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卡拉胶控释片剂基质:压缩与溶出度研究。

Controlled-release tablet matrices from carrageenans: compression and dissolution studies.

作者信息

Hariharan M, Wheatley T A, Price J C

机构信息

Department of Pharmaceutics, University of Georgia, Athens 30602, USA.

出版信息

Pharm Dev Technol. 1997 Nov;2(4):383-93. doi: 10.3109/10837459709022637.

Abstract

This study investigates the potential of two commercial carrageenans, Gelcarin GP-379 (iota-carrageenan) and Viscarin GP-209 (lambda-carrageenan) to be used for the preparation of controlled-release tablet matrices. Tablets were compressed on an instrumented Stokes single punch machine and compression characteristics of the carrageenans were analyzed. Heckel plots using out-of-die tablet densities were linear with calculated yield pressures of 81.3 MPa and 105.2 MPa for iota- and lambda-carrageenan, respectively. Drug release from tablet formulations that contained equal amounts of the two carrageenans had near zero-order release profiles. There was little or no effect of tablet compression pressure on the drug release profiles from 70 to 175 MPa. As drug loading was increased from 5 to 20%, the diffusional exponent decreased from 1.056 to 0.678. Thirty percent drug loading resulted in breakup of tablets during dissolution and departure from zero-order release. Multiple regression analysis was used to predict the time for 50% release as a function of the concentration of the two carrageenans and a third filler material, microcrystalline cellulose. Predicted values were in good agreement with observed values and R2 for the final cubic model was 0.9984.

摘要

本研究考察了两种商业角叉菜胶,即Gelcarin GP - 379(ι-角叉菜胶)和Viscarin GP - 209(λ-角叉菜胶)用于制备控释片剂基质的潜力。片剂在一台配备仪器的斯托克斯单冲压片机上压制,并对角叉菜胶的压缩特性进行了分析。使用模外片剂密度绘制的赫克尔图呈线性,ι-角叉菜胶和λ-角叉菜胶的计算屈服压力分别为81.3 MPa和105.2 MPa。含有等量两种角叉菜胶的片剂配方的药物释放具有接近零级的释放曲线。片剂压缩压力在70至175 MPa范围内对药物释放曲线几乎没有影响或没有影响。随着药物载量从5%增加到20%,扩散指数从1.056降至0.678。30%的药物载量导致片剂在溶解过程中破裂并偏离零级释放。使用多元回归分析来预测50%释放时间,作为两种角叉菜胶和第三种填充材料微晶纤维素浓度的函数。预测值与观察值吻合良好,最终立方模型的R2为0.9984。

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