| 摘要 |
PURPOSE:To provide a cyclosporin preparation composed of an alpha-cyclodextrin and/or its derivative and cyclosporin, having excellent solubility and suppressed side effect and usable as an oral drug for internal use, injection and ophthalmic instillation. CONSTITUTION:The objective preparation can be produced by mixing cyclosporin with one or more compounds selected from alpha-cyclodextrin and/or its derivative at a ratio (cyclosporin: alpha-cyclodextrin) of 1:(0.5-1,000), preferably 1:(1-200) and converting the mixture into a drug preparation by conventional means. In the case of a solution, the concentration of alpha-cyclodextrin is 10-130mg/ml and that of cyclosporin is 0.1-2.0mg/ml. Although the solubility- increasing effect to cyclosporin is about two fold in the case of beta- or gamma- cyclodextrin, it reaches an order of 100 times in the case of alpha-cyclodextrin having minimum cavity size.
|
