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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 establish a HPLC-fluorescence method for the determination of capsaicin in rabbits plasma and to compare the pharmacokinetic parameters of rabbits with capsaicin nanoemulsion and capsaicin solution. Methods: The double-cycle crossover design was used. Six rabbits were injected with capsaicin nanoemulsion and solution respectively. Blood samples were collected at 3, 6, 9, 12, 15, 25, 40, 60, 90 and 120 min after administration , HPLC-fluorescence determination of plasma concentration, and calculate the main pharmacokinetic parameters. Results: Capsaicin had good linearity in the range of 0.197-49.3 g.L-1 (r = 0.999 6). The lowest detection limit was 5.9 ng.mL-1. The recovery was 102.5% -107.6% with RSD <5%. The elimination half-life (t1 / 2) of capsaicin nanoemulsion and its solution were (11.77 ± 2.32) min and (9.53 ± 2.19) min, respectively. The AUC was (5 311 ± 1 324.6) ng.mL-1.kg- 4 909.5 ± 1 110.4) ng.mL-1.kg-1.min. Conclusion: HPLC-fluorescence method is simple, accurate and sensitive for the determination of capsaicin in plasma. Rabbits intravenous injection of capsaicin nanoemulsion and the main pharmacokinetic parameters were no significant difference.