Steroid hormone pharmaceutical composition

• US 10,532,059 B2
• Filed: 02/21/2018
• Issued: 01/14/2020
• Est. Priority Date: 04/01/2016
• Status: Active Grant

• Current Assignee: TherapeuticsMD Inc.
• Original Assignee: TherapeuticsMD Inc.
• Inventors: Shadiack, Annette, Persicaner, Peter H. R., Inskeep, Philip B., Thorsteinsson, Thorsteinn, Sancilio, Frederick D., Legassie, Jason D.
• Primary Examiner(s): Henley, III, Raymond J
• Application Number:
  US15/901,467
• Publication Number:
  US 20180280411A1
• Time in Patent Office: 692 Days
• Field of Search: 514177
• 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 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• 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 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• 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 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61K 9/4875 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/4858
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

This disclosure provides a novel pharmaceutical composition for delivering steroid hormones to a patient in need thereof.

Claims

1. A pharmaceutical composition suitable for administering a steroid hormone to a subject in need thereof, the pharmaceutical composition comprising:

a steroid hormone;

a lipophilic surfactant system comprising a first lipophilic surfactant and a second lipophilic surfactant, wherein the first and second lipophilic surfactants are different from each other;

a hydrophilic surfactant system comprising a first and second hydrophilic surfactant; and

an optional terpene.

2. The pharmaceutical composition of claim 1, wherein the first lipophilic surfactant is a first partial triglyceride and wherein the second lipophilic surfactant is a second partial triglyceride.

3. The pharmaceutical composition of claim 2, wherein the first hydrophilic surfactant is a polyoxyethylene sorbitan fatty acid derivative and the second hydrophilic surfactant is a castor oil or hydrogenated castor oil ethoxylate.

4. The pharmaceutical composition of claim 3, wherein the terpene is not optional.

5. The pharmaceutical composition of claim 1, wherein the steroid hormone is estradiol, progesterone, or a combination thereof.

6. The pharmaceutical composition of claim 5, wherein the steroid hormone is progesterone and wherein the progesterone is fully solubilized.

7. A method of treating a disease or condition associated with reduced progesterone levels, the method comprising administering to a subject in need thereof a pharmaceutical composition according to claim 1.

8. The method of claim 7, wherein the first lipophilic surfactant is a first partial triglyceride and wherein the second lipophilic surfactant is a second partial triglyceride.

9. The method of claim 8, wherein the first hydrophilic surfactant is a polyoxyethylene sorbitan fatty acid derivative the second hydrophilic surfactant is a castor oil or hydrogenated castor oil ethoxylate.

10. The method of claim 9, wherein the terpene is not optional.

11. The method of claim 7, wherein the disease or condition associated with reduced progesterone levels is selected from the group consisting of menopause, endometrial hyperplasia;

secondary amenorrhea;

prevention of preterm birth; and

osteoporosis.

18. A method of treating a disease or condition associated with reduced progesterone levels, the method comprising administering to a subject in need thereof a pharmaceutical composition according to claim 1, wherein the steroid hormone in the pharmaceutical composition is progesterone and further wherein the concentration of progesterone in the pharmaceutical composition is between about 0.025% and about 15% by weight.

19. The method of claim 18 wherein the concentration of progesterone in the pharmaceutical composition is between about 1% and about 9% by weight.

20. The method of claim 19 wherein the concentration of progesterone in the pharmaceutical composition is between about 5% and about 7% by weight.

21. The method of claim 20 wherein the concentration of progesterone in the pharmaceutical composition is about 6% by weight.

12. A method of increasing the bioavailability of a steroid hormone, the method comprising incorporating the steroid hormone in a composition comprising a lipophilic surfactant system comprising a first lipophilic surfactant and a second lipophilic surfactant, wherein the first and second lipophilic surfactants are different from each other, a hydrophilic surfactant system comprising a first and second hydrophilic surfactant, and an optional terpene.

13. The method of claim 12, wherein the first lipophilic surfactant is a first partial triglyceride and wherein the second lipophilic surfactant is a second partial triglyceride.

14. The method of claim 13, wherein the first hydrophilic surfactant is a polyoxyethylene sorbitan fatty acid derivative and the second hydrophilic surfactant is a castor oil or hydrogenated castor oil ethoxylate.

15. The method of claim 14, wherein the terpene is not optional.

16. The method of claim 12, wherein the steroid hormone is estradiol, progesterone, or a combination thereof.

17. The method of claim 16, wherein the steroid hormone is progesterone and wherein the progesterone is fully solubilized.