棕榈酸帕利哌酮注射液的制备及释放度方法学研究  

Preparation and release of paliperidone palmitate injection:a study

作　　者：付伟[1] 孙建绪[1] 张慧[1] 李迎[1] 郭飞[1] 郑爱萍[1] 

机构地区：[1]军事医学科学院毒物药物研究所药物制剂室,北京100850

出　　处：《国际药学研究杂志》2016年第4期748-752,共5页Journal of International Pharmaceutical Research

摘　　要：目的制备棕榈酸帕利哌酮注射液,建立该注射液释放度的检测方法,并进行方法学验证。方法湿磨法制备本品,采用高效液相色谱法建立释放度检测方法并进行方法学验证。结果自制制剂的平均粒径约为1μm,透射电镜下观察为不规则块状;所建立的释放度检测方法的精密度为1.5%,回收率为100.70%,稳定性RSD为0.33%。3批自制制剂的体外平均释放分别为:1.5 min 8.00%、20 min 62.26%、45 min 85.44%。结论所制备缓释注射液的粒度分布和释放度与原研制剂一致,释放度检查法简单、灵敏、准确,可有效监控本品的质量,3批制剂平均释放度均在质量标准范围之内。Objective To prepare paliperidone palmitate injection,establish the testing method for its release rate,and validate the methodology. Methods Wet grinding was used to prepare paliperidone palmitate injection,high performance liquid chromatography was adopted to establish release rate detection,and validate its methodology. Results The average particle diameter of home-made agent was about 1 μm,and it was an irregular bulk observed under transmission electron microscope;the precision of established release rate detection was 1.5%,recovery rate was 100.70% and stability RSD was 0.33%. The average release rate in vitro of home-made agent in three batches was：8.00% in 1.5min,62.26% in 20 min,and 85.44% in 45 min. Conclusion The particle size distribution and release rate of prepared sustained-release injection are consistent with those of original research,and the testing method of release rate is simple,sensitive and accurate,which could effectively monitor the product quality. The average release rates of agent in three batches are within the scope of quality standards.

关 键 词：棕榈酸帕利哌酮 缓释 注射液 释放度 

分 类 号：R943[医药卫生—药剂学]