Pharmaceutical composition with sodium lauryl sulfate as an extra-granular absorption/compression enhancer and the process to make the same

• US 20050051922A1
• Filed: 09/14/2004
• Published: 03/10/2005
• Est. Priority Date: 09/20/2002
• Status: Abandoned Application

• Current Assignee: Andrx Labs LLC (Abbvie Incorporated)
• Original Assignee: Andrx Labs LLC (Abbvie Incorporated)
• Inventors: Cardinal, John R., Nangia, Avinash, Li, Boyong
• Application Number:
  US10/940,587
• Publication Number:
  US 20050051922A1
• Time in Patent Office: Days
• US Class Current: 264/109
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 31/425 Thiazoles
• CPC Class Codes: A61K 31/426 1,3-Thiazoles
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats

Abstract

A process for preparing a pharmaceutical dosage form or core wherein an absorption/compression agent is introduced into the formulation extra-granularly, and a pharmaceutical tablet prepared by said process.

Claims

1. A process for preparing a pharmaceutical dosage form comprising the following steps:

(a) granulating;

(i) a drug; and

(ii) at least one pharmaceutically acceptable excipient;

(b) blending the granules prepared in step (a) with an absorption/compression enhancer; and

optionally a lubricant; and

(c) compressing the blended material from step (b) into a tablet.

2. A process as defined in claim 1 further comprising the step of applying a seal coat to said tablet prepared in step (c).

3. A process as defined in claim 1 further comprising the step of applying a membrane coating to said tablet prepared in step (c).

4. A process as defined in claim 3 further comprising the step of forming a passageway in said membrane coating.

5. A process as defined in claim 1 further comprising the steps of

(d) applying a seal coat to said tablet prepared in step (c);

(e) applying a membrane coating to the seal coated tablet of step (d) and

(f) forming a passageway in said membrane.

6. A process as defined in claim 1 wherein said drug is water soluble.

7. A process as defined in claim 1 wherein said drug is an antihyperglycemic drug.

8. A process as defined in claim 7 wherein said antihyperglycemic drug is metformin or a pharmaceutically acceptable salt thereof.

9. A process as defined in claim 7 wherein said antihyperglycemic drug is buformin or a pharmaceutically acceptable salt thereof.

10. A process as defined in claim 1 wherein said pharmaceutical excipient is a water soluble binding agent.

11. A process as defined in claim 10 wherein said water soluble binding agent is selected from the group consisting of polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose, waxes or mixtures thereof.

12. A process as defined in claim 1 wherein said pharmaceutical excipient is an absorption/compression enhancer selected from the group consisting of fatty acids, surfactants, chelating agents, bile salts or mixtures thereof.

13. A process as defined in claim 3 wherein said membrane coating is a water insoluble cellulose derivative.

14. A process as defined in claim 13 wherein said water insoluble cellulose derivative is cellulose acetate.

15. A process as defined in claim 3 wherein said membrane coating further comprises a plasticizer and a flux enhancer.

16. A process as defined in claim 15 wherein said flux enhancer is selected from the group consisting of sodium chloride, potassium chloride, sucrose, sorbitol, mannitol, polyethylene glycol, propylene glycol, hydroxypropyl cellulose, hydroxypropyl methycellulose, poloxamers, hydroxypropyl methycellulose phthalate, cellulose acetate phthalate, polyvinyl alcohols, methacrylic acid copolymers or mixtures thereof.

17. A process as defined in claim 16 wherein said plasticizer is selected from the group consisting of triacetin, acetylated monoglyceride, grape seed oil, olive oil, sesame oil, acetyltributylcitrate, acetyltriethylcitrate, glycerin sorbitol, diethyloxalate, diethylmalate, diethylfumarate, dibutylsuccinate, diethylmalonate, dioctylphthalate, dibutylsebacate, poloxamers, triethylcitrate, tributylcitrate, glyceroltributyrate and mixtures thereof.

18. A process as defined in claim 17 wherein said plasticizer is triacetin.

19. A process as defined in claim 4 wherein at least two passageways are formed in the membrane coating.

20. A solid dosage form prepared according to claim 1.

21. A pharmaceutical dosage form, prepared by:

(a) granulating a drug; and

at least one pharmaceutically acceptable excipient;

(b) blending the granules of step (a) with an absorption/compression enhancer and optionally a lubricant; and

(c) compressing the blended material from step (b) into a tablet.

