Dai Ya-Jie, Chen Xiao-Lan, Tang Hong-Yan, Deng Xian-Yi, Xie Lang
School of Pharmaceutical Sciences, Heilongjiang University of Chinese Medicine, Harbin 150040, China.
Zhongguo Zhong Yao Za Zhi. 2017 Jul;42(14):2767-2772. doi: 10.19540/j.cnki.cjcmm.20170523.010.
To evaluate the optimum administration routes of saikosaponin in the treatment of epilepsy by comparing the plasma pharmacokinetics and the brain pharmacokinetics after different administration routes of saikosaponin. After receiving saikosaponin in different administration routes, the mice were sacrificed to collect the blood and brain tissues. The acetonitrile and methanol (9∶1) were used to precipitate the plasma protein. The concentration of the SSa in mice plasma and brain was determined by UPLC-MS/MS, and the pharmacokinetic parameters, bioavailability, the brain targeting coefficient (Re) and the brain drug targeting index (DTI) were calculated with Kinetica software. The relative brain Re was 142.17% by intranasal administration, with DTI of 3.06, significantly higher than those by the injections; in addition, the brain DTI was 1.25 by gavage administration. The brain drug targeting of saikosaponin by intranasal administration was higher than that by injection and gavage administration, indicating the advantages of the intranasal administration on medicine absorption into the brain.
通过比较柴胡皂苷不同给药途径后的血浆药代动力学和脑药代动力学,评估柴胡皂苷治疗癫痫的最佳给药途径。给予小鼠不同给药途径的柴胡皂苷后,处死小鼠收集血液和脑组织。用乙腈和甲醇(9∶1)沉淀血浆蛋白。采用超高效液相色谱-串联质谱法测定小鼠血浆和脑中柴胡皂苷a(SSa)的浓度,并用Kinetica软件计算药代动力学参数、生物利用度、脑靶向系数(Re)和脑药物靶向指数(DTI)。鼻腔给药的相对脑Re为142.17%,DTI为3.06,显著高于注射给药;此外,灌胃给药的脑DTI为1.25。鼻腔给药的柴胡皂苷脑靶向性高于注射给药和灌胃给药,表明鼻腔给药在药物脑内吸收方面具有优势。