泊沙康唑肠溶片的质量评价与生物等效性研究  

Quality evaluation and bioequivalence study ofposaconazole enteric-coated tablets

作　　者：王华伟[1] 隋鑫[1] 吴秀君[1] 曹莹 陈璐 李晓斌[1] 李美烨 葛雨鑫 王文萍[1] WANG Hua-wei;SUI Xin;WU Xiu-jun;CAO Ying;CHEN Lu;LI Xiao-bin;LI Mei-ye;GE Yu-xin;WANG Wen-ping(The Affiliated Hospital of Liaoning University of Traditional Chinese Medicine,Shenyang 100032,China)

机构地区：[1]辽宁中医药大学附属医院Ⅰ期临床试验病房,沈阳100032

出　　处：《中国新药杂志》2025年第8期843-849,共7页Chinese Journal of New Drugs

基　　金：国家中医药管理局师承项目([2022]76);辽宁省自然科学基金项目(20180550690);辽宁省“兴辽英才计划”项目(XLYC1802008);辽宁省中药临床药物代谢动力学重点实验室资助项目。

摘　　要：目的:对国产与原研泊沙康唑肠溶片进行质量对比和生物等效性研究,探究二者是否存在质量和生物利用度差异。方法:对2厂家生产泊沙康唑肠溶片的质量标准进行对比,性状、UV图谱、HPLC图谱、有关物质、水分、溶出度、含量均匀度、含量、微生物限度进行比较。以国产泊沙康唑肠溶片(100 mg·片-1)为受试制剂,原研泊沙康唑肠溶片(100 mg·片-1)作为参比制剂,分别在空腹和餐后条件下,开展人体生物等效性试验。结果:国产泊沙康唑肠溶片的有关物质杂质控制严格,其他指标如性状、水分、含量均匀度、含量、微生物限度等均符合质量标准,与原研制剂无显著差异。生物等效性试验中,国产泊沙康唑肠溶片在禁食与餐后情况下与原研制剂主要参数C max,AUC几何均值比值90%CI在80%~125%的可接受范围内,经统计学分析可判断为生物等效。结论:国产与原研泊沙康唑肠溶片的质量均在限度之内,人体生物等效性试验显示国产与原研泊沙康唑肠溶片具有生物等效性。Objective:To compare the quality of domestic and original posaconazole enteric-coated tablets and investigate whether there are quality and bioavailability differences between the two preparations.Methods:The quality standards of posaconazole enteric-coated tablets produced by the two manufacturers were compared,and the appearance,UV spectrum,HPLC chromatogram,related substances,water content,dissolution rate,content uniformity,content and microbial limit were compared.The test preparation was domestic posaconazole enteric-coated tablets(100 mg),and the reference preparation was the original posaconazole enteric-coated tablets(100 mg).Human bioequivalence tests were carried out under fasting and fed conditions,respectively.Results:The impurity control of related substances in domestic posaconazole enteric-coated tablets was stricter than that of the reference preparation.Other indicators such as appearance,moisture content,content uniformity,content and microbial limit met the quality standards,and there was no significant difference between domestic and original products.In the bioequivalence study,the 90%confidence intervals of the geometric mean ratios of C max and AUC of domestic posaconazole enteric-coated tablets to the original preparation were within the acceptable range of 80%~125%under fasting and fed conditions,which could be judged as bioequivalent by statistical analysis.Conclusion:The qualities of domestic and original posaconazole enteric-coated tablets are both within the limit,but domestic posaconazole enteric-coated tablets are superior to the original tablets in terms of related substances.Bioequivalence studies in human have shown that domestic and originator posaconazole enteric-coated tablets are bioequivalent.

关 键 词：泊沙康唑肠溶片 质量对比 生物等效性 

分 类 号：R917[医药卫生—药物分析学] R969.1[医药卫生—药学]