液相色谱-质谱联用法测定人血浆阿奇霉素浓度及生物等效性研究

目的建立阿奇霉素血药浓度的液相色谱-质谱联用（LC—MS）测定法，为临床用药提供参考依据。方法采用随机双交叉试验设计，20名健康受试者口服受试制剂和参比制剂0．5g，用LC—MS法测定人血浆中的阿奇霉素浓度。结果受试制剂和参比制剂的0～144h药时曲线下面积（AUC0-144）分别为（6617．87±2669．96）μg·h／L和（6456．05±2739．62）μg·h／L；0～∞药时曲线下面积（AUC0-n）分别为（7146．36±2848．25）μg·h／L（7089．33±3073．11）μg·h／L；峰浓度（Cmax）分别为（546．69±198．75）μg／L和（536．47±192．27）μg／L；峰时间（Tmax）分别为（2．1±0．9）h和（2．2±0．9）b；半衰期（t1/2）分别为（41．17±8．68）h和（44．22μ8．48）h。受试制剂的相对生物利用度为（102．7±9．7）％。结论两种国产阿奇霉素片剂具有生物等效性。

Study on Determination of Azithromycin in Human Plasma by LC-MS and Its Bioequivalence

Objective To study the pharmacokinetics and relative bioavailability of azithromycin tablets made in China in healthy volunteers and to establish a determination method of plasma azithromycin by LC- MS. Methods Twenty healthy volunteers received 0.5g azithromycin tablets orally in a random crossover design. The drug concentrations in plasma were determined by LC- MS. Results The main pharmacokinetic parameters of tested and reference tablets were as follows： AUC0-144： （6617. 87 ±2669.96） μg · h/Lvs （6456.05 ±2739.62）μg · h/L, AUC0-n （7 146. 36 ± 2 848.25）μg · h/L vs（7 089.33 ± 3 073. 11 ）μg · h/L, Cmax： （546. 69 ± 198.75）μg/L vs （536.47 ± 192.27）μg/L, tmax： （2. 1 ± 0. 9） h vs（2.2 ± 0. 9） h, t1/2：（41.17 ± 8.68） h vs（44.22 ± 8.48） h, respectively. The relative bioavailability of the test tablet was（102.7 ± 9.7）%. Conclusion The two domestic tablets are bioequivalent.