苦参碱乳膏剂的动物药动学及生物利用度研究

Studies on pharmacokinetics and bioavailability of matrine creams

目的 建立家兔血清苦参碱的反相高效液相色谱分析法 ,测定药动学参数和绝对生物利用度。方法 采用C18柱 ,流动相为甲醇 水 氨水 (780∶2 2 0∶9)。血清用高氯酸沉淀蛋白后 ,取上清液直接进样。结果 苦参碱在 4～ 5 6mg·L-1范围内呈良好线性关系 (r=0 .9996 ) ,最低检出限量 0 .3mg·L-1。日间和日内误差均小于 2 .2 % ,方法回收率 95 .3%。结论 方法操作简便 ,避免了血浆或血清萃取操作 ,保留时间 (5 .3min)较正相层析保留时间 (8.0min)短[1～ 2 ] 。乳膏中苦参碱以零级药动学透过皮肤 ;可提供比注射剂稳定的血药浓度 ,生物利用度为 80 .82 %。

OBJECTIVE To establish a reversed phase high performance liquid chromatography in the determination of matrine in serum.METHODS C 18 column was used as the analytical colum.The mobile phase was consisted of methanol water ammonia solution (780∶220∶9).The 0.58 mol·L -1 Perchloric acid was used to precipitate proteins in serum.RESULTS The linearity ranged from 4 to 56 mg·L -1 .The detection limit was 0.3 mg·L -1 .The RSD (%) of within day and between day was less than 2.2%.The recovery of this method was 95.3% .CONCLUSIONS This assay was rapid,accurate;sensitive and simple.The bioavailability of matrine cream was 80.82%.