Prabhu Sunil, Kanthamneni Naveen, Ma Chan
College of Pharmacy, Western University of Health Sciences, Pomona, California 91766-1854, USA.
Drug Deliv. 2008 Feb;15(2):119-25. doi: 10.1080/10717540801905157.
Our objective was to investigate the controlled release and transport of leuprolide acetate polypeptide in the colon using novel combinations of rate-controlling polymers. Polymer swelling, disintegration, drug release, and transport characteristics were measured using different polymers, carbopol, chitosan and polyox, alone and in combination. Studies demonstrated Carbopol-containing combination formulations had maximum swelling and the slowest disintegration properties. A decrease in dissolution rate was observed from all combination formulations when compared with their individual counterparts. Carbopol combinations showed the slowest overall release. Drug transport studies using the everted sac technique demonstrated good correlation to the swelling, disintegration, and dissolution studies. Thus, novel polymer combinations can be used to deliver polypeptide drug to the colon effectively compared with individual polymers.
我们的目标是使用控速聚合物的新型组合来研究醋酸亮丙瑞林多肽在结肠中的控释和转运。使用不同的聚合物，即卡波姆、壳聚糖和聚氧乙烯，单独使用或组合使用，来测量聚合物的溶胀、崩解、药物释放和转运特性。研究表明，含卡波姆的组合制剂具有最大的溶胀度和最慢的崩解特性。与单独的制剂相比，所有组合制剂的溶解速率均有所降低。卡波姆组合显示出最慢的整体释放。使用外翻肠囊技术进行的药物转运研究表明，其与溶胀、崩解和溶解研究具有良好的相关性。因此，与单一聚合物相比，新型聚合物组合可有效地将多肽药物递送至结肠。
