Orugun Oluwaseun, Oyi Avosuahi, Olowosulu Adeniji, Apeji Yonni, Olayemi Olubunmi
Ceska Slov Farm. 2016 Winter;65(6):226-231.
The purpose of this study was to extend the release of theophylline using Eudragit® RS 100 and Eudragit® RSPO as carriers. Solid dispersions of theophylline were prepared by the solvent evaporation technique using Eudragit® RS 100, Eudragit® RSPO and their blend in various drug : polymer ratios. The prepared solid dispersions were characterized with respect to entrapment efficiency, solubility and recovery yield. In vitro drug release of theophylline from the solid dispersions was evaluated in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) without enzymes. Solubility studies demonstrated a decrease in the solubility of the drug from the solid dispersions. The solubilities of pure drug and solid dispersions were lowered in SGF compared to SIF. Solid dispersions prepared with Eudragit® RS 100 entrapped a greater amount of theophylline in comparison to those with Eudragit® RSPO or the polymer blends and were able to extend the release of theophylline over 24 hrs. Formulation SD4 released 95.52% of the drug in SIF and 93.56% in SGF. Hence, it was selected as the optimized formulation because it was able to extend the release of theophylline over 24 hrs.Key words: solid dispersion extended release Eudragit® drug release.
本研究的目的是使用尤特奇®RS 100和尤特奇®RSPO作为载体来延长茶碱的释放。采用溶剂蒸发技术，以不同的药物:聚合物比例，使用尤特奇®RS 100、尤特奇®RSPO及其混合物制备了茶碱固体分散体。对所制备的固体分散体进行了包封率、溶解度和回收率的表征。在无酶的模拟胃液（SGF）和模拟肠液（SIF）中对茶碱从固体分散体中的体外药物释放进行了评估。溶解度研究表明，药物从固体分散体中的溶解度有所降低。与SIF相比，纯药物和固体分散体在SGF中的溶解度较低。与使用尤特奇®RSPO或聚合物混合物制备的固体分散体相比，用尤特奇®RS 100制备的固体分散体包封了更多的茶碱，并且能够在24小时内延长茶碱的释放。制剂SD4在SIF中释放了95.52%的药物，在SGF中释放了93.56%。因此，它被选为优化制剂，因为它能够在24小时内延长茶碱的释放。关键词：固体分散体；缓释；尤特奇®；药物释放
