采用微透析法研究雷公藤甲素在正常和糖尿病大鼠皮肤中的药动学差异
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篇名: 采用微透析法研究雷公藤甲素在正常和糖尿病大鼠皮肤中的药动学差异
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摘要: 目的:研究雷公藤甲素在正常和糖尿病大鼠皮肤中的药动学差异,为其临床合理应用提供参考。方法:将12只Wistar大鼠随机分为正常组和糖尿病模型组(ip 0.1%链脲佐菌素造模),每组6只。两组大鼠分别于腹部皮肤给予雷公藤甲素乳膏0.5 g后,采用微透析法每30 min收集1管透析液,连续12 h。采用高效液相色谱-质谱联用(HPLC-MS/MS)技术检测皮下药物浓度,分析比较两组大鼠皮下药物浓度-时间曲线图,并采用Winnonlin 5.0.1软件计算药动学参数。结果:正常组和糖尿病模型组大鼠皮下药物cmax分别为(1.54±0.37)、(5.12±1.34) μg/ml,tmax分别为(7.32±0.24)、(6.21±0.35) h,AUC0-12 h分别为(12.65±4.64)、(37.43±5.23) μg·h/ml,差异均有统计学意义(P<0.05)。结论:糖尿病引起大鼠皮肤结构的改变会造成雷公藤甲素经皮透过量增加,用药时应酌情减小剂量,以减少毒副作用。
ABSTRACT: OBJECTIVE: To study the dermal pharmacokinetic difference of triptolide in normal and diabetic rats, and to provide reference for rational drug use in the clinic. METHODS: 12 Wistar rats were randomly divided into normal group and diabetic model group (0.1% streptozotocin intraperitoneally), with 6 rats in each group. Both group were given Triptolide cream 0.5 g to abdominal skin, and dialysate was collected by microdialysis every 30 min for consecutive 12 h. Subcutaneous concentration was detected by HPLC-MS, and subcutaneous concentration-time curves were analyzed and compared between two groups, and Winnonlin 5.0.1 software was used to calculate pharmacokinetic parameters. RESULTS: The pharmacokinetic parameters of normal group and diabetic model group were that cmax  were (1.54±0.37) and (5.12±1.34) μg/ml; tmax were (7.32±0.24) and (6.21±0.35) h; AUC0-12 h were (12.65±4.64) and (37.43±5.23) μg·h/ml, with statistical significance (P<0.05). CONCLUSIONS: The change of dermal structure caused by diabetes can increase percutaneous penetration amount of triptolide in rats, and drug dosage should be reduced according to circumstances so as to reduce side effects.
期刊: 2016年第27卷第19期
作者: 张紫萍,曾维东,郭秀彩,赵博欣,邓英光
AUTHORS: ZHANG Ziping,ZENG Weidong,GUO Xiucai,ZHAO Boxin,DENG Yingguang
关键字: 雷公藤甲素;微透析法;皮肤药动学;糖尿病;经皮透过量;大鼠
KEYWORDS: Triptolide; Microdialysis; Dermal pharmacokinetics; Diabetes; Percutaneous penetration amount; Rats
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