摘要
目的评价精氨酸布洛芬颗粒受试制剂和参比制剂在中国健康受试者中空腹和餐后状态下的生物等效性和安全性,为该药的一致性评价和临床应用提供依据。方法采用单中心、单剂量、随机、开放、空腹和餐后、两周期、两交叉试验设计,空腹与餐后试验各纳入中国成年健康受试者24例,随机交叉单次口服精氨酸布洛芬颗粒受试制剂和参比制剂各0.4 g,按时间点采血后,用高效液相色谱-质谱联用法进行血药浓度检测,用Phoenix WinNonlin 8.3进行数据分析。结果空腹组受试者服用精氨酸布洛芬颗粒受试制剂和参比制剂后,血浆中布洛芬主要药代动力学参数如下:C_(max)分别为(51.07±7.43)和(50.10±7.64)μg·mL^(-1),AUC_(0-t)分别为(122.78±20.62)和(119.94±21.03)μg·h·mL^(-1),AUC_(0-∞)分别为(125.84±21.31)和(122.64±21.87)μg·h·mL^(-1);餐后组受试者服用精氨酸布洛芬颗粒受试制剂和参比制剂后,血浆中布洛芬主要药代动力学参数如下:C_(max)分别为(17.47±3.56)和(17.89±4.47)μg·mL^(-1),AUC_(0-t)分别为(114.33±17.12)和(122.13±29.46)μg·h·mL^(-1),AUC_(0-∞)分别为(134.04±36.72)和(133.96±30.35)μg·h·mL^(-1)。两制剂几何均值比的90%置信区间如下:空腹组C_(max) 97.96%~106.02%、AUC_(0-t) 98.77%~105.14%、AUC_(0-∞)99.34%~105.19%;餐后组C_(max) 92.37%~103.05%、AUC_(0-t) 93.31%~99.56%、AUC_(0-∞)93.89%~102.91%。结论本研究中精氨酸布洛芬颗粒的受试制剂和参比制剂在中国健康成年受试者中具有生物等效性。
Objective To evaluate the bioequivalence and safety of ibuprofen arginine granules test and reference formulations in Chinese healthy volunteers under fasting and postprandial conditions,and to provide evidence for consistency evaluation and clinical application of the drugs.Methods A single-center,single-dose,randomized,open-label,fasting and postprandial,two-period,two-crossover trial design was used.Twenty-four healthy Chinese volunteers were enrolled in the fasting and postprandial trial,respectively.The test preparation and reference preparation of ibuprofen arginine granules 0.4 g were taken orally in a randomized crossover single dose.Data analysis was performed using Phoenix WinNonlin 8.3.Results In the fasting group,the main pharmacokinetic parameters of ibuprofen in plasma after administration of the test and reference formulations of ibuprofen arginine granules were as foll ow s:C_(max) were(51.07±7.43)and(50.10±7.64)μg·mL^(-1);AUC0-t were(122.78±20.62)and(119.94±21.03)μg·h·mL^(-1);AUC_(0-∞)were(125.84±21.31)and(122.64±21.87)μg·h·mL^(-1),respectively.In the postprandial group,the main pharmacokinetic parameters of ibuprofen in plasma after administration of the test and reference formulations of ibuprofen arginine granules were as follows:C_(max) were(17.47±3.56)and(17.89±4.47)μg·mL^(-1);AUC0-twere(114.33±17.12)and(122.13±29.46)μg·h·mL^(-1);AUC_(0-∞)were(134.04±36.72)and(133.96±30.35)μg·h·mL^(-1),respectively.The 90%confidence intervals of the geometric mean ratio of the two preparations were as follows:C_(max) 97.96%-106.02%,AUC0-t 98.77%-105.14%,AUC_(0-∞)99.34%-105.19%in fasting group;in postprandial group,C_(max) was 92.37%-103.05%,AUC0-t was 93.31%-99.56%,AUC_(0-∞)was 93.89%-102.91%.Conclusion The test preparation and reference preparation of ibuprofen arginine granules in this study are bioequivalent in healthy adult Chinese volunteers.
作者
石盼盼
沈芬
宋丽梅
赵丰丽
李望
张伟臣
田禹
SHI Pan-pan;SHEN Fen;SONG Li-mei;ZHAO Feng-li;LI Wang;ZHANG Wei-chen;TIAN Yu(Drug Clinical Trial Center,Yuncheng Central Hospital,Shanxi Province,Yuncheng 044000,Shanxi Province,China;Hainan Huluwa Pharmaceutical Group Co.Ltd,Haikou 570000,Hainan Province,China)
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2024年第1期107-111,共5页
The Chinese Journal of Clinical Pharmacology
关键词
精氨酸布洛芬
健康受试者
药代动力学
高效液相色谱-质谱联用法
生物等效性
ibuprofen arginine granules
healthy volunteers
pharmacokinetic
high performance liquid chromatography-mass spectrometry(HPLC-MS/MS)
bioequivalence
