Chowdary K P, Nalluri B N
Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.
Drug Dev Ind Pharm. 2000 Nov;26(11):1217-20. doi: 10.1081/ddc-100100995.
Complex formation of nimesulide (N) and beta-cyclodextrin (beta CD) in aqueous solution and in solid state and the possibility of improving the solubility and dissolution rate of nimesulide via complexation with beta CD were investigated. Phase solubility studies indicated the formation of a 1:1 complex in solution. The value of the apparent stability constant Kc was 158.98 M-1. Solid inclusion complexes of N and beta CD were prepared by kneading and coevaporation methods. Differential scanning calorimetry (DSC) studies indicated the formation of solid inclusion complexes of N-beta CD at a 1:2 molar ratio in both the methods. Solid complexes of N-beta D (1:1 and 1:2 M) exhibited higher rates of dissolution and dissolution efficiency values than the corresponding physical mixtures and pure drug. Higher dissolution rates were observed with kneaded complexes than with those prepared by coevaporation. Increases of 25.6- and 38.7-fold in the dissolution rate were observed, respectively, with N-beta CD 1:1 and 1:2 kneaded complexes.
研究了尼美舒利（N）与β-环糊精（β-CD）在水溶液和固态下的络合物形成情况，以及通过与β-CD络合提高尼美舒利溶解度和溶解速率的可能性。相溶解度研究表明溶液中形成了1:1的络合物。表观稳定常数Kc的值为158.98 M-1。通过捏合和共蒸发法制备了N与β-CD的固体包合物。差示扫描量热法（DSC）研究表明，两种方法中N-β-CD均以1:2的摩尔比形成固体包合物。N-β-D（1:1和1:2 M）的固体络合物比相应的物理混合物和纯药物表现出更高的溶解速率和溶解效率值。观察到捏合络合物的溶解速率高于共蒸发制备的络合物。N-β-CD 1:1和1:2捏合络合物的溶解速率分别提高了25.6倍和38.7倍。
