Polymeric compositions and dosage forms comprising the same

• US 20050196442A1
• Filed: 03/05/2004
• Published: 09/08/2005
• Est. Priority Date: 03/05/2004
• Status: Abandoned Application

• Current Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Original Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Inventors: Lee, Der-Yang, Li, Shun Por, Huang, Hai Yong
• Application Number:
  US10/794,448
• Publication Number:
  US 20050196442A1
• Time in Patent Office: Days
• US Class Current: 424/468
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

A dosage form comprises: (a) at least one active ingredient; (b) a core having an outer surface; and (c) a shell which resides upon at least a portion of the core outer surface, wherein at least a portion of the shell is semipermeable, such that the liquid medium diffuses through the semipermeable shell or shell portion to the core due to osmosis. The shell also provides for delivery of the active ingredient to a liquid medium outside the shell after contacting of the dosage form with the liquid medium. The dosage form delivers one or more active ingredients in a controlled manner upon contacting of the dosage form with a liquid medium. The dosage form may be employed to provide a burst release of the active ingredient, or to provide release of the active ingredient at an ascending release rate over an extended time period upon contacting of the dosage form with a liquid medium. At least a portion of the shell may be comprised of a polymeric composition containing film former, gelling agents, which can be dissolved in a multisolvent system comprised of water and an organic solvent.

Claims

1. A composition comprising, based upon the total wet weight of the composition:

a) from about 5 percent to about 50 percent of a water insoluble, film forming polymer;

b) from about 0.05 percent to about 15 percent of a gelling agent; and

c) from about 40 percent to about 95 percent of a multisolvent system, wherein the multisolvent system is comprised of, based upon the total weight of the multisolvent system, from about 10 percent to about 50 percent of water and from about 50 percent to about 90 percent of a water miscible organic solvent.

2. The composition of claim 1, wherein the multisolvent system is comprised of, based upon the total weight of the multisolvent system, from about 10 percent to about 35 percent of the water and from about 65 percent to about 90 percent of the water miscible organic solvent.

3. The composition of claim 1 comprising, based upon the total wet weight of the composition:

a) from about 10 percent to about 40 percent of the water insoluble film forming polymer; and

b) from about 0.1 percent to about 5 percent of the gelling agent.

4. The composition of claim 1, wherein the water insoluble, film forming polymer is comprised of at least one of the following:

cellulose esters, cellulose ethers, cellulose ester-ethers, polyvinyl alcohols, polyvinyl acetate, polycaprolactones, polyacrylate, polymethacrylate, derivatives or copolymers of acrylates, methacrylate, acrylic acid, or methacrylic acid.

5. The composition of claim 4, wherein the water insoluble, film forming polymer is selected from the group consisting of cellulose acetate;

cellulose diacetate;

cellulose triacetate and derivatives, copolymers, and mixtures thereof.

6. The composition of claim 4, wherein the water insoluble, film forming polymer is selected from the group consisting of cellulose acetate, cellulose acetate butyrate, cellulose acetate propionate, ethyl cellulose, polyacrylate, polymethacrylate, and derivatives, copolymers and mixtures thereof.

7. The composition of claim 1, wherein the gelling agent is comprised of at least one of the following:

hydrocolloids, gelling starches, or derivatives or copolymers thereof.

8. The composition of claim 7, wherein the gelling agent is comprised of at least one of the following:

carrageenan, gellan gum, agar, alginate, or pectin.

9. The composition of claim 8 further comprising locust bean gum, potassium salt, or calcium salt.

10. The composition of claim 1, wherein the multisolvent system is comprised of, based upon the total wet weight of the multisolvent system, from about 10 percent to about 50 percent of water and from about 50 percent to about 90 percent of a solvent selected from the group consisting of methanol, ethanol, isopropanol, acetone, and mixtures thereof.

11. The composition of claim 1 further comprising, based upon the total wet weight of the composition, from about 1 percent to about 30 percent of a plasticizer.

