engines.
US2061184A (en) * 1931-04-10 1936-11-17 Curtis B Camp Food product
US2638433A (en) * 1949-11-17 1953-05-12 James T George Pharmaceutical preparation for peptic ulcers
US3019109A (en) * 1960-05-10 1962-01-30 American Cyanamid Co Stabilization of antibiotics in feeds and feed supplements
US3253988A (en) * 1962-11-20 1966-05-31 Robert I Pearlman Antacid composition and method of using same
US3843778A (en) * 1970-04-28 1974-10-22 Rorer Inc William H Antacids
US4542019A (en) * 1983-03-11 1985-09-17 John Lezdey Antacid compositions

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB190826894A (en) * 1908-12-11 1909-08-19 Thomson Bennett Ltd Improvements relating to Electric Ignition Apparatus for Internal Combustion Engines.
US2061184A (en) * 1931-04-10 1936-11-17 Curtis B Camp Food product
US2638433A (en) * 1949-11-17 1953-05-12 James T George Pharmaceutical preparation for peptic ulcers
US3019109A (en) * 1960-05-10 1962-01-30 American Cyanamid Co Stabilization of antibiotics in feeds and feed supplements
US3253988A (en) * 1962-11-20 1966-05-31 Robert I Pearlman Antacid composition and method of using same
US3843778A (en) * 1970-04-28 1974-10-22 Rorer Inc William H Antacids
US4542019A (en) * 1983-03-11 1985-09-17 John Lezdey Antacid compositions

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP0222881A4 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2342292A (en) * 1998-10-06 2000-04-12 Mars Uk Ltd Composition for the treatment of animal stereotypy comprises fat, fibre and optionally, a stomach antacid
WO2001051064A1 (fr) * 2000-01-15 2001-07-19 Demontfort University Stereotypies buccales
US20110195130A1 (en) * 2010-02-09 2011-08-11 Sanford Siegal Edible compositions
WO2011099998A2 (fr) * 2010-02-09 2011-08-18 Sanford Siegal Compositions comestibles
WO2011099998A3 (fr) * 2010-02-09 2014-03-20 Sanford Siegal Compositions comestibles

Also Published As

Publication number Publication date
EP0222881A4 (fr) 1987-09-02
DK10387D0 (da) 1987-01-09
DK10387A (da) 1987-03-09
EP0222881A1 (fr) 1987-05-27

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