阿维菌素微囊在家兔体内的药动学研究

为了考察阿维菌素微囊在家免体内的药动学行为，将10只家兔随机分为2组，皮下注射阿维菌素微囊注射液（1．0mg／kg）和普通阿维菌素注射液（0．2mg／kg），用高效液湘色谱法测定家兔血浆中阿维菌素的浓度，3P87药动学软件处理血浆药物浓度-时间数据。研究结果表明，阿维菌素微囊注射液和普通阿维菌素注射液药-时数据都符合一级吸收二室开放模型，阿维菌素微囊注射液的主要动力学参数分别是t1/2kα=21．72h；t1/2α=56．65h；t1／2β=239．43h；tmax=63．05h；Cmax=34．30ng／mL；AUC=11573．88ng／mL·h。普通阿维菌素注射液的主要动力学参数分别是t1/2kα=7．38h；t1/2α=14．59h；t1／2β=32．84h；tmax=19．78h；Cmax=20．88ng／mL；AUC=1482．04ng／mL·h。说明阿维菌素微囊化后。与普通阿维菌素注射泣相比，吸收慢，消除慢，作用时间长．生物利用度显著提高。

Study on the pharmacokinetics of avermectins microcapsule in rabbits

The experiment was conducted in 10 healthy rabbits to investigate the pharmacokineties of avermections microcansules.Avermectms microcapsules suspensions were given to the rabbits suboutaneously at the dose of 1.0mg/kg,avermectins injection （0.2mg/kg,s.c） was given in the experiment for compurison.Then plasma concentrations of overmectin were dectermined by HPLC with UV detection at 245nm,Pharmacokinetic parameters were calculated by 3P87 program using the obtained data.The results were as follows：Avermeetins microcapsule injection：t1/2kα=21.72h;t1/2α=56.65h;t1/2β=239.43h;tmax=63.05h;Cmax=34.30ng/mL;AUC=11573.88ng/mL·h.Avermectins injection：t1/2kα=7.38h;t1/2α=14.59h;t1/2β=32.84h;tmax=19.78h;Cmax=20.88ng/mL;AUC=1482.03ng/mL·h.It is concluded that avermectins give a slow absorption and elimination,long half-lif and high bioavailability after it was made into microcapsule.