摘要
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.
出处
《中药材》
CAS
CSCD
北大核心
2012年第8期1295-1298,共4页
Journal of Chinese Medicinal Materials
基金
科技部十一五重大新药创制项目(2009ZX09103-342)