摘要
目的 采用HPLC-MS法测定志愿者口服阿奇霉素胶囊（250mg）后的血药浓度，对受试制剂与参比制剂的生物等效性进行评价。方法 20名健康志愿者交叉口服受试制剂或参比制剂2．50mg。计算主要药动学参数及相对生物利用度，以判断生物等效性。结果 在5—1200ng·ml^-1范围内阿奇霉索峰面积与内标峰面积的比值与阿奇霉素的浓度之间呈良好线性关系，最低定量限为5ng·ml^-1。受试制剂和参比制剂的t1／2分别为（4s．89±8．69）h、（51．04±10．31）h，tmax分别为（2．0±0．7）h、（2．2±0．7）h，cmax分别为（532．55±182．6s）ng·ml^-1、（466．00±180．21）ng·ml^-1。以AUC0-τ计算的受试胶囊的相对生物利用度为（107．4±25．5）％。两制剂的药动学主要参数无显著性差异。结论 2种制剂具有生物等效性。
AIM Using a HPLE-MS assay for the determination of azithromycin in human plasma and investigating the pharmacokinetics and bioequivalence of azithromycin capsule in human body. MTHODS A randomized crossover design was performed in 20 healthy volunteers, with a single oral dose of 250 mg. The main parameters of pharmacokinetics and the relative bioavalability were calculated. RESULTS Calibration curves were linear over the range of 5 - 1200 ng· ml^- 1. The limit of quantification for azithromycin in plasma was 5 ng·ml^- 1 The main pharmacokinetic parameters t 1/2, tmax and cmax were （45.89 ± 8.69） h, （2.0 ± 0.7） h and （532.55 ± 182.65）ng·ml^-1 for the test capsules; （51.04 ± 10.31） h, （2.2 ± 0.7） h and （466.00 ± 180.21） ng· ml^-1 for the reference tablets, respectively. The relative bioavalability of the test capsules was （107.4 ± 25.5）% .The results of variance analysis and two one-sided t-test showed that there was no significant difference between the reference and test formulations in the AUC and cmax CONCLUSION The assay is proved to be sensitive, accurate and convenient. The reference and test formulations are bioequivalent.
出处
《江苏药学与临床研究》
2006年第6期354-357,共4页
Jiangsu Pharmacertical and Clinical Research
