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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Sustained release of propranolol hydrochloride based on ion-exchange resin entrapped within polystyrene microcapsules
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Sustained release of propranolol hydrochloride based on ion-exchange resin entrapped within polystyrene microcapsules

机译：基于包裹在聚苯乙烯微胶囊中的离子交换树脂的盐酸普萘洛尔的持续释放

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Propranolol-HCl,a water soluble drug,was bound to Indion 254~R,a cation exchange resin,and the resulting resinate was microencapsulated with polystyrene using an oil-in-water emulsion-solvent evaporation method with a view to achieve prolonged drug release in simulated gastric and intestinal fluid.The effect of various formulation parameters on the characteristics of the microcapsules was studied.The diameter of the resinate-loaded polystyrene microcapsules increased with increase in the concentration of emulsion stabilizer and coat/core ratio and decreased with increase in the volume of organic disperse phase.The variation in the size of the microcapsules appeared to be related with the inter-facial viscosity which was influenced by the viscosity of both the aqueous dispersion medium and the organic disperse phase.The resinate encapsulation efficiency and hence the drug entrapment efficiency of the microcapsules increased with increase in the concentration of emulsion stabilizer and coat/core ratio and decreased with increase in the volume of organic disperse phase.These characteristics were found to depend on the extent of formation of fractured microcapsules and subsequent partitioning of the resinate into the aqueous dispersion medium.The degree of fracture on the microcapsules depended on the viscosity of the aqueous dispersion medium and the organic disperse phase.The uncoated resinate discharged the drug quite rapidly following the typical particle diffusion process.Although the desorption of the drug from the resinate was independent of pH of the dissolution media,increase in ionic strength increased the drug desorption.On the other hand,release of drug from the coated resinate was considerably prolonged and followed a diffusion controlled model.The prolongation of drug release was dependent on the uniformity of coating which was influenced by the formulation parameters.The drug release from the microcapsules was also found to be independent of pH of the dissolution media and increased with increase in ionic strength.The pH-independent release of the drug from both the uncoated and microencapsulated resinate was due to pH-independent solubility of the drug and high equilibrium concentration of the resinate in both the dissolution media.Polystyrene appeared to be a suitable polymer to provide prolonged release of propranolol independent of pH of the dissolution media.
机译：将水溶性药物普萘洛尔-HCl与阳离子交换树脂Indion 254〜R结合，并使用水包油型乳液-溶剂蒸发法将所得的树脂酸酯与聚苯乙烯微囊化，以延长药物释放时间研究了各种配方参数对微胶囊特性的影响。载有树脂酸酯的聚苯乙烯微胶囊的直径随乳液稳定剂浓度和包衣/芯比的增加而增加，而随乳化稳定剂浓度的增加而减小。微胶囊尺寸的变化似乎与界面粘度有关，界面粘度受水性分散介质和有机分散相的粘度的影响。微胶囊的药物截留效率随着乳液稳定剂和c的浓度增加而增加燕麦/核比随着有机分散相体积的增加而降低，这些特性取决于破裂的微胶囊的形成程度以及随后树脂酸酯分配到水性分散介质中的程度。在典型的颗粒扩散过程中，未包衣的树脂酸酯会很快释放出药物。尽管药物从树脂酸酯中的解吸与溶解介质的pH无关，但离子型离子的增加强度增加了药物的解吸;另一方面，药物从包衣的树脂酸酯的释放大大延长并遵循扩散控制模型。药物释放的延长取决于包衣的均匀性，该均匀性受配方参数的影响。还发现微胶囊的释放与dis的pH无关药物从未包被的和微囊包封的树脂酸酯中释放出来的pH值无关，这是由于药物的pH依赖性不溶性以及两种溶解介质中树脂盐的平衡浓度高引起的。成为适合的聚合物，可独立于溶出介质的pH值而提供心得安的延长释放。

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