国产布地奈德鼻喷雾剂在中国健康受试者体内的生物等效性研究  

Study on bioequivalence of domestic budesonide nasal spray in Chinese healthy subjects

作　　者：雷程灏 朱叶 程凤 徐洁 张燕 肖大伟 熊文海 郝光涛 LEI Cheng-hao;ZHU Ye;CHENG Feng;XU Jie;ZHANG Yan;XIAO Da-wei;XIONG Wen-hai;HAOGuang-tao(Department of PhaseⅠClinical Trial Research,Nanjing Gaoxin Hospital,Nanjing JIANGSU 210031,China;Nanchang Baiji Pharmaceutical Co.,Ltd.,Nanchang JIANGXI 330115,China;Beijing Sunshine Demei Pharmaceutical Technology Co.,Ltd.,BEIJING 100071,China)

机构地区：[1]南京高新医院Ⅰ期临床试验研究部,江苏南京210031 [2]南昌百济制药有限公司,江西南昌330115 [3]北京阳光德美医药科技有限公司,北京100071

出　　处：《中国新药与临床杂志》2025年第3期200-205,共6页Chinese Journal of New Drugs and Clinical Remedies

基　　金：赣江新区重大科技攻关项目(2020003)。

摘　　要：目的评价布地奈德鼻喷雾剂在中国健康受试者体内的生物等效性。方法采用随机、开放、单剂量、两序列交叉设计。36例健康受试者空腹状态下鼻腔吸入布地奈德鼻喷雾剂受试制剂或参比制剂。采用LC-MS/MS法定量检测人血浆中布地奈德的浓度,非房室分析法计算布地奈德药动学参数,采用SAS 9.4软件进行生物等效性统计分析。结果布地奈德鼻喷雾剂受试制剂和参比制剂的cmax几何均值分别为445.76 pg·mL^(-1)和439.74 pg·mL^(-1),90%CI为92.32%~111.31%;AUC_(0-t)的几何均值分别为1221.43 pg·h·mL^(-1)及1218.77 pg·h·mL^(-1),90%CI为95.07%~105.64%;AUC_(0-∞)的几何均值分别为1305.81 pg·h·mL^(-1)及1312.87 pg·h·mL^(-1),90%CI为94.09%~105.14%。结论布地奈德鼻喷雾剂受试制剂和参比制剂在空腹吸入试验中具有生物等效性,且安全性良好。AIM To evaluate the bioequivalence of budesonide nasal spray in Chinese healthy subjects.METHODS A randomized,open,single-dose,two-sequence crossover design was applied.A total of 36 healthy subjects inhaled test formulation or reference formulation of budesonide nasal spray under fasting administration.The plasma concentration of budesonide was analysed by LC-MS/MS assay.The pharmacokinetic parameters of budesonide were calculated by non-chamber analysis method and the bioequivalence evaluation was analysed by SAS 9.4 software.RESUITS The geometric mean values of cmax for the test formulation and reference formulation of budesonide nasal spray were 445.76 pg·mL^(-1)and 439.74 pg·mL^(-1),respectively,with a 90%confidence interval(90%CI)of 92.32%to 111.31%.The geometric mean values of AUC_(0-t)were 1221.43 pg·h·mL^(-1)and 1218.77 pg·h·mL^(-1),respectively,with a 90%CI of 95.07%to 105.64%.The geometric mean values of AUC_(0-∞)were 1305.81 pg·h·mL^(-1)and 1312.87 pg·h·mL^(-1),respectively,with a 90%CI of 94.09%to 105.14%.CONCLUSION The test formulation and reference formulation of budesonide nasal spray demonstrated bioequivalence under fasting inhalation conditions,with favorable safety profiles.

关 键 词：布地奈德 鼻喷雾剂 生物等效性 安全性 

分 类 号：R969.1[医药卫生—药理学]