红霉素stinoprate胶囊的药物动力学。

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引用

王LQ,胡锦涛ZY,于问,郭X,熊J,郑黄ZZ,锌

红霉素stinoprate胶囊的药物动力学。

钟南达雪雪宝易雪禁令。2005年4月;(2):197 - 201。

PubMed ID
15898434 (在PubMed
]
文摘

目的:确定红霉素stinoprate胶囊的药物代谢动力学情况,为临床研究提供指导。方法:30健康志愿者(15男性和15位女性)随机分为3组,每一个包括5男5女。单一口服剂量的250、500和750毫克是每个志愿者。丙酸的浓度红霉素和红霉素基地在等离子体由HPLC-MS决定。结果:所有30个志愿者完成实验,没有不良反应。用3 p87我们分析模型和计算药代动力学参数。三个剂量组进行高、中、低剂量都是单室模型。红霉素丙酸的药代动力学参数在红霉素stinoprate胶囊如下:低剂量组:Ka(2.007 + / - 1.281) /小时,最高温度(实际值)(1.9 + / - 0.6)h, Cmax (437.0 + / - 295.0) microg / L, AUC0-14(梯形区)(1840.2 + / - 1476.87)microg x h / L,柯(0.329 + / - 0.119)/ h, T1/2 (2.45 + / - 0.9) h。中间剂量组: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) /小时,最高温度(1.7 + / - 0.3)h, Cmax (1336.5 + / - 366.0) microg / L, AUC0-14 (7481.5 + / - 2496.2) microg x h / L,柯(0.266 + / - 0.051)/ h, T1/2 (2.7 + / - 0.5) h。红霉素的药代动力学参数如下:低剂量组:Ka(1.410 + / - 0.626) /小时,最高温度(1.8 + / - 0.5)h, Cmax (197.5 + / - 227.6) microLg / L, AUC0-14 (766.4 + / - 981.0) microg x h / L,柯(0.519 + / - 0.240)/ h, T1/2 (1.6 + / - 0.8) h。中间剂量组:Ka(1.900 + / - 1.049) /小时,最高温度(1.6 + / - 0.2)h, Cmax (488.3 + / - 216.7) microg / L, AUC0-14 (488.3 + / - 216.7) microg / L,柯(0.329 + / - 0.057)/ h, T1/2 (2.2 + / - 0.4) h;高剂量组:Ka(1.934 + / - 0.794) /小时,最高温度(1.7 + / - 0.3)h, Cmax (749.3 + / - 387.2) microg / L, AUC0-14 (3820.1 + / - 1966.4) microg x h / L,柯(0.373 + / - 0.174)/ h, T1/2 (2.2 + / - 0.7) h。AUC丙酸红霉素和红霉素碱与剂量线性相关; 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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