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口服不同剂型替米考星在鸡体内相对生物等效性研究
引用本文:刘桂兰,刘爱玲,鲍恩东.口服不同剂型替米考星在鸡体内相对生物等效性研究[J].畜牧与兽医,2009,41(4).
作者姓名:刘桂兰  刘爱玲  鲍恩东
作者单位:1. 瑞普(天津)生物药业有限公司,天津,300300
2. 瑞普(天津)生物药业有限公司,天津300300;南京农业大学动物医学院,江苏南京210095
摘    要:本试验按单剂量口服的方法对健康蛋鸡进行替米考星可溶性粉和替米考星溶液中主要组分替米考星的生物利用度和药代动力学研究。利用HPLC方法分析不同时间点试验鸡血浆中的药物浓度。药物的药动学参数结果显示,替米考星可溶性粉和替米考星溶液的平均血药浓度-时间曲线下面积(AUC0-48)分别为(16.947±0.624)μg/mL.h和(16.020±0.631)μg/mL.h,没有显著差异;二者AUC0-48比值为1.058,Cmax分别为(0.759±0.012)μg/mL和(0.764±0.012)μg/mL,比值为0.993;替米考星可溶性粉和替米考星溶液的t1/2β、C l(s)、t1/2 Ka和V/F(c)均没有显著差异;二者的tmax分别为(1.211±0.036)h和(1.030±0.063)h虽然有显著差异,但并不能以此说明二者生物学的非等效性。试验结果说明,单剂量口服替米考星可溶性粉和替米考星溶液后,替米考星被迅速吸收,消退缓慢,依据生物等效性的重要评判指标,得出替米考星可溶性粉和替米考星溶液在治疗中可以相互替代。

关 键 词:生物利用度    HPLC  替米考星  药动学

Relative bioequivalence of tilmicosin (powder or liquid) oral formulations in chickens
LIU Gui-lan,LIU Ai-ling,BAO En-dong.Relative bioequivalence of tilmicosin (powder or liquid) oral formulations in chickens[J].Animal Husbandry & Veterinary Medicine,2009,41(4).
Authors:LIU Gui-lan  LIU Ai-ling  BAO En-dong
Abstract:The bioavailability and pharmacokinetics of tilmicosin were investigated in the healthy chickens given a single oral dose of the soluble powder or the liquid of tilmicosin.A modified rapid and sensitive HPLC method was used for determination of tilmicosin concentrations in the tested chicken plasma.Various pharmacokinetic parameters including area under plasma concentration-time curve(AUC0-48),maximum plasma concentration(Cmax),time to peak concentration(tmax),elimination half-life(t1/2β),body clearance(Cl),absorption half-life(t1/2 Ka) and coefficient of volume of distribution/ absorption(V/F) were determined for both administrations,respectively.The average means of AUC0-48 for the soluble powder(16.947±0.624) g/mL·h and the liquid(16.020±0.631) g/mL·h were very close,without a significant difference based on ANOVA.The relative bioavailability of tilmicosin powder was 106% compared to the tilmicosin liquid.There were no significant differences in the Cmax,t1/2β,Cl(s),t1/2 Ka and V/F(c) between the soluble powder and the liquid of tilmicosin.In addition,there exists a significant difference in tmax between the soluble powder(1.211±0.036) h and the liquid(1.030± 0.063) h,but this difference couldn't deny the relative bioequivalence of the two preparations.Tilmicosin could be rapidly absorbed and slowly eliminated after a single dose of oral administration in whether aqueous or its soluble powder formulations.It suggested that the two formulations of Tilmicosin could be used interchangeably in drug therapy.
Keywords:HPLC
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