대한약학회:학술대회논문집 (Proceedings of the PSK Conference) (Proceedings of the PSK Conference)
대한약학회 (The Pharmaceutical Society of Korea)
- 기타
과학기술표준분류
- 보건의료 > 의약품/의약품개발
대한약학회 2000년도 춘계총회 및 학술대회
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DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag
$\varepsilon$ nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$ ), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$ as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$ st. Pharmacokinetics of DA-50 18 were studied after topical application of${14}^C$ -Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$ r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in -
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Joo, Chang-Hun;Kim, Mi-Hee;Cho, Mi-Young;Kwon, Tae-Hyuk;Lee, Kwang-Moon;Lee, Tae-Ho;Lee, Bok-Luel 95.1
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Choi, Y.M.;Jeong, J.H.;Choi, S.U.;Min, Y.S.;Choi, K.B.;La, H.O.;Kim, J.H.;Huh, I.H.;Sohn, U.D. 105.1
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Choi, K.H.;Ahn, M.R.;Yoo, T.M.;Park, H.J.;Chung, M.W.;Y, ChungS.Y.;Son, D.H.;Kim, Y.C.;Rheu, H.M. 109.1
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Kim, S.S.;Park, K.H.;Yoo, T.M.;Sohn, S.J.;Park, I.S.;Suh, S.K.;Yi, S.W.;Ahn, M.R.;Dong, M.S. 113.1
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Yang, H.J.;Cho, D.I.;Kuo, N.Y.;Chung, W.