【摘要】 目的制备甘草酸二铵二元脂质体温敏凝胶,并评价其体外释药行为。方法冷溶法制备凝胶。以胶凝温度为评价指标,泊洛沙姆407(P407)、泊洛沙姆188(P188)、白芨多糖用量为影响因素,星点设计-效应面法优化处方。再采用HPLC和Franz立式扩散池法评价其体外释药行为。结果最优处方为P407用量18%,P188用量4%,多糖用量0.6%,胶凝温度(37.5±0.3)℃。所得二元脂质体温敏凝胶在48 h内的累积释放率为(65.52±0.63)%,与脂质体及温敏凝胶相比缓释作用更明显。结论甘草酸二铵二元脂质体温敏凝胶可减缓药物在直肠内的释放速率,并增加其滞留时间。更多还原

【Abstract】 AIM To prepare thermo-sensitive diammonium glycyrrhizinate binary liposome gel and to evaluate the in vitro drug-release behaviors. METHODS Cold dissolution method was adopted in the preparation of gel.With gel transition temperature as an evaluation index,amounts of Poloxamer 407(P407),Poloxamer 188(P188) and polysaccharides from Bletillae Rhizoma as influencing factors,central composite design-response surface method was applied to optimizing the formulation. Then the in vitro drug-release behaviors were evaluated by HPLC and Franz vertical diffusion cell method. RESULTS The optimal formulation was determined to be 18%for P407 amount,4% for P188 amount,and 0. 6% for polysaccharides’ amount,the gel transition temperature was(37. 5 ± 0. 3) ℃. The accumulative release rate of obtained thermo-sensitive binary liposome gel was(65. 52 ±0. 63) % within 48 h,which showed more obvious sustained-release effect as compared with liposome and thermosensitive gel. CONCLUSION Thermo-sensitive diammonium glycyrrhizinate binary liposome gel can reduce drug-release rate and increase its retention time in the rectum.更多还原