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Development of metformin hydrochloride sustained release pellets

机译：盐酸二甲双胍持续释放颗粒的发展

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This study was performed in order to develop a sustained-release pellet formulation containing metformin hydrochloride (MET), an extremely water-soluble drug, prepared by combination of wax matrices and double layer coatings. The influence of both double layer polymeric coats and wax matrices on the release of MET from sustained-release pellets was investigated. The pellets were prepared by wet-mass extrusion-spheronization methods and then coated with a fluidized bed coater. For the pellets coated with Eudragit NE30D alone, a coating level of nearly 30% was required to pass the dissolutiontest compared with commercial product, and it was accompanied by an unacceptable lag time. The application of an alcohol-soluble polymeric subcoat, Opadry I, was added before the Eudragit NE30D coating process, which resulted in a marked delay in drug release. However, a faster release was observed for the formulation coated with a high subcoat level 8%) at the end of the dissolution test. A further delay in drug release was observed when a wax matrix, octadecanol, was added to the core pellet formulation. The kinetics of drug release changed from the Higuchi model to a zero order model and the predominant mechanism controlling drug release changed from diffusion to dissolution on increasing the amount of octadecanol within the matrix pellets. In addition, the drug release was markedly influenced by the drug to matrix ratio. In conclusion, the 70% drug-loaded core pellets with double layer coatings (6% Opadry I and 9% Eudragit NE30D) and 20% octadecanol matrix, produced the desired profile for sustained release compared with the commercial product and these pellets remained stable during storage.
机译：进行该研究以开发含有盐酸二甲双胍（Met）的缓释颗粒制剂，通过蜡基质和双层涂层组合制备的极其水溶性药物。研究了双层聚合物涂层和蜡质基质对来自缓释颗粒的筛选释放的影响。通过湿式挤出 - 球形方法制备粒料，然后用流化床涂布机涂覆。对于单独使用Eudragit Ne30d的颗粒，与商业产品相比，需要近30％的涂层水平，并伴随着不可接受的滞后时间。在Eudragit NE30D涂覆方法之前加入醇溶溶解的聚合物子涂层，OPADRY IMAD，导致药物释放的显着延迟。然而，在溶解试验结束时，在涂覆具有高亚涂层9％的制剂的制剂释放更快的释放。当向核心颗粒制剂中加入蜡基质时，观察到药物释放的进一步延迟。药物释放的动力学从HIGUCHI模型改变为零阶模型，控制药物释放的主要机制从扩散改变以溶解对基质粒料内的十八碳醇量的溶解。此外，药物释放明显受药物对基质比的影响。总之，通过双层涂层（6％OPADRY I和9％EUDRAGIT NE30D）和20％十八烷醇基质的70％的药物负载芯颗粒，与商业产品相比，为持续释放的持续释放产生了所需的曲线，并且这些颗粒保持稳定贮存。

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