오메프라졸과 베타-시클로덱스트린과의 포접화합물 형성에 따른 특성

• 영문명: Studies on the Formation of Inclusion Complex between Omeprazole and beta-cyclodextrin
• 발행기관: 대한약학회
• 저자명: 소재일(Jae Il So) 이창현(Chang Hyun Lee) 이계주(Gye Ju Rhee)
• 간행물 정보: 『약학회지』제35권 제5호 (1991년), 372~378쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1991.10.30

영문 초록

To increase the stability and bioavailability of Omeprazole(OMP), which is used newly as a proton-pump inhibitor, inclusion complex of OMP with beta-cyclodextrin(beta-CD) was prepared by coprecipitation method and its characteristics were ascertained by means of solubility test, DSC, IR, and the accelerated stability analysis. The type of OMP inclusion complex is classified as Bs-type on phase solubility diagram, and the stoichiometric ratio of OMP: P-CD complex is 1 : 2 and formation constant is 80.82/mole. The solubility of the complex could be increased remarkably by complexation compare with OMP. Degradation process of both OMP and OMP complex followed apparent first-order kinetics, of which degradation rate constants and activation energies are k25 = 8.1 X 10-4/day, Ea = 22 Kcal/mole (OMP), and k25 = 4.65 X 10-6/day, Ea = 35 Kcal/mole (complex), respectively. These results show the increase of the stability and solubility of OMP markedly, therefore it is believed that the improvement of stabilization for OMP by inclusion complexation might be practically available.

키워드

Omeprazole inclusion complex solubility diagram apparent first-order activation energy.