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Development and evaluation of buccoadhesive patches of Glipizide usingpolymer blend of Ethylcellulose and Polyvinylpyrrolidone K-30

机译:使用乙基纤维素和聚乙烯吡咯烷酮K-30的聚合物共混物开发和评估格列吡嗪的颊黏膜贴剂

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In the present study, an attempts were made to formulate buccal patches of glipizide using bioadhesive polymers to avoid the hepatic first pass metabolism, to achieve controlled release and to improve better clinical efficacy. Buccal patches of glipizide were designed using ethylcellulose (EC) alone and blends of EC:Polyvinylpyrrolidone (PVP K- 30) at different ratios using glycerol as plasticizer adopting solvent evaporation method. All patches were evaluated for physical appearance, surface texture, weight uniformity, thickness uniformity, folding endurance, surface pH, swelling index, moisture content and absorption, bioadhesive strength, drug content uniformity. Various bioadhesive parameters like bioadhesive strength, force of adhesion, and bond strength exhibited by various patches of glipizide was satisfactory. All buccal patches of glipizide showed sustained and prolonged release the drug over a period of 8 h. When the patches were prepared with the blends of EC:PVP the flux and permeation rates were increased compared to patches prepared with EC alone. The increasing order of drug release from the EC:PVP patches was found in the order, A4 A3 A2 A1 (i.e., 1:1 1:0.75 1:0.5 1:0.25). Further, increase in concentration of EC has a negative effect on drug release i.e., drug release decreased with increase in concentrations of EC. The release of glipizide from all patches followed Higuchi kinetic model and the mechanism of drug release was concluded as non–Fickian diffusion controlled.
机译:在本研究中,尝试使用生物粘附性聚合物配制格列吡嗪的口腔贴剂,以避免肝首过代谢,实现控释并改善更好的临床疗效。格列吡嗪的颊部贴剂仅使用乙基纤维素(EC)设计,并使用甘油作为增塑剂,采用溶剂蒸发法,将不同比例的EC:聚乙烯吡咯烷酮(PVP K-30)共混物设计。评价所有贴剂的物理外观,表面质地,重量均匀性,厚度均匀性,耐折性,表面pH,溶胀指数,水分含量和吸收率,生物粘附强度,药物含量均匀性。由格列吡嗪的各种斑块表现出的各种生物粘附性参数如生物粘附强度,粘附力和结合强度是令人满意的。格列吡嗪的所有颊部贴剂均在8小时内显示出该药物的持续和延长释放。当用EC:PVP的混合物制备贴剂时,与单独使用EC制备的贴剂相比,通量和渗透率增加了。从EC:PVP贴剂释放的药物的增加顺序为A4> A3> A2> A1(即1:1> 1:0.75> 1:0.5> 1:0.25)。此外,EC浓度的增加对药物释放具有负面影响,即,药物释放随着EC浓度的增加而降低。格列吡嗪从所有贴剂中的释放均遵循Higuchi动力学模型,并且药物释放的机理被归结为非费克扩散控制。

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