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Claims for Patent: 6,103,262

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Claims for Patent: 6,103,262

Title: Modified-release metronidazole compositions and methods for making and using same
Abstract:Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise: (a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole; (b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent; (c) about 0.1 wt % to about 2.0 wt % detackifier; (d) 0 to about 23 wt % of a first aqueous soluble pharmaceutical diluent; (e) 0 to about 23 wt % of a second aqueous soluble diluent which is suitable for forming a pharmaceutical tablet when compressed with the granules of (a), the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent; (f) 0 to about 20 wt % of a second portion of metronidazole; (g) 0 to about 0.2 wt % glidant; and (h) 0 to about 2 wt % lubricant; wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt % and about 79 wt %, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt % and about 23 wt %.
Inventor(s): Desai; Subhash (Grayslake, IL), Mancini; Alan Mark (Indian Head Park, IL), Schumann; Steven Charles (Elgin, IL)
Assignee: G. D. Searle & Company (Chicago, IL)
Application Number:08/187,568
Patent Claims: 1. A granular pharmaceutical composition for compression into a modified release, once daily tablet dosage form of metronidazole, the composition comprising:

(a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole;

(b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent;

(c) about 0.1 wt % to about 2.0 wt % detackifier;

(d) 0 to about 23 wt % of a first aqueous soluble pharmaceutical diluent;

(e) 0 to about 23 wt % of a second aqueous soluble diluent for forming a pharmaceutical tablet, the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent;

(f) 0 to about 20 wt % of a second portion of metronidazole;

(g) 0 to about 0.2 wt % glidant; and

(h) 0 to about 2 wt % lubricant;

wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt % and about 79 wt %, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt % and about 23 wt %.

2. A pharmaceutical composition according to claim 1, wherein the first aqueous soluble diluent is present in an amount of from about 5% and about 11% by weight and the second aqueous soluble diluent is present in an amount of from about 8% and about 18% by weight.

3. A pharmaceutical composition according to claim 2, wherein the first aqueous soluble diluent and the second aqueous soluble diluent are lactose.

4. A pharmaceutical composition according to claim 1 which comprises from about 0.01 wt % to about 0.2 wt % of a pharmaceutically acceptable glidant and from about 0.1 wt % to about 2 wt % of a pharmaceutically acceptable lubricant.

5. A pharmaceutical composition according to claim 1 comprising (i) from about 1.9% to about 2.5% of the aqueous insoluble poly(meth)acrylic acid ester copolymer; (ii) from about 6% to about 9% of the first aqueous soluble diluent; and (iii) from about 12% to about 17% of the second aqueous soluble diluent; and wherein the sum of the percentage of the first portion of metronidazole and the second portion of metronidazole is from about 72.5% to about 74.5%.

6. A pharmaceutical composition according to claim 1 wherein the detackifying agent is talc.

7. A pharmaceutical composition according to claim 1 which comprises about 74.05% metronidazole, about 8.22% hydrous lactose, about 2.47% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 1.23% talc, about 0.03% simethicone emulsion, about 12.90% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

8. A pharmaceutical composition according to claim 1 which comprises about 72.99% metronidazole, about 6.48% hydrous lactose, about 1.95% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 0.97% talc, about 0.03% simethicone emulsion, about 16.49% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

9. A pharmaceutical tablet dosage form for once daily dosing of metronidazole, the tablet comprising a therapeutically effective amount of a pharmaceutical composition comprising:

(a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole;

(b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent;

(c) about 0.1 wt % to about 2.0 wt % detackifier;

(d) 0 to about 23 wt % of a first aqueous soluble pharmaceutical diluent;

(e) 0 to about 23 wt % of a second aqueous soluble diluent for forming a pharmaceutical tablet, the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent;

(f) 0 to about 20 wt % of a second portion of metronidazole;

(g) 0 to about 0.2 wt % glidant; and

(h) 0 to about 2 wt % lubricant;

wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt % and about 79 wt %, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt % and about 23 wt %.

