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目的探讨载平阳霉素离子交换型微球(PYM-MS)在兔体内的药代动力学特征。方法健康成年日本大耳白兔12只,雌雄各半,随机分为2组,每组6只。兔颈外动脉为实验模型,分别注射平阳霉素溶液(PYM)和PYM-MS。于2,5,10,20,40,60,90,120 min依次取血,处理血样,用高效液相色谱法(HPLC)测定平阳霉素浓度,绘制血药浓度-时间曲线,计算药代动力学参数。结果 PYM-MS组与PYM组相比,血药浓度-时间曲线下降缓慢;PYM-MS组Cmax(11.62±2.66)mg·L-1较PYM组的(58.96±4.51)mg·L-1小(P<0.01);PYM-MS组与PYM组的AUC分别为(221.06±31.33),(791.98±55.30)mg·L-1·min(P<0.01);PYM-MS组体内平均滞留时间(MRT0-60 min)延长,2组分别为(22.29±1.52),(14.20±1.24)min(P<0.01)。结论 PYM-MS有缓释作用,外周血药浓度低。
Objective To investigate the pharmacokinetics of PYM-MS in rabbits. Methods Twelve male Japanese white rabbits were randomly divided into 2 groups (6 in each group). Rabbit external carotid artery as experimental model, were injected Pingyangmycin solution (PYM) and PYM-MS. Blood samples were taken at 2, 5, 10, 20, 40, 60, 90 and 120 min, blood samples were processed, the pingyangmycin concentration was determined by high performance liquid chromatography (HPLC), and the plasma concentration- time curve was plotted to calculate the pharmacokinetics parameter. Results Compared with PYM group, the plasma concentration-time curve of PYM-MS group decreased slowly. Cmax (11.62 ± 2.66) mg · L-1 in PYM-MS group was smaller than that in PYM group (58.96 ± 4.51) mg · L-1 (P <0.01). The AUC of PYM-MS group and PYM group were (221.06 ± 31.33) and (791.98 ± 55.30) mg · L-1min MRT0-60 min), the two groups were (22.29 ± 1.52) and (14.20 ± 1.24) min respectively (P <0.01). Conclusion PYM-MS has slow release and low concentration of peripheral blood.