摘要
目的研究健康人po盐酸伐昔洛韦片后的药动学和生物等效性。方法20个健康受试者采用随机分组自身交叉对照试验设计，口服盐酸伐昔洛韦片600mgHPLC—MS联用法测定血浆中代谢产物阿昔洛韦浓度，以BAPP程序计算其药动学参数和评价生物等效性.结果在选定的色谱／质谱奈件下阿昔洛韦与内标及血浆杂质分离良好，在41．6～5．34×10μg·L^-1内线性良好.阿昔洛韦的相对回收率大于96．7％，日内和日间RSD小于10．2％。盐酸伐昔洛韦片受试制剂（T）和参比制别（R）的主要药动学参数：tmax分别为（1．5±0．6）（T）和（1．5±0．6）h（R），Pmax、分别为（2．83×10^7±7．76×10^2）（T）和（2．72×10^3±8．50×10^2）μg·L^-1（R）；t1/2分别为（3．21±0．29）（T）和（3．23±0．30）h（R）；AUC0-14分别为（1．02×10^4±2．03×10^3）（T）和（9．91×10^3±2．46×10^3）μg·h·L^-1（R）；盐酸伐昔洛韦片相对生物利用度为（104．5±14．0）％.结论用LC—MS测定血浆中代谢产物阿昔洛韦浓度，杂质无干扰，定量限低，重复性好，准确度高.受试的盐酸伐昔洛韦片与参比的盐酸伐昔洛韦片生物等效.
OBJECTIVE To study the pharmacokinetics and bioequivalence of valaciclovir in human. METHODS Twenty volunteers orally took the valaeiclovir tablets with 2-way crossover design. The concentration of aeyclovir, the melabolite of valaciclovir in plasma, was determined by HPLC-MS. The phannacokinetic parameters were calculated by BAPP software. RESULTS The calibration curve was linear in the range from 41.6 to 5.34 × 10^3 μg · L^-1. The relative recovery was more than 96. 7%. The intra- and inter- RSDs were less than 10. 2%. The main pharmacokinetie parameters of t1/2, pmax and AUC0 -14 for the test tahlet were （3.21 ± 0. 29） h, （2.83×10^3 ± 7. 76 ×10^2 ） μg· L^-1, （1.5±0.6） h and （1.02×104 ± 2. 03 ×10^3 ） μg· h·L^-1, respectively. The pharmacokinetic paramelers of t1/2, pmax and AUC0-14 for the reference tablet were （3.23 ±0. 30） h, （2. 72 × 10^3 ±8. 50 × 102 ）μg· h·L^-1, （ 1.5 ＋ 0. 6） h and （9. 91 × 10^3 ± 2.46 × 103 ） μg· h·L^-1, respectively. The relative bioavailability of the test tablet was （ 104. 5 ± 14.0）%. CONCLUSION The HPLC-MS method for the determination of acyelovir in plasma was proved to be sensitive, accurate and convenient. The reference and test tablets were bioequivalent.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2008年第21期1647-1650,共4页
Chinese Pharmaceutical Journal
