奥氮平双羟萘酸盐的制备及体外释放度的研究

The resarch of Preparation of olanzapine pamoate monohydrate and its release in vitro

目的采用无菌生产工艺制备由不同粒度组成的奥氮平双羟萘酸盐,并对其体外累计释放度进行评价。方法 研究了奥氮平双羟萘酸盐在不同溶剂及不同浓度条件下的溶解度,找到其漏槽条件,通过体外释放度试验,对比制备的不同粒径奥氮平双羟萘酸盐与原研制剂体外释放行为的差异。结果 为了保证奥氮平双羟萘酸盐在体内能够缓慢、持续、有效地释放,我们需要对奥氮平双羟萘酸盐的粒度及其分布进行控制,即d(0.1)约为0.7μm,d(0.5)约为1.7μm,d(0.9)约为3.7μm。结论 通过气流磨粉碎技术适合于控制奥氮平双羟萘酸盐的粒度及其分布,制备的样品较普通制剂体外释放具有明显的缓释特征,能够提高患者的顺应性,更方便用药。

OBJECTIVE To Prepare Olanzapine pamoate monohydrafe containing different particle sizes and in- vestigate the release behavior of olanzapine pamoate monohydrate in vitro. METHODS Olanzapine pamoate mono- hydrate was studied under the condition of different solvents and different concentrations of solubility, so as to find the sink condition. Based on in vitro release behavior of the differences, we investigated Olanzapine pamoate monohydrate with different particle sizes and RLD. RESULTS In order to ensure that olanzapine pamoate monohydrate in the body could be slow, continuous, effectively release, we need to control its particle size and its distribution. The idea results were as follows：d（0. 1 ） ：0. 7μm,d（0. 5） ：1.7μm,d（0. 9） ：3.7μm. CONCLUSION The technology by jet mill grinding is suitable for eontroling the particle size and distribution of olanzap pie exhibited delayed-release property in vitro and could improve the compliance venient to use. ine pamoate monohydrate, the sam- of patients, which were more con-venient to use.