穿心莲内酯纳米混悬剂的制备及评价  

Study on Preparation and Evaluation of Andrographolide Nanosuspensions

作　　者：王静娴[1] 李文[1] 陈婷[1] 李俊松[1] 

机构地区：[1]南京中医药大学药学院,江苏南京210023

出　　处：《南京中医药大学学报》2017年第3期313-316,共4页Journal of Nanjing University of Traditional Chinese Medicine

基　　金：江苏省自然科学基金(BK20151002)

摘　　要：目的制备穿心莲内酯纳米混悬剂(ADG-NS),并对其进行表征和评价。方法采用介质研磨法制备ADG-NS,对其粒径及分布、Zeta电位、粒子形态、结晶状态进行表征,采用体外溶出度试验和Caco-2细胞转运试验对ADG-NS进行初步评价。结果 ADG-NS的粒径、多分散性系数、Zeta电位分别为(215.6±3.3)nm、0.165±0.020和(-36.9±2.8)mV。扫描电子显微镜(SEM)分析结果显示,粒子多呈棒状或块状,大小分布较均匀。差示扫描量热(DSC)和x射线粉末衍射(XRPD)分析结果显示,纳米混悬剂中的药物以无定型态存在。与原料药及穿心莲内酯滴丸比较,ADG-NS在不同pH值溶出介质中,溶出速率显著提高。Caco-2细胞单层细胞渗透试验表明,与原料药相比,ADG-NS显示较高的膜渗透性。结论ADG-NS可以提高穿心莲内酯的体外溶出度与膜渗透性。OBJECTIVE To established the andrographolide nanosuspensions （ADG-NS） with improved its dissolution and membrane permeability. METHODS ADG-NS were prepared by wet media milling technique. The quality of the nanosuspen- sions was characterized including the particle size and distribution, Zeta potential, particle morphology and crystal physical state. In vitro dissolution test and Caco-2 permeability test were used to preliminarily evaluate the ADG-NS. RESULTS The particle size, polydispersity index （PDI） and Zeta potential of ADG-NS were （215.6 ± 3.3） nm, 0. 165 ± 0. 020 and （-36. 9 ± 2.8） mV, respectively. SEM analysis showed that there was no adhesion and aggregation between particles, the particles were rod or block, and the size distribution was uniform. DSC and XRPD results showed that the nanoparticles were present in the amorphous form. The dissolution rate of ADG-NS were significantly enhanced in different pH buffer solutions compared to ADG and commercial dripping pills. Caeo-2 permeability test revealed that ADG-NS showed a significant increase in the mem- brane permeability （Papp） compared to the group of ADG （P〈0.01）. CONCLUSION The ADG-NS prepared by wet media milling technique can improve the in vitro dissolution rate and membrane permeability of andrographolide （ADG）.

关 键 词：穿心莲内酯 纳米混悬剂 介质研磨 体外溶出 CACO-2细胞 

分 类 号：R283.6[医药卫生—中药学]