Solid pharmaceutical compositions comprising a cyclosporin and an anionic surfactant

• US 6,197,335 B1
• Filed: 05/17/1999
• Issued: 03/06/2001
• Est. Priority Date: 09/16/1997
• Status: Expired due to Fees

• Current Assignee: Bernard Charles Sherman
• Original Assignee: Bernard Charles Sherman
• Inventors: Sherman, Bernard Charles
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): TRAN, SUSAN T
• Application Number:
  US09/308,272
• Time in Patent Office: 659 Days
• Field of Search: 424/451, 424/456, 424/464, 424/465, 514/9
• US Class Current: 424/464
• CPC Class Codes: A61K 38/13 Cyclosporins
• 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: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1623 Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection

Abstract

A solid pharmaceutical composition for oral administration comprising a cyclosporin and an anionic surfactant, preferably sodium lauryl sulfate, wherein the amount of anionic surfactant is at least about forty percent of the minimum amount needed to dissolve the cyclosporin in water.

Claims

1. A solid pharmaceutical composition for oral administration comprising a cyclosporin and a surfactant, wherein said surfactant consists essentially of an anionic surfactant and wherein the amount of said anionic surfactant is at least about forty percent of the minimum amount that would be needed to dissolve the cyclosporin in water using a quantity of water small enough that the concentration of the anionic surfactant in the water would exceed the critical micelle concentration and wherein the amount of anionic surfactant by weight is from about 40% to about 400% of the amount of the cyclosporin.

2. A composition as in claim 1 wherein the amount of said anionic surfactant is not more than about four times the minimum amount that would be needed to dissolve the cyclosporin in water using a quantity of water small enough that the concentration of the anionic surfactant in water would exceed the critical micelle concentration.

3. A composition as in claim 1 wherein the anionic surfactant is selected from the group consisting sodium alkyl sulfates, sodium alkyl sulfonates and sodium alkyl aryl sulfonates.

4. A composition as in claim 1 wherein the anionic surfactant is sodium lauryl sulfate.

5. A composition as in claim 1 wherein the amount of sodium lauryl sulfate by weight is from about 80% to about 300% of the amount of the cyclosporin.

6. A composition as in claim 1, wherein the cyclosporin comprises more than ten percent of the composition by weight.

7. A composition as in claim 1, wherein the cyclosporin comprises more than twenty percent of the composition by weight.

8. A composition as in claim 1, wherein the cyclosporin is cyclosporine.

9. A composition as in claim 1 contained within a 2-piece hard gelatin capsule.

10. A composition as in claim 1 in the form of a tablet.

11. A process of making a composition as in claim 1 comprising the steps of dissolving the cyclosporin and anionic surfactant in a solvent or a combination of solvents and then evaporating the solvent or solvents.

12. A process as in claim 11 wherein water is used as solvent.

13. A process as in claim 11 wherein the evaporation is done by spray-drying.

14. A solid pharmaceutical composition comprising a cyclosporin and a surfactant wherein said surfactant consists essentially of sodium lauryl sulfate, wherein the amount of sodium lauryl sulfate by weight is from about 80% to about 400% of the cyclosporin.

15. A process of making a composition in claim 14 comprising the steps of dissolving the cyclosporin and anionic surfactant in a solvent or a combination of solvents and then evaporating the solvent or solvents.

16. The process as in claim 15 wherein water is used as solvent.

17. The process as in claim 15 or 16 wherein the evaporation is done by spray-drying.

18. The composition as in claim 14, wherein the cyclosporin comprises more than ten percent of the composition by weight.

19. The composition as in claim 14, wherein the cyclosporin comprises more than twenty percent of the composition by weight.

20. A composition as in claim 14, wherein the cyclosporin is cyclosporin.

21. A composition as in claim 14, contained within a 2-piece hard gelatin capsule.

22. A composition as in claim 14 in the form of a tablet.