Title: Study of pharmacokinetics and relative bioavailability of azithromycin dry suspension by HPLC-MS
Abstract: Objective:To establish an accurate and sensitive HPLC-MS method for the determination of azithromy- cin in plasma and to evaluate its pharmacokinetic parameters and bioavailability in healthy male volunteers after a single oral dose of 500 mg azithromycin or its dry suspensions.Methods:A single oral dose of 500 mg azithromycin or its dry suspensions was given to 18 healthy male volunteers in a two-way cross-over design,the plasma sam- ples were collected at predetermined time points after the administration,after adding the internal reference(clar- ithromycin,12.5 μg·mL~(-1)),0.2 mL of each plasma sample was alkalized with saturated solution of carbonate az- ithromycin were determined by HPLC-MS method using HyPutiy C_(18)column(2.1 mm×150 mm,5 μm)at 40℃, a mixture of NH_4Ac(10 mmol·L~(-1),pH 5.2)-acetonitrile-methanol(50:40:10)as mobile phase at a flow rate of 0.2 mL·min~(-1),with positive iron ESI detection of azithromycin([MH]~(2+),m/z=375)using clarithromycin ([MH]~+,m/z=749)as internal reference.Results:The limit of detection was 3.91 μg·L~(-1).A good linearity was obtained in the range of 3.91-1000 μg·L(-1)(r=0.9993).The extraction recoveries were in the range of (72.6±4.6)%-(81.3±5.7)% ,The intra-day and inter-day RSD were both lower than 12%.The main pharmacokinetics parameters after a single oral dose of 500 mg azithromycin or dry suspensions were as follow:C_(max) (ng·mL~(-1)):(557.68±110.91)and(567.90±93.58);T_(max)(h):(2.00±0.69)and(2.00±0.77);T_(1/2) (h):(30.95±9.37)and(28.94±8.71);AUC_(0→120)(ng·mL~(-1)):(5544.31±1852.17)and(5637.46± 1652.44).The relative bioavailability(F)was(98.07±15.51 )%.Conclusins:The established HPLC-MS method is sensitive,rapid and accurate.The pharmacokinetic parameters determined is reliable.The statistic results show that azithromycin and its dry suspensions of the test and reference is bioequivalent.
Publication Year: 2006
Publication Date: 2006-01-01
Language: en
Type: article
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Cited By Count: 1
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