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Claims for Patent: 6,099,859

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Claims for Patent: 6,099,859

Title: Controlled release oral tablet having a unitary core
Abstract:A controlled release antihyperglycemic tablet that does not contain an expanding polymer and comprising a core containing the antihyperglycemic drug, a semipermeable membrane coating the core and at least one passageway in the membrane.
Inventor(s): Cheng; Xiu Xiu (Davie, FL), Chen; Chih-Ming (Davie, FL), Jan; Steve (Coral Springs, FL), Chou; Joseph (Coral Springs, FL)
Assignee: Andrx Pharmaceuticals, Inc. (Fort Lauderdale, FL)
Application Number:09/045,330
Patent Claims: 1. A controlled release pharmaceutical tablet comprising:

(a) a core comprising:

(i) 50-98% of an antihyperglycemic drug;

(ii) 0-40% of a binding agent;

(iii) 0-20% of an absorption enhancer; and

(b) a semipermeable membrane coating covering said core wherein the membrane is permeable to the passage of water and biological fluids and is impermeable to the passage of the antihyperglycemic drug wherein said coating comprises 50-99% of a polymer; 0-40% of a flux enhancer and 0-25% of a plasticizer; and

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

2. A controlled release pharmaceutical tablet as defined in claim 1 wherein the antihyperglycemic drug is a biguanide.

3. A controlled release pharmaceutical tablet as defined in claim 2 wherein the antihyperglycemic drug is metformin or a pharmaceutically acceptable salt thereof.

4. A controlled release pharmaceutical tablet as defined in claim 2 wherein the antihyperglycemic drug is buformin or a pharmaceutically acceptable salt thereof.

5. A controlled release pharmaceutical tablet as defined in claim 1 wherein the binding agent is water soluble.

6. A controlled release pharmaceutical tablet as defined in claim 1 wherein the water soluble binding agent is polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxyethyl cellulose, waxes or mixtures thereof.

7. A controlled release pharmaceutical tablet as defined in claim 6 wherein the water soluble binding agent is polyvinyl pyrrolidone.

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

9. A controlled release pharmaceutical tablet as defined in claim 1 wherein the absorption enhancer is a fatty acid selected from the group consisting of capric acid, oleic acid or their monoglycerides.

10. A controlled release pharmaceutical tablet as defined in claim 1 wherein the absorption enhancer is a surfactant selected from the group consisting of sodium lauryl sulfate, sodium taurocholate and polysorbate 80.

11. A controlled release pharmaceutical tablet as defined in claim 1 wherein the absorption enhancer is a chelating agent selected from the group consisting of citric acid, phytic acid, ethylene diamine tetraacetic acid and ethylene glycol-bis(.beta.-aminoethyl ether)-N,N,N,N-tetraacetic acid.

12. A controlled release pharmaceutical tablet as defined in claim 1 wherein the absorption enhancer is a bile salt.

13. A controlled release pharmaceutical tablet as defined in claim 1 wherein the absorption enhancer is sodium lauryl sulfate.

14. A controlled release pharmaceutical tablet as defined in claim 1 wherein the semipermeable membrane around the core is a water insoluble cellulose derivative.

15. A controlled release pharmaceutical tablet as defined in claim 14 wherein the water insoluble cellulose derivative in the membrane around the core is cellulose acetate.

16. A controlled release pharmaceutical tablet as defined in claim 1 wherein semipermeable membrane comprises a flux enhancer.

17. A controlled release pharmaceutical tablet as defined in claim 16 wherein the 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.

18. A controlled release pharmaceutical tablet as defined in claim 17 wherein the flux enhancer is polyethylene glycol with an average molecular weight between 380 and 420.

19. A controlled release pharmaceutical tablet as defined in claim 1 wherein the semipermeable membrane comprises a plasticizer.

20. A controlled release pharmaceutical tablet as defined in claim 19 wherein the plasticizer is triacetin.

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

22. A controlled release pharmaceutical tablet as defined in claim 1 wherein the peak plasma level is obtained 8-12 hours after administration.

23. A controlled release pharmaceutical tablet as defined in claim 1 further comprising an effective amount of the antihyperglycemic drug coated onto the semipermeable membrane or mixed into the semipermeable membrane to provide an immediate release of an effective amount of the antihyperglycemic drug.

24. A controlled release pharmaceutical tablet as defined in claim 1 that exhibits the following dissolution profile when tested in a USP type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37.degree. C.:

after 2 hours 0-25% of the drug is released;

after 4 hours 10-45% of the drug is released;

after 8 hours 30-90% of the drug is released;

after 12 hours not less than 50% of the drug is released;

after 16 hours not less than 60% of the drug is released;

and after 20 hours not less than 70% of the drug is released.

25. A controlled release pharmaceutical tablet as defined in claim 1 that exhibits the following dissolution profile when tested in a USP type 2 apparatus at 75 rpm in 900 ml of simulated intestinal fluid (pH 7.5 phosphate buffer) and at 37.degree. C.:

after 2 hours 0-15% of the drug is released;

after 4 hours 20-40% of the drug is released;

after 8 hours 45-90% of the drug is released;

after 12 hours not less than 60% of the drug is released;

after 16 hours not less than 70% of the drug is released;

and after 20 hours not less than 80% of the drug is released.

26. A controlled release pharmaceutical tablet as defined in claim 1 that is administered with or shortly after the evening meal.

27. 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; and

(b) a semipermeable membrane coating covering said core comprising:

(i) cellulose acetate;

(ii) a flux enhancer; and

(iii) a plasticizer; and

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

28. A controlled release pharmaceutical tablet as defined in claim 27 wherein the peak plasma level is obtained 8-12 hours after administration.

29. 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; and

(b) 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) 2-20% of a flux enhancer;

(iii) 2-15% of a plasticizer; and

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