Cyclosporin-containing pharmaceutical composition

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules

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514937, 514962, 514975, 424452, A61K 910, A61K 948, A61K 4724, A61K 4734

Patent

active

059809396

ABSTRACT:
The present invention relates to a pharmaceutical composition containing cyclosporin. More specifically, the present invention relates to a pharmaceutical composition containing cyclosporin, an oil component, a hydrophilic cosurfactant consisting of propylene carbonate or a mixture of propylene carbonate and polyoxyethylene-polyoxypropylene block copolymer, and a surfactant. The composition of the present invention is characterized in that it can be dissolved in an external phase such as water, artificial gastric juice and intestinal juice, etc. to form a self-emulsion with mild stirring and therefore, by appropriately adjusting the constitutional ratio of each component the diameter of particles in the inner phase of the emulsion thus formed can be readily controlled to 100 nm or below. The composition of the present invention can be formulated into the oral preparations such as soft capsules, hard capsules sealed with gelatin bending at the conjugated portion, oral liquid preparations, etc. When the composition of the present invention using propylene carbonate or its mixture with polyoxyethylene-polyoxypropylene block copolymer in a liquid state at room temperature is formulated into the soft capsule, it provides some advantages that it can inhibit the change in the capsule appearance and the precipitation of active ingredient due to the change in the solvent content, reduces the manufacturing cost to provide an economical effect and is substantially less toxic, in comparison to the soft capsule using ethanol, transcutol, propylene glycol, glycofurol, dimethylisosorbide, etc., in the prior art.

REFERENCES:
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CA 123: 266,72 Abstract of Japan Patent Document JP 07188046 AZ, Jul. 25, 1995.
Hee-Jong Shin et al, "Preparation and Bioequivalence Test of New Oral Solid Dosage Form of Cyclosporin A", Proceed. Intern. Symp. Control. Rel. Bioact. Mater., 23 (1996), Controlled Release Society, Inc., pp. 519-520.
Chong-Kook Kim et al, "Preparation and Characterization of Cytarabine-Loaded w/o/w Multiple Emulsions", International Journal of Pharmaceutics, 124 (1995), pp. 61-67.
Zhong-Gao Gao et al, "Physicochemical Characterization and Evaluation of a Microemulsion System for Oral Delivery of Cyclosporin A", International Journal of Pharmaceuticals, 161 (1998), pp. 75-86.
Abstract No. 3217: Zhong-Gao Gao et al, "Pysiocochemical Characterization and Evaluation of Microemulsion System for Oral Delivery of Cyclosporin A", Pharmaceutical Research, AAPS, Nov. 1997 (Supplement), vol. 14, No. 11.
Abstract No. 3255; Hee-Jong Shin et al, "Preparation and Evaluation of Cyclosporin A Oral controlled Release Dosage Form Using Solid-State Microemulsion", AAPS Annual Meeting and Exposition, Bridging Gaps Within Drug Discovery and Development, Nov. 15-19, 1998, San Francisco, California.

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