Formulation and Evaluation of Mucoadhesive Buccal Tablets of Repaglinide

M. Patel, C. C. Patil
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引用次数: 3

Abstract

Objective: Delivery of the desired drug as mucoadhesive drug delivery systems has been subject of interest since 1980s. The various advantages associated with these systems made the buccal drug delivery as a novel route of drug administration. Buccal region offers an attractive route for the administration of systemic drug delivery. The objective of the study was to develop mucoadhesive buccal tablets of repaglinide. Methodology: The tablets were prepared by wet granulation method using a combination of mucoadhesive polymers like chitosan, hydroxyethyl cellulose, guar gum and carbopol 934P in different ratios. Results: Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation. The tablets were evaluated for in vitro release in phosphate buffer of pH 6.8 for 12 h. In order to determine the mode of release, the data was subjected to zero order, first order, Higuchi and Korsmeyer-Peppas model. The mucoadhesive strength was evaluated by measuring the force required to detach the tablets from sheep buccal mucosal membrane. Carbopol 934P showed maximum mucoadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. DSC and XRD study of the pure drug indicated that the drug is in the crystalline form. But in the formulations, peaks indicated that the drug is in the amorphous form. FTIR spectroscopic studies indicated that there is no drug-excipient interaction. Conclusion: The prepared formulations showed good mucoadhesive strength and ability to sustain the drug release over 12 h; hence, these are the versatile drug delivery systems for repaglinide.
瑞格列奈黏附口腔片的处方及评价
目的:自20世纪80年代以来,作为黏附给药系统递送所需药物一直是人们感兴趣的主题。这些系统的各种优点使得口腔给药成为一种新的给药途径。颊区为全身给药提供了一个有吸引力的途径。本研究的目的是研制瑞格列奈黏附口腔片。方法:以壳聚糖、羟乙基纤维素、瓜尔胶、卡波波尔934P等黏附聚合物按不同比例组合,采用湿造粒法制备片剂。结果:采用不同方法对口腔片的厚度、硬度、重量均匀性、药物含量均匀性、表面pH、体外黏附强度、体外停留时间、体外药物释放、体外药物渗透等参数进行评价。采用零阶、一阶、Higuchi和korsmeier - peppas模型对其体外释放度进行分析,以确定其释放模式。通过测定片剂与绵羊口腔粘膜分离所需的力来评价粘接强度。Carbopol 934P黏附最大,需要最大的剥离力;分离所需的力与其内容成正比。对该纯药物的DSC和XRD研究表明,该药物为结晶形式。但在配方中,峰表示药物是无定形的。傅里叶红外光谱研究表明没有药物-赋形剂相互作用。结论:所制制剂具有良好的黏附强度和12 h的缓释能力;因此,这些是瑞格列奈的通用给药系统。
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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