- Pranoprofen Argininate 및 Pranoprofen Lysinate의 약제학적 연구
- ㆍ 저자명
- 지웅길,Jee. Ung-Kil
- ㆍ 간행물명
- 藥劑學會誌
- ㆍ 권/호정보
- 1987년|17권 4호|pp.197-204 (8 pages)
- ㆍ 발행정보
- 한국약제학회
- ㆍ 파일정보
- 정기간행물| PDF텍스트
- ㆍ 주제분야
- 기타
Novel pranoprofen algininate and lysinate salts were manufactured and their salt formation was confirmed by melting point, infrared spectroscopy, nuclear magnetic resornance spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. The physical properties of pranoprofen lysinate and argininate salts were compared with those of pranoprofen through in vitro and in vivo tests. Solubility, $pK_a$ and lipid-water partition coefficient were measured through in vitro experiments, while antiinflammatory efficacy, analgesic effect, acute toxicity and in situ absorption were tested through in vivo experiments. The results obtained were as follows: 1) The solubilities of pranoprofen argininate and lysinate salts were increased markedly in pH 6.8 and pH 7.5 phosphate buffer solutions, comparing with that of pranoprofen itself. 2) $pK_a$ values of pranoprofen, pranoprofen argininate and lysinate salts were 6.34, 7.99 and 7.56 in carbon tetrachloride, and 5.86, 6.69 and 7.92 in chloroform, respectively by liquid-liquid partition method. 3) The lipid-water partition coefficients of pranoprofen argininate and lysinate salts were increased more than that of pranoprofen in carbon tetrachloride, chloroform, or benzene-pH 6.8 buffer system, but were nearly identical using pH 1.2 buffer as water phase. 4) Antiinflammatory effects of pranoprofen argininate and lysinate salts were remarkably increased and analgesic effects of the salts were as same as that of pranoprofen. 5) Pranoprofen argininate and lysinate salts were safer than pranoprofen itself in acute toxicity, and the in situ absorption rates of pranoprofen, pranoprofen argininate and lysinate salts were 0.392, 0.960 and $0.762;hr^{-1}$, respectively according to the rat intestine recirculation experiment.