盐酸阿米替林/海藻酸钠/壳聚糖微球的制备及释放性能  

Preparation of Amitriptyline Hydrochloride/Alginate/Chitosan Microspheres and Their Drug-Releasing Performance

作　　者：李国明[1] 刘聪[1] 林跃[1] 高回春[1] 骆小伟[1] 汪朝阳[1] 

机构地区：[1]华南师范大学化学与环境学院,广州510631

出　　处：《应用化学》2008年第11期1351-1355,共5页Chinese Journal of Applied Chemistry

基　　金：广东省自然科学基金资助项目(5300082)

摘　　要：以三环类抗抑郁药盐酸阿米替林(Amitriptyline Hydrochloride,AH)为模型药物,海藻酸钠为内层,壳聚糖为外层,以乙二醇二缩水甘油醚(ethylene glycol diglycidyl ether,EGDE)为壳聚糖的交联剂,采用乳化分散-化学交联法,制备了盐酸阿米替林/海藻酸钠/壳聚糖微球,考察了其理化性质和释放性能。结果表明,所得微球形状较规整,乳白色,平均粒径18.70μm,载药量为9.5%,药物包封率达53.25%。XRD分析结果表明,微球内部盐酸阿米替林药物主要以无定形聚集态存在。结果表明,盐酸阿米替林/海藻酸钠/壳聚糖微球有较好的药物缓释效果。所制得的微球释药速率,随着海藻酸钠浓度增大而减慢;随反应pH值的增大而增大;随药物/海藻酸钠投料比的增大而增大。在碱性和酸性缓冲溶液中,释药速率在酸性缓冲溶液中略大于碱性缓冲溶液中的释药速率。With a tricyclic antidepressant amitriptyline hydrochloride（AH） as the model drug, Alginate as the inside layer, and chitosan as the outside layer, amitriptyline hydrochloride-Alginate-chitosan microspheres were prepared by emulsion cross-linking technique with ethylene glycol diglycidyl ether（EGDE） as the cross-linking agent. The physicochemical properties and the drug-release performance of the microspheres were investigated. The microspheres had a spherical shape and were white in color, and the averaged diameter was about 18. 70 μm. The drug content was 9. 5% （mass fraction） and the drug loading efficiency could reach 53. 25%. XRD analysis indicated that the AH in the microspheres were amorphous. The microspheres had a satisfactory performance of slowly releasing the AH. With the increase of the concentration of Alginate, the releasing rate of amitriptyline hydrochloride decreased; with the increase of pH, the releasing rate of amitriptyline hydrochloride increased ; with the increase of the ratio of amitriptyline hydrochloride to Alginate by weight, the releasing rate of AH increased. The release rate of AH in acidic buffer was faster than that of AH in alkaline buffer.

关 键 词：盐酸阿米替林 海藻酸钠 壳聚糖 微球 交联 乙二醇二缩水甘油醚 

分 类 号：O536[理学—等离子体物理]