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使用天然和合成聚合物的二元混合物的齐多夫定口服控释片。

Oral sustained release tablets of zidovudine using binary blends of natural and synthetic polymers.

机构信息

Department of Pharmaceutical Technology and Raw Materials Development, National Institute for Pharmaceutical Research and Development, Abuja, Nigeria.

出版信息

Biol Pharm Bull. 2010;33(9):1561-7. doi: 10.1248/bpb.33.1561.

Abstract

Oral sustained release matrix tablets of zidovudine (ZDV) were prepared using different types, proportions and blends of carbopol 71G (C71) and a plant gum obtained from Abelmoschus esculentus (AEG). The effect of various formulation factors like polymer proportion, polymer type and pH of the dissolution medium on the in vitro release of the drug was studied, using the half change technique, in 900 ml of dissolution medium, at 100 rpm. Release kinetics were analyzed using Zero-order, Higuchi's square-root and Ritger-Peppas' empirical equations. In vitro release performance as revealed by the time taken for 70% of the drug to be released (t70%), showed that the release rate decreased with increase in polymer proportion. Matrix tablets containing 10 and 20% AEG were found to exhibit immediate-release characteristics. Matrix tablets containing 30% AEG showed t70% value of 204 min and extended the release up to 5 h, while matrix tablets containing 30% carbopol showed t70% value of 234 min and extended the release up to 6 h. Three blends of AEG and C71 at the ratio of 1:2, 2:1 and 1:3 showed t70% values of 132, 312 and 102 min respectively and extended the release up to 8 h. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets followed Fickian and anomalous release. Drug release from matrix tablets of zidovudine containing blends of AEG and C71 demonstrates the advantage of blending a natural and synthetic polymer over single polymer use.

摘要

齐多夫定(ZDV)的口腔持续释放基质片剂采用不同类型、比例和混合物的卡波姆 71G(C71)和从黄蜀葵(Abelmoschus esculentus)获得的植物胶(AEG)制备。使用半变化技术,在 900ml 溶解介质中,在 100rpm 下,研究了各种制剂因素,如聚合物比例、聚合物类型和溶解介质的 pH 值对药物体外释放的影响。使用零级、Higuchi 平方根和 Ritger-Peppas 经验方程分析了释放动力学。通过达到 70%药物释放所需的时间(t70%)来揭示体外释放性能,结果表明释放速率随聚合物比例的增加而降低。含有 10%和 20%AEG 的基质片剂显示出即刻释放特征。含有 30%AEG 的基质片剂显示 t70%值为 204min,并将释放延长至 5h,而含有 30%卡波姆的基质片剂显示 t70%值为 234min,并将释放延长至 6h。AEG 和 C71 的三种混合物以 1:2、2:1 和 1:3 的比例显示 t70%值分别为 132、312 和 102min,并将释放延长至 8h。释放动力学的数学分析表明,药物从基质片剂中的释放性质遵循菲克定律和异常释放。包含 AEG 和 C71 混合物的齐多夫定基质片剂的药物释放显示出混合天然和合成聚合物比单独使用聚合物的优势。

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