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用于包含弱碱性模型药物的控释基质的三元聚合物共混物的制备和评价。

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug.

机构信息

Department of Pharmaceutical Technology, Jordan University of Science and Technology, Irbid, Jordan.

Faculty of Pharmacy, Jerash University, Jerash, Jordan.

出版信息

Curr Drug Deliv. 2021;18(1):54-64. doi: 10.2174/1567201817666200731170040.

DOI:10.2174/1567201817666200731170040
PMID:32735522
Abstract

OBJECTIVE

The objective of this study was to evaluate the suitability of a ternary mixture of smart polymers comprised of EudragitE100, EudragitL100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole.

METHODS

Matrix tablet formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8, and 6.8). Tablets made of low to intermediate proportions of sodium alginate and approximately equal proportions of EudragitE100 and EudragitL100 were found to have a significant modification of drug release rates.

RESULTS

Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit polymers and the ratio of EudragitE100 to EudragitL100 within the ternary polymeric composition were found critical in determining the controlled release performance.

CONCLUSION

Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of a weakly basic drug, Metronidazole.

摘要

目的

本研究的目的是评估由 EudragitE100、EudragitL100 和海藻酸钠组成的三元混合物智能聚合物作为弱碱性药物缓释载体的适用性。本研究选用甲硝唑作为模型药物。

方法

采用直接压片或湿法制粒法制备基质片剂。使用 USP XXΠ 旋转桨装置在三个连续阶段(pH 1.2、4.8 和 6.8)进行溶出度研究。发现低至中等比例海藻酸钠和等量 EudragitE100 和 EudragitL100 的片剂显著改变了药物释放速率。

结果

表明,根据配方中聚合物的比例,有可能控制药物释放 12 小时。海藻酸钠与总 Eudragit 聚合物的比例以及三元聚合物组成中 EudragitE100 与 EudragitL100 的比例对于确定控释性能至关重要。

结论

溶胀研究结果与片剂的溶出行为一致。研究结果表明,三元聚合物组合物在控制弱碱性药物甲硝唑的释放方面具有重要意义。

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