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Details for Patent: 5,639,724

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Details for Patent: 5,639,724

Title: Cyclosporin galenic forms
Abstract:Pharmaceutical compositions comprising a cyclosporin as active ingredient, a fatty acid triglyceride, a glycerol fatty acid partial ester or propylene glycol or sorbitol complete or partial ester, preferably, and a tenside having an HLB of at least 10.
Inventor(s): Cavanak; Thomas (Biel-Benken, CH)
Assignee: Sandoz Ltd. (Basel, CH)
Filing Date:Dec 06, 1993
Application Number:08/163,193
Claims:1. A pharmaceutical composition for oral administration comprising cyclosporin A as active ingredient in a carrier medium comprising a transesterification product of a natural vegetable oil with glycerol, wherein said transesterification product comprises a mixture of monoglycerides, diglycerides and triglycerides.

2. The composition of claim 1, wherein said vegetable oil is selected from the group consisting of corn oil, almond oil, ground-nut oil, olive oil and palm oil.

3. The composition of claim 2, wherein said vegetable oil is corn oil.

4. The composition of claim 1, wherein the amount of monoglyceride is 35 to 50% by weight, based on the total weight of said transesterification product.

5. The composition of claim 2, wherein the amount of diglyceride is less than 40% by weight, based on the total weight of said transesterification product.

6. The composition of claim 1, wherein the amount of triglyceride is less than 10% by weight, based on the total weight of said transesterification product.

7. The composition of claim 1, wherein said carrier medium comprises free glycerol.

8. The composition of claim 7, wherein the amount of free glycerol is less than 10%, based on the total weight of said transesterification product.

9. The composition of claim 1, wherein said carrier medium further comprises ethanol.

10. The composition of claim 1, wherein said carrier medium further comprises a transesterification product of a natural vegetable oil triglyceride and a polyalkylene polyol.

11. The composition of claim 1, wherein said carrier medium further comprises a reaction product of a natural or hydrogenated castor oil and ethylene oxide.

12. The composition of claim 1, wherein said cyclosporin A and transesterification product are present in a weight ratio of from about 1:4 to about 1:50.

13. A pharmaceutical composition for oral administration comprising cyclosporin A as active ingredient in a carrier medium comprising a transesterification product of a natural vegetable oil with sorbitol.

14. The composition of claim 13, wherein said vegetable oil is selected from the group consisting of corn oil, almond oil, ground-nut oil, olive oil and palm oil.

15. The composition of claim 14, wherein said vegetable oil is corn oil.

16. The composition of claim 13, wherein said transesterification product comprises a mixture of sorbitol mono-, di-, tri- and tetra-esters.

17. The composition of claim 13, wherein the carrier medium comprises free sorbitol.

18. The composition of claim 17, wherein the amount of free sorbitol is less than 10% by weight, based on the total weight of said transesterification product.

19. The composition of claim 13, wherein said carrier medium further comprises ethanol.

20. The composition of claim 13, wherein said carrier medium further comprises a transesterification product of a natural vegetable oil triglyceride and a polyalkylene polyol.

21. The composition of claim 13, wherein said carrier medium further comprises a reaction product of a natural or hydrogenated castor oil and ethylene oxide.

22. The composition of claim 13, wherein said cyclosporin A and transesterification product are present in a weight ratio of from about 1:4 to about 1:50.
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