Controlled release composition with semi-permeable membrane and poloxamer flux enhancer

• US 20050048119A1
• Filed: 09/14/2004
• Published: 03/03/2005
• 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, Dely, Aaron, Li, Boyong, Lodin, Unchalee
• Application Number:
  US10/940,588
• Publication Number:
  US 20050048119A1
• Time in Patent Office: Days
• US Class Current: 424/473
• 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 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

A controlled release pharmaceutical tablet comprising a core containing the antihyperglycemic drug, a water soluble seal coat, a semipermeable membrane coating the core and at least one passageway in the membrane.

Claims

1. A controlled release pharmaceutical tablet comprising:

(a) a core comprising;

(i) a drug;

(ii) at least one pharmaceutically acceptable excipient;

(b) optionally a water soluble seal coat;

(c) a semipermeable membrane coating covering said core wherein the membrane comprises;

i) a material that is permeable to the passage of water and biological fluids and is impermeable to the passage of the drug; and

(ii) a poloxamer.

(d) at least one passageway in the semipermeable membrane

2. A controlled release pharmaceutical tablet as defined in claim 1 wherein the drug is water soluble.

3. A controlled release pharmaceutical tablet as defined in claim 1 wherein the drug is an antihyperglycemic.

4. A controlled release pharmaceutical tablet as defined in claim 3 wherein the antihyperglycemic drug is a metformin or a pharmaceutically acceptable salt thereof.

5. A controlled release pharmaceutical tablet as defined in claim 3 wherein the antihyperglycemic drug is buformin or a pharmaceutically acceptable salt thereof.

6. A controlled release pharmaceutical tablet as defined in claim 1 wherein the pharmaceutical excipient in the core comprises a binding agent that is water soluble.

7. A controlled release pharmaceutical tablet as defined in claim 6 wherein the water soluble binding agent is polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose, waxes or mixtures thereof.

8. A controlled release pharmaceutical tablet as defined in claim 1 wherein the pharmaceutical excipient in the core comprises an absorption enhancer is selected from the group consisting of poloxamers, fatty acids, surfactants, chelating agents, bile salts or mixtures thereof.

9. A controlled release pharmaceutical tablet as defined in claim 1 wherein the material that is permeable to the passage of water an biological fluids is a water insoluble cellulose derivative.

11. A controlled release pharmaceutical tablet as defined in claim 1 wherein the semipermeable membrane further comprises a flux enhancer poloxamer.

12. A controlled release pharmaceutical tablet as defined in claim 15 wherein the second flux enhancer is sodium chloride, potassium chloride, sucrose, sorbitol, mannitol, polyethylene glycol, propylene glycol, hydroxypropyl cellulose, hydroxypropyl methycellulose, hydroxypropyl methycellulose phthalate, cellulose acetate phthalate, polyvinyl alcohols, methacrylic acid copolymers or mixtures thereof.

14. A controlled release pharmaceutical tablet as defined in claim 1 wherein the semipermeable membrane further comprises a second plasticizer in addition to the poloxamer.

15. A controlled release pharmaceutical tablet as defined in claim 1 wherein at least two passageways are formed in the semipermeable membrane.

16. A controlled release pharmaceutical tablet comprising:

(a) a core consisting essentially of;

(i) a drug;

(ii) a binding agent;

(iii) optionally an absorption enhancer; and

(iv) optionally a lubricant;

(b) optionally a water soluble seal coat;

(c) a semipermeable membrane coating covering said core consisting essentially of;

(i) a water insoluble cellulose derivative; and

(ii) a flux enhancer;

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

10. A controlled release pharmaceutical tablet as defined in claim 13 wherein the water insoluble cellulose derivative in the membrane around the core is cellulose acetate.

13. A controlled release pharmaceutical tablet as defined in claim 16 wherein the flux enhancer is poloxamer.

17. A controlled release antihyperglycemic tablet comprising:

(a) a core consisting essentially of;

(i) metformin or a pharmaceutically acceptable salt thereof;

(ii) a water soluble binding agent; and

(iii) an absorption enhancer;

(b) optionally a water soluble seal coat;

(c) a semipermeable membrane coating covering said core comprising;

(i) cellulose acetate;

(ii) a poloxamer; and

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

18. A controlled release pharmaceutical tablet consisting essentially of:

(a) a core comprising;

(i) 75-95% of an antihyperglycemic drug;

(ii) 3-15% of a binding agent; and

(iii) 2-15% of an absorption enhancer;

(b) a water soluble seal coat;

(c) a semipermeable membrane coating covering said core wherein the semipermeable membrane is permeable to the passage of water and biological fluids and is impermeable to the passage of the antihyperglycemic drug and comprises;

(i) 75-95% of a polymer;

(ii) 4-35% of a poloxamer; and

(d) at least one passageway in the semipermeable membrane for the release of the antihyperglycemic drug.