Pharmaceutical composition

• US 6,121,314 A
• Filed: 11/10/1999
• Issued: 09/19/2000
• Est. Priority Date: 05/20/1991
• Status: Expired due to Fees

• Current Assignee: Novartis Ag
• Original Assignee: Novartis Ag
• Inventors: Steiger, Michel, Richter, Friedrich
• Primary Examiner(s): Weddington, Kevin E.
• Application Number:
  US09/437,843
• Time in Patent Office: 314 Days
• Field of Search: 514/481, 514/864, 514/944, 514/947
• US Class Current: 514/481
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• 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 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• 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

Abstract

Non-greasy topical solutions, emulsion gels or lotions comprising as the active agent a compound of formula I ##STR1## and a lower alkanol, and if desired together with a solubilizing agent or an oil phase such as isopropyl myristate are useful delivery systems.

Claims

1. A topical pharmaceutical composition comprising as the active agent a compound of formula I ##STR3## and a lower alkanol.

2. A composition according to claim 1 containing water.

3. A composition according to claim 2 containing from 50 to 85% of water.

4. A composition according to claim 1 containing from 5 to 35% of a lower alkanol.

5. A composition according to claim 4 wherein the alkanol is ethanol.

6. A composition according to claim 1 which is substantially free of fatty material.

7. A composition claim 1 containing a surfactant being non-anionic.

8. A composition claim 1 for the treatment of fungal infections wherein the active agent is the compound of formula I as defined in claim 1 in free base form or in acid addition salt form, together with a solubilizing agent and excipients as appropriate.

9. A composition according to claim 8 which is a spray, a gel or a fluid gel.

10. A composition according to claim 8 wherein the solubilizing agent is a polyoxyethylene fatty alcohol ether.

11. A composition according to claim 8 or wherein the ratio between the compound of formula I and the solubilizing agent is from about 1:

0.5 to about 1;

15.

12. A composition according to claim 1 wherein the active agent is the compound of formula I as defined in claim 1 in free base form or in acid addition salt form, together with an oil phase and further excipients as appropriate.

13. A composition according to claim 1 containing isopropyl myristate as an oil phase.

14. A composition according to claim 12 or wherein the ratio between the compound of formula I and the oil phase is from about 1:

5 to about 1;

40 on a w/w basis.

15. A composition according to claim 1 wherein the compound of formula I is present from about 0.1% to about 5% of the total weight of the composition on a w/w basis.

16. A process for the preparation of a topical pharmaceutical composition according to claim 1 comprising working up a compound of formula I as defined in claim 1 together with a lower alkanol and adding further excipients as appropriate.

17. A method for the treatment of fungal infections comprising administering a pharmaceutically effective amount of a composition according to claim 1 to a patient in need of such treatment.