盐酸伐昔洛韦片在健康志愿者体内的生物等效性  

Study on bioequivalence of valacyclovir hydrochloride tablets in healthy volunteers

作　　者：秦晓怡[1] 胡卢丰[1] 代宗顺[2] 

机构地区：[1]温州医学院药学院药理教研室,温州325027 [2]华中科技大学同济医学院药理教研室,武汉430030

出　　处：《药物分析杂志》2007年第6期918-920,共3页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:研究盐酸伐昔洛韦片的人体相对生物利用度和生物等效性。方法:采用高效液相色谱法测定健康志愿者随机双交叉单剂量口服2种制剂的盐酸伐昔洛韦片后血浆中阿昔洛韦浓度。血浆经高氯酸沉淀蛋白,用 Zorbax SB-C_(18)(4.6 mm×150 mm,5 μm)为色谱柱,以乙腈-水-2%冰醋酸(4:86:10)为流动相,流速为1.0 mL·min^(-1),检测波长为274 nm。结果:单剂量口服盐酸伐昔洛韦试验制剂和参比制剂后血浆阿昔洛韦的 C_(max)分别为(3.04±0.51)μg·mL^(-1)和(3.15±0.62)μg·mL^(-1);T_(max)分别为(1.20±0.25)h 和(1.15±0.33)h;AUC_(0～14)分别为(10.71±1.94)μg·h·mL^(-1)和(10.36±2.37)μg·h·mL^(-1);AUC_(0～∞)分别为(11.12±1.94)μg·h·mL^(-1)和(10.76±2.42)μg·h·mL^(-1)。试验制剂与参比制剂的人体相对生物利用度为(105.48±15.42)%。结论:2种制剂具有生物等效性。Objective：To study the relative bioavailability and bioequivalence of valacyclovir hydrochloride tablets in healthy volunteers. Methods：A sensitive and rapid HPLC method was developed to determine the aciclovir plasma concentration. A single oral dose of two formulations of valacyclovir hydrochloride were given to healthy volunteers in randomized crossover design. The plasma were precipitated by perchloric acid. The analytical column was packed with Zorbax SB -C18 （4. 6 mm× 150 mm,5 μm）. The mobiie phase consisted of acetonitrile -water- 2% glacial acetic acid （4： 86： 10）with flow rate of 1.0 mL · min^-1. The UV detection wavelength was 274 nm. Results：After a single dose of valacyclovir hydrochloride of test and reference formulations, the pharmacokinetics parameters for aciclovir were as follows,respectively：Cmax were （3.04 ±0. 51 ） μg · mL^-1 and （3.15 ±0. 62） μg · mL^-1;Tmax were （1.20 ±0.25） h and （1.15±0.33） h;AUC0-14 were （10.71 ±1.94） μg · h · mL^-1 and （10.36±2.37） μg· h · mL^-1;AUC0-∞ were （11.12±1.94） μg· h. mL^-1 and （10.76±2.42） μg· h. mL^- 1 for test and reference formulations, respectively. The relative bioavailability of test formulation to reference formulation was （105. 48 ± 15. 42 ）%. Conclusion：The two formulations were bioequivalence.

关 键 词：伐昔洛韦 阿昔洛韦 相对生物利用度 生物等效性 高效液相色谱法 

分 类 号：R917[医药卫生—药物分析学]