天然树胶黏附格列齐特微胶囊的制备与表征

S. K. Mankala, Nishanth Kumar Nagamalli, Ramakrishna Raprla, Rajyalaxmi Kommula
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引用次数: 27

摘要

格列齐特是一种口服降糖药,用于治疗非胰岛素依赖型糖尿病。在患有长期疾病的人群中,主要被归类为糖尿病,因此需要一种能够提供高安全边际的持续治疗的剂型,这种剂型可以通过微胶囊化来实现。采用不同浓度(1:0.25、1:0.5、1:0.75、1:1)的孔口离子凝胶和乳化离子凝胶法制备了海藻酸钠(包被材料)、孔大胶、瓜尔胶和黄原胶(黏合剂)的格列齐特微球。然后评估配方的表面形态,颗粒形状,卡尔指数,微胶囊化效率,药物释放,黏附研究。通过FTIR、DSC和XRD技术进行了配伍性研究,发现药物与所用的异构物之间没有相互作用。采用乳液离子凝胶技术制备的微球粒径为400 ~ 600μm,呈球形且自由流动。含量为55% ~ 68%,包封率为86.23% ~ 94.46%。所有微球均表现出良好的粘接性能。体外药物释放研究表明,瓜尔胶与其他胶和浓度相比具有更大的延缓药物释放的潜力。药物从微球中缓慢释放,符合零级释放动力学,其释放机制取决于包芯比和所采用的方法。以SA: GG(肌电图4)1:1的浓度制备格列齐特控释制剂效果最好。关键词:格列齐特;自然牙龈;孔板离子凝胶技术;乳化离子凝胶技术DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011;38 - 48。4 (1)
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums
Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed. Key words : Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48
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