丹参总酚酸生物黏附漂浮微丸体外释放和大鼠药代动力学研究  

Study on in Vitro Release of Salvianolic Acid Bioadhesive Floating Pellets and Pharmacokinetics in Rats

作　　者：杨丹丹[1] 黎迎[1] 朱春燕[1] YANG Dan-dan;LI Ying;ZHU Chun-yan(Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100193, China)

机构地区：[1]中国医学科学院北京协和医学院药用植物研究所,北京100193

出　　处：《中国中医药信息杂志》2018年第6期77-81,共5页Chinese Journal of Information on Traditional Chinese Medicine

基　　金：中国医学科学院医学与健康科技创新工程(2016-I2M-1-012)

摘　　要：目的制备丹参总酚酸生物黏附漂浮微丸,延长其在体内的滞留时间,提高其口服生物利用度。方法采用挤出滚圆法,分别以壳聚糖、羟丙基甲基纤维素(HPMC)和卡波姆为黏附材料,十八醇为漂浮材料,微晶纤维素为成型剂,制备丹参总酚酸黏附漂浮微丸。考察制备的2种黏附漂浮微丸的体外释放及其在大鼠体内生物利用度。结果体外释放试验结果表明,空白微丸中丹酚酸B在4 h即释放完全,而制备的2种黏附漂浮微丸的体外释放时间达12 h。大鼠体内药代动力学研究结果表明,大鼠分别灌胃丹参总酚酸原料药、丹参总酚酸壳聚糖微丸、丹参总酚酸HPMC微丸后,丹酚酸B在大鼠体内Tmax分别为(12.00±2.74)min、(17.00±7.58)min、(27.00±12.55)min,丹参总酚酸壳聚糖微丸、丹参总酚酸HPMC微丸相对生物利用度分别为177.08%、172.03%。结论丹参总酚酸黏附漂浮微丸在体外释放缓慢,黏附漂浮微丸可延长药物在体内的滞留时间,提高丹参总酚酸在大鼠体内的口服生物利用度。Objective To prepare salvianolic acid bioadhesive floating pellets; To prolong its residence time in vivo; To improve the oral bioavailability. Methods Salviae miltiorrhizae total phenolic acid adhering floating pellets were prepared by extrusion-spheronization. Chitosan, HPMC and carbomer were used as adherent material, stearyl alcohol was used as floating material and MCC as forming agent. The in vitro release of two adherent floating pellets were prepared and their bioavailability in rats were investigated. Results The results of in vitro release test showed that the salvianolic acid B in the blank pellets was completely released at 4 h, and the two adherent floating pellets prepared in vitro were released for 12 h. The results of pharmacokinetic studies in rats showed that after intragastric administration of salvianolic acid, salvianolic acid chitosan pellets and salvianolic acid HPMC pellets, Tmax were（12.00±2.74）min,（17.00±7.58）min and（27.00±12.55）min, respectively. The relative bioavailability of salvianolic acid chitosan pellets and salvianolic acid HPMC pellets were 177.08% and 172.03%, respectively. Conclusion Salvia total phenolic acid adherent floating pellets release slowly in vitro, and floating pellets can prolong the retention time in vivo and increase the oral bioavailability of salvianolic acid in rats.

关 键 词：丹参总酚酸 生物黏附漂浮 微丸 体外释放 药代动力学 

分 类 号：R285.5[医药卫生—中药学]