Pharmaceutical compositions and process of manufacture thereof

• US 5,431,916 A
• Filed: 04/29/1993
• Issued: 07/11/1995
• Est. Priority Date: 04/29/1993
• Status: Expired due to Term

• Current Assignee: The Procter & Gamble Company
• Original Assignee: The Procter & Gamble Company
• Inventors: White, Richard K.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US08/054,762
• Time in Patent Office: 803 Days
• Field of Search: 424/451, 424/452, 424/455, 424/443, 424/445, 424/456
• US Class Current: 424/451
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

The present invention describes a product comprising least one pharmaceutically acceptable active in a mixture of a tri-ester and polyvinylpyrrolidone, and a process for producing the same. In further embodiments, the present invention also relates to a process for encapsulating the composition within soft gelatin shells. The resulting compositions and capsules provide an effective means for oral delivery of a wide variety of pharmaceutically acceptable actives.

Claims

1. A pharmaceutical encapsulated composition comprising:

(i) a safe and effective amount of a tri-ester;

(ii) a safe and effective amount of polyvinylpyrrolidone;

(iii) a safe and effective amount of at least one pharmaceutically acceptable active selected from the group consisting of analgesics, anti-inflammatory agents, anti-pyretics, calcium channel blockers, beta-blockers, antibacterials, antidepressants, antidiabetics, anti-emetics, antihistamines, cerebral stimulants, sedatives, anti-parasitics, expectorants, diuretics, decongestants, antitussives, muscle relaxants, anti-Parkinsonian agents, bronchodilators, cardiotonics, antibiotics, antivirals, nutritional supplements, their pharmaceutically-acceptable salts and compatible mixtures thereof; and

(iv) an orally acceptable carrier

wherein the ratio of tri-ester to polyvinylpyrrolidone is from about 2.0 to about 0.5, to about 1.0 to about 1.0.

2. A pharmaceutical composition according to claim 1 which comprises from about 10% to about 50% of the tri-ester and is selected from the group consisting of triethyl citrate, glyceryl triacetate, acetyltriethyl citrate, acetyltri-n-butyl citrate and mixtures thereof.

3. A pharmaceutical composition according to claim 2 which comprises from about 10% to about 50% of the polyvinylpyrrolidone and has an average molecular weight of about 2,900 to about 1,100,000.

4. A pharmaceutical composition according to claim 3 which comprises from about 0.01% to about 50% of the pharmaceutically acceptable active, and is selected from the group consisting of an antitussive;

an antinauseant;

a nutritional supplement;

a laxative;

an appetite suppressant;

an analgesic;

an antiasthmatic;

an antihistamine;

a decongestant;

a xanthine;

an expectorant;

an antacid;

an antidiarrheal, a H2-Receptor antagonist and mixtures thereof.

5. A pharmaceutical composition according to claim 4 wherein the pharmaceutically acceptable active is an analgesic selected from the group consisting of acetaminophen, acetylsalicylic acid, ketoprofen, fenoprofen, flurbiprofen, ibuprofen, naproxen, and mixtures thereof.

7. A pharmaceutical composition according to claim 1 which additionally contains from about 0.1% to about 10% of a surfactant.

8. A pharmaceutical composition according to claim 4 which further contains a second pharmaceutically acceptable active selected from the group consisting of an antitussive;

an antinauseant;

a nutritional supplement;

a laxative;

an appetite suppressant;

an analgesic;

an antiasthmatic;

an antihistamine;

a decongestant;

a xanthine;

an expectorant;

an antacid;

an antidiarrheal;

a H2-Receptor antagonist and mixtures thereof.

9. A pharmaceutical composition according to claim 8 which further contains a third pharmaceutically acceptable active selected from the group consisting of an antitussive;

an antinauseant;

a nutritional supplement;

a laxative;

an appetite suppressant;

an analgesic;

an antiasthmatic;

an antihistamine;

a decongestant;

a xanthine;

an expectorant;

an antacid;

an antidiarrheal;

a H2-Receptor antagonist and mixtures thereof.

10. A pharmaceutical composition according to claim 9 which further contains a fourth pharmaceutically acceptable active selected from the group consisting of an antitussive;

an antinauseant;

a nutritional supplement;

a laxative;

an appetite suppressant;

an analgesic;

an antiasthmatic;

an antihistamine;

a decongestant;

a xanthine;

an expectorant;

an antacid;

an antidiarrheal;

a H2-Receptor antagonist and mixtures thereof.

11. A composition according to claim 10 wherein the pharmaceutically acceptable actives are acetaminophen, dextromethorphan, pseudoephedrine and doxylamine or chlorpheniramine.

12. A pharmaceutical composition according to claim 1 encapsulated within a gelatin shell.

19. A method of providing relief of cold symptoms by administering a safe and effective amount of a composition of claim 1.

6. A pharmaceutical composition according to claim which additionally contains from about 0.1% to about 20% water or polyethylene glycol and mixtures thereof.

13. A process for preparing soft gelatin capsules containing a pharmaceutical composition comprising the steps of:

(a) combining, mixing and heating a first component comprising;

(i) a safe and effective amount of a tri-ester;

(ii) a safe and effective amount of polyvinylpyrrolidone;

(iii) a safe and effective amount of at least one pharmaceutically acceptable active;

wherein the ratio of tri-ester to polyvinylpyrrolidone is from about 2.0 to about 0.5, to about 1.0 to about 1.0;

(b) combining and admixing with component (a) a second component comprising;

(i) from about 0.01% to about 50% of at least one pharmaceutically acceptable active; and

(c) encapsulating the composition formed by admixing component (a) and component (b) within a soft gelatin shell.

14. A process according to claim 13 wherein the pharmaceutically acceptable active is selected from the group consisting of an antitussive;

an antinauseant;

a nutritional supplement;

a laxative;

an appetite suppressant;

an analgesic;

an antiasthmatic;

an antihistamine;

a xanthine;

a decongestant;

an expectorant;

an antacid;

an antidiarrheal, a H2-Receptor antagonist and mixtures thereof.

15. A process according to claim 13 which additionally contains from about 0.1% to about 20% of water or polyethylene glycol and mixtures thereof.

16. A process according to claim 13 which additionally requires heat when combining component (b).

17. A process according to claim 13 which additionally contains from about 0.1% to about 10.0% of a surfactant.

18. A method of providing relief of cold symptoms by administering a safe and effective amount of a composition produced according to claim 13.