METHOD OF PRODUCING DRUG-CONTAINING WAX MATRIX PARTICLES, EXTRUDER TO BE USED IN THE METHOD AND SUSTAINED-RELEASE PREPARATION CONTAINING CILOSTAZOL
申请人:OTSUKA PHARMACEUTICAL CO., LTD.
公开号:EP1970040A1
公开(公告)日:2008-09-17
The present invention aims to provide a method for producing, by a simple method, drug-containing wax matrix granules, particularly drug-containing wax matrix granules having an average particle diameter of 1 mm or lower, while avoiding liquid blockage due to the recrystallization of a molten drug during the period from a melting step to a spray step.
Drug-containing wax matrix granules having at least one wax and at least one drug are produced by the following steps (i) and (ii): (i) supplying the at least one drug and the at least one wax to an extruder in which the temperature of a barrel and the temperature of a die are adjusted to be higher than the melting point of the at least one wax; and (ii) while melting and kneading the at least one drug and the at least one wax in the extruder to give a molten kneaded drug and wax, spraying the molten kneaded drug and wax into an atmosphere having a temperature lower than the melting point of the wax from a spray nozzle directly mounted onto a die provided at a top end of the barrel of the extruder, thereby forming the mixture into granules.
本发明旨在提供一种用简单方法生产含药蜡基质颗粒的方法,特别是平均颗粒直径为1毫米或更小的含药蜡基质颗粒,同时避免在从熔化步骤到喷雾步骤期间由于熔融药物的再结晶而造成的液体堵塞。
通过以下步骤(i)和(ii)生产具有至少一种蜡和至少一种药物的含药蜡基质颗粒:(i) 将至少一种药物和至少一种蜡提供给挤压机,在挤压机中,机筒的温度和模具的温度被调节到高于至少一种蜡的熔点;(ii) 在挤压机中熔化和揉捏至少一种药物和至少一种蜡以得到熔融的揉捏药物和蜡时,从直接安装在挤压机机筒上端模头的喷嘴向温度低于蜡熔点的大气中喷射熔融的揉捏药物和蜡,从而将混合物制成颗粒。