用球形结晶技术改善甲苯磺丁脲的溶出速率

Improvement of dissolution rate of tolbutamide by the spherical crystallization technique

用球形结晶技术将难溶性药物甲苯磺丁脲在羧甲基纤维素钠(CMC—Na)的溶液中制成球形结晶聚集体(简称球晶)。用扫描电镜法观察到原药结晶为棱状结晶,而球形结晶为小片状及小梭状结晶的聚集体。用粉末X线衍射谱检测了球晶与原晶,发现衍射峰有不同之处,说明有部分晶型发生改变。其球晶的溶解过程由Hixson—Crowll方程式描述,溶解比原药快。

Poorly soluble crystals of tolbutamide were modified in the presence of a sodi-um carboxymethyl cellulose by the spherical crystallization technique. The objec-tive is to improve the dissolution rate and to transform platelet crystals into sp-herical agglomerates.The dissolution process was described in terms of the Hixson-Crowell equation. The dissolution rate of the agglomerate was faster than that ofconventionally crystallized tolbutamide. Therefore, the solubility and flowabilityof tolbutamide can be improved in using the spherical crystallization technique.