Novel Compounding Approach to Floating Alginate Microbeads for Glipizide: Influence of Polymer Matrix on Swelling, Buoyancy, and Drug Release Kinetics.

Q4 Medicine
Shiv Kumar Srivastava, Antesh Kumar Jha, Ritesh Kumar Srivastav, Arun Kumar Tiwari, Mahesh Prasad
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引用次数: 0

Abstract

Background: A BCS class II medication, glipizide has a short half-life and limited solubility; frequent dosage is necessary for efficient glycemic management. A compounding-based gastroretentive drug delivery method employing floating alginate microbeads for prolonged release was created to circumvent these limitations.

Methods: Sodium alginate was used in the ionic gelation process to create floating microbeads, which were then refined by adjusting the quantities of polymers and crosslinkers. The formulations were evaluated for buoyancy, swelling behavior, entrapment efficacy, particle size, and in vitro drug release. Release data were fitted into kinetic models (Zero-order, First-order, Higuchi, and Korsmeyer-Peppas) in order to determine the mechanism of drug release.

Results: Every formulation demonstrated acceptable floating capacity and physicochemical characteristics. With great entrapment efficiency, outstanding buoyancy for more than 12 hours, and a total drug release of 98.86% at 12 hours, formulation F9 outperformed the others. According to kinetic modeling, F9 best matched the Korsmeyer-Peppas model (R2 = 0.998, n = 0.71), suggesting that both diffusion and polymer relaxation/erosion are responsible for anomalous (non-Fickian) release.

Conclusion: According to the study, floating alginate microbeads made using a compounding-based method provide a potentially effective gastroretentive substrate for Glipizide's prolonged release. This approach may improve patient compliance, extend the therapeutic effect, and increase bioavailability. To support the in vitro results, more in vivo research is advised.

格列吡嗪浮藻酸盐微球的新配制方法:聚合物基质对溶胀、浮力和药物释放动力学的影响。
背景:格列吡嗪是BCS II类药物,半衰期短,溶解度有限;频繁给药是有效控制血糖的必要条件。一种基于复合的胃保留药物递送方法,采用漂浮藻酸盐微珠延长释放,以克服这些限制。方法:采用海藻酸钠离子凝胶法制备漂浮微珠,通过调整聚合物和交联剂的用量对微珠进行细化。评价了该制剂的浮力、溶胀行为、包封效果、粒径和体外药物释放。将释放数据拟合为动力学模型(零级、一阶、Higuchi和Korsmeyer-Peppas),以确定药物释放机制。结果:各配方均具有良好的漂浮能力和理化特性。F9具有良好的包封效率,12 h以上浮力突出,12 h总释药率为98.86%。根据动力学模型,F9最符合korsmemeyer - peppas模型(R2 = 0.998, n = 0.71),表明扩散和聚合物弛缓/侵蚀都是异常(非菲克式)释放的原因。结论:采用复合法制备的海藻酸盐微球为格列吡嗪的缓释提供了一种有效的胃保留底物。这种方法可以提高患者的依从性,延长治疗效果,提高生物利用度。为了支持体外结果,建议进行更多的体内研究。
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
CiteScore
0.40
自引率
0.00%
发文量
62
期刊介绍: The International Journal of Pharmaceutical Compounding (IJPC) is a bi-monthly, scientific and professional journal emphasizing quality pharmaceutical compounding. IJPC is the only publication that covers pharmaceutical compounding topics relevant and necessary to empower pharmacists to meet the needs of today"s patients. No other publication features hands-on, how-to compounding techniques or the information that contemporary pharmacists need to provide individualized care.
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