EBASTINE TOPICAL COMPOSITION

• US 20200129495A1
• Filed: 10/29/2018
• Published: 04/30/2020
• Est. Priority Date: 10/29/2018
• Status: Abandoned Application

• Current Assignee: LEO Pharma A/S (LEO Holding A/S (Denmark))
• Original Assignee: Biopharmx, Inc. (Timber Pharmaceuticals, Inc.)
• Inventors: CHEN, Xin, JUMAA, Mouhannad, NAGAVARAPU, Usha, HERMSMEIER, Maiko C.
• Application Number:
  US16/174,216
• Publication Number:
  US 20200129495A1
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/4515 having a butyrophenone group in position 1, e.g. haloperidol pipamperone A61K31/4545
• 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 47/38 Cellulose; Derivatives thereof
• 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: A61P 17/14 for baldness or alopecia

Abstract

Provided herein is a topical composition for treatment of a hair-loss related condition or disease and related methods for making and using the topical composition. The topical composition generally comprises ebastine dissolved in a solvent. In some exemplary embodiments, the solvent comprises a monohydric aliphatic alcohol and an ester. In some exemplary embodiments, the solvent comprises a polyol.

Claims

1. A topical pharmaceutical composition, comprising:

ebastine, and

a solvent,

wherein the ebastine is dissolved in the composition at room temperature.

2. The topical pharmaceutical composition of claim 1,

wherein the solvent comprises a volatile solvent and a non-volatile solvent.

3. The topical pharmaceutical composition of claim 2, wherein the non-volatile solvent is evaporated to form a residual composition, and ebastine is dissolved in the residual composition.

4. The topical pharmaceutical composition of claim 2, wherein ebastine is more soluble at room temperature in the volatile solvent than in the non-volatile solvent.

5. The topical pharmaceutical composition of claim 2, wherein ebastine is more soluble at room temperature in the non-volatile solvent than in the volatile solvent.

6. The topical pharmaceutical composition of claim 2, wherein ebastine is more soluble at room temperature in the solvent than in either the volatile solvent or the non-volatile solvent.

7. The topical pharmaceutical composition of claim 2, wherein the volatile solvent is a monohydric aliphatic alcohol and the non-volatile solvent is an ester.

8. The topical pharmaceutical composition of claim 7, wherein the monohydric aliphatic alcohol is ethanol.

9. The topical pharmaceutical composition of claim 7, wherein the ester is selected from the group consisting of diethyl sebacate, dimethyl succinate, and ethyl acetate.

10. The topical pharmaceutical composition of claim 7, wherein the ratio of concentrations by weight of monohydric aliphatic alcohol to ester is in the range of 1:

1 to 99;

1.

11. The topical pharmaceutical composition of claim 7, wherein the monohydric aliphatic alcohol comprises 40 percent to 99 percent of the composition by weight.

12. The topical pharmaceutical composition of claim 1, wherein the solvent comprises a polyol.

13. The topical pharmaceutical composition of claim 12, wherein the polyol is propylene glycol.

14. The topical pharmaceutical composition of claim 1, wherein the ebastine is stable when stored in a sealed glass container for at least 2 months or longer at 40°

C. in a dark environment.

15. The topical pharmaceutical composition of claim 1,

wherein the solvent comprises

a concentration of water and

a concentration of a non-aqueous solvent,

wherein the concentration of the non-aqueous solvent exceeds the concentration of water, and

wherein the pH of the composition is in the range of 3 to 7.

16. The topical pharmaceutical composition of claim 1, wherein the composition is non-aqueous.

17. The topical pharmaceutical composition of claim 1, wherein the composition does not comprise an active pharmaceutical ingredient other than ebastine.

18. A method for the treatment of a hair-loss related condition or disease, comprising:

topically applying a composition comprising ebastine dissolved in a solvent to the scalp of a human patient at least once daily for a period of at least one month.

19. The method of claim 18, wherein the hair-loss related condition or disease is selected from the group consisting of scarring alopecia, non-scarring alopecia, androgenetic alopecia, and alopecia areata .

20. The method of claim 18, wherein the daily dosage of ebastine is in the range of 1.0 mg/cm² to 10 mg/cm².

21. The method of claim 18, wherein the composition does not comprise an active pharmaceutical ingredient other than ebastine.

22. A kit for the delivery of a topical pharmaceutical composition, comprising:

a container closure,

a topical pharmaceutical composition comprising ebastine dissolved in a solvent, and instructions for use,

wherein the instructions for use comprises instructions to apply the composition to the scalp of a patient.