Enhanced Dissolution and Stability of Lansoprazole by Cyclodextrin Inclusion Complexation: Preparation, Characterization, and Molecular Modeling

被引:28
|
作者
Lu, Yi [1 ,2 ]
Guo, Tao [3 ]
Qi, Jianping [1 ,2 ]
Zhang, Jiwen [3 ,4 ]
Wu, Wei [1 ,2 ]
机构
[1] Fudan Univ, Sch Pharm, Key Lab Smart Drug Delivery, Minist Educ, Shanghai 201203, Peoples R China
[2] Fudan Univ, PLA, Shanghai 201203, Peoples R China
[3] Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Delivery Syst, State Key Lab Drug Res, Shanghai 201203, Peoples R China
[4] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
来源
AAPS PHARMSCITECH | 2012年 / 13卷 / 04期
关键词
cyclodextrin; dissolution; inclusion complex; lansoprazole; molecular modeling; stability; BED COATING TECHNIQUE; BETA-CYCLODEXTRIN; PHARMACEUTICAL APPLICATIONS; PHASE SOLUBILITY; SOLID-STATE; IN-VITRO; OMEPRAZOLE; PHARMACOKINETICS; METHODOLOGY; EFFICACY;
D O I
10.1208/s12249-012-9842-z
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In this study, lansoprazole (LSP)/cyclodextrin (CD) inclusion complexes were prepared using a fluid bed coating technique, with beta-cyclodextrin (beta-CD) and 2-hydroxypropyl-beta-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/beta-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 HPCDthan beta-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.
引用
收藏
页码:1222 / 1229
页数:8
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