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http://dx.doi.org/10.4333/KPS.2004.34.4.269

Preparation and Evaluation of Inclusion Complex of Lansoprazole with 2-HP-β-Cyclodextrin and Meglumine  

Lee, Jung-Woo (College of Pharmacy, Chungnam National University)
Kim, Jung-Su (College of Pharmacy, Chungnam National University)
Chang, Hye-Jin (College of Pharmacy, Chungnam National University)
Lee, Gye-Won (Dept. of Pharmaceutical Engineering, Konyang University)
Jee, Ung-Kil (College of Pharmacy, Chungnam National University)
Publication Information
Journal of Pharmaceutical Investigation / v.34, no.4, 2004 , pp. 269-274 More about this Journal
Abstract
To enhance the solubility and stability of lansoprazole (LAN), new proton pump inhibitor, we were prepared various molar ratio of inclusion complex with $2-hydroxypropyl-{\beta}-cyclodextrin$ (HPCD) and organic alkali agent, meglumine (MEG). Inclusion complex formation of LAN with HPCD was investigated by Differential Scanning Calorimetry and X-ray diffractometry. The aqueous solubilities of inclusion complexes, and the stabilities of 1:4 and 1:5 inclusion complexes in aqueous solutions containing different concentrations of MEG were examined. The stability of 1:5 LAN-HPCD inclusion complex containing MEG, which was equaled to amount of LAN, was performed in 0.9% NaCl and 5% dextrose solution. The formation of inclusion complex of LAN with HPCD was $A_L$ type and the molar ratio of complex was 1:1. The stability constant was $41.557\;M^{-1}$. As molar ratio of LAN to HPCD was increased, solubility of inclusion complex was increased. 1:5 LAN-HPCD inclusion complex was more stable than 1:4 LAN-HPCD inclusion complex. And as contained MEG amount in LAN solution was increased, stability of 1:4 and 1:5 LAN-HPCD inclusion complexes was improved. Also stability of 1:5 LAN-HPCD-MEG inclusion complex in 0.9% NaCl solution and 5% dextrose solution was similar to it in water at room temperature, but it was unstable at $40^{\circ}C$.
Keywords
Lasoprazole; $Hydroxypropyl-{\beta}-cyclodextrin$; Inclusion complex; Meglumine; Solubility; Stability;
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