局部给药甲硝唑缓释的detarium油基有机凝胶的制备及评价

M. Ilomuanya, U. Ubani-Ukoma, A. Sowemimo, Gbemisola W. Akande, Pal Kunal
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引用次数: 1

摘要

这项研究的基本原理是通过配制一种有机凝胶,用茴香油代替药物配方中使用的传统油,如液体石蜡,来增加模型药物甲硝唑的吸收。以甲硝唑为模型药物,采用充液机制制备了有机凝胶。将药物-表面活性剂混合物溶解在油中,然后加入水,形成特定组成的有机凝胶。采用显微镜、流变学、体外释药和x射线衍射(XRD)对制剂进行分析。显微镜下的研究表明,凝胶中含有充满水的球形结构簇。FTIR研究表明,有机凝胶的组分具有相容性。DSC结果表明,所有有机凝胶在形成过程中都释放热量。有机凝胶的黏度表现为先弹性流动后非弹性流动。10 h时甲硝唑的累积释放率在63% ~ 85%之间,其中ogm9的释放率最高。XRD结果表明该有机凝胶具有结晶性。甲硝唑在有机凝胶中的释放表现为溶解、形状、大小和表面积依赖性释放。结果表明,各辅料的配伍性良好。以茴香油为原料成功制备了甲硝唑缓释有机凝胶。
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Formulation and evaluation of detarium oil based organogel for sustained release of metronidazole via topical delivery
The rationale for this study was to increase the absorption of model drug metronidazole by formulating an organogel using detarium oil in place of conventional oils used in drug formulation such as liquid paraffin. The organogels were prepared by fluid-filled mechanism using metronidazole as the model drug. The drug-surfactant mixtures were dissolved in oil followed by the addition of water which led to the formation of organogels at specific compositions. The formulations were analyzed by microscopy, rheology, in vitro drug release and X-ray diffraction (XRD). Microscopic studies revealed the gels contained clusters of water-filled spherical structures. FTIR study showed compatibility of components of the organogels. DSC result showed all the organogels released heat during formation. The viscosity of the organogels showed an elastic flow followed by a non-elastic phase. The cumulative percentage release of metronidazole was found to be between 63% and 85% at the end of 10 h, with OGM 9 having the highest release. XRD result indicated the crystalline nature of the organogels. Metronidazole release from the organogels indicated dissolution, shape, size, and surface area dependent release. The results also showed good compatibility of all the excipients. Sustained release metronidazole organogel was successfully developed using detarium oil.
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