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WO1998024455A1 - Compositions pharmaceutiques ingerables pour le traitement des troubles du tractus gastro-intestinal superieur - Google Patents

Compositions pharmaceutiques ingerables pour le traitement des troubles du tractus gastro-intestinal superieur Download PDF

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Publication number
WO1998024455A1
WO1998024455A1 PCT/US1997/022737 US9722737W WO9824455A1 WO 1998024455 A1 WO1998024455 A1 WO 1998024455A1 US 9722737 W US9722737 W US 9722737W WO 9824455 A1 WO9824455 A1 WO 9824455A1
Authority
WO
WIPO (PCT)
Prior art keywords
magnesium
aluminum
bismuth
gastrointestinal tract
agents
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US1997/022737
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English (en)
Inventor
Sekhar Mitra
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Procter and Gamble Co
Original Assignee
Procter and Gamble Co
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 Procter and Gamble Co filed Critical Procter and Gamble Co
Publication of WO1998024455A1 publication Critical patent/WO1998024455A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • 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
    • A61K9/282—Organic compounds, e.g. fats

Definitions

  • the present invention relates to ingestible pharmaceutical tablet compositions comprising pharmaceutical actives useful for treating upper gastrointestinal tract distress and having a coating of 3-1-menthoxy propane 1,2- diol ("MPD") in amounts effective for providing a cooling sensation in the throat.
  • Pharmaceutical compositions such as antacids, useful for treating upper gastrointestinal tract distress (such as heartburn, indigestion, stomachache, etc.) are widely used. They vary depending on the active ingredients, and increasingly differ in the flavors, texture and even forms. The excipients for such compositions are chosen not only as appropriate for the dose form, but also to provide the best possible aesthetics for the compositions, including texture, flavor, after-taste, etc.
  • the time for the therapeutic effect of the active ingredient to be meaningful to the consumer will vary. Frequently, however, the time when the consumer actually begins to receive the benefit of the active ingredient and the time when the consumer perceives the product as starting to "work" are different. Dose form, flavorants, texture, etc. probably all contribute at least in part to this perception. Obviously, for the consumer in need of relief for upper gastrointestinal tract distress, perceiving that the product is working as quickly as possible after ingestion is of great benefit in addition to the true therapeutic relief eventually provided by the active ingredient.
  • an object of the present invention to provide ingestible pharmaceutical compositions containing a pharmaceutical active useful for treating upper gastrointestinal tract distress (e.g., upset stomach, heartburn, indigestion) which are perceived as providing faster relief and/or greater perceived efficacy and/or longer duration of activity. Furthermore, an object is to provide methods for treating upper gastrointestinal distress by administering pharmaceutical compositions according to the present invention.
  • a pharmaceutical active useful for treating upper gastrointestinal tract distress e.g., upset stomach, heartburn, indigestion
  • the present invention is directed to ingestible pharmaceutical tablet compositions comprising: (a) a safe and effective amount of a pharmaceutical active useful for treating upper gastrointestinal tract distress; and (b) at least one excipient comprising an amount of 3-1-menthoxy propane 1,2-diol effective for providing a cooling sensation to the throat as a coating on such tablets.
  • the present invention is also directed to methods for treating upper gastrointestinal tract distress. These methods comprise orally administering to a human patient in need of such treatment a safe and effective amount of a pharmaceutical active useful for treating upper gastrointestinal tract distress and an amount of 3-1-menthoxy propane 1,2-diol effective for providing a cooling sensation to the throat.
  • the present invention relates to pharmaceutical tablet compositions comprising: (a) at least one pharmaceutical active useful for treating upper gastrointestinal tract distress (preferably antacid actives); and (b) at least one excipient comprising 3-1-menthoxy propane 1,2-diol (hereinafter "MPD") as a coating on said tablet effective for providing a cooling sensation to the throat.
  • MPD 3-1-menthoxy propane 1,2-diol
  • Pharmaceutical actives useful for treating upper gastrointestinal tract distress are those materials which are safe and effective when administered orally for treating disorders of the upper gastrointestinal tract (typically the stomach and/or esophagus) which result in symptoms of upper gastrointestinal tract distress (e.g., heartburn, stomachache, indigestion).
  • Such actives include antacid agents and acid secretion prevention agents (e.g., H receptor-blocking antisecretory agents).
  • Antacid agents include, for example, aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxy-carbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum amino acetate, dihydroxy aluminum aminoacetic acid, calcium carbonate, calcium phosphate, aluminum magnesium hydrated sulfates, magnesium aluminate, magnesium alumino silicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide, magnesium trisilicate, sucralfate, and mixtures thereof.
  • acid secretion prevention agents include cimetidine, ranitidine, famotidine, omeprazole, lansoprazole, pantoprazole and mixtures thereof.
  • bismuth-containing agents such as, for example, bismuth subsalicylate, bismuth aluminate, bismuth citrate, bismuth subcitrate, bismuth nitrate, bismuth subcarbonate, bismuth subgalate, and mixtures thereof.
  • a particularly preferred bismuth salt is bismuth subsalicylate.
  • Preferred for use herein are antacid agents.
  • Preferred antacid agents are aluminum hydroxide, magnesium hydroxide, dihydroxy aluminum sodium carbonate, calcium carbonate, and mixtures thereof. Most preferred is calcium carbonate.
  • the tablet compositions of the present invention comprise a safe and effective amount of at least one pharmaceutical active useful for treating upper gastrointestinal tract distress.
  • the pharmaceutical active(s) comprise from about 1 % to about 99%, by weight, of the pharmaceutical tablet compositions of the present invention, preferably from about 25% to about 60%, and most preferably from about 30% to about 50%.
  • the pharmaceutical tablet compositions of the present invention also comprise an amount of MPD as a coating on said tablets effective for providing a cooling sensation to the throat.
  • MPD is described in detail in U.S. Patent 4,459,425, issued July 10, 1984 to Amano et al., incorporated herein by reference in its entirety. While not to be limited by theory, it is believed that the surprising benefits obtained by the use of MPD in the compositions of the present invention are the result of the unique cooling profile for this compound, which is very noticeable in the throat.
  • MPD is commercially available, being sold by Takasago Perfumery Co., Ltd., Tokyo, Japan.
  • excipients may be included in the uncoated tablet of the present compositions.
  • excipients means one or more compatible solid or liquid filler diluents which are suitable for oral administration to a human.
  • compatible means that the components of the compositions of the present invention are capable of being commingled with the pharmaceutical active, and with each other, in a manner such that there is no interaction which would substantially reduce the pharmaceutical efficacy of the compositions under ordinary use situations. Excipients must, of course, be of sufficiently high purity and sufficiently low toxicity to render them suitable for administration to the human being treated.
  • substances which can serve as excipients are sugars such as lactose, glucose and sucrose; starches such as corn-starch and potato starch; cellulose and its derivatives such as sodium carboxymethylcellulose, ethyl- cellulose, cellulose acetate; powdered tragacanth; malt; gelatin; talc; stearic acid; magnesium stearate; calcium sulfate; vegetable oils such as peanut oil, cottonseed oil, sesame oil, olive oil, corn oil and oil of theobroma; polyols such as propylene glycol, glycerine, sorbitol, mannitol, and polyethylene glycol; agar; and alginic acid; as well as other non-toxic compatible substances used in pharmaceutical formulations.
  • sugars such as lactose, glucose and sucrose
  • starches such as corn-starch and potato starch
  • cellulose and its derivatives such as sodium carboxymethylcellulose, ethyl- cellulose, cellulose
  • wetting agents and lubricants such as sodium lauryl sulfate, as well as coloring agents, flavoring agents, sweetening agents (including nonnutritive sweeteners such as aspartame and saccharin), tableting agents, stabilizers, antioxidants, cooling agents, and preservatives, can also be present.
  • Other compatible pharmaceutical additives and actives which are not pharmaceutical actives useful for treating upper gastrointestinal tract distress (e.g., NSAI drugs; pain killers; muscle relaxants) may be included in the compositions of the present invention.
  • Another agent found useful in the present compositions is an antiflatulant such as simethicone.
  • excipients such as menthol, menthol-like compounds such as N-ethyl-p-menthane- 3-carboxamide ("WS-3", supplied by Sterling Drugs), as well as MPD and mixtures thereof in the uncoated tablet.
  • WS-3 N-ethyl-p-menthane- 3-carboxamide
  • MPD MPD and mixtures thereof in the uncoated tablet.
  • any of the excipients mentioned above may also be included in the coolant layer.
  • excipients to be used in conjunction with the pharmaceutical active of the present compositions is basically determined by the tablet dose form for the compositions.
  • Excipients suitable for the preparation of tablet dosage forms for oral administration are well-known in the art. Their selection will depend on secondary considerations like taste, cost, shelf stability, which are not critical for the purposes of the present invention, and can be made without difficulty by a person skilled in the art. The only requirement is that the pharmaceutical active is available in safe and effective amounts.
  • the excipients employed in the present ingestible compositions are used at concentrations sufficient to provide a practical size to dosage relationship.
  • excipients comprise from about 1 % to about 99% by weight of the pharmaceutical tablet compositions of the present invention, preferably from about 40% to about 75%, and most preferably from about 50% to about 70%.
  • the MPD coating typically comprises from about 0.01 % to about 0.50% by weight of the pharmaceutical tablet compositions of the present invention, preferably from about 0.02% to about 0.20%, and most preferably from about 0.04% to about 0.10% .
  • the amount of total coating material is from about 0.1 mg to about 40 mg per dose.
  • the present invention also relates to methods for treating upper gastrointestinal tract distress in humans. These methods comprise orally administering to a human in need of such treatment a safe and effective amount of a pharmaceutical active useful for treating upper gastrointestinal tract distress and an amount of MPD effective for providing a cooling sensation to the throat. Most preferred is administering a safe and effective amount of an ingestible pharmaceutical composition of the present invention.
  • An ingestible pharmaceutical composition according to the present invention in the form of a chewable antacid tablet is prepared as follows: Ingredients Weight %
  • Mannitol Q.S. 1 Granulated calcium carbonate containing 93.3% calcium carbonate, 6.3% glucose and 0.4% gelatin; supplied by Whittaker Clark & Daniels, Philadelphia, Pa.
  • the above ingredients are dry blended in a mixer until homogeneous, and then direct compressed in a tableting machine to approximately 8.5 Strong Cobb units hardness to produce chewable antacid tablets each weighing 1.25g (500mg calcium carbonate per tablet).
  • the tablets are coated with the two coolants and mannitol by applying them as a liquid solution.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention se rapporte à des compositions pharmaceutiques se présentant sous forme de comprimés ingérables et contenant des agents pharmaceutiques actifs s'agissant de traiter des troubles du tractus gastro-intestinal supérieur (par exemple, des agents antiacides), lesdits comprimés étant enrobés de 3-1-menthoxy-propane-1,2-diol en quantité efficace s'agissant de procurer une sensation rafraîchissante au niveau de la gorge.
PCT/US1997/022737 1996-12-06 1997-12-08 Compositions pharmaceutiques ingerables pour le traitement des troubles du tractus gastro-intestinal superieur Ceased WO1998024455A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US76169596A 1996-12-06 1996-12-06
US08/761,695 1996-12-06

Publications (1)

Publication Number Publication Date
WO1998024455A1 true WO1998024455A1 (fr) 1998-06-11

Family

ID=25063000

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1997/022737 Ceased WO1998024455A1 (fr) 1996-12-06 1997-12-08 Compositions pharmaceutiques ingerables pour le traitement des troubles du tractus gastro-intestinal superieur

Country Status (1)

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WO (1) WO1998024455A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020150683A1 (fr) * 2019-01-17 2020-07-23 Takasago International Corporation (Usa) Utilisation de matériaux de refroidissement pour la réduction ou l'inhibition de la salinité dans des produits de consommation administrés par voie orale, imbibés ou ingérés

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5244670A (en) * 1991-04-04 1993-09-14 The Procter & Gamble Company Ingestible pharmaceutical compositions for treating upper gastrointestinal tract distress
WO1994025009A1 (fr) * 1993-04-30 1994-11-10 The Procter & Gamble Company Compositions pharmaceutiques enrobees

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5244670A (en) * 1991-04-04 1993-09-14 The Procter & Gamble Company Ingestible pharmaceutical compositions for treating upper gastrointestinal tract distress
WO1994025009A1 (fr) * 1993-04-30 1994-11-10 The Procter & Gamble Company Compositions pharmaceutiques enrobees

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020150683A1 (fr) * 2019-01-17 2020-07-23 Takasago International Corporation (Usa) Utilisation de matériaux de refroidissement pour la réduction ou l'inhibition de la salinité dans des produits de consommation administrés par voie orale, imbibés ou ingérés

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