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评价用于苯磺酰吡酸二钠控释的Eudragit RS-PO和乙基纤维素100基质。

Evaluation of Eudragit RS-PO and Ethocel 100 matrices for the controlled release of lobenzarit disodium.

作者信息

Boza A, Caraballo I, Alvarez-Fuentes J, Rabasco A M

机构信息

Department of Chemical Synthesis, Center of Pharmaceutical Chemistry, La Habana, Cuba.

出版信息

Drug Dev Ind Pharm. 1999 Feb;25(2):229-33. doi: 10.1081/ddc-100102164.

DOI:10.1081/ddc-100102164
PMID:10065357
Abstract

Lobenzarit disodium is a drug for the treatment of rheumatoid arthritis. In this work, inert matrix tablets of lobenzarit disodium were prepared by direct compression using Ethocel 100 and Eudragit RS-PO as polymeric materials in different ratios. The obtained powder mixtures and tablets were evaluated from the rheological and technological points of view. The dissolution test was performed to evaluate the in vitro release kinetic of the matrices. The obtained dissolution profiles demonstrated that the matrices containing Eudragit RS-PO showed a slower release rate and therefore were more suitable for controlling the release of drug. The fit to the Higuchi model indicates that the drug release mechanism from these matrices was controlled by the diffusion step.

摘要

洛苯达唑二钠是一种用于治疗类风湿性关节炎的药物。在这项工作中,以不同比例使用乙基纤维素100和聚丙烯酸乙酯-聚甲基丙烯酸甲酯共聚物(Eudragit RS-PO)作为聚合物材料,通过直接压片法制备了洛苯达唑二钠的惰性基质片。从流变学和工艺学角度对所得粉末混合物和片剂进行了评估。进行了溶出度试验以评估基质的体外释放动力学。所得溶出曲线表明,含有Eudragit RS-PO的基质显示出较慢的释放速率,因此更适合于控制药物释放。与Higuchi模型的拟合表明,这些基质中的药物释放机制受扩散步骤控制。

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