Microemulsion preconcentrates comprising cyclosporins

• US 5,998,365 A
• Filed: 06/15/1998
• Issued: 12/07/1999
• Est. Priority Date: 12/15/1995
• Status: Expired due to Fees

• Current Assignee: Bernard C. Sherman
• Original Assignee: Bernard C. Sherman
• Inventors: Sherman, Bernard Charles
• Primary Examiner(s): MOEZIE, FATEMEH T
• Application Number:
  US09/077,803
• Time in Patent Office: 540 Days
• Field of Search: 514/11, 514/885, 514/937, 514/938, 514/963, 514/964, 514/970, 424/455, 424/489
• US Class Current: 514/20.5
• CPC Class Codes: A61K 38/13 Cyclosporins
• 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 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A pharmaceutical composition in the form of a microemulsion preconcentrate comprising a cyclosporin dissolved in a solvent system further comprising a hydrophobic component, a hydrophilic component, and a surfactant, wherein either the hydrophobic component is selected from tocol, tocopherols, tocotrienols, and derivatives thereof, or the hydrophilic component is selected from propylene carbonate or polyethylene glycol having an average molecular weight of less than 1000.

Claims

1. A pharmaceutical composition wherein said composition is a microemulsion preconcentrate comprising a cyclosporin dissolved in a solvent system, said solvent system comprising a hydrophilic component, a hydrophobic component, and a surfactant, wherein the hydrophilic component is propylene carbonate or polyethylene glycol having average molecular weight of less than 1000.

2. A pharmaceutical composition according to claim 1 wherein the hydrophilic component is propylene carbonate.

3. A pharmaceutical composition according to claim 1 wherein the hydrophilic component is polyethylene glycol having average molecular weight of less than 1000.

4. A pharmaceutical composition according to claim 1 wherein the hydrophilic component is polyethylene glycol having average molecular weight of not more than 600.

5. A pharmaceutical composition according to claim 1 wherein the hydrophobic component is selected from the group consisting of tocol, a tocol derivative, a tocopherol, a tocopherol derivative, a tocotrienol and a tocotrienol derivative wherein said hydrophobic component comprises at least two percent of the composition by weight.

6. A composition according to claim 5 wherein the hydrophobic component constitutes at least four percent of the composition by weight.

7. A composition according to claim 6 wherein the hydrophobic component constitutes at least eight percent of the composition by weight.

8. A composition according to claim 5 wherein the hydrophobic component is selected from the group consisting of tocopherol and a tocopherol derivative.

9. A composition according to claim 8 wherein the hydrophobic component is vitamin E or vitamin E acetate.

10. A composition according to claim 8 wherein the hydrophobic component is natural mixed tocopherols.

11. A composition according to claim 1 wherein the cyclosporin is cyclosporine.

12. A composition according to claim 1 wherein the surfactant comprises a polyoxyethylene glycolated natural or hydrogenated vegetable oil.

13. A composition according to claim 1 suitable for oral administration.

14. A composition according to claim 1 comprising from 5 to 20% by weight of cyclosporin.