探索玉米纤维胶在制作胃内滞留性差药物的黏附性浮动片剂中的潜力

Q3 Medicine
Bhumika Mangla, Anurekha Jain, Deepinder Singh Malik
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引用次数: 0

摘要

目的:配制并初步评估基于多糖的辛纳利嗪粘附浮动片剂:背景:胃黏膜给药系统已被证明是一种成功的方法,可通过特定部位靶向提高药物在胃内的停留时间,从而达到局部或全身的效果。全球范围内也有多项采用胃黏膜给药方法的专利申请:本研究旨在探索玉米纤维胶(CFG)的粘附性和低密度特性,以制备保胃型辛那利嗪浮动片剂:采用不同浓度的 CFG(45%、50%、60% w/w),通过直接压片技术制备浮动片剂。对所配制的浮动片剂批次进行了硬度、易碎性、药物含量、浮动持续时间/滞后时间、溶胀行为、生物黏附强度和体外药物释放等方面的评价:结果:粘附力随着多糖浓度的增加而增加。膨胀指数随着 CFG 浓度的增加和药片在培养基中停留时间的延长而增加。体外药物释放研究表明,随着聚合物浓度的增加,药物释放量减少(从 91% 减少到 77%)。释放数据被进一步拟合到各种动力学模型中,结果显示药物释放符合零阶模型和樋口模型,这表明聚合物具有形成可溶胀基质的能力。Korsemeyer Peppas 模型中的 n 值(介于 0.458 和 0.997 之间)表明,药物从制剂中释放的机制可能不止一种,即扩散和侵蚀。稳定性研究表明,制剂在不同的储存条件下都能保持其完整性和药物特性:因此,从研究结果中可以得出结论,CFG 具有潜在的粘合剂、缓释剂和粘合剂特性,可成功用于配制胃保留浮动片剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Exploring the Potentials of Corn Fiber Gum in Fabricating Mucoadhesive Floating Tablet of Poorly Gastro-retainable Drug.

Aim: To formulate and preliminary evaluated polysaccharide based mucoadhesive floating tablets of Cinnarizine.

Background: Gastro-retentive drug delivery systems has proved to be a successful approach to enhance the gastric residence with site specific targeting for achieving local or generalized effect. Various patents has also been filed globally employing gastro-retentive approach.

Objective: The study is designed to explore the mucoadhesive and low density characteristics of corn fibre gum (CFG) for preparation of gastro-retentive floating tablets of cinnarizine.

Methods: Floating tablets were prepared by direct compression technique using different concentrations of CFG (45, 50, 60% w/w). The formulated floating tablet batches were evaluated for their hardness, friability, drug content, floating duration/ lag time, swelling behavior, bioadhesive strength and in vitro drug release.

Results: Mucoadhesive strength was found to increase with an increment in the polysaccharide concentration. Swelling index was found to increase both with the increase in CFG concentration and with duration for which tablet remains in medium. The in vitro drug release studies indicated decrease in drug release (91% to 77%) with the increase in polymer concentration. The release data was further fitted to various kinetic models which revealed the drug release to be in accordance with Zero-order and Higuchi models, indicating polymer to exhibit the swellable matrix forming abilities. The value of n (between 0.458 and 0.997) from Korsemeyer Peppas model depicted the possibility of drug to follow more than one mechanism of release from the formulation i.e. diffusion and erosion. Stability studies revealed the preparations to retain their integrity and pharmaceutical characteristics at variable storage conditions.

Conclusion: Thus from the research findings, CFG could be concluded to possess potential binder, release retardant and mucoadhesive characteristics which could be successfully employed for the formulation of gastro-retentive floating tablets.

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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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