IP Library › Patent Application 14671655
Patent Application
App. No. 14/671,655

PROGESTERONE FORMULATIONS HAVING A DESIRABLE PK PROFILE

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Patent No.
US None
App. No.
14/671,655
Abstract

This disclosure provides progesterone formulations, methods of using these formulations, and their related pharmacokinetic parameters. In particular embodiments, the formulations disclosed herein allow for a reduction in the amount of progesterone administered to a patient in need thereof, while still providing the benefits of a larger dosage amount.

Claims (35)

1 . A pharmaceutical composition for orally administering progesterone to a subject in need thereof, the composition comprising:

an amount of progesterone;

a solubilizing agent; and

a nonionic surfactant selected from the group consisting of lauroyl macrogol-32 glycerides EP (GELUCIRE 44/11), lauroyl polyoxyl-32 glycerides (GELUCIRE 44/14), and caprylocaproyl macrogol-8 glycerides EP;

wherein the solubilizing agent comprises at least one C 6 -C 12 fatty acid mono-, di-, or tri-ester of glycerol and wherein the composition has a total mass.

2 . The pharmaceutical composition of claim 1 , wherein the solubilizing agent comprises at least one C 6 -C 12 fatty acid mono-ester of glycerol.

3 . The pharmaceutical composition of claim 1 , wherein the solubilizing agent comprises at least one C 6 -C 12 fatty acid di-ester of glycerol.

4 . The pharmaceutical composition of claim 1 , wherein the solubilizing agent comprises at least one C 6 -C 12 fatty acid tri-ester of glycerol.

5 . The pharmaceutical composition of claim 4 , wherein the tri-ester of glycerol comprises predominantly esters of caprylic fatty acid (C 8 ) and capric fatty acid (C 10 ).

6 . The pharmaceutical composition of claim 4 , wherein the tri-ester of glycerol is MIGLYOL® 812.

7 . The pharmaceutical composition of claim 1 , wherein the solubilizing agent is medium chain triglycerides (MIGLYOL® 812).

8 . The pharmaceutical composition of claim 7 , wherein the nonionic surfactant is lauroyl polyoxyl-32 glycerides (GELUCIRE® 44/14).

9 . The pharmaceutical composition of claim 1 , wherein the amount of progesterone is from 25 mg to 200 mg.

10 . The pharmaceutical composition of claim 1 , wherein the amount of progesterone is 75 mg or 150 mg.

11 . The pharmaceutical composition of claim 1 , wherein the amount of progesterone includes a solubilized amount of progesterone and a suspended amount of progesterone.

12 . The pharmaceutical composition of claim 1 , wherein the composition is provided in a gelatin capsule.

13 . The pharmaceutical composition of claim 12 , wherein the total mass of the composition is less than 500 mg.

14 . The pharmaceutical composition of claim 1 , wherein the composition provides increased progesterone bioavailability compared to micronized progesterone suspended in peanut oil.

15 . The pharmaceutical composition of claim, 1 wherein the solubilizing agent comprises predominantly at least one C 6 -C 12 fatty acid mono-, di-, or tri-ester of glycerol.

16 . A pharmaceutical composition for orally administering progesterone to a subject in need thereof, the composition comprising:

75, 150, 200, or 300 mg of progesterone;

a solubilizing agent comprising predominantly a triglyceride oil of C8 and C10 fatty acid esters; and

lauroyl polyoxyl-32 glycerides (GELUCIRE 44/14).

17 . A method of preventing endometrial hyperplasia, the method comprising administering to a patient in need thereof a composition according to claim 1 .

18 . The method of preventing endometrial hyperplasia of claim 17 , wherein the amount of progesterone is 150 mg.

19 . A method of treating amenorrhea, the method comprising administering to a patient in need thereof a composition according to claim 1 .

20 . The method of treating amenorrhea of claim 19 , wherein the amount of progesterone is 150 mg or 300 mg.

21 . The pharmaceutical composition of claim 1 , wherein the amount of progesterone comprises about 33% by weight of the composition; the solubilizing agent comprises about 65% by weight of the composition, the non-ionic surfactant comprises about 1.7% by weight of the composition.

22 . The pharmaceutical composition of claim 1 , wherein the amount of progesterone comprises about 33.33% by weight of the composition; the solubilizing agent comprises about 64.93% by weight of the composition, the non-ionic surfactant comprises about 1.67% by weight of the composition.

23 . The pharmaceutical composition of claim 21 , further comprising an antioxidant.

24 . The pharmaceutical composition of claim 23 , wherein the antioxidant is butylated hydroxy toluene.

25 . The pharmaceutical composition of claim 21 , wherein the solubilizing agent is MIGLYOL 812.

26 . The pharmaceutical composition of claim 25 , wherein the non-ionic surfactant is lauroyl polyoxyl-32 glycerides (GELUCIRE 44/14).

27 . The pharmaceutical composition of claim 26 , wherein the amount of progesterone is 200 mg.

28 . The pharmaceutical composition of claim 26 , wherein the amount of progesterone is 150 mg.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2015
From: CACASE, JANICE; PERSICANER, PETER; THORSTEINNSON, THORSTEINN; SANCILLIO, FREDERICK; AMADIO, JULIA; BERNICK, BRIAN
To: THERAPEUTICSMD, INC.
Reel/Frame 035496/0596 →