灵仙新苷微乳的制备及其初步药效学研究  

The preparation and preliminary pharmacodynamics of clematichinenoside microemulsion

作　　者：董彩霞[1] 李默影[1] 姚岚[1] 李丰文[1] 李运曼[2] 刘丽芳[1] 

机构地区：[1]中国药科大学中药分析教研室,江苏南京211198 [2]中国药科大学药理学教研室,江苏南京210009

出　　处：《中成药》2011年第7期1158-1163,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(30772770)

摘　　要：目的制备均一稳定的灵仙新苷(clematichinenoside,AR)油包水微乳,并初步考察其对佐剂性关节炎原发病变小鼠的治疗作用,为威灵仙中药单体药物制剂的开发提供药效学基础。方法选用卵磷脂和乙醇分别作为表面活性剂和助表面活性剂,油酸聚乙二醇甘油酯(Labrafil M 1944Cs)作为油相,AR水溶液为水相,绘制伪三元相图以确定各成分质量比。通过在小鼠右后足跖皮内注射弗氏完全佐剂(CFA)制备佐剂性关节炎(adjuvant arthritis,AA)模型。以体质量、肿胀率、胸腺与脾脏指数为主要检测指标,并观察小鼠病变部位的组织形态来比较AR微乳与AR溶液及阳性对照药白芍总苷的差异。结果确定Km=1∶1,处方组成为油相50%,混合表面活性剂35%,水相15%,得到AR微乳为澄清的淡黄色溶液,平均粒径为10.7 nm。AR微乳对佐剂性关节炎原发病变小鼠疗效略好于AR溶液,且AR微乳能更好地改善佐剂性关节炎原发病变小鼠的病理形态及病变部位的组织形态。结论 AR皂苷微乳粒径较小,脂溶性强,能够增加药物在体内的生物利用度。这表明微乳作为新的药物剂型具有广泛的应用前景。另一方面由于制剂促进药物吸收的机制并不是单一的,仍需进一步研究。AIM To prepare homogeneous and stable water in oil（W/O） microemulsion,and evaluate its therapeutic effect to primary adjuvant arthritis mice,provide background of pharmacodynamics for clematichinenoside AR.METHODS To use lecithin and ethanol as surfactant and cosurfactant,Labrafil M 1944Cs as the oil phase and AR solution as aqueous phase,determine the mass ratio of the components by pseudo-ternary phase diagram.Adjuvant arthritis（AA） model was established through intradermal injection of Freund＇s complete adjuvant（CFA） to right metaleg voix pedis of mice.To use the body weight,swelling rate,thymus and spleen index as the main detection index and to observe the morphology of the diseased region in mice to evaluate the difference among AR solution,AR microemulsion,and TGP which was used as the positive control drug.RESULTS The formulation of AR microemulsion which was clear light yellow solution was as follows： Km=1∶ 1,50% oil,35% of mixed surfactants,aqueous 15%,with the mean particle size of 10.7 nm.The results showed AR microemulsion could improve the pathological lesion and the morphology in diseased region of primary AA mice.CONCLUSION AR microemulsion,with smaller particle size and better liposolubility,is able to increase drug bioavailability in vivo,which shows that the microemulsion has broad application prospects as a new formulation of drugs.On the other hand,the mechanism of promoting drug absorption is not single and further study is still needed.

关 键 词：灵仙新苷 油包水微乳 药效学 

分 类 号：R944.27[医药卫生—药剂学]