Benita S, Hoffman A, Donbrow M
J Pharm Pharmacol. 1985 Jun;37(6):391-5. doi: 10.1111/j.2042-7158.1985.tb03021.x.
Methacrylate copolymers were used for microencapsulation of paracetamol by phase separation from chloroform with polyisobutylene 6% in cyclohexane. With polyisobutylene as an anti-aggregating agent, high quality microcapsules were obtained. Drug release appeared to fit both first order and Higuchi matrix model kinetics. However, on application of the differential rate treatment, the evidence supported the first order description, which was further supported by computed simulations of the models. Variation of production conditions showed that increasing the proportion of core material raised the microcapsule drug content and the release rate. Reduction of core particle size correlated with reduced coating thickness and faster release rate. The rate constants correlated with the estimated surface areas and wall thicknesses of the various batches. The data were used to estimate an apparent permeability constant for paracetamol in Eudragit RS microcapsules, which was constant and comparable with values found single core, non-aggregated microcapsules containing other similar drugs and different wall materials.
甲基丙烯酸酯共聚物用于通过与6%聚异丁烯的环己烷溶液在氯仿中进行相分离来微囊化对乙酰氨基酚。以聚异丁烯作为抗聚集剂,获得了高质量的微胶囊。药物释放似乎符合一级动力学和Higuchi基质模型动力学。然而,应用微分速率处理时,证据支持一级描述,模型的计算模拟进一步支持了这一点。生产条件的变化表明,增加核心材料的比例会提高微胶囊药物含量和释放速率。核心粒径的减小与包衣厚度的减小和更快的释放速率相关。速率常数与各批次估计的表面积和壁厚相关。这些数据用于估计对乙酰氨基酚在Eudragit RS微胶囊中的表观渗透常数,该常数是恒定的,并且与含有其他类似药物和不同壁材的单核、非聚集微胶囊的值相当。