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目的考察马钱子碱、马钱子总生物碱和优化马钱子总生物碱凝胶剂经皮给药后在小鼠体内的药动学过程。方法建立测定小鼠血浆中马钱子碱质量浓度的HPLC法,比较含相同剂量(10.8 mg/kg)马钱子碱各凝胶剂经皮给药后,马钱子碱的血药浓度,并对结果进行药动学拟合。结果经皮给药后马钱子生物碱类成分的药动学行为均符合二室模型。优化马钱子总生物碱凝胶剂能显著增加马钱子碱的体内吸收,相对生物利用度显著提高,AUC0→t是马钱子碱凝胶剂的1.74倍,是马钱子总生物碱凝胶剂的1.89倍,其他药动学参数无显著差异。结论以优化马钱子总生物碱经皮给药,可有效改善单体马钱子碱和总生物碱的体内药动学行为,有利于对马钱子碱的减毒增效。
Objective To investigate the pharmacokinetics of strychnine, Strychnos nux - vomica alkaloids, and optimized strychnos alkaloids gels in mice after transdermal administration. Methods The HPLC method for the determination of brucine in mice plasma was established. The serum concentration of brucine was compared after transdermal administration of brucine with the same dose (10.8 mg / kg) The results of pharmacokinetic fitting. Results Pharmacokinetic behavior of the constituents of Strychnos nux vomica after percutaneous transdermal administration accorded with two-compartment model. Optimization of Strychnos alkaloids gel can significantly increase strychnine absorption in vivo, the relative bioavailability significantly increased, AUC0 → t is 1.74 times the brucine gel, is the total Strychnos alkaloids Gel 1.89 times, no significant difference in other pharmacokinetic parameters. Conclusion Optimizing the transdermal administration of total Strychnos alkaloids can improve the pharmacokinetics of strychnine and total alkaloids in vivo, which is beneficial to the reduction of toxicity and efficiency of brucine.