| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a method for producing an active drug comprising a biodegradable microsphere that can place an intraocular implant releasable of a therapeutic agent at a sustained or controlled rate for long period of time and in an amount with few or no negative side effects. <P>SOLUTION: The method for producing the active drug comprising the biodegradable microsphere includes steps of: preparing a viscous organic phase including a TKI (tyrosine kinase inhibitor) having 4 or more of partition coefficients logP in a two-phase system composed of n-octanol and water, a biodegradable polymer, and a solvent; preparing a first aqueous phase so as to have a pH of pH 6-8; forming an emulsion by mixing the viscous organic phase and the first aqueous phase; preparing a second aqueous phase so as to have a pH of pH 4-9, forming a solution by adding the second aqueous phase to the emulsion; stirring the solution; and producing the biodegradable microsphere wherein the TKI is encapsulated by evaporating the solution. The produced biodegradable microsphere releases the TKI at a rate effective to sustain the release of the TKI from the microsphere for the period exceeding one month from when placed in the vitreous of an eye. <P>COPYRIGHT: (C)2012,JPO&INPIT |
