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Formulation and Evaluation of Mucoadhesive Buccal Tablets of Repaglinide

机译:瑞格列奈粘膜粘膜颊片的制备与评价

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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.
机译:目的:自1980年代以来,作为粘膜粘附药物递送系统的所需药物的递送一直是人们关注的主题。与这些系统相关的各种优点使颊部药物递送成为药物施用的新途径。颊部区域为全身药物输送的管理提供了一条有吸引力的途径。该研究的目的是开发瑞格列奈的粘膜粘膜口腔片剂。方法:通过湿法制粒,使用不同比例的壳聚糖,羟乙基纤维素,瓜尔豆胶和卡波普934P等粘膜粘附性聚合物组合制备片剂。结果:通过不同方法评估颊片的参数,例如厚度,硬度,重量均匀性,药物含量均匀性,表面pH,离体粘膜粘附强度,离体停留时间,离体药物释放,离体药物渗透。评价片剂在pH 6.8的磷酸盐缓冲液中体外释放12小时。为了确定释放方式,对数据进行了零阶,一阶,Higuchi和Korsmeyer-Peppas模型的处理。通过测量将片剂从绵羊颊粘膜上分离所需的力来评估粘膜粘附强度。 Carbopol 934P表现出最大的粘膜粘附力和最大的分离力。拆卸所需的力与其含量成正比。纯药物的DSC和XRD研究表明该药物为结晶形式。但是在制剂中,峰表明该药物为无定形形式。 FTIR光谱研究表明没有药物-赋形剂相互作用。结论:所制备的制剂显示出良好的粘膜粘附强度和能够在12 h内维持药物释放的能力,因此,它们是瑞格列奈的通用药物递送系统。

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