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作 者:吕鹏[1] 卞广兴[1] 温利青[1] 任建平[1] 吕秋军[1]
机构地区:[1]军事医学科学院放射与辐射医学研究所,北京100850
出 处:《中国新药杂志》2008年第8期661-666,共6页Chinese Journal of New Drugs
摘 要:目的:研究甘草素(liquirtigenin)的肠吸收及血脑屏障(BBB)通透性。方法:利用大鼠单向肠灌流模型及联用高效液相色谱(HPLC)方法研究甘草素的吸收。分离鼠脑微血管内皮细胞(BMEC)和星形胶质细胞(AC),建立体外BBB模型,研究甘草素的BBB通透性。结果:在体肠灌流模型中甘草素在空肠处的有效渗透系数(Peff)为(101.1±4.7)×10-6cm.s-1,高于工具药盐酸普萘洛尔的Peff(77.4±15.2)×10-6cm.s-1。BBB通透实验中90 min时甘草素的BBB通透率为(29.73±6.83)%,工具药青霉素钠和氯霉素的BBB通透率分别为(1.64±0.17)%和(34.03±4.92)%。结论:甘草素肠壁通透性较好,也较易透过BBB。Objective:To investigate the properties of intestinal absorption and in vitro blood-brain barrier (BBB) permeability of liquirtigenin. Methods: A single pass intestinal perfusion model was used to evaluate the intestinal absorption of liquirtigenin as assayed by HPLC in rats. An in vitro model of BBB using cultured rat brain microvascular endothelial cells and astrocytes was established to study the permeability of liquirtigenin. Results: The effective permeability values (Peff) of liquirtigenin in jejunum was higher [ ( 101. 1 ± 4.7) × 10^-6 cm·s^-1] than that of the intestinal transport marker propranolol hydrochloricde [ (77.4 ± 15.2) × 10^- 6 cm· s^-1 ] in the single pass intestinal perfusion model. The quantity of in vitro BBB penetration of liquiritigenin, benzylpenicilin and chloramphenicol were (29.73 ± 6.83 ) %, ( 1.64± 0. 17) % and (34.03 ±4.92) %, respectively, within 90 min. Conclusions: Liquirtigenin exhibits better intestinal absorption and BBB permeability.
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