Raghunathan Y, Amsel L, Hinsvark O, Bryant W
J Pharm Sci. 1981 Apr;70(4):379-84. doi: 10.1002/jps.2600700409.
Ion-exchange resin-drug complexes have been used to formulate sustained-release products of acidic and basic drugs. However, sustained release may be difficult to achieve due to many variables. A novel technique is reported that minimizes these variables by providing a polymeric film coating to the ion-exchange resin-drug complex particles, making drug release from these particles diffusion controlled. Direct application of an atomized polymer solution to the fluidized ion-exchange resin-drug complex particles was ineffective in controlling drug release since the coating came off in the dissolution medium due to swelling and fracturing of the particles. Pretreatment of the ion-exchange resin-drug complex particles with an agent such as polyethylene glycol was essential for the particles to retain their geometry and coating during dissolution. With divinylbenzenesulfonic acid resin complexed with phenylpropanolamine as a model, mixtures of ethylcellulose-coated and uncoated resin-drug complex particles were prepared. These mixtures gave varying drug release profiles that showed rank-order correlation with plasma concentration profiles obtained in bioavailability studies with suspension dosage forms.
离子交换树脂 - 药物复合物已被用于制备酸性和碱性药物的缓释产品。然而，由于许多变量，可能难以实现持续释放。据报道，一种新技术通过为离子交换树脂 - 药物复合物颗粒提供聚合物薄膜包衣来最小化这些变量，使药物从这些颗粒中的释放受扩散控制。将雾化的聚合物溶液直接应用于流化的离子交换树脂 - 药物复合物颗粒在控制药物释放方面是无效的，因为由于颗粒的溶胀和破裂，包衣在溶解介质中脱落。用聚乙二醇等试剂对离子交换树脂 - 药物复合物颗粒进行预处理对于颗粒在溶解过程中保持其几何形状和包衣至关重要。以与苯丙醇胺复合的二乙烯基苯磺酸树脂为模型，制备了乙基纤维素包衣和未包衣的树脂 - 药物复合物颗粒的混合物。这些混合物呈现出不同的药物释放曲线，这些曲线与用混悬剂型进行生物利用度研究时获得的血浆浓度曲线呈等级相关性。
