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Optimization of the Composition and Production Technology of Fucoidan Tablets and their Biopharmaceutical Evaluation
Pharmaceutical Chemistry Journal ( IF 0.8 ) Pub Date : 2020-08-01 , DOI: 10.1007/s11094-020-02237-4
E. D. Obluchinskaya , O. N. Pozharitskaya , E. V. Flisyuk , A. N. Shikov

The discovery and development of drugs that can compete in effectiveness with direct anticoagulants is a critical problem. Fucoidan is a complex branched heteropolysaccharide with anticoagulant and antithrombic activity. Fucoidan drug substance is hygroscopic and possesses poor technological properties. This study was aimed at development of the optimum composition and technology of fucoidan tablets and their biopharmaceutical evaluation. The generalized Harrington desirability function and dispersion and regression analyses were used for optimization of the fucoidan tablet formulation. The contents of crospovidone and lactose were the most significant factors affecting the disintegration and compressibility of model tablets. The lactose content had the greatest impact on the Carr index and Hausner ratio. The in vitro dissolution curves of the tablets were compared (at pH 1.2, 5.7, and 6.8). The in vitro release of fucoidan from the developed tablets obeyed a first-order kinetic equation.

中文翻译:

褐藻糖胶片组成、生产工艺优化及生物药学评价

能够与直接抗凝剂在有效性上竞争的药物的发现和开发是一个关键问题。褐藻糖胶是一种复杂的支链杂多糖,具有抗凝血和抗血栓活性。褐藻糖胶原料药具有吸湿性,工艺性能较差。本研究旨在开发岩藻依聚糖片的最佳组成和工艺及其生物药学评价。广义 Harrington 合意性函数以及分散和回归分析用于优化岩藻依聚糖片剂配方。交聚维酮和乳糖的含量是影响模型片剂崩解性和可压性的最显着因素。乳糖含量对卡尔指数和豪斯纳比的影响最大。比较了片剂的体外溶出曲线(pH 1.2、5.7 和 6.8)。从开发的片剂中岩藻依聚糖的体外释放遵循一级动力学方程。
更新日期:2020-08-01
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