Claims for Patent: 5,474,979

Summary for Patent: 5,474,979

Title:	Nonirritating emulsions for sensitive tissue
Abstract:	A pharmaceutical composition is disclosed in the form of a nonirritating emulsion which includes at least one cyclosporin in admixture with a higher fatty acid glyceride and polysorbate 80. More particularly, the cyclosporin may be cyclosporin A and the higher fatty acid glyceride may be castor oil. Composition has been found to be of a high comfort level and low irritation potential suitable for delivery of medications to sensitive areas such as ocular tissues. In addition, the composition has stability for up to nine months without crystallization of cyclosporin.
Inventor(s):	Ding; Shulin (Irvine, CA), Tien; Walter L. (Irvine, CA), Olejnik; Orest (Trabuco Canyon, CA)
Assignee:	Allergan, Inc. (Irvine, CA)
Application Number:	08/243,279
Patent Claims:	1. A pharmaceutical composition comprising a nonirritating emulsion of at least one cyclosporin in admixture with a higher fatty acid glyceride, polysorbate 80 and an emulsion stabilizing amount of Pemulen in water suitable for topical application to ocular tissue. 2. The pharmaceutical composition according to claim 1 wherein the cyclosporin comprises cyclosporin A. 3. The pharmaceutical composition according to claim 2 wherein the weight ratio of the higher fatty acid glyceride to the polysorbate 80 is between about 0.3 and about 30. 4. The pharmaceutical composition according to claim 3 wherein the higher fatty acid glyceride comprises castor oil and the weight ratio of cyclosporin to castor oil is below about 0.16. 5. The composition according to claim 1 wherein the higher fatty acid glyceride and polysorbate 80 are present in amounts sufficient to prevent crystallization of cyclosporin for a period of up to about nine months. 6. A pharmaceutical emulsion comprising of cyclosporin A, castor oil, Pemulen, glycerine, polysorbate 80 water in amounts sufficient to prevent crystallization of cyclosporin A for a period of up to about nine months, said pharmaceutical emulsion being suitable for topical application to ocular tissue. 7. The pharmaceutical emulsion according to claim 6 wherein the cyclosporin A is present in an amount of between about 0.05 to and about 0.40%, by weight, the castor oil is present in an amount of between about 0.625%, by weight, and about 5.0%, by weight, the polysorbate 80 is present in an amount of about 1.0%, by weight, the Pemulen is present in an amount of about 0.05%, by weight, and the glycerine is present in an amount of about 2.2%, by weight. 8. A pharmaceutical emulsion consisting of between about 0.05% and about 0.40%, by weight, cyclosporin A, between about 0.625% and about 5.0%, by weight, castor oil, about 1.0%, by weight, polysorbate 80, about 0.05%, by weight, Pemulen and about 2.2%, by weight, glycerine in water with a pH of between about 7.2 and 7.6 suitable for topical application to ocular tissue.