Acartürk F, Imai T, Saito H, Ishikawa M, Otagiri M
Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Etiler, Ankara, Turkey.
J Pharm Pharmacol. 1993 Dec;45(12):1028-32. doi: 10.1111/j.2042-7158.1993.tb07174.x.
The complexation of fucosterol with three kinds of beta-cyclodextrin (beta-CyD) was investigated in aqueous solution and in the solid state. The solubility of fucosterol increased significantly on its complexation with maltosyl-beta-CyD and heptakis(2,6-di-O-methyl)-beta-CyD (DM-beta-CyD), while no appreciable increase was observed when complexed with beta-CyD. The stability constant of complexation with beta-CyD estimated from solubility determinations was greater for a 1:2 complex than for a 1:1 complex. On the other hand, 1:1 complexation of fucosterol with maltosyl-beta-CyD or DM-beta-CyD was greater than 1:2 complexation. The solid complexes were obtained in molar ratios of 1:2 and 1:3 for beta-CyD and maltosyl-beta-CyD complexes, respectively. The inclusion behaviour of fucosterol with maltosyl-beta-CyD was compared with beta-CyD in the solid state using DSC, powder X-ray diffractometry and CP/MAS 13C NMR. Maltosyl-beta-CyD showed different inclusion behaviour compared with beta-CyD, and produced an amorphous structure of fucosterol on complex formation. The dissolution rate of fucosterol-maltosyl-beta-CyD complex was significantly faster than other complexes due to its high aqueous solubility and amorphous structure.
在水溶液和固态条件下研究了岩藻甾醇与三种β-环糊精（β-CyD）的络合作用。岩藻甾醇与麦芽糊精-β-CyD和七（2,6-二-O-甲基）-β-CyD（DM-β-CyD）络合时，其溶解度显著增加，而与β-CyD络合时未观察到明显增加。根据溶解度测定估算，岩藻甾醇与β-CyD的1:2络合物的络合稳定常数大于1:1络合物。另一方面，岩藻甾醇与麦芽糊精-β-CyD或DM-β-CyD的1:1络合作用大于1:2络合作用。分别以1:2和1:3的摩尔比得到了β-CyD和麦芽糊精-β-CyD络合物的固体络合物。采用差示扫描量热法（DSC）、粉末X射线衍射法和交叉极化/魔角旋转13C核磁共振法（CP/MAS 13C NMR），比较了岩藻甾醇与麦芽糊精-β-CyD在固态下与β-CyD的包合行为。麦芽糊精-β-CyD与β-CyD相比表现出不同的包合行为，在形成络合物时产生了岩藻甾醇的无定形结构。由于其高水溶性和无定形结构，岩藻甾醇-麦芽糊精-β-CyD络合物的溶解速率明显快于其他络合物。