22. A pharmaceutical dosage form, as defined in claim 21, further comprising a seal coat.

23. A pharmaceutical dosage form, as defined in claim 21, further comprising a membrane coating covering said tablet.

24. A pharmaceutical dosage form as defined in claim 23 wherein said membrane comprises a water insoluble cellulose derivative.

25. A pharmaceutical dosage form as defined in claim 23 wherein said tablet comprises 75-95% of an antihyperglycemic drug;

3-15% of a binding agent;

1-10% of an absorption/compression enhancer and 0-10% of a lubricant; and

said membrane coating covering said tablet comprises 75-95% of a film forming water insoluble polymer;

2-20% of a flux enhancer and 2-15% of a plasticizer; and

further comprises at least one passageway in said membrane for release of said antihyperglycemic drug.

26. A pharmaceutical dosage form, as defined in claim 22, further comprising a membrane coating covering said tablet.

27. A pharmaceutical dosage form, as defined in claim 26, wherein said membrane coating further comprises a film forming water insoluble polymer.

28. A pharmaceutical dosage form, as defined in claim 27 wherein said membrane coating further comprises a flux enhancer.

29. A pharmaceutical dosage form, as defined in claim 28 wherein said membrane coating further comprises a plasticizer.

30. A pharmaceutical dosage form, as defined in claim 29 wherein said membrane coating further comprises at least one passageway in said membrane coating for release of said drug.

31. A pharmaceutical dosage form, as defined in claim 21, wherein said granules comprise an antihyperglycemic drug and a binding agent, said tablet comprising 50-98% by weight of said tablet of said antihyperglycemic drug;

0-40% by weight of said tablet of said binding agent;

0.1-20% by weight of said tablet of said absorption/compression enhancer and 0-20% by weight of said tablet of said lubricant.

32. A pharmaceutical dosage form as defined in claim 21 wherein said drug is water soluble.

33. A pharmaceutical dosage form as defined in claim 21 wherein said drug is an antihyperglycemic drug.

34. A pharmaceutical dosage form as defined in claim 31 wherein said antihyperglycemic drug is metformin or a pharmaceutically acceptable salt thereof.

35. A pharmaceutical dosage form as defined in claim 33 wherein said antihyperglycemic drug is buformin or a pharmaceutically acceptable salt thereof.

36. A pharmaceutical dosage form as defined in claim 31 wherein said binding agent is a water soluble binding agent.

37. A pharmaceutical dosage form as defined in claim 31 wherein said binding agent is selected from the group consisting of polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose, waxes or mixtures thereof.

38. A pharmaceutical dosage form as defined in claim 27 wherein said water insoluble polymer is a cellulose derivative.

39. A pharmaceutical dosage form as defined in claim 31 wherein at least two passageways are formed in the membrane.

40. A pharmaceutical dosage form consisting essentially of a tablet prepared by

(a) forming granules consisting essentially of:

(i) metformin or a pharmaceutically acceptable salt thereof; and

(ii) a binding agent;

(b) blending said granules with an absorption/compression enhancer and a lubricant;

(c) surrounding said tablet with a seal coat;

(c) covering said seal coated tablet with a membrane coating consisting of;

(i) a film forming water insoluble cellulose derivative;

(ii) a plasticizer;

(iii) a flux enhancer; and

(d) forming at least one passageway in the membrane.

41. A pharmaceutical dosage form, according to claim 40 wherein said tablet consists essentially of 75-95% of metformin hydrochloride;

3-15% of said binding agent;

2-15% of said absorption/compression enhancer;

0-10% of said lubricant; and

said membrane coating consists essentially of 75-95% of said water insoluble cellulose derivative;

2-20% of said plasticizer;

2-15% of said flux enhancer; and

further comprising at least one passageway in the membrane for the release of the antihyperglycemic drug.

42. A pharmaceutical dosage form, according to claim 41 wherein said absorption/compression enhancer is sodium lauryl sulfate.