Application of Spherical Crystallization Technique on Particle Design in Pharmaceutics

摘要

@@Spherical crystallization technique is a novel agglomeration method occurring in liquid system, which was developed by Kawashima in 1980’s1). In this system, the agglomeration can be carried out simultaneously during crystallization process with a bridging liquid, and spheronized by stirring. Initially, the technique was focused on direct tabletting, the resultant agglomerates dramatically improved flowability, packability and compressibility2,3). Afterwards, functional drug devices such as microsphere, microcapsule, microballoon, and biodegradable nanosphere4) have been further prepared by using polymeric spherical crystallization technique. In the previous study, sustained release microspheres were produced mainly for water soluble drugs5) or partially water soluble drugs by adding retarding agents6）. Recently, our study focused on those practically water insoluble drugs, such as nimodipine, nitrendipine7）, ketoprofen8）, ibuprofen and oily drug9）etc. It is well known that the solid dispersion technique is widely used for water insoluble drugs to improve the dissolution rate and to improve the bioavailability. Generally, after preparation of solid dispersion, grinding, sieving, mixing and granulating processes were continued to produce various preparations as required.