12. The composition of claim 11, wherein the plasticizer is selected from the group consisting of polyethylene glycol;

propylene glycol;

glycerin;

sorbitol;

triethyl citrate;

tribuyl citrate;

dibutyl sebecate;

vegetable oils;

polysorbates;

sodium lauryl sulfates;

dioctyl-sodium sulfosuccinates;

mono acetate of glycerol;

diacetate of glycerol;

triacetate of glycerol;

natural gums;

triacetin;

acetyltributyl citrate;

diethyloxalate;

diethylmalate;

diethyl fumarate;

diethylmalonate;

dioctylphthalate;

dibutylsuccinate;

glycerol tributyrate;

hydrogenated castor oil;

fatty acids;

glycerides; and

or mixtures thereof.

13. The composition of claim 11, wherein the plasticizer is selected from the group consisting of triethyl citrate, dibutylsebacate, triacetin, and mixtures thereof.

14. The composition of claim 1 further comprising, based upon the total wet weight of the composition, from about 0.05 percent to about 5 percent of at least one of the following permeation modifying, water-soluble polymers:

polyalkylene glycol, hydroxypropylmethylcellulose, hydroxypropylcellulose, or hydroxyethylcellulose.

15. The composition of claim 1 further comprising, based upon the total wet weight of the composition, from about 0.5 percent to about 5 percent of a pore former selected from the group consisting of polyethylene glycol, hydroxypropylmethylcellulose, hydroxypropylcellulose, and copolymers and mixtures thereof.

16. A composition comprising, based upon the total wet weight of the composition:

a) from about 10 percent to about 40 percent of a water insoluble, film forming polymer, wherein the water insoluble, film forming polymer is cellulose acetate and/or ethyl cellulose;

b) from about 0.5 percent to about 5 percent of a carrageenan gelling agent; and

c) from about 55 percent to about 89.5 percent of a multisolvent system, wherein the multisolvent system is comprised of, based upon the total weight of the multisolvent system, from about 10 percent to about 30 percent of water and from about 70 percent to about 90 percent of acetone.

17. The composition of claim 16 further comprising, based upon the total wet weight of the composition, from about 5 percent to about 25 percent of a plasticizer selected from the group consisting of triethyl citrate, triacetin, dibutyl sebacate, and mixtures thereof, and/or from about 0.5 percent to about 5 percent of a pore former selected from the group consisting of polyethylene glycol, hydroxypropylmethylcellulose, hydroxypropylcellulose, and copolymers and mixtures thereof.

18. A method of preparing a composition comprised of:

a) adding at least one gelling agent to a mixture comprised of a water insoluble film forming polymer and a multisolvent system at a temperature above the gelation temperature of the at least one gelling agent, said multisolvent system comprised of water and an organic solvent.

19. The method of claim 18, wherein the gelling agent is selected from the group consisting of carrageenan, gellan gum, locust bean gum, and mixtures thereof, and the water insoluble film forming polymer is cellulose acetate and/or ethyl cellulose.

20. The method of claim 18, wherein the gelling agent is added to the mixture in an amount, based upon the total wet weight of the composition, from about 0.5 percent to about 5 percent, and the water insoluble film forming polymer is present in the mixture in an amount, based upon the total wet weight of the composition, from about 10 percent to about 40 percent.

21. The method of claim 20, wherein the weight ratio of water to organic solvent is from about 30:

70 to about 10;

90.

22. A method of preparing a composition comprised of:

a) combining a first premixture of at least one organic solvent and at least one water insoluble film forming polymer with a second premixture of water and at least one gelling agent under temperature conditions above the gelation temperature of the at least one gelling agent.

23. The method of claim 22, wherein the gelling agent is selected from the group consisting of carrageenan, gellan gum, locust bean gum, and mixtures thereof, and the water insoluble film forming polymer is cellulose acetate and/or ethyl cellulose.

24. The method of claim 23, wherein the gelling agent is present in the first premixture in an amount, based upon the total wet weight of the composition, from about 0.5 percent to about 5 percent, and the water insoluble film forming polymer is present in the second premixture in an amount, based upon the total wet weight of the composition, from about 10 percent to about 40 percent.

25. The method of claim 22, wherein the weight ratio of water to organic solvent is from about 30:

70 to about 10;

90.