PROGESTERONE FORMULATIONS

• US 20150148323A1
• Filed: 06/18/2013
• Published: 05/28/2015
• Est. Priority Date: 06/18/2012
• Status: Active Grant

• Current Assignee: TherapeuticsMD Inc.
• Original Assignee: TherapeuticsMD Inc.
• Inventors: Cacace, Janice Louise, Periscaner, Peter H.R.
• Granted Patent: US 10,052,386 B2
• Time in Patent Office: Days
• US Class Current: 514/177
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/566 having an oxo group in position 17, e.g. estrone
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61K 9/48 Preparations in capsules, e.g. of gelatin, of chocolate A61K9/0004 takes precedence; bite capsules A61K9/0056
• CPC Class Codes: A61K 9/4825 Proteins, e.g. gelatin gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/06 Antiabortive agents; Labour repressants
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

Various pharmaceutical formulations are disclosed herein. For example, a pharmaceutical formulation is disclosed comprising ultra-micronized progesterone.

Claims

1-17. -17. (canceled)

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

suspended progesterone;

solubilized progesterone;

a carrier, the carrier comprising a C6-C14 medium chain oil; and

a non-ionic surfactant.

19. The pharmaceutical composition of claim 18, wherein the carrier comprises at least one of mono-, di-, triglycerides, and combinations thereof, wherein the at least one mono-, di-, and triglycerides are predominantly C6-C12 fatty acid chain lengths.

20. The pharmaceutical composition of claim 19, wherein the at least one mono-, di-, and triglycerides are predominantly about >

50 wt % C6-C12 fatty acid chain lengths.

21. The pharmaceutical composition of claim 19, wherein the medium chain oils are predominantly about >

50 wt % C6-C12 mono- and diglycerides.

22. The pharmaceutical composition of claim 19, wherein the medium chain oils are predominantly about <

10 wt % C6-C12 triglycerides.

23. The pharmaceutical composition of claim 18, wherein the non-ionic surfactant comprises C8 to C18 fatty acid esters of glycerol and polyethylene glycol and has an HLB value of about 15.

24. The pharmaceutical composition of claim 18, wherein the total suspended progesterone and solubilized progesterone comprises from about 25 mg to about 200 mg of progesterone.

25. The pharmaceutical composition of claim 24, wherein the total suspended progesterone and solubilized progesterone is one of the group consisting of 75 mg and 150 mg.

26. The pharmaceutical composition of claim 18, wherein the composition is formulated as a gelatin capsule.

27. The pharmaceutical composition of claim 18, wherein the composition provides increased bioavailability compared to micronized progesterone suspended in peanut oil.

28. A method comprising:

administering to a subject having endometrial hyperplasia a pharmaceutical composition comprising;

suspended progesterone;

solubilized progesterone;

a carrier; and

a non-ionic surfactant;

wherein the carrier comprises a C6-C14 medium chain oil.

29. The method of claim 28, wherein the carrier comprises at least one of mono-, di-, triglycerides, and combinations thereof, wherein the at least one mono-, di-, and triglycerides are predominantly C6-C12 fatty acid chain lengths.

30. The pharmaceutical composition of claim 28, wherein the total suspended progesterone and solubilized progesterone comprises from about 25 mg to about 200 mg of progesterone.

31. The method of claim 28, wherein the composition is formulated as a gelatin capsule.

32. The method of claim 28, wherein the composition comprises increased bioavailability compared to micronized progesterone suspended in peanut oil.

33. A method comprising:

administering to a subject in need of treatment for amenorrhea a pharmaceutical composition comprising;

suspended progesterone;

solubilized progesterone;

a carrier; and

a non-ionic surfactant;

wherein the carrier comprises a C6-C14 medium chain oil.

34. The method of claim 33, wherein the carrier comprises at least one of mono-, di-, triglycerides, and combinations thereof, wherein the at least one mono-, di-, and triglycerides are predominantly C6-C12 fatty acid chain lengths.

35. The pharmaceutical composition of claim 33, wherein the total suspended progesterone and solubilized progesterone comprises from about 25 mg to about 200 mg of progesterone.

36. The method of claim 33, wherein the composition is formulated as a gelatin capsule.

37. The method of claim 33, wherein the composition comprises increased bioavailability compared to micronized progesterone suspended in peanut oil.