盐酸莫西沙星片在中国健康受试者体内的药代动力学及生物等效性  

Pharmacokinetics and bioequivalence of moxifloxacin hydrochloride tablets in Chinese healthy volunteers

作　　者：周理想[1,2] 孙华[2] 李相鸿[2] 梁大虎[2] 王伟佳[2] 谢海棠[2] 陈飞虎[1] ZHOU Li- xiang1,2, SUN Hua2, LI Xiang - hong2, LIANG Da - hu2 , WANG Wei - jia2, XIE Hai - tang2, CHEN Fei - hu1(1. College of Pharmacy, Anhui Medical University, Hefei 230032, China ; 2. Institute of Clinical Pharmacology, Yijishan Hospital of Wannan Medical College, Wuhu 241001, Anhui Province , Chin)

机构地区：[1]安徽医科大学药学院,合肥230032 [2]皖南医学院弋矶山医院药学部,安徽芜湖241001

出　　处：《中国临床药理学杂志》2018年第14期1608-1611,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家自然科学基金资助项目(81173134)

摘　　要：目的建立人血浆中莫西沙星药物浓度的液质联用(HPLC-MS/MS)检测方法,分别研究空腹和餐后条件下莫西沙星在人体的药代动力学,并评价其生物等效性。方法空腹和餐后各24例健康受试者,用单剂量、随机、开放、双交叉试验设计,受试者单次口服盐酸莫西沙星片受试药物0.4 g和参比药物0.4g,清洗期为1周,用HPLC-MS/MS法测定健康受试者血浆中莫西沙星浓度,用WinNonlin 6.1计算莫西沙星药代动力学参数,评价受试药物和参比药物的生物等效性。结果空腹单次给药后莫西沙星主要药代动力学参数如下:受试药物、参比药物的C_(max)分别为(3.72±0.83),(3.51±0.69)μg·mL^(-1);t_(max)分别为(1.63±1.52),(1.81±1.18)h;t_(1/2)分别为(11.81±1.66),(11.54±1.26)h;AUC_(0-48h)分别为(52.49±10.87),(51.93±10.31)μg·h^(-1)·mL^(-1);AUC0-∞分别为(56.05±11.57),(55.17±11.04)μg·h^(-1)·mL^(-1);餐后单次给药后莫西沙星主要药代动力学参数如下:受试药物、参比药物的C_(max)分别为(3.05±0.46),(3.03±0.61)μg·mL^(-1);t_(max)分别为(2.52±1.40),(2.62±1.23)h;t_(1/2)分别为(12.21±1.87),(12.13±2.04)h;AUC_(0-48 h)分别为(44.52±7.13),(45.93±9.09)μg·h^(-1)·mL^(-1);AUC_(0-∞)分别为(47.73±8.09),(49.31±10.07)μg·h^(-1)·mL^(-1)。结论空腹和餐后给药条件下,国产盐酸莫西沙星片受试药物和进口盐酸莫西沙星片参比药物主要药代动力学参数指标相近,具有生物等效性。Objective A high performance liquid chromatography mass spectrometry（ HPLC-MS/MS） method was established for the determination of moxifloxacin in human plasma. The pharmacokinetics and the bioequivalence of moxifloxacin were studied under fasting and fed conditions. Methods Twenty four healthy volunteers were recruited respectively in fasting and fed conditions,using single dose,open,randomized,two crossover design,a single oral dose of moxifloxacin were test preparation（ T） 0. 4 g and reference preparation（ R） 0. 4 g,the cleaning period was one week,the concentration of moxifloxacin in the plasma of healthy subjects was determined by HPLC-MS/MS,using Win Nonlin 6. 1 to calculate the pharmacokinetic parameters and evaluate the bioequivalence of the tested preparation and the reference preparation. Results The main pharmacokinetic parameters of a single oralmoxifloxacin tablet under fasting condition for T and R were as follows： Cmax（ 3. 72 ± 0. 83）,（ 3. 51 ± 0. 69） μg·mL^-1;tmax（ 1. 63 ± 1. 52）,（ 1. 81 ± 1. 18） h; t1/2（ 11. 81 ± 1. 66）,（ 11. 54 ± 1. 26） h; AUC（0-48 h）（ 52. 49 ± 10. 87）,（ 51. 93 ± 10. 31）μg·h^-1·mL^-1; AUC0-∞（ 56. 05 ± 11. 57）,（ 55. 17 ± 11. 04） μg·h^-1·mL^-1. The main pharmacokinetic parameters of a single oral moxifloxacin tablet under fed conditions for T and R were as follows： Cmax（ 3. 05 ± 0. 46）,（ 3. 03 ±0. 61） μg·mL^-1; tmax（ 2. 52 ± 1. 40）,（ 2. 62 ±1. 23） h; t1/2（ 12. 21 ± 1. 87）,（ 12. 13 ± 2. 04） h; AUC（0-48 h）（ 44. 52 ±7. 13）,（ 45. 93 ± 9. 09） μg ·h^-1·mL^-1; AUC0-∞（ 47. 73 ± 8. 09）,（ 49. 31 ± 10. 07） μg · h^-1· mL^-1.Conclusion The bioequivalence of the domestic moxifloxacin hydrochloride tablets test preparation and the imported moxifloxacin hydrochloride tablets reference preparation is similar to the bioequivalence of the major pharmacokinetic parameters.

关 键 词：莫西沙星 液质联用法 药代动力学 生物等效性 

分 类 号：R978.1[医药卫生—药品]