Title: Studies of Relative Bioavailability of Clarithromycin Sustained-Release Capsules
Abstract: OBJECTIVE To establish a LC-MS/MS method for the determination of clarithromycin in human plasma and to study pharmacokinetics and relative bioavailability of clarithromycin sustained-release capsule and clarithromycin sustained-release tablet in market. METHODS The tested drug and internal standard roxithromycin were extracted from plasma samples by ether-dichloromethane(3∶2) and chromatgraphed on a C18 column. The mobile phase consisted of methanol-water-formic acid (80∶20∶0.05).Detection was performed on a triple quadrupole tandem mass spectrometer via electrospray ionization source(ESI) in the positive mode. RESULTS The linear calibration curves were obtained in the concentration range of 10.0~4 000 μg·L-1. The intra-and inter-run precisions were lower than 15% in terms of relative standard deviation. Pharmacokinetic parameters of the two products after the administration of 0.5 g clarithromycin to 18 volunteers were as follows:tmax (5.36±1.14) and (5.25±0.88) h,ρmax (1 218±433) and (1 333±370)μg·L-1,t1/2 (4.59±1.67) and (4.24±2.10)h,AUC0-t (8 239±1 553) and (8 467±1 364)μg·h·L-1,AUC0-∞ (8 662±1 829) and (8 795±1 331)μg·h·L-1,CL (60.9±15.1) and (58.9±11.3)L·h-1,Vd(382±103) and (366±224)L,for a single dose,respectively;tmax (5.31±1.11) and (5.28±0.96) h,ρssmax (1 387±396) and (1 488±401) μg·L-1,ρssmin (64.6±26.8) and (70.1±30.0) μg·L-1,ρav (399 ±99.2) and (410±107) μg·L-1,AUCss (9 585±2 382) and (9 830±2 578) μg·h·L-1,DF(3.32±0.62) and (3.49±0.66) for multiple doses,respectively. The relative bioavailability of the test drug for single dose and multiple doses were(98.2±16.3)% and (99.5±19.0)%. CONCLUSION This method is fast,sensitive and accurary.There is no difference between the test and the reference drugs of clarithromycin in the relative bioavailability (P0.05).
Publication Year: 2009
Publication Date: 2009-01-01
Language: en
Type: article
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