Journal of Pharmaceutical Investigation

  • 제34권4호
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  • Pages.269-274
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  • 2004
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  • 2093-5552(pISSN)
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  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
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2-HP-β-시클로덱스트린과 메글루민을 이용한 란소프라졸의 포접화합물 제조 및 평가

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)
  • 발행 : 2004.08.20
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초록

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 $40^{\circ}C$.

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