摘要
以拜耳公司的尼群地平片为参比制剂,评价云南白药集团股份有限公司尼群地平片与参比制剂的生物等效性。采用双周期自身交叉对照设计,将16名受试者随机分为空腹组和餐后组,分别于餐后及空腹服用尼群地平片,采集血浆样品,用LC-MS/MS测定人血浆中尼群地平的浓度,以DAS3.3.0软件计算药动学参数,评价尼群地平片的生物等效性。结果表明,空腹状态下受试制剂与参比制剂的主要药动学参数:Cmax分别为(10.78±5.32) ng·m L^(-1)、(9.69±8.35) ng·mL^(-1),AUC0-t分别为(53.66±25.82) ng·h·mL^(-1)、(40.87±32.12) ng·h·mL^(-1);餐后状态下受试制剂与参比制剂的主要药动学参数:Cmax分别为(17.21±9.02) ng·mL^(-1)、(16.37±10.04) ng·mL^(-1),AUC0-t分别为(50.04±24.57) ng·h·mL^(-1)、(54.60±28.86) ng·h·mL^(-1),空腹状态或餐后状态服药Cmax、AUC的90%置信区间均超出80%～125%。尼群地平两制剂不具有生物等效性,云南白药集团股份有限公司需优化尼群地平片处方和改善尼群地平片生产工艺,提高尼群地平片质量。
ObjectiveTo evaluate the bioequivalence of YunNan BaiYao Group Co. LTD’s nitrendipine tablets and Bayer’s nitrendipine tablets. MethodsIn a randomized two-way crossover study, 16 healthy volunteers were randomly divided into fasting group or postprandial group, and were givennitrendipine tablets under fasting or fed conditions. Blood samples were collected. The plasma concentration of nitrendipine was determined by LC-MS/MS. Pharmacokinetic parameters were calculated and bioequivalence of two preparations were evaluated by DAS3.0 software. ResultsThe pharmacokinetic parameters before diet as follows: Cmax were(10.78±5.32) ng·m L^-1 and(9.69±8.35) ng·m L^-1, AUC0-twere( 53.66 ±25.82) ng·h·m L^-1 and( 40.87 ±32.12) ng·h·m L^-1, The pharmacokinetic parametersafter diet as follows: Cmax were(17.21±9.02) ng·m L^-1 and(16.37±10.04) ng·m L^-1, AUC0-twere(50.04±24.57) ng·h·m L^-1 and(54.60±28.86) ng·h·m L^-1. The 90% confidence intervalsof AUC0-t,AUC0-∞ and Cmaxunder fasting and fed conditions were more than 80%~ 125%. ConclusionThe two formulations ofnitrendipine tablet were not bioequivalent. YunNan BaiYao Group Co. LTD needs be improve the quality of nitrendipine tabletsthrough optimizing the prescription and process improvement.
作者
鲁婷婷
崔佳丽
梅晶
赵高琼
李窦红
刘红斌
王京昆
Lu Tingting;Cui Jiali;Mei Jing;Zhao Gaoqiong;Li Douhong;Liu Hongbin;Wang Jingkun(Dali university YunnanDali 671000;Yunnan Institute of Materia Medica Yunnan Kunming 650111;YUNNAN BAI R&D CENTER Yunnan Kunming 650111;Yunnan Province Company Key Laboratory for TCM and Ethnic Drug of New Drug Creation Yunnan Kunming 650111)
出处
《云南化工》
CAS
2019年第2期18-22,共5页
Yunnan Chemical Technology
