药物缓释用生物降解材料聚乳酸-乙醇酸的合成

Synthesis of Biodegradable Drug Delivery Material Poly(lactic acid-glycolic acid)

以D,L 乳酸、乙醇酸为原料,通过熔融聚合法直接合成生物降解材料聚乳酸 乙醇酸(PLGA)。在165℃、70Pa下熔融聚合10h,以w(SnCl2)=0 5%的氯化亚锡为催化剂时,特性黏数[η]最高可达0 2382dL/g。当使用人体营养添加剂如乳酸锌、乳酸钙、乙酸锌、硫酸锌、牛磺酸等作为无毒催化剂反应时,[η]为0 1036～0 2150dL/g。金属Lewis酸型催化剂乳酸锌与质子酸型催化剂牛磺酸复合使用,[η]为0 1068～0 1357dL/g,比牛磺酸催化时(0 1036dL/g)高,比乳酸锌催化时(0 1507dL/g)低,未见明显的协同效果。简单易行的直接熔融聚合法,尤其是用无毒催化剂催化合成,有利于拓展PLGA在药物缓释领域的应用。

Starting from D,Llactic acid and glycolic acid,biodegradable drug delivery material poly(lactic acid-glycolic acid) (PLGA) was directly synthesized via melt polycondensation.Catalyzed by SnCl2 and w(SnCl2)=05%,under 165 ℃ and 70 Pa,PLGA with the highest intrinsic viscosity 02382 dL/g was produced.When using some nutrition additives such as zinc lactate,calcium lactate,zinc acetate,ZnSO4 and taurine (a sulfonic acid with amino group) as nontoxic catalysts,the intrinsic viscosity ranged between 01036 dL/g and 02150 dL/g.When catalyzed by the compound catalyst of zinc lactate and taurine,the intrinsic viscosity ranged between 01068 dL/g and 01357 dL/g,higher than that catalyzed by taurine (01036 dL/g) and lower than that by zinc lactate (01507 dL/g).No obvious synergistic effect was found between metal Lewis acid catalyst and protonic acid catalyst.The direct melt polycondensation method for the synthesis of PLGA,especially with nontoxic catalysts, is simple and practicable and beneficial for more extensive application of PLGA in drug delivery field.