目的 评价盐酸克林霉素胶囊在中国健康受试者中的药代动力学特征,并评价两种制剂的生物等效性.方法 空腹、餐后各入组24例健康受试者,采用随机、开放、两序列、两周期双交叉给药的试验设计,受试者单次口服盐酸克林霉素胶囊受试药物和参比药物150 mg,采用液相色谱-串联质谱法(LC-MS/MS)检测人血浆中克林霉素的浓度,使用WinNonlin7.0软件计算药代动力学参数,评价两种制剂的生物等效性.结果 单剂量空腹给药受试药物和参比药物克林霉素的主要药代动力学参数如下:Cmax分别为(2.91±0.86),(2.83±0.83)μg·mL-1,AUC0-t分别为(7.86±3.06),(7.39±2.39)μg·h·mL-1,AUC0-∞分别为(8.06±3.23),(7.59±2.50)μg·h·mL-1.单剂量餐后给药受试药物和参比药物克林霉素后的主要药代动力学参数如下:受试制剂和参比制剂的Cmax分别为(1.98±0.52),(2.05±0.41)μg·mL-1,AUC0-t分别为(9.68±3.35),(9.16±2.66)μg·h·mL-1,AUC0-∞分别为(9.53±2.98),(9.60±3.24)μg·h·mL-1.两药物的主要药代动力学参数Cmax、AUC0-t、AUC0-∞经对数转换后进行方差分析,其90％置信区间空腹状态下分别为94.75％～111.37％,198.81％～111.74％,98.34％～111.66％;餐后状态下分别为84.81％ ～104.19％、94.33％ ～112.92％,93.99％ ～113.64％.结论 空腹和餐后状态下,两种盐酸克林霉素胶囊的主要药代动力学参数相近,具有生物等效性.

AIM:To prepare O/W microemulsion formulation containing sinomenine and investigate the effect of different penetration enhancers on transermal delivery character of microemulsion in vitro. METHODS: The microemulsions were prepared and characterized using Zetasize potential/particle size analysis instrument.The stability tests were performed to evaluate the sinomenine microemulsions.Franz diffusion cell was adopted as the apparatus for in vitro transdermal test.Excised Wistar-rat abdomen skin was pretreated with penetration enhancers,such as menthol,borneol and isopropyl myristate. RESULTS: The average droplet size of the microemulsion was about(31.3 nm.)A high permeation rate of(32.238±1.13)μg/cm~(2)·h was showed in vitro.Ail the enhancers showed significant enhancement effect on the transdermal behavior of sinomenine microemulsion.2% borneol had the strongest effect in all. CONCLUSION: These results indicate that the studied microemulsion system with high permeation rate may be a promising vehicle for the transdermal delivery of sinomenine.Menthol,borneol and isopropyl myristate were found to be the proper penetration enhancers in the transdermal preparation.