家兔静脉注射辣椒碱纳米乳及溶液的药动学比较研究

Pharmacokinetcs in Rabbits after Intravenous Injection of Capsaicin Nanoemulsions and Soluion

目的:建立HPLC-荧光法测定家兔血浆中辣椒碱含量,并比较家兔静脉注射辣椒碱纳米乳及辣椒碱溶液的药动学参数差异。方法:采用双周期交叉试验设计,6只家兔分别单剂量注射辣椒碱纳米乳及溶液,分别在给药后3,6,9,12,15,25,40,60,90,120 min时取血,以HPLC-荧光法测定血药浓度,并计算主要药动学参数。结果:辣椒碱在0.197～49.3 g.L-1(r=0.999 6)内线性良好,最低检测限为5.9 ng.mL-1,回收率为102.5%～107.6%,RSD<5%。辣椒碱纳米乳及溶液的消除半衰期t1/2分别为(11.77±2.32)min和(9.53±2.19)min,AUC为(5 311±1 324.6)ng.mL-1.kg-1.min和(4 909.5±1 110.4)ng.mL-1.kg-1.min。结论:HPLC-荧光法简便、准确、灵敏,适用于辣椒碱的血药浓度测定。家兔静脉注射辣椒碱纳米乳及溶液的主要药动学参数比较无显著性差异。

Objective：To develop an HPLC-FLU method for the determination of capsaicin in rabbit plasma and to study its pharmacokinetics.Method： Six rabbits were given capsaicin nanoemulsions and ethanol solution（1mg.kg-1） via ear vein by double cycle crossover design,and after 3,6,9,12,15,25,40,60 and 120 min,blood samples were collected.HPLC-FLU was established to determine the plasma concentration of capsaicin and the pharmacokinetic evaluation was carried out.Result：The linear range of capsaicin was 0. 197-49.3 mg·L^-1（r =0. 999 6） and the limit of detection of capsaicin was 5.9 ng· mL^-1 , the average recovery was 102.5% - 107.6% with RSD 〈 5%. The t1/2 of capsaicin nanoemulsions and solution was （11.77 ±2.32） min and （9.53 ± 2. 19 ） min respectively, and the AUC was （5 311±1 324.6） ng·mL^-1·kg^-1.min and （4 909.5±1 110.4） ng·mL^-1·kg^-1. min respectively. Conclusion：This assay method is simple, precise and sensitive enough for the pharmacokinetic study of capsaicin. The pharmacokinectics parameters between capsaicin nanoemulsions and solution had no significant difference （ t test, P 〉 O. 05）.