| OBJECTIVETo establish a LC-MS method for determination of blood concentration of azithromycin oral preparations. Comparison of human bioequi valence of azithromycin for different manufacturers. For preparation, pharmacokinetics, clinical application and offer important reference.METHODSSelected eight kinds of (2kinds of Capsules,2kinds of Tablets,3kinds of Granules, lkind of dry suspension agent) different Azithromycin oral preparation from institute of pharmacology of Shandong University Qilu Hospital. Each preparation was the same dosage form and the reference preparations were bioequivalence test. Application of "DAS2.0" and SPSS software to eight group (sixteen preparations) for data analysis of the pharmacokinetic parameters. Compare the differences of azithromycin pharmacokinetics parameters from different manufacturers and different preparations.1. Contrast of the experimenter chose Each test20volunteers in the eight group (sixteen preparations), healthy male, between22-24years of age, body weight between65-70kg. All volunteers to test before blood, routine urine and liver, kidney function tests. All volunteers, physical examination, laboratory examination of liver kidney function is normal, no acute, chronic disease and family history, in the first2weeks of useless medicine history, not to participate in other clinical trials of new drugs in March.2. Contrast of experiment design This test will choose single agent two cross experimental design. Each of the20volunteers were randomly divided into two groups from eight group.Two groups of volunteers personal data and laboratory data were analyzed statistically no significant difference, comparable. Volunteer number was1-20. Volunteers fasting the day before after10p.m. Test day morning extraction blank blood sample immediately after an empty stomach oral test agents or the agents500mg.1～10volunteers took the test preparation,11～20volunteers took the reference preparation.200mL water delivery service, drinking water after2h administration,4h in unified standard meal. In the medicine before and after administration of the0.5,1,1.5,2,2.5,3,4,8,12,24,48,72,96,120h vein blood samples of5mL, static1H,3000rpm centrifuge for10min, separation of serum, divided into two-20℃refrigerator, rainy. Periodic cleaning for a period of two weeks. Second cycle dose, blood duration, sample method with the first cycle3. Determination of blood concentration of azithromycin Blood concentration in eight groups of azithromycin oral preparation using the LC-MS method for detection4. Contrast of data processing According to the measured azithromycin blood concentration-time data, using the "DAS practical pharmacokinetics program" the main pharmacokinetics parameters t1/2, AUC0-120? AUCo-∞, Cmax and Tmax, according to the AUCo-120calculation of relative bioavailability of test preparation from. The pharmacokinetic parameters of data t1/2, AUC, Cmax and Tmax were analyzed by the software of SPSS, have a look whether there are differences between the same dosage forms and various preparationRESULTSCollect the pharmacokinetic parameters of azithromycin oral preparations in sixteen different forms are obtained, and they are t1/2, Cmax, Tmax, AUCo-120and AUC0-∞. No significant differences in t1/2,but they are significant difference in Cmax> Tmax, AUC0-120and AUC0-∞o. Cmax, AUCo-120and AUCo-∞are significant difference from Azithromycin tablets. Tmax is significant difference from Azithromycin particles.CONCLUSION AND SIGNIFICANCEPharmacokinetics of azithromycin oral preparation is significant difference from different factories and different dosage forms. Azithromycin tablets in Cmax, AUCo-120and AUC0-∞have significant difference on other preparations, there was significant difference between the Tmax and other preparations of azithromycin granules, which shows different forms in the preparation process, choose different accessories, can make the same variety drug pharmacokinetic differences. This paper relates to the different time, different season test, during sample analysis is also used in the HPLC column is different, but the effects of these factors on the test results, no testing. As can be seen, difference analysis and experimental conditions and not to bring significant error test.The conclusion of this paper for azithromycin preparation, pharmacokinetics, clinical applications and provides an important reference... |
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