醋酸曲安奈德巩膜植入剂的制备及体外释放特性考察

Preparation and in vitro release feature of a scleral implant containing triamcinolone acetonide acetate

目的制备醋酸曲安奈德(triamcinolone-acetonide-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,其中TAA的载药量为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。

Objective To prepare a biodegradable sckeral implant containing triamcinolone-acetonide-acetate （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 O. 8 mm in diameter. The drug loading was 30%. The drug was released at a steady and slow rate. Its ac- cumulation 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 slera] 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.