聚酰胺-胺树状大分子作为药物载体的体外增溶、缓释试验  

In Vitro Test of PAMAM Dendrimer as a Drug Carrier in Solubilization and Sustained Release

作　　者：唐杨[1] 马丽芳[1] 郭丽[2] 戴华胄[1] 贺世超[1] 

机构地区：[1]四川大学化工学院制药与生物工程系,成都市610065 [2]四川大学华西药学院,成都市610041

出　　处：《中国药房》2009年第1期21-24,共4页China Pharmacy

基　　金：国家自然科学基金资助项目(20472055)

摘　　要：目的:考察以聚酰胺-胺树状大分子(PAMAM)作为喹诺酮类药物载体在增溶、缓释方面的作用。方法:根据文献合成PAMAM,并作结构分析;以巴洛沙星为模型药物,检测不同代数不同浓度的PAMAM对巴洛沙星的增溶作用;同时用不同代数的PAMAM与巴洛沙星复合,检测PAMAM对巴洛沙星体外释放的影响,以及在水及模拟肠液中的释放情况。结果:巴洛沙星在水中溶解度约为1.5g·L-1,完全释药时间约为4h。随着PAMAM代数和浓度的增加巴洛沙星溶解度增加(2～5.25g·L-1),PAMAM与巴洛沙星复合物在水中24h释放80%,在模拟肠液中72h释放73%。结论:PAMAM对巴洛沙星具有增溶、缓释作用,有可能促进其制成具有缓释作用的溶液剂或注射剂。OBJECTIVE： To investigate the effect of PAMAM as drug carrier of quilonones on the solubilization and sustained release. METHODS： PAMAM was synthesized in accordance with literature, and its structure was analyzed; With balofloxacin being the model drug and the increase of solubility of balofloxacin brought about by PAMAM molecules of different generations and concentrations was detected. Meanwhile, by combining various generations of PAMAM molecules with balofloxacin, the influence of PAMAM on the in vitro drug release as well as the release of the drug in water and simulated intestinal fluid were detected. RESULTS： Balofloxaein solubility in water was about 1.5 g· L^-1, and fully drug release time was about 4 h. With the increase of PAMAM generation and concentration, the solubility of balofloxaein increased from 2 g · L^-1 to 5.25 g · L^- 1. The 24 h release of PAMAM balofloxacin complex in water reached 80%, 73% in simulated intestinal fluid 72 h later. CONCLUSIONS： PAMAM can increase solubility and slow drug release of balofloxacin, which is expected to be made into slow release liquid and injection preparations.

关 键 词：聚酰胺-胺树状大分子 巴洛沙星 喹诺酮类药物 增溶 缓释 

分 类 号：R944.9[医药卫生—药剂学]