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Claims for Patent: 7,799,331

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Claims for Patent: 7,799,331

Title:Oral suspension of prednisolone acetate
Abstract: The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation.
Inventor(s): Asotra; Satish (Brampton, CA), Gao; Shen (Botton, CA), Yacobi; Avraham (Englewood, NJ)
Assignee: Taro Pharmaceutical North America, Inc. (Grand Cayman, KY)
Application Number:11/457,197
Patent Claims: 1. A pharmaceutical composition for oral delivery, comprising a pharmaceutically effective amount of prednisolone acetate particles dispersed in suspension in the composition, wherein the composition is suitable for oral delivery and wherein the prednisolone acetate has a median particle size in the range of about 1.mu.m to about 30.mu.m.

2. The pharmaceutical composition of claim 1, further comprising a thickening agent.

3. The pharmaceutical composition of claim 1, comprising from about 0.5 mg/mL to about 5 mg/mL of prednisolone acetate.

4. The pharmaceutical composition of claim 1, wherein the prednisolone acetate has a median particle size of about 5.mu.m to about 20 .mu.m.

5. The pharmaceutical composition of claim l, wherein the prednisolone acetate has a median particle size of about 6.mu.m to about 8.mu.m.

6. The pharmaceutical composition of claim 2 wherein the thickening agent is a carbomer.

7. The pharmaceutical composition of claim 1, further comprising a wetting agent.

8. The pharmaceutical composition of claim 2 having a pH of between about 4.0 to about 5.9.

9. The pharmaceutical composition of claim 2 having a pH of between about 4.6 to about 5.4.

10. The pharmaceutical composition of claim 1, comprising from about 0.5 mg/mL to about 5 mg/mL of prednisolone acetate, water, glycerin, sorbitol in an amount up to about 20m % (w/w), propylene glycol in an amount up to about 20% (w/w), wetting agent in an amount up to about 3% (w/w) and a thickening agent in an amount up to about 1% (w/w).

11. The pharmaceutical composition of claim 1, comprising: a. from about 5 mg/5 mL to about 15 mg/5 mL prednisolone acetate in suspension in the composition; b. 0.1% poloxamer 188; c. 50% glycerin; d. 5% sorbitol crystalline; e. 5% propylene glycol; f. 0.065% edetate disodium; g. 0.2% sucralose; h. carbomer in an amount up to about 1%; i. 0.04% butylparaben; and j. sodium hydroxide.

12. The pharmaceutical composition of claim 1, wherein the pH is between about 4.8 to about 5.2.

13. A method of treating a patient in need of prednisolone comprising the step of orally administering a therapeutically effective amount of the pharmaceutical composition of claim 1.

14. The method of claim 13 wherein the patient is suffering from a medical condition selected from the group consisting of endocrine disorders, rheumatic disorders, collagen diseases, dermatologic diseases, allergic states, respiratory diseases, hemaologic disorders, neoplastic diseases, edema, gastrointestinal diseases or nervous diseases.

15. The composition of claim 1, wherein the median particle size is below about 20.mu.m.

16. The composition of claim 1, wherein the median particle size is below about 10.mu.m.

17. The composition of claim 1, wherein the median particle size is below about 8.mu.m.

18. The composition of claim 1, wherein the prednisolone acetate particles stay within the median particle size range over time.

19. The pharmaceutical composition of claim 1, wherein a 5 mg dose of the composition, when administered to a human, is bioequivalent, within the 80-125% confidence interval and with a statistical power of at least 80%, to a 5 mg tablet of prednisolone.

20. The pharmaceutical composition of claim 1, wherein the composition exhibits an in vitro dissolution profile of about 85% released after about 15 minutes, about 95% released after about 30 minutes, about 97% released after about 45 minutes and about 97% released after about 60 m minutes.

21. The pharmaceutical composition of claim 1, wherein the prednisolone acetate remains dispersed in the suspension without agitation during the shelf life of the composition.

22. The pharmaceutical composition of claim 1, comprising carbomer and poloxamer.

23. A pharmaceutical composition for oral delivery comprising a pharmaceutically effective amount of micronized prednisolone acetate particles in suspension in the composition, wherein the composition, when administered to humans and tested for one or more pharmacokinetic parameters selected from the group consisting of C.sub.max, T.sub.max, AUC.sub.T, AUC.sub..infin., K.sub.el, and T.sub.1/2 el, is bioequivalent to a 5 mg tablet of prednisolone, within the 80-125% confidence interval and with a statistical power of at least 80% , and wherein the composition is suitable for oral delivery and wherein the prednisolone acetate has a median particle size in the range of about 1 .mu.m to about 30 .mu.m.

24. The pharmaceutical composition of claim 23, wherein the composition has pharmacokinetic parameters within the 80-125% confidence interval, with a statistical power of at least 80%, of one or more of the following values: a. C.sub.max of 176.27 ng/mL; b. T.sub.max of 1.00 hour; c. AUC.sub.T of 812.39 ng h/mL; d. AUC.sub..infin.of 846.53 ng h/mL; e. K.sub.el of 0.2629 hr.sup.-1; and f. T.sub.1/2 el of 2.66 hours.

25. A pharmaceutical composition comprising a pharmaceutically effective amount of prednisolone acetate particles dispersed in suspension in the composition, wherein the composition is suitable for oral delivery, comprises components that are mutually compatible, comprises carbomer and a wetting agent, has a pH between about 4.0 and 5.9, is palatable, has a viscosity of about 5,000 to about 15,000 cps, and is storage stable.

26. The composition of claim 25, wherein the pH is between about 4.6 and about 5.4.

27. The composition of claim 25, wherein the pH is between about 5 and about 5.4.

28. The composition of claim 25, wherein the wetting agent is poloxamer.

29. The composition of claim 25, wherein the composition comprises an aqueous vehicle.

30. The pharmaceutical composition of claim 25, wherein the prednisolone acetate remains dispersed in the suspension without agitation during the shelf life of the composition and has a crystalline stability such that the prednisolone particles stay within a target particle size range over time.

31. The pharmaceutical composition of claim 25, wherein the composition is spill-resistant.

32. A pharmaceutical composition comprising a pharmaceutically effective amount of fine milled prednisolone acetate particles in suspension in a vehicle, wherein the composition exhibits an in vitro dissolution profile of about 45% released after about 5 minutes, about 85% released after about 15 minutes, about 95% released after about 30 minutes, about 97% released after about 45 minutes and about 97% released after about 60 minutes, wherein the composition is suitable for oral delivery and comprises carbomer and a wetting agent, and has a pH between about 4.0 and 5.9.
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