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目的:利用在体皮肤微透析技术研究吴茱萸提取物经皮吸收的特性。方法:以裸鼠为研究对象,建立在体经皮微透析采样技术,以吴茱萸碱和吴茱萸次碱为指标成分,采用高效液相色谱测定吴茱萸提取物经皮给药后透析液中的药物浓度,通过相对损失率的校正,计算皮肤药物浓度,并利用Kinetica 5.0软件对皮肤药物浓度和时间进行非房室模型拟合,计算相关统计参数。结果:吴茱萸提取物中吴茱萸碱的达峰时间为(150±15.3)min,半衰期(t1/2)(263.7±41.6)min;吴茱萸次碱的达峰时间为(90±2.1)min,半衰期(t1/2)(194±17.3)min;二者均能较快地达到峰值,并在较长的时间内保持稳定释放,使皮下组织中的药物浓度保持在一个相对恒定的水平。结论:本研究中所建立的微透析方法可用于吴茱萸提取物的皮肤药动学研究,吴茱萸碱和吴茱萸次碱可透过皮肤吸收而发挥临床药效。
OBJECTIVE: To study the characteristics of transdermal absorption of Evodia rutaecarpa extract by in-vivo dermal microdialysis technique. Methods: The nude mice were selected as the experimental subjects. Based on the dermal microdialysis sampling technique, evodiamine and rutaecarpine were used as indexes to determine the drug concentration in the dialysate after transdermal administration of Evodia rutaecarpa extract , Calculate the concentration of dermatological drug by correcting the relative loss rate and calculate the relevant statistical parameters by using Kinetica 5.0 software to fit non-compartmental model of skin drug concentration and time. Results: The peak time of evodiamine in Fructus Evodiae was (150 ± 15.3) min and the half-life (t1 / 2) was 263.7 ± 41.6 min. The peak time of evodiamine was (90 ± 2.1) min and the half- t1 / 2) (194 ± 17.3) min, respectively. Both of them could reach the peak faster and maintain stable release for a longer period of time, which kept the concentration of drug in subcutaneous tissue at a relatively constant level. Conclusion: The microdialysis method established in this study can be used to study skin pharmacokinetics of Evodia rutaecarpa extract. Evodiamine and rutaecarpine can exert their clinical efficacy through skin absorption.