Suppr超能文献

口服及静脉注射头孢他美在犬体内的药代动力学和药效学

Pharmacokinetics and pharmacodynamics of oral and intravenous cefetamet in dog.

作者信息

Wang Wei, Zhu Xiao-Mao, Wang Chun-Mei, Gou Si, Chen Zhong-Hua, Zhao Yuan

机构信息

Department of Pharmacology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, People's Republic of China.

Si Chuan Chuan Tou Medicine Biological Technology Co., LTD, Chengdu, 610023, People's Republic of China.

出版信息

Eur J Drug Metab Pharmacokinet. 2015 Dec;40(4):401-7. doi: 10.1007/s13318-014-0217-6. Epub 2014 Jul 13.

Abstract

The pharmacokinetic (PK) and pharmacodynamic (PD) properties of intravenously (IV) administered cefetamet-Na and per os (PO) administered cefetamet pivoxil were investigated in eighteen healthy dogs at three different dose levels. The three doses for IV cefetamet-Na were 95, 190 and 380 mg, while those for oral cefetamet pivoxil were 125, 250 and 500 mg (both equivalent to 90, 180 and 360 mg of cefetamet). An efficacy predictor, measured as the ratios of the time that the concentration of the free drug is over the MIC90 (T > MIC90) and the dosing interval (f% T > MIC90) of IV and PO administration were calculated. The PK parameters' maximum concentration (C max), half-life (t 1/2) and area under the curve (AUC0-t ) after three IV doses were 42.85 ± 11.79 μg/mL, 1.66 ± 0.36 h and 80.10 ± 28.92 mg h/L (95 mg); 93.50 ± 30.51 μg/mL, 1.47 ± 0.13 h and 1.47 ± 0.13 mg h/L (190 mg); 185.74 ± 113.83 μg/mL, 1.60 ± 0.38 h and 263.20 ± 73.27 mg h/L (380 mg). After PO administration, the C max, t 1/2 and AUC0-t at three doses were 9.25 ± 1.02 μg/mL, 1.79 ± 0.50 h and 31.90 ± 4.76 mg h/L (125 mg); 9.75 ± 1.77 μg/mL, 1.93 ± 0.65 h and 42.69 ± 8.93 mg h/L (250 mg); 15.55 ± 6.65 μg/mL, 2.02 ± 0.54 h, and 68.72 ± 24.11 mg h/L (500 mg). The IV f% T > MIC90 was greater than PO f% T > MIC90 when MIC90 was within the range of 0.25-256 mg/L.

摘要

在18只健康犬中,于三个不同剂量水平研究了静脉注射头孢他美钠和口服头孢他美酯的药代动力学(PK)和药效学(PD)特性。静脉注射头孢他美钠的三个剂量分别为95、190和380毫克,而口服头孢他美酯的剂量分别为125、250和500毫克(两者均相当于90、180和360毫克头孢他美)。计算了一个疗效预测指标,即游离药物浓度超过MIC90的时间(T > MIC90)与静脉注射和口服给药的给药间隔(f% T > MIC90)的比值。静脉注射三次后,PK参数的最大浓度(C max)、半衰期(t 1/2)和曲线下面积(AUC0-t)分别为42.85±11.79μg/mL、1.66±0.36小时和80.10±28.92毫克·小时/升(95毫克);93.50±30.51μg/mL、1.47±0.13小时和1.47±0.13毫克·小时/升(190毫克);185.74±113.83μg/mL、1.60±0.38小时和263.20±73.27毫克·小时/升(380毫克)。口服给药后,三个剂量的C max、t 1/2和AUC0-t分别为9.25±1.02μg/mL、1.79±0.50小时和31.90±4.76毫克·小时/升(125毫克);9.75±1.77μg/mL、1.93±0.65小时和42.69±8.93毫克·小时/升(250毫克);15.55±6.65μg/mL、2.02±0.54小时和68.72±24.11毫克·小时/升(500毫克)。当MIC90在0.25 - 256毫克/升范围内时,静脉注射的f% T > MIC90大于口服的f% T > MIC90。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验