摘要
目的 制备醋酸曲安奈德(triameinolone-aeetonide-acetate,TAA)-聚乳酸(polylactic acid,PLA)植入剂(Im-plant),考察醋酸曲安奈德植入剂的体外释药特性.方法 采用熔融-挤出法制备TAA-PLA植入剂,高效液相色谱法测定TAA含量,绘制体外释放曲线.结果 制得的植入剂为直径0.8 mm,长约8 mm,质量约8 mg的白色柱状物,其巾TAA的载药鼍为30%,体外释放速率平稳且缓慢,第30天时TAA的累积释放率为75.84%,药物体外释放符合Higuchi方程Q=0.137×(t-0.752)1/2.结论 所制备的TAA-PLA植入剂对药物TAA有明显的缓释效果,且在体内可生物降解,毒副作用小,有望成为TAA的眼部新型给药制剂.
Abstract
Objective To prepare a biodegradable sckeral implant containing triamcinolone-acetonide-ace-tate (TAA) and polylactic acid (PLA) and investigate its release in vitro. Methods The TAA-PLA implant was prepared by melt-extrude technique. The drug release of TAA in vitro was determined by high performance liquid chromatography ( HPLC ). Results The implant was white pillar with 8 mm in length, 8 mg in weight, and 0.8 mm in diameter. The drug loading was 30%. The drug was released at a steady and slow rate. Its accumulation release rate is 75. 84% on the 30th day. Drug release profile in vitro was in accordance with Higuchi equation Q =0. 137 (t -0.752)1/2. Conclusion A sleral implant containing TAA-PLA is prepared, which has the evident feature in delaying the release of TAA and is biological degradable. It might be a novel vehicle for the topical use of TAA.