- Norfloxacin과 ${eta}-Cyclodextrin$간의 Inclusion Complex에 관한 약제학적 연구
- ㆍ 저자명
- 지웅길,박목순,권중무,Jee. Ung-Kil,Park. Mork-Soon,Kwon. Joong-Moo
- ㆍ 간행물명
- 藥劑學會誌
- ㆍ 권/호정보
- 1987년|17권 1호|pp.1-14 (14 pages)
- ㆍ 발행정보
- 한국약제학회
- ㆍ 파일정보
- 정기간행물| PDF텍스트
- ㆍ 주제분야
- 기타
To increase the bioavailability of norfloxacin, inclusion complex of antimicrobial agent norfloxacin with ${eta}-Cyclodextrin$ was prepared and studied by the solubility method, spectrophotometric methods(UV, IR, $^1H-NMR$), differential thermal analysis, powder X-ray diffractometry, the physical properties, the antimicrobial activity, DNA binding and in situ recirculation technique. The conclusions are summerized as following; 1) The inclusion complexation was identified by means of solubility, spectrophotometry(UV, IR, NMR), DTA and X-ray diffraction. 2) The molar ratio of $norfloxacin-{eta}-cyclodextrin$ complex was 1 : 1. 3) The stability constant of $norfloxacin-{eta}-cyclodextrin$ complex was $21.5;M^{-1}$, and both true and apparent partition coefficients of the inclusion complex were larger than those of norfloxacin. 4) The time required to dissolve 60% $(T_{60}%)$ of the inclusion complex was 120 min. in distilled water and in the artificial intestinal juice, while norfloxacin did not reach to 60% dissolution within 120 min. 5) The antimicrobial activity of the inclusion complex against Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus showed no significant difference compared to that of norfloxacin alone. 6) Studies on binding properties between the inclusion complex and norfloxacin alone to DNA according to equilibrium dialysis showed no significant differency. 7) In situ absorption rates (Ka) of inclusion complex and norfloxacin alone were 0.229 and $0.102hr^{-1}$, respectively.