Efentakis M, Vlachou M
University of Athens, School of Pharmacy, Department of Pharmaceutical Technology, Greece.
Pharm Dev Technol. 2000;5(3):339-46. doi: 10.1081/pdt-100100549.
The powder characteristics and the effect of the molecular weight of polymers as diluents on the release rate of furosemide and captopril from hard gelatin capsules were evaluated. The high molecular weight polymers studied were poly(oxyethylene) homopolymers (Polyox), with molecular weight ranging from 4,000,000 to 7,000,000. Powder characteristics suggested good flowability for these materials and predicted capsule fill weight uniformity. Swelling experiments showed a very high degree of swelling for these materials in both gastric and buffer solution. These polymers can sustain the release rate of both water-soluble and insoluble drugs from drug delivery systems. The low molecular weight polymers have a less pronounced sustained-release effect compared to the high molecular weight polymer material (i.e., those with 7,000,000 molecular weight). An increase in the content of polymer results in a decrease in the release rate of the drug. The solubility of the drugs clearly influenced the release rate. Release kinetics were evaluated and appeared to be influenced by the molecular weight of the polymer, the solubility of drug, and the ratio of the drug to polymer in the capsule. Bimodal release kinetics were exhibited by a number of furosemide formulations (i.e., F5 and F8).
评估了聚合物作为稀释剂的粉末特性以及聚合物分子量对速尿和卡托普利从硬明胶胶囊中释放速率的影响。所研究的高分子量聚合物是聚(氧乙烯)均聚物(聚氧乙烯),分子量范围为4,000,000至7,000,000。粉末特性表明这些材料具有良好的流动性,并预测了胶囊填充重量的均匀性。溶胀实验表明这些材料在胃液和缓冲溶液中都有很高的溶胀度。这些聚合物可以维持药物递送系统中水溶性和不溶性药物的释放速率。与高分子量聚合物材料(即分子量为7,000,000的材料)相比,低分子量聚合物的缓释效果不太明显。聚合物含量的增加导致药物释放速率的降低。药物的溶解度明显影响释放速率。评估了释放动力学,其似乎受聚合物的分子量、药物的溶解度以及胶囊中药物与聚合物的比例影响。许多速尿制剂(即F5和F8)呈现出双峰释放动力学。