Formulations for solubilizing hormones

• US 10,328,087 B2
• Filed: 07/22/2016
• Issued: 06/25/2019
• Est. Priority Date: 07/23/2015
• Status: Active Grant

• Current Assignee: TherapeuticsMD Inc.
• Original Assignee: TherapeuticsMD Inc.
• Inventors: Thorsteinsson, Thorsteinn, Sancilio, Frederick D., Bernick, Brian A., Amadio, Julia M.
• Primary Examiner(s): Neagu, Irina
• Application Number:
  US15/217,301
• Publication Number:
  US 20170056418A1
• Time in Patent Office: 1,068 Days
• 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 31/015 carbocyclic
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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 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 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• 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: A61K 9/4858 Organic compounds
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives

Abstract

Compositions and methods for the solubilization of steroid hormones are disclosed.

Claims

1. A method of treating amenorrhea or endometrial hyperplasia in a patient in need thereof comprising orally administering to the patient an effective amount of a liquid composition comprising progesterone and d-limonene.

2. The method of claim 1, wherein the liquid composition is encapsulated in a soft gelatin capsule.

3. The method of claim 1, wherein the liquid composition further comprises an antioxidant.

4. The method of claim 3, wherein the antioxidant is selected from the group consisting of a-tocopherol acetate, acetone sodium bisulfite, acetylcysteine, ascorbic acid, ascorbyl palmitate, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), cysteine, cysteine hydrochloride, α

-tocopherol, dithiothreitol, monothioglycerol, nordihydroguaiaretic acid, propyl gallate, sodium bisulfite, sodium formaldehyde sulfoxylate, sodium metabisulfite, sodium sulfite, sodium thiosulfate, thiourea, tocopherol, and combinations thereof.

5. The method of claim 1, wherein the liquid composition comprises from about 25 mg of progesterone to about 500 mg of progesterone.

6. The method of claim 5, wherein the liquid composition comprises about 25, about 50, about 75, about 100, about 125, about 150, about 175, about 200, about 225, about 250, about 275, about 300, about 325, about 350, about 375, about 400, about 425, about 450, about 475, or about 500 mg of progesterone.