Quigley K J, Deasy P B
Department of Pharmaceutics, Trinity College, University of Dublin, Ireland.
J Microencapsul. 1992 Jan-Mar;9(1):1-7. doi: 10.3109/02652049209021217.
Deacetylated gellan gum (Gelrite) was used to produce a bead formulation containing sulphamethizole by a hot extrusion process into chilled ethylacetate. The spherical dried beads recovered had a porous surface which could be reduced in porosity by increasing the Gelrite concentration. Energy dispersive analysis showed the drug to be uniformly distributed throughout the beads. Dissolution studies confirmed that the drug was slowly released from the beads, the retardation of which could be extended by the use of increasing Gelrite concentration or by post-treatment of dried beads with either a waxy sealant or gamma irradiation. In-vivo studies in dogs confirmed that dried beads prepared by extruding a suspension of 10 per cent w/w sulphamethizole in 3 per cent aqueous Gelrite dispersion had effective sustained properties on oral dosing in comparison to a conventional capsule formulation but had a possible small loss in relative bioavailability.
通过热挤压工艺将脱乙酰基结冷胶(结冷胶)制成含有磺胺甲噻二唑的微丸制剂,该工艺是将其挤压到冷却的乙酸乙酯中。回收得到的球形干燥微丸具有多孔表面,通过增加结冷胶浓度可降低其孔隙率。能量色散分析表明药物均匀分布于整个微丸中。溶出度研究证实药物从微丸中缓慢释放,通过增加结冷胶浓度或用蜡质密封剂或γ射线对干燥微丸进行后处理可延长药物释放的延迟时间。犬体内研究证实,与传统胶囊制剂相比,将10%(w/w)磺胺甲噻二唑悬浮于3%结冷胶水溶液中经挤压制备的干燥微丸口服给药具有有效的缓释特性,但相对生物利用度可能略有损失。