School of Pharmacy, Key Laboratory of Smart Drug Delivery of Ministry of Education and PLA, Fudan University, Shanghai, 201203, China.
AAPS PharmSciTech. 2012 Dec;13(4):1222-9. doi: 10.1208/s12249-012-9842-z. Epub 2012 Sep 12.
In this study, lansoprazole (LSP)/cyclodextrin (CD) inclusion complexes were prepared using a fluid bed coating technique, with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HPCD) as the host molecules, respectively, to simultaneously improve the dissolution and stability of LSP. The dissolution rate and stability of LSP was dramatically enhanced by inclusion complexation regardless of CD type. LSP/HPCD inclusion complex was more stable under illumination than LSP/β-CD inclusion complex. Differential scanning calorimetry and powder X-ray diffractometry proved the absence of crystallinity in both LSP/CD inclusion complexes. Fourier transform infrared spectroscopy together with molecular modeling indicated that the benzimidazole of LSP was included in the cavity of both CDs, while LSP was more deeply included in HPCD than β-CD. The enhanced photostability was due to the inclusion of the sulfinyl moiety into the HPCD cavity. CD inclusion complexation could improve the dissolution and stability of LSP.
在这项研究中，采用流化床包衣技术制备了兰索拉唑（LSP）/环糊精（CD）包合物，分别以β-环糊精（β-CD）和 2-羟丙基-β-环糊精（HPCD）为主体分子，以同时提高 LSP 的溶解和稳定性。无论 CD 类型如何，包合作用都能显著提高 LSP 的溶解速率和稳定性。与 LSP/β-CD 包合物相比，LSP/HPCD 包合物在光照下更稳定。差示扫描量热法和粉末 X 射线衍射法证明了两种 LSP/CD 包合物均无结晶度。傅里叶变换红外光谱和分子建模表明，LSP 的苯并咪唑部分被包含在两种 CD 的腔中，而 LSP 被 HPCD 包合的程度比β-CD 更深。光稳定性的提高是由于亚砜部分被包含在 HPCD 腔中。CD 包合作用可以提高 LSP 的溶解和稳定性。
