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Last Updated: October 31, 2020

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Claims for Patent: 10,179,140

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Summary for Patent: 10,179,140
Title:Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same
Abstract: A pharmaceutical composition comprising an active contraceptive drug and one or more pharmaceutically-acceptable excipients. The pharmaceutical composition, when subjected to an in vitro dissolution test according to the USP XXIII Paddle Method, results in no more than 50% of said active drug initially present being dissolved within 30 minutes, and at least 50% of the active drug being dissolved in a time range from about 3 hours to about 4 hours. The pharmaceutical composition is administered daily to a patient having a BMI of about 25 kg/m.sup.2 or more for at least a portion of a treatment cycle. The pharmaceutical composition does not cause a number of days of bleeding events in the patient exceeding an average of 15% per treatment cycle in consecutive treatment cycles of administration after an initial treatment cycle of administration.
Inventor(s): Perrin; Philippe (Paris, FR), Drouin; Dominique (Verrieres, FR), Boyer-Joubert; Cecile (Fontenay aux Roses, FR)
Assignee: Laboratorios Leon Farma SA (Leon, ES)
Application Number:15/433,427
Patent Claims: 1. A method of providing contraception in a patient having a BMI of 25 kg/m.sup.2 or more and bleeding events, the method comprising: administering a pharmaceutical composition comprising 2.5 mg to 5.5 mg of crystalline drospirenone and one or more pharmaceutically-acceptable excipients to a patient having a BMI of 25 kg/m.sup.2 or more for an initial treatment cycle and for subsequent consecutive treatment cycles, the pharmaceutical composition being administered daily for at least portions of the initial and subsequent consecutive treatment cycles; wherein the administering results in a limited number of days of bleeding events per treatment cycle in at least one of the subsequent consecutive treatment cycles and wherein the pharmaceutical composition does not contain an estrogen.

2. The method of claim 1, wherein the limited number of days of bleeding events in at least one of the subsequent consecutive treatment cycles of administration does not exceed about 13% per treatment cycle.

3. The method of claim 1, wherein the limited number of days of bleeding events in at least one of the subsequent consecutive treatment cycles of administration does not exceed about 11% per treatment cycle.

4. The method of claim 1, wherein the limited number of days of bleeding events in at least one of the subsequent consecutive treatment cycles of administration does not exceed about 10% per treatment cycle.

5. The method of claim 1, wherein the limited number of days of bleeding events in at least one of the subsequent consecutive treatment cycles of administration does not exceed about 7%.

6. The method of claim 1, wherein the limited number of days of bleeding events in at least one of the subsequent consecutive treatment cycles of administration does not exceed about 5%.

7. The method of claim 1, wherein the number of days of limited bleeding events in one of a second through ninth treatment cycles is reduced by about 44% to about 85% as compared to the initial treatment cycle.

8. The method of claim 1, wherein the number of days of limited bleeding events in one of the second through ninth treatment cycle is reduced by about 50% to about 75% as compared to the initial treatment cycle.

9. The method of claim 1, wherein the number of days of limited bleeding events in one of the second through the ninth treatment cycle is reduced by at least about 20% as compared to the initial treatment cycle.

10. The method of claim 1, wherein the number of days of limited bleeding events in one of the second through ninth treatment cycle is reduced by at least about 40% as compared to the initial treatment cycle.

11. The method of claim 1, wherein the number of days of limited bleeding events in one of the second through the ninth treatment cycle is reduced by at least about 60% as compared to the initial treatment cycle.

12. The method of claim 1, wherein the administering causes weight loss in the patient measured from the initial treatment cycle and an end of one of a first through thirtieth subsequent consecutive treatment cycles.

13. The method of claim 12, wherein the weight loss is about 1 kg to about 10 kg.

14. The method of claim 12, wherein the weight loss is about 1 kg to about 4 kg.

15. The method of claim 12, wherein the weight loss results in a reduction in the patient's BMI of about 1% to about 20%.

16. The method of claim 12, wherein the weight loss results in a reduction in the patient's BMI of about 1% to about 5%.

17. The method of claim 1, wherein the administration of the pharmaceutical composition causes a decrease in a resting heart rate in the patient as measured from the initial treatment cycle and an end of one of a first through thirtieth subsequent consecutive treatment cycles.

18. The method of claim 17, wherein the decrease in the resting heart rate is at least 5 beats per minute.

19. The method of claim 17, wherein the decrease in the resting heart rate is at least 15 beats per minute.

20. The method of claim 17, where the decrease in the resting heart rate is about 2% to about 20%.

21. The method of claim 17, wherein the decrease in the resting heart rate is about 5% to about 7%.

22. The method of claim 1, wherein the subsequent consecutive treatment cycles are a first to thirtieth treatment cycles following the initial treatment cycle of administration.

23. The method of claim 1, wherein the drospirenone is non-micronized.

24. The method of claim 1, wherein the drospirenone is provided in a particle form.

25. The method of claim 24, wherein the particle form has a specific surface area from about 2,000 cm.sup.2/g to about 8,500 cm.sup.2/g.

26. The method of claim 24, wherein the particle form has a diameter of about 200 .mu.m or less.

27. The method of claim 24, wherein the particle form has a d.sub.50 in the range of about 10 .mu.m to about 60 .mu.m.

28. The method of claim 24, wherein a particle size distribution of the active contraceptive drug is characterized by: (i) a d.sub.90 particle size less than about 100 .mu.m, and/or (ii) a d.sub.50 particle size ranging from about 10 .mu.m to about 60 .mu.m, and/or (iii) a d.sub.10 particle size more than about 3 .mu.m.

29. The method of claim 28, wherein the d.sub.90 particle size ranges from about 20 .mu.m to about 40 .mu.m.

30. The method of claim 28, wherein the d.sub.50 particle size ranges from about 10 .mu.m to about 30 .mu.m.

31. The method of claim 28, wherein the d.sub.10 particle sizes range from about 3 .mu.m to about 9 .mu.m.

32. The method of claim 1, wherein the crystalline drospirenone is present in an amount of 3.0 mg to 4.5 mg.

33. The method of claim 1, wherein the crystalline drospirenone is present in an amount of 4 mg.

34. The method of claim 1, wherein the pharmaceutical composition is provided in a single daily oral tablet dosage form.

35. The method of claim 34, wherein the pharmaceutical composition comprising 3.2 mg to 4.8 mg of crystalline drospirenone.

36. The method of claim 35, wherein the pharmaceutical composition provides a pharmacokinetic profile for the drospirenone having: i) T.sub.max ranging from about 2.2 hours to 6 hours and ii) a mean C.sub.max which is less than 30 ng/ml when orally administered to the patient under fasting conditions.

37. The method of claim 36, wherein the pharmacokinetic profile for the drospirenone additionally comprises an AUC.sub.0h-tlast which is at least 300 ngh/ml.

38. The method of claim 36, wherein the mean C.sub.max ranges from 15 ng/ml to 30 ng/ml.

39. The method of claim 35, wherein when the pharmaceutical composition is subjected to an in vitro dissolution test according to the USP XXIII Paddle Method: no more than 50% of the drospirenone initially present in the pharmaceutical composition is dissolved within 30 minutes, and at least 50% of the drospirenone is dissolved in a time range from 3 hours to 4 hours.

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