盐酸坦洛新缓释胶囊在人体内的药动学和生物等效性

Relative bioavailability and phamacokinetics of tamsulosin hydrochloride controlled-release capsules in human volunteers

目的建立血浆中坦洛新的HPLC-MS测定方法,考察2种坦洛新缓释胶囊的生物等效性,同时估算其药动学参数。方法20名受试者采用单剂双交叉试验设计和多剂双交叉试验设计,分别口服2种缓释制剂,测定血浆中坦洛新浓度。结果单剂量给药受试缓释胶囊与市售缓释胶囊的tmax、cmax分别为(5.3±1.2)h和(5.79±1.57)μg·L^(-1)及(5.5±1.1)h和(5.99±1.61)μg·L^(-1)。和市售缓释胶囊相比,受试缓释胶囊相对生物利用度(101.4±14.3)%。多剂量服药5d后达到稳态浓度,至稳态后受试缓释胶囊与市售缓释胶囊的tmax、cmax分别为(5.3±1.3)h和(7.47±2.27)μg·L^(-1)及(5.4±1.5)h和(6.70±2.23)μg·L^(-1)。受试胶囊的相对生物利用度为(101.1±12.9)%。结论2种缓释制剂生物等效。

AIM To establish a HPLC-MS determination method of plasma concentration of tamsulosin and to investigate the bioavailatility and pharmacokinetic characteristics of tamsulosin hydrochloride controlled-release capsules in human volunteers. METHODS A single oral dose and multiple doses were given to 20 volunteers in a randomized crossover study. Tamsulosin concentration in human plasma was determined by a sensitive HPLC-MS method. After a single oral dose admininstration, cmax was （5.79 ± 1.57）μg·L^-1 at （5.3 ± 1.2）h for the test and （5.99 ± 1.61）μg·L^-1 at （5.5 ±1.1）h for the reference.The relative bioavailability of the test was （101.4 ± 14.3）% .Steady state was achieved after approximately 5 d.After steady state, cmax was （7.47 ± 2.27）μg·L^-1 at （5.3 ± 1.3）h for the test and （6.70 ± 2.23）μg·L^-1 at （5.4 ± 1.5）h for the reference. The relative bioavailability of the test was （101.1 ± 12.9）%. CONCLUSION The bioavailability of the test is equal to that of the reference.