Quality by Design approach for Optimization and Development of Cyclodextrin-Surfactant Complex Based Formulations for Bioavailability Enhancement of Valsartan

Q3 Biochemistry, Genetics and Molecular Biology

Biointerface Research in Applied Chemistry Pub Date : 2022-10-31 DOI:10.33263/briac134.388

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引用次数: 0

Abstract

The main objective of the present research is to increase the oral bioavailability of Valsartan by inclusion complexes (ICVs) with a cyclodextrin-surfactant combination followed by the formulation of fast-dissolving tablets (FDTs). The solvent evaporation method was used for the preparation of ICVs. Methyl-ß-cyclodextrin and Hydroxypropyl-ß- cyclodextrin were evaluated with the combination of poloxamer 188 to get the formulations with the desired solubility. Central composite design (CCD) was used as the experimental design as a part of the quality by design (QbD) approach. The optimized ICVs were further developed into FDTs by direct compression technique. Taking concentration of povidone, type and concentration of disintegrant as the formulation factors, the FDTs were optimized using CCD. In-vivo bioavailability study in rats was performed for the optimized FDTs against the marketed tablets. The optimized ICVs were found to have a 3.12 mg/mL solubility. The optimized FDTs were found to be disintegrated in 18.7 sec and dissolved 90% of the dose in 6.3 min. The In-vivo results indicated that the FDTs exhibited rapid absorption and an increase in bioavailability by 24.1% against the marketed tablets. The results indicated that the QbD approach successfully improved Valsartan's oral bioavailability through cyclodextrin-surfactant complexation.

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环糊精-表面活性剂复合制剂提高缬沙坦生物利用度的质量设计优化与研制

本研究的主要目的是通过包合物（ICVs）与环糊精-表面活性剂的组合，然后配制快溶片（FDTs），提高缬沙坦的口服生物利用度。溶剂蒸发法用于制备ICVs。用泊洛沙姆188组合评价甲基-ß-环糊精和羟丙基-坙-环状糊精，得到具有所需溶解度的制剂。中心复合设计（CCD）被用作实验设计，作为设计质量（QbD）方法的一部分。通过直接压缩技术将优化后的ICV进一步发展为FDT。以聚维酮的浓度、崩解剂的种类和浓度为处方因素，利用CCD对FDTs进行了优化。针对市售片剂，对优化的FDTs进行了大鼠体内生物利用度研究。发现优化的ICVs具有3.12mg/mL的溶解度。发现优化的FDTs在18.7秒内崩解，并在6.3分钟内溶解90%的剂量。体内结果表明，与市售片剂相比，FDTs表现出快速吸收和24.1%的生物利用度增加。结果表明，QbD方法通过环糊精-表面活性剂的络合作用，成功地提高了缬沙坦的口服生物利用度。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Biointerface Research in Applied Chemistry CHEMISTRY, APPLIED-

CiteScore

4.80

自引率

0.00%

发文量

256

期刊介绍： Biointerface Research in Applied Chemistry is an international and interdisciplinary research journal that focuses on all aspects of nanoscience, bioscience and applied chemistry. Submissions are solicited in all topical areas, ranging from basic aspects of the science materials to practical applications of such materials. With 6 issues per year, the first one published on the 15th of February of 2011, Biointerface Research in Applied Chemistry is an open-access journal, making all research results freely available online. The aim is to publish original papers, short communications as well as review papers highlighting interdisciplinary research, the potential applications of the molecules and materials in the bio-field. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible.