OPTIMASI FORMULA TABLET BUKAL MUKOADHESIVE GLIBENKLAMID MENGGUNAKAN MATRIKS CMC NA SERTA ASAM OLEAT SEBAGAI ENHANCHER

Asa Falahi, Dewi - Rashati
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Abstract

Glibenclamide is a sulfonylurea class of antidiabetic drugs that works by stimulating insulin secretion in the pancreas so that it is effective only when the β-cells of the pancreas can still produce. The glibenclamide dosage form that is on the market is a conventional oral tablet which has various disadvantages in terms of pharmacokinetics. Based on this, it is necessary to develop a more effective drug delivery system for glibenclamide in order to avoid first-pass metabolism so as to increase the bioavailability of glibenclamide, namely by making mucoadhesive buccal tablets. This glibenclamide mucoadhesive buccal tablet is formulated using a variety of mucoadhesive polymers, namely CMC Na and oleic acid as enhancers. The manufacture of four mucoadhesive buccal tablet formulas used the direct compression method. The results of the weight uniformity test showed that they did not meet the NP requirements specified, all formulas had an NP of more than 15. The tablet hardness test also showed results that did not meet the test requirements. However, the results of the physical properties of the brittleness, pH and swelling index showed the results that met the test requirements. In this research, the optimum variation of CMC Na polymer and oleic acid as enhancers to physical properties (hardness, brittleness, pH, swelling ability) and the release of glibenclamide mucoadhesive tablets were CMC Na of 37.5 mg and oleic acid of 3.5. ml.
格列本脲是一种磺脲类抗糖尿病药物,通过刺激胰腺胰岛素分泌起作用,因此只有当胰腺β细胞仍能产生胰岛素时才有效。市场上的格列苯脲剂型是一种传统的口服片剂在药代动力学方面有各种缺点。基于此,有必要开发一种更有效的格列本脲给药系统,以避免首过代谢,从而提高格列本脲的生物利用度,即制作黏附口腔片。这种格列本脲黏附含片采用多种黏附聚合物,即CMC Na和油酸作为增强剂配制而成。采用直接压缩法制备四种黏附含片配方。重量均匀性测试结果表明,它们不符合规定的NP要求,所有公式的NP都大于15。片剂硬度试验结果也不符合试验要求。但脆性、pH值、溶胀指数等物理性能的测试结果均满足试验要求。在本研究中,CMC Na聚合物和油酸对格列本脲黏合剂片的物理性能(硬度、脆性、pH值、溶胀能力)和释放量的最佳影响为CMC Na为37.5 mg,油酸为3.5 mg。毫升。
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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