以醋酸淀粉为控速基质的格列吡嗪CR片的设计与评价

P. Seenivasan , K.P.R. Chowdary , C. Uma Maheswara Reddy , J.S.N. Murthy
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引用次数: 3

摘要

背景/目的合成醋酸淀粉为缓释基质材料,对其进行表征和评价。方法以醋酸淀粉为原料,以不同的药物和聚合物比例配制格列吡嗪基质片,并对其释放动力学和释药机理进行评价。结果马铃薯淀粉与乙酸酐在碱性介质中乙酰化制备淀粉醋酸酯(SA)。乙酰化率为42.38%,取代度为2.75。以不同浓度醋酸淀粉为基质制备的格列吡嗪(10 mg)基质片缓释和控释均大于24 h。格列吡嗪的缓释与基质片中醋酸淀粉的浓度(%)和稀释剂的性质/类型有关。聚合物、醋酸淀粉含量与片剂的释放度(K0)呈线性关系。在短期加速稳定性研究中,醋酸淀粉基质片的控释特性保持不变。结论醋酸淀粉可作为格列吡嗪基质片的缓释基质,醋酸淀粉配制的格列吡嗪基质片在24 h内具有良好的缓释效果。
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Design and evaluation of glipizide CR tablets employing starch acetate as rate controlling matrix former

Background/Objectives

In the present work, starch acetate was synthesized, characterized and evaluated as effective release retarding matrix materials.

Methods

Matrix tablets of glipizide were formulated employing starch acetate in different proportions of drug and polymer and the tablets were evaluated for drug release kinetics and mechanism.

Results

Starch acetate (SA) was prepared by acetylation of potato starch with acetic anhydride in alkaline medium. The percent acetylation was 42.38% and the degree of substitution was 2.75. Glipizide (10 mg) matrix tablets prepared using starch acetate as matrix former in different concentrations gave slow and controlled release more than 24 h. Glipizide release from the tablets formulated was slow and depends on the concentration (%) of starch acetate in the matrix tablets and nature/type of diluent. A linear relationship was found out between percent of polymer, starch acetate and release rate (K0) of the tablets. The controlled release characteristics of the starch acetate matrix tablets of the drug remained unaltered during short time accelerated stability study.

Conclusions

Starch acetate was found suitable as matrix former for controlled release and the matrix tablets of glipizide formulated employing starch acetate gave controlled release of glipizide over 24 h.

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