Oral vehicle compositions

• US 5,458,879 A
• Filed: 09/30/1994
• Issued: 10/17/1995
• Est. Priority Date: 03/03/1994
• Status: Expired due to Fees

• Current Assignee: The Procter & Gamble Company
• Original Assignee: The Procter & Gamble Company
• Inventors: Singh, Nikhilesh N., Smith, Ronald L., Carella, Anne M.
• Primary Examiner(s): Kishore, Gollamudi S.
• Application Number:
  US08/316,172
• Time in Patent Office: 382 Days
• Field of Search: 424/400, 424/486, 424/484, 514/772, 514/772.2, 514/772.3, 514/772.5, 514/772.6, 514/781
• US Class Current: 424/400
• CPC Class Codes: A61K 9/0007 Effervescent A61K9/0065 takes precedence
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006

Abstract

Disclosed are oral pharmaceutical vehicle compositions comprising from about 0.05 to about 20% of a water-soluble mucoadhesive.

Claims

1. An aqueous oral liquid pharmaceutical mucoadhesive composition consisting essentially of:

(a) from about 0.05 to about 20% of a water-soluble mucoadhesive polymer selected from the group consisting of poly(ethylene oxide), poly(ethylene glycol), poly(vinyl alcohol), poly(vinyl pyrrolidine), poly(acrylic acid), poly(hydroxy ethyl methacrylate), hydroxyrpropyl cellulose, hydroxyethyl ethyl cellulose, hydroxyethyl ethyl cellulose and chitosan and mixtures thereof,

(b) from about 0.02% w/v to about 5% w/v of sodium carboxymethyl cellulose; and

(c) one or more pharmaceutically active agents wherein said composition has an adhesive strength (measured as force of detachment) of from about 0.5 to about 10 Newtons-sec, a tackiness of from about 1.0 to about 10N, a coefficient of viscoelasticity from about 0.20 to about 30 dynes/cm² and mechanical impedance of from about 0.15 to 0.6 measured between the frequency range of 1 to 10 Hz.

2. A pharmaceutical composition according to claim 1 wherein said mucoadhesive is poly(oxyethylene oxide) having a molecular weight of from about 2000 to about 10,000,000.

3. A pharmaceutical vehicle composition according to claim 1 which has a Newtonian viscosity of from about 3 to about 100 cPs.

4. A pharmaceutical vehicle composition according to claim 2 wherein said composition has a non-Newtonian viscosity of from about 100 to 300 cPs^n-1 at a the shear rate between 1 to 200 per sec.

5. A pharmaceutical composition according to claim 4 wherein said pharmaceutically active agent is selected from the group consisting of analgesics, decongestants, expectorants, antitussives, antihistamines, anticholinergics, antacids, gastroprotectants, H₂ -receptor antagonists, laxative, gastrokinetics, proton pump inhibitors, antidiarrheals and mixtures thereof.

6. A pharmaceutical composition according to claim 5 wherein said analgesic is selected from the group consisting of aspirin, acetaminophen, acetylsalicylic acid, ibuprofen, naproxen, flurbiprofen, carprofen, tiaprofenic acid, cicloprofen, ketoprofen, ketorolac, etodolac, indomethacin, sulindac, fenoprofen, diclofenac, piroxicam, nabumetone, pharmaceutically acceptable salts thereof, optically active isomers thereof and mixtures thereof;

decongestants selected from the group consisting of pseudoephedrine, phenylpropanolamine, phenylephrine and ephedrine, pharmaceutically acceptable salts thereof and mixtures thereof;

expectorants selected from the group consisting of glyceryl guaicolate, terpin hydrate, ammonium chloride, N-acetylcysteine, bromhexine, vasicine, ambroxol, carbocistein, sobrerol, pharmaceutically acceptable salts thereof and mixtures thereof;

antitussives selected from the group consisting of dextromethorphan, chlophedianol, carbetapentane, caramiphen, noscapine, diphenhydramine, codeine, hydrocodone, hydromorphone, fominoben, and phenol, pharmaceutically acceptable salts thereof and mixtures thereof;

antihistamines selected from the group consisting of chlorpheniramine, brompheniramine, dexchlorpheniramine, dexbrompheniramine, triprolidine, doxylamine, tripelennamine, cuproheptadine, carbinoaxime, doxylamine, bromdiphenhydramine, pyrilamine, acrivastine, rocastine, phenindamine, astemizole, azatadine, azelastine, cetirizine, ebastine, ketotifen, lodoxine, loratidine, levocabastine, mequitazine, oxatomide, setastine, tazifyline, temelastine terfenadine, and terfenadine carboxylate, pharmaceutically acceptable salts thereof and mixtures thereof;

anticholinergics selected from the group consisting of atropine, clidinium and dicyclomine;

antacids selected from the group consisting of aluminum hydroxide, bismuth subsalicylate, bismuth subcitrate, simethicone, calcium carbonate, magaldrate, H₂ -receptor antagonists selected from the group consisting of cimetidine, famotidine, nizatidine and ranitidine;

laxatives selected from the group consisting of phenolphthalein and casanthrol; and

antidiarrheals selected from the group consisting of diphenoxylate and loperamide and mixtures thereof.

7. A pharmaceutical composition according to claim 6 which further comprises an aromatic agent selected from the group consisting of menthol, eucalyptus oil, camphor, L-menthyl acetate, N-ethyl-p-menthane-3-carboxamide, N, 2,3-trimethyl-2-isopropylbutanamide, 3- and L-menthoxy-propane 1,2 diol and mixtures thereof.

8. A method for the treatment of cough in humans or animals in need of such relief comprising the administration of a safe and effective amount of the composition of claim 7.

9. A method for the treatment of or reducing the irritation, pain and discomfort associated with laryngopharyngitis in humans or animals in need of such relief comprising the administration of a safe and effective amount of the composition of claim 7.

10. A method for the treatment of upper gastrointestinal disorders in humans or animals in need of such relief comprising the administration of a safe and effective amount of the composition of claim 7.