中国临床药学杂志

目的:观察Poloxamer 407凝胶的形成及液体/凝胶互相转化的条件和喃氟啶在该凝胶中的体外释放.方法:以磷酸盐缓冲液[pH(7.40±0.01)作为Poloxamer 407的稀释剂,以喃氟啶作为实验药物做体外溶出.结果:Poloxmer 407的浓度在15%～40%之内时,随着温度从0℃上升到37℃,其混合物从液体迅速转化成凝胶.相变温度随着Poloxamer407的浓度升高而降低.喃氟啶在该凝胶中的体外释放为零级释放,且随Poloxamer 407浓度的增加,释放速度变慢.8h时.含Poloxamer 407分别为20%,25%,30%,35%(m/m)的凝胶中时喃氟啶的累积释放率分别是(98.22±0.12)%,(86.20±0.20)%,(68.25±0.14)%,(50.02±0.08)%.结论:鉴于Poloxamr 407所具有的特殊的逆温相变性质,作为血管外注射型缓释植入剂的载体是有前途的.

AIM:To study the property of poloxamer 407,a reverse-thermal gelation,and the release of fluorofur from fluorofur/poloxamer 407 gel matrices. METHODS:The fluoro-fur/poloxamer 407 formulations were made up in a pH(7. 40±0. 01) phosphate buffer,and the in vitro release studies were conducted at 37℃. RESULTS:The formulations of fluorofur/poloxamer 407 gel matrices existed as a mobile viscous liquid at reduced temperatures but formed a rigid semisolid gel network with an increase in temperature. The release of fluorofur from the gel matrices in vitro at 37℃ followed zero-order release kinetics. The cumulative percentages of fluorofur released at 37℃,8hr were (98.22±0.12)%, (86.20±0. 20)%, (68.25±0.14)%,(50.02±0.08)% for the 20%, 25%, 30% and 35 %(m/m) fluorofur/ poloxamer 407 formulations,respectively.CONCLUSION:Based on the rapid sol-to-gel transition, it appears that poloxamer 407,may potentially be useful for the formulation and sustained delivery of select drug Pharmaceuticals following extravascular administration.