严一铭

摘 要 目的：比较自制和原研地氯雷他定片剂的溶出行为。方法：根据普通口服固体制剂溶出曲线测定与比较指导原则，采用浆法，高效液相色谱法检测自制和原研片剂分别在pH 1.0、pH 4.5、pH 6.8的缓冲液和水中的溶出度，f2相似因子法比较溶出曲线的相似程度，初步评价其体外释放行为的一致性。结果：主成分的溶液稳定性良好，自制片剂和原研片剂在不同介质中的溶出曲线均相似，四组f2因子都大于50，符合评价要求。结论：自制片剂和原研片剂的体外释放度一致。

关键词 地氯雷他定片 溶出曲线 相似因子 一致性评价

中图分类号：R927.11 文献标志码：A 文章编号：1006-1533（2018）17-0068-04

Comparative study and evaluation on the dissolution profiles of home-made desloratadine tablets and its reference listed drug

YAN Yiming*

（Shanghai SPH New Asia Pharmaceutical Co.， Ltd.， Shanghai 201203， China）

ABSTRACT Objective： To compare and evaluate the dissolution behaviors between home-made desloratadine tablet and its reference listed drug. Methods： The dissolution of desloratadine tablets was analyzed by an HPLC method according to guiding principles of determination and comparison on dissolution profile of general oral solid preparation. The dissolution of both drugs was determined in buffer solutions at pH 1.0， pH 4.5， pH 6.8 and water， respectively. The degree of similarity of the dissolution curve was compared by similarity factor f2 and then the consistency of the in vitro release behavior was initially evaluated. Results： The solutions containing main components were stable， and the dissolution profiles of both drugs were similar in various types of media （f2 factors>50）. The f2 factors were all met the quoted requirements. Conclusion： The in vitro release behavior of both drugs is consistent.

KEy WORDS desloratadine tablets； dissolution profiles； consistency； f2 factor

地氯雷他定是一種强效、非镇静性的长效组胺拮抗剂，具有选择性地拮抗外周H1受体的作用及抗过敏、抗组胺及抗炎作用，可用于缓解与慢性特发性荨麻疹及过敏性鼻炎相关的症状[1]。

随着国家有关部门对仿制药质量与疗效一致性评价工作的深入，药品的体外溶出度对比试验受到越来越广泛的重视。药物在体外的释放行为，可以用来判断其生产工艺的优劣，进而在一定程度上提示该药在体内的消化、吸收和利用的情形，是临床前鉴别药品质量高低、更是与原研药品进行质量比较的重要手段[2]。

本研究通过对自制地氯雷他定片和市售的原研片剂溶出度的测定，比较在不同溶出介质下溶出曲线的相似性，分析自制片剂的体外释放行为，从而进一步提升制剂品质，促进仿制药一致性评价工作在本企业的开展[2]。……