10. A method for treating a patient infected with a microorganism which is susceptible to metronidazole, which method comprises administering a pharmaceutical tablet of claim 9 once daily to the patient for a number of days sufficient to eliminate the infection.

11. A method according to claim 10 wherein the microorganism causes a disease which is selected from the group consisting of trichomoniasis, amoebiasis, and bacterial vaginosis.

12. A method according to claim 10 wherein the microorganism is a species of Helicobacter.

13. A method according to claim 12, wherein the microorganism is Helicobacter pylori.

14. A method according to claim 10, wherein the pharmaceutical tablet dosage form comprises about 74.05% metronidazole, about 8.22% hydrous lactose, about 2.47% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 1.23% talc, about 0.03% simethicone emulsion, about 12.90% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

15. A method according to claim 14, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

16. A method according to claim 15, wherein the pharmaceutical tablet dosage form comprises about 750 milligrams of metronidazole.

17. A method according to claim 10, wherein the pharmaceutical tablet dosage form comprises about 72.99% metronidazole, about 6.48% hydrous lactose, about 1.95% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 0.97% talc, about 0.03% simethicone emulsion, about 16.49% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

18. A method according to claim 17, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

19. A method according to claim 18, wherein the pharmaceutical tablet dosage form comprises about 750 milligrams of metronidazole.

20. A pharmaceutical tablet dosage form according to claim 9, wherein the first aqueous soluble diluent is present in an amount of from about 5% and about 11% by weight and the second aqueous soluble diluent is present in an amount of from about 8% and about 18% by weight.

21. A pharmaceutical tablet dosage form according to claim 20, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

22. A pharmaceutical tablet dosage form according to claim 21, wherein the first aqueous soluble diluent and the second aqueous soluble diluent are lactose.

23. A pharmaceutical tablet dosage form according to claim 22 which comprises from about 0.01 wt % to about 0.2 wt % of a pharmaceutically acceptable glidant and from about 0.1 wt % to about 2 wt % of a pharmaceutically acceptable lubricant.

24. A pharmaceutical tablet dosage form according to claim 9 which comprises about 750 milligrams of metronidazole.

25. A pharmaceutical tablet dosage form according to claim 9 comprising (i) from about 1.9% to about 2.5% of the aqueous insoluble poly(meth)acrylic acid ester copolymer; (ii) from about 6% to about 9% of the first aqueous soluble diluent, and (iii) from about 12% to about 17% of the second aqueous soluble diluent; and wherein the sum of the percentage of the first portion of metronidazole and the second portion of metronidazole is from about 72.5% to about 74.5%.

26. A pharmaceutical tablet dosage form according to claim 25, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

27. A pharmaceutical tablet dosage form according to claim 26 which comprises about 750 milligrams of metronidazole.

28. A pharmaceutical tablet dosage form according to claim 9 which comprises about 74.05% metronidazole, about 8.22% hydrous lactose, about 2.47% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 1.23% talc, about 0.03% simethicone emulsion, about 12.90% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

29. A pharmaceutical tablet dosage form according to claim 28, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

30. A pharmaceutical tablet dosage form according to claim 29 which comprises about 750 milligrams of metronidazole.

31. A pharmaceutical tablet dosage form according to claim 29, wherein the tablet is coated with an aqueous soluble polymeric coat.

32. A pharmaceutical tablet dosage form according to claim 9 which comprises about 72.99% metronidazole, about 6.48% hydrous lactose, about 1.95% of the aqueous insoluble poly(meth)acrylic acid ester copolymer, about 0.97% talc, about 0.03% simethicone emulsion, about 16.49% anhydrous lactose, about 0.10% colloidal silicon dioxide, and about 0.99% magnesium stearate.

33. A pharmaceutical tablet dosage form according to claim 32, wherein the aqueous insoluble poly(meth)acrylic acid ester copolymer is Eudragit NE30.

34. A pharmaceutical tablet dosage form according to claim 33 which comprises about 750 milligrams of metronidazole.

35. A pharmaceutical tablet dosage form according to claim 33, wherein the tablet is coated with an aqueous soluble polymeric coat.
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