[红霉素胶囊药代动力学研究]。

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王丽强,胡志智,于强,郭旭,熊杰,黄泽忠,程振忠

[红霉素胶囊药代动力学研究]。

中南大学学报,2005年4月30日(2):197-201。

PubMed ID
15898434 (PubMed视图
摘要

目的:测定噻硝普酸红霉素胶囊的药代动力学,为临床研究提供指导。必威国际app方法:30名健康志愿者(男15名,女15名)随机分为3组,每组男5名,女5名。每名志愿者分别口服250、500和750毫克。采用高效液相色谱-质谱法测定血浆中丙酸红霉素和红霉素碱的浓度。结果:30名志愿者均完成实验,无不良反应。利用3P87对模型进行分析,并计算药代动力学参数。高、中、低剂量组均为单室模型。低剂量组:Ka (2.007 +/- 1.281)/h, tmax(实际值)(1.9 +/- 0.6)h, Cmax (437.0 +/- 295.0) μ g/L, AUC0-14(梯形面积)(1840.2 +/- 1476.87)μ g × h/L, Ke (0.329 +/- 0.119)/h, T1/2 (2.45 +/- 0.9) h。中剂量组:Ka(1.451 + / - 0.380) /小时,最高温度(1.7 + / - 0.3)h, Cmax (923.1 + / - 217.5) microg / L, AUC0-14 (4542.44 + / - 1579.4) microg x h / L,柯(0.237 + / - 0.057)/ h, T1/2 (3.1 + / - 1.1) h;高剂量组:Ka (2.076 +/- 1.559)/h, tmax (1.7 +/- 0.3) h, Cmax(1336.5 +/- 366.0)微克/L, AUC0-14(7481.5 +/- 2496.2)微克/h, Ke (0.266 +/- 0.051)/h, T1/2 (2.7 +/- 0.5) h。红霉素药动学参数如下:低剂量组:Ka (1.410 +/- 0.626)/h, tmax (1.8 +/- 0.5) h, Cmax (197.5 +/- 227.6) microLg/L, AUC0-14(766.4 +/- 981.0)微克/h, Ke (0.519 +/- 0.240)/ h, T1/2 (1.6 +/- 0.8) h。中剂量组: Ka (1.900 +/- 1.049)/h, tmax (1.6 +/- 0.2) h,Cmax (488.3 +/- 216.7) microg/L, AUC0-14( 488.3 +/- 216.7) microg/L, Ke (0.329 +/- 0.057)/h, T1/2(2.2 +/- 0.4) h; High dose group: Ka (1.934 +/- 0.794)/h, tmax (1.7 +/- 0.3) h, Cmax (749.3 +/- 387.2) microg/L, AUC0-14(3820.1 +/- 1966.4) microg x h/L, Ke (0.373 +/- 0.174)/h, T1/2( 2.2 +/- 0.7) h. AUC of both erythromycin propionate and erythromycin base was linearly correlated to the doses; T1/2 was not correlated to the doses, so they followed the first order processes. The pharmacokinetic parameters of erythromycin The erythromycin stinoprate propionate and erythromycin base had no gender differences. Conclusion was absorbed as erythromycin propionate. Cmax reached at about 1.6 h. T1/2 of elimination was 2.4-3.1 h. The active component of erythromycin propionate was erythromycin. Cmax of erythromycin is 1.8, T1/2 is 2.4-3.1 h. In the range of oral dose of 250 to 750 mg, both erythromycin propionate and erythromycin base accorded the first order processes. The pharmacokinetic parameters were different with those reported in foreign documents while the gender difference did not exist in Chinese adults.

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