曲安奈德巩膜植入剂的制备及体外释放特性考察-第三军医大学学报.DOC

曲安奈德巩膜植入剂的制备及体外释放特性考察 胡 蕾，刘松青，郭 薇，代 青 （第三军医大学西南医院药学部，重庆 400038） 摘要：目的 制备醋酸曲安奈德（TAA）-聚乳酸（PLA）植入剂（Implant），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㎜，长约8㎜，重约8mg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。 关键词：聚乳酸；醋酸曲安奈德；眼色素层炎；巩膜植入剂 中图法分类号： 文献标识码：A Preparation and release study of triamcinolone acetonide acetate scleral implant in vitro HU Lei, LIU Song-qing, GUO Wei, Dai Qing (Department of Pharmacy, Southwest Hospital, Third Military Medical University, Chongqing 400038) Abstract: Objective To prepare triamcinolone-acetonide-acetate (TAA)-polylactic acid(PLA) Implant and investigate its drug 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 release was 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 These results, indicating that the studied TAA-PLA Implant system had the evident effect in delaying the release of TAA and could be biological degradation in vivo with little side effect, might be a novel vehicle for the topical use of TAA. Key words: PLA; Triamcinolone Acetonide Acetate; Uveitis; Scleral implant 眼植入剂[1]（Eye Implant）是一种长效定量缓释的新型药物制剂，可在眼内长期保持药物的有效治疗浓度，克服药物全身毒性大和玻璃体内半衰期短的缺点，适用于需要长期治疗的某些眼科疾患，分为非蚀解型和蚀解型两类[2]。Alza公司上市了一种乙烯-醋酸乙烯共聚物的载万古霉素植入剂来实现药物的控释，可以在下眼睑持续释放1周，显示出这一新剂型在临床应用的可喜前景。 眼色素层的炎症反应称眼色素层炎，通常以一慢性过程进行，要求长期的药物治疗，最佳的类皮质甾酮疗法是在玻璃体内维持一个长期的治疗浓度水平，现在， 作者简介：胡 蕾，女，重庆市人，硕士研究生，主要从事缓释、靶向药物制剂方面的研究。电话：（023）68