이부프로펜의 피페라진 유도체에 대한 약리활성연구

• 영문명: Studies of Pharmacological Activity on the Piperazine Derivatives of Ibuprofen
• 발행기관: 대한약학회
• 저자명: 조한진(Han Jin Jo) 나성범(Sung Bum La) 남상철(Sang Cheol Nam) 박목순(Mork Soon Park) 지웅길(Ung Kil Jee)
• 간행물 정보: 『약학회지』제34권 제2호 (1990년), 126~132쪽, 전체 7쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1990.04.28

영문 초록

To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, lbu-P.A., and lbu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The LD50 was 495mg/kg for ibuprofen, 187mg/kg for Ibu-M.P., and over 1250mg/kg for Ibu-P.A.. 6) The absorption rate constants(k) and half-life(t1/2) were 0.74(hr-1) and 0.94(hr) for ibuprofen, and 0.72 (hr-1) and 0.96 (hr) respectively for Ibu-M.P..

키워드

Ibuprofen piperazine anhydrous 1-methylpiperazine lipid: water partition coefficient pka value antiinflammatory effect analgesic effect LD50 intestinal absorption