马钱子碱贴膏剂的制备与药物动力学研究

Preparation and Pharmacokinetics of Brucine Hydrogel Patch

目的:考察剂量对马钱子碱贴膏剂的体内药物动力学过程的影响。方法:建立了应用HPLC法测定血浆中马钱子碱浓度的分析方法。制备了马钱子碱贴膏剂并考察了药剂学性质。测定3个不同剂量马钱子碱贴膏剂经皮给药后血药浓度经时过程,采用DAS软件拟合药物动力学参数。结果:马钱子碱贴膏剂的药剂学性质符合要求。3个剂量(30、60、180 mg/kg)下马钱子碱贴膏剂经皮给药后的AUC0-t分别为7.24±0.61、16.02±2.34和54.84±26.59μg·h/mL,峰浓度分别为0.73±0.23、1.45±0.28和4.59±1.85μg/mL,达峰时间分别为8.67±2.07、11.67±2.66和8.33±2.65 h。结论:马钱子碱贴膏剂经皮给药后未发现存在剂量依赖性。

Objective：To investigate the effect of dose on pharmacokinetic properties of brucine hydrogel patch.Methods：The plasma concentration of brucine was determined by HPLC.Brucine hydrogel patch was prepared and its pharmaceutical characterization was investigated.After transdermal administration of different dose brucine hydrogel patch;Plasma concentration versus time profiles were determined and pharmacokinetic parameters were calculated by DAS program.Results：The pharmaceutical properties of brucine hydrogel patch were satisfactory.The AUC0-t values were 7.24±0.61,16.02±2.34和54.84±26.59 μg·h/mL after administration of 30,60 and 180 mg/kg brucine hydrogel patch,respectively.The corresponding Cmax values were 0.73±0.23、1.45±0.28 and 4.59±1.85 μg/mL,respectively.And the corresponding Tmax values were 8.67±2.07,11.67±2.66 and 8.33±2.65 h,respectively.Conclusion：The pharmacokinetic properties of brucine do not vary with the dose of brucine hydrogel patch.