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Claims for Patent: 5,342,625

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Claims for Patent: 5,342,625

Title: Pharmaceutical compositions comprising cyclosporins
Abstract:Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva].sup.2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C.sub.1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
Inventor(s): Hauer; Birgit (Lahr, DE), Meinzer; Armin (Freiburg/Munzingen, DE), Posanski; Ulrich (Freiburg, DE), Richter; Friedrich (Schonbuhl-Urtenen, CH)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:07/990,734
Patent Claims: 1. A pharmaceutical composition comprising a cyclosporin as active ingredient,

1) a hydrophilic phase component comprising

1.1) a pharmaceutically acceptable di- or partial-ether of the formula

wherein R.sub.1 is C.sub.1-5 alkyl or tetrahydrofurfuryl, R.sub.2 is hydrogen, C.sub.1-5 alkyl or tetrahydrofurfuryl, and X is an integer from 1 to 6, or

1.2) 1,2-propylene glycol;

2) a lipophilic phase component; and

3) a surfactant;

wherein said composition is a microemulsion pre-concentrate, which upon dilution with water to a ratio of 1:1 parts by weight pre-concentrate to water or more of said water, is capable of providing an oil-in-water microemulsion having average particle size of less than about 1,000 .ANG..

2. A composition of claim 1 wherein said ratio is 1:5 parts by weight pre-concentrate to water or more of said water.

3. The composition according to claim 1 wherein said hydrophilic phase component comprises 1,2-propylene glycol.

4. The composition according to claim 3 wherein said hydrophilic phase component comprises a C.sub.1-5 alkanol as additional hydrophilic phase component.

5. The composition according to claim 4 wherein said C.sub.1-5 alkanol is ethanol.

6. The composition according to claim 1 wherein said lipophilic phase (2) comprises a fatty acid triglyceride.

7. The composition according to claim 1 wherein said surfactant (3) comprises a polyoxyethylene glycolated natural or hydrogenated vegetable oil.

8. The composition according to claim 1 wherein said surfactant (3) comprises an additional co-surfactant.

9. The composition according to claim 8 wherein said surfactant (3) comprises a polyoxyethylene glycolated natural or hydrogenated vegetable oil as surfactant and a monoglyceride as said co-surfactant.

10. The composition according to claim 1 which further comprises a thickening agent.

11. The composition according to claim 1 adapted for oral administration.

12. The composition according to claim 11 in unit dosage form.

13. The composition according to claim 12 in a gelatin capsule.

14. The composition according to claim 11 comprising from 5 to 20% by weight of said cyclosporin based upon the total weight of the composition.

15. The composition according to claim 1 containing 1,2-propylene glycol in an amount of from 3 to 45% by weight based upon the total weight of the composition.

16. The composition according to claim 11 wherein the ratio of said cyclosporin to 1,2-propylene glycol is from 1:0.5 to 1:3 parts per weight.

17. The composition according to claim 1 wherein said lipophilic phase component (2) is present in an amount of from 2 to 45% by weight based on the total weight of the composition.

18. The composition of claim 11 containing 1,2-propylene glycol and wherein the ratio of said lipophilic phase component (2) to 1,2-proppylene glycol is from 1:0.15 to 1:6 parts by weight.

19. The composition of claim 11 wherein said component 3) is present in an amount of from 20 to 90% by weight based on the total weight of said composition.

20. The composition of claim 11 wherein the ratio of said cyclosporin to said component 3) is from 1:1 to 1:10 parts by weight.

21. The composition according to claim 1 comprising from 0.05 to 15% by weight of said cyclosporin based on the total weight of said composition, wherein said composition is in a form suitable for topical application.

22. The composition according to claim 21 comprising from 0.1 to 10% by weight of said cyclosporin based on the total weight of said composition.

23. A pharmaceutical microemulsion composition comprising water and the composition of claim 1.

24. The composition of claim 1, wherein said cyclosporin is Ciclosporin.

25. The composition of claim 1 wherein said cyclosporin is [Nva].sup.2 -Ciclosporin.

26. An oral pharmaceutical composition comprising Ciclosporin or [Nva].sup.2 -Ciclosporin as an active ingredient;

1) a hydrophilic phase component which comprises a pharmaceutically acceptable C.sub.1-5 alkyl di-or partial-ether, or tetrahydrofurfuryl di-or partial-ether, of a mono- or poly-oxy-C.sub.2-12 -alkanediol, or 1,2-propylene glycol;

2) a lipophilic phase component which comprises a fatty acid triglyceride; and

3) a surfactant which comprises a polyoxyethylene glycolated natural or hydrogenated vegetable oil and monoglyceride;

wherein said composition is a microemulsion pre-concentrate capable, on contacting with water, of forming an oil-in-water microemulsion having an average particle size of less than 1,000 .ANG..
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