PHARMACEUTICAL COMPOSITIONS OF LAVENDUSTIN

• US 20080242686A1
• Filed: 06/05/2008
• Published: 10/02/2008
• Est. Priority Date: 08/19/2003
• Status: Abandoned Application

• Current Assignee: Katrin Kriwet
• Original Assignee: Katrin Kriwet
• Inventors: Kriwet, Katrin
• Application Number:
  US12/133,810
• Publication Number:
  US 20080242686A1
• Time in Patent Office: Days
• US Class Current: 514/266.1
• CPC Class Codes: A61K 31/517 ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• CPC Class Codes: A61K 47/10 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 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 9/0014 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: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/08 Antiseborrheics
• CPC Class Codes: A61P 17/12 Keratolytics, e.g. wart or anti-corn preparations
• CPC Class Codes: A61P 17/16 Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 35/04 specific for metastasis

Abstract

Topical pharmaceutical compositions, e.g. in form of an emulsion, comprising a lavendustin derivative of formula (I): wherein R is methyl, methoxy or ethyl, or a pharmaceutically acceptable salt thereof, and an emollient, and optionally further excipients.

Claims

1. :

A topical pharmaceutical composition comprising a lavendustin derivative of formula I

2. :

A composition according to claim 1 wherein the emollient is isopropyl myristate.

3. :

A composition according to claim 1 in the form of an emulsion.

4. :

A composition according to claim 3 in the form of an oil-in-water emulsion.

5. :

A topical pharmaceutical composition according to claim 1 which avoids high local concentration of the lavendustin derivative of formula I in the skin or mucous membrane and is well tolerated.

6. :

A process for the preparation of a composition according to claim 1, comprising

(a) dissolving a lavendustin derivative of formula I

7. :

A composition according to claim 1 for use in the treatment of hyperproliferative disorders such as actinic keratosis, anogenital warts and seborrhoic keratosis, and skin cancer.

8. :

Use of a composition according to claim 1 in the preparation of a medicament for the treatment of hyperproliferative disorders such as actinic keratosis, anogenital warts and seborrhoic keratosis, and skin cancer.

9. :

A method for the treatment of hyperproliferative disorders such as actinic keratosis, anogenital warts and seborrhoic keratosis, and skin cancer comprising administering a composition according to claim 1 to the skin or mucous membrane of a patient in need thereof.

10. A composition according to claim 1 wherein the emollient comprises liquid fatty alcohols, oleyl alcohol, liquid waxes, isopropyl myristate, oleyl erucate, diisopropyl adipate, oleyl oleate, diglycerides having C₈ to C₂₄ fatty acids, triglycerides having C₈ to C₂₄ fatty acids, medium chain fatty acid triglycerides, propylene glycol mono-fatty acid esters, propylene glycol di-fatty acid esters, propylene glycol caprylate, propylene glycol dilaurate, propylene glycol hydroxystearate, propylene glycol isostearate, propylene glycol laurate, propylene glycol ricinoleate, and propylene glycol stearate, petrolatum, or mixtures thereof.

11. A composition according to claim 1 wherein the lavendustin derivative is present in an amount of from about 0.01% to about 10% by weight based on the total weight of the composition.

12. A composition according to claim 1 wherein the emollient is present in an amount of about 1% to about 40% by weight based on the total weight of the composition.

13. A composition according to claim 1 wherein the hydrophilic component comprises propylene glycol, hexylene glycol, liquid polyethylene glycol, glycerol, or mixtures thereof.

14. A composition according to claim 1 wherein the hydrophilic component is present in an amount of about 1% to about 20% by weight based on the total weight of the composition.

15. A composition according to claim 3 in the form of a water-in-oil emulsion.

16. A composition according to claim 1 wherein the water is present in an amount of from about 20% to about 80% by weight based on the total weight of the composition.

17. A composition according to claim 1 wherein the compound comprising a lavendustin derivative of formula I is 6-[2-(2,5-dimethoxyphenyl)ethyl]-4-ethyl-quinazoline.

18. The process of claim 6 wherein the temperature is from about 60°

C. to about 80°

C.

19. The method of claim 9 wherein the hyperproliferative disorder is selected from the group consisting of actinic keratosis, anogenital warts and seborrhoic keratosis.