基于纳米混悬技术盐酸齐拉西酮胶囊的制备及质量评价  

Preparation and quality evaluation of ziprasidone hydrochloride capsules based upon nanosuspension technique

作　　者：曾艳玲 盘赛昆 ZENG Yan-ling;PAN Sai-kun(College of Food Science and Engineering Jiangsu Ocean University,Jiangsu Lianyungang 222006,China;Research Institute Chia Tai Tianqing Pharmaceutical Group Co Ltd,Jiangsu Lianyungang 222062,China)

机构地区：[1]江苏海洋大学食品科学与工程学院,江苏连云港222006 [2]正大天晴药业集团股份有限公司研究院,江苏连云港222062

出　　处：《中国医院药学杂志》2021年第14期1423-1429,共7页Chinese Journal of Hospital Pharmacy

摘　　要：目的:制备盐酸齐拉西酮纳米混悬剂,提高其体外溶出度,并对其进行质量评价。方法:采用超声辅助沉淀法制备纳米混悬剂,以粒径、多分散性指数为评价指标。通过单因素考察初步优化纳米混悬剂的处方和制备工艺,采用拟中心复合设计,对处方用量进行优化设计。采用扫描电镜、差式扫描量热法和粉末X射线衍射法对固化后的粉末进行表征,高效液相法测定盐酸齐拉西酮体外溶出度。结果:基于纳米混悬技术制备的盐酸齐拉西酮胶囊的体外溶出度与市售胶囊相比得到显著的提高。结论:以Soluplus和SDS为稳定剂成功制备盐酸齐拉西酮纳米混悬剂,提高其体外溶出度,具有较好的应用前景。OBJECTIVE To prepare ziprasidone hydrochloride nanosuspension to improve its dissolution in vitro and to evaluate its quality.METHODS Ultrasound-assisted precipitation method was employed for preparing nanosuspensions.And particle size and polydispersity index were adopted as evaluation parameters.The formulation and preparation process of nanosuspension were initially optimized through single factor investigation and quasi-central composite design was adopted for optimizing the formulation dosage.Solidified powder was characterized by scanning electron microscopy(SEM),differential scanning calorimetry(DSC)and X-ray powder diffraction(XRPD)and in vitro dissolution of ziprasidone hydrochloride was determined by high performance liquid chromatography(HPLC).RESULTS The in vitro dissolution rate of ziprasidone hydrochloride capsules prepared through nanosuspension technology significantly improved compared with commercially available counterparts.CONCLUSION Ziprasidone hydrochloride nanosuspension has been successfully prepared with Soluplus and SDS as stabilizers.With improved in vitro dissolution,it has a bright application prospect.

关 键 词：盐酸齐拉西酮 纳米混悬剂 体外溶出度 

分 类 号：R943[医药卫生—药剂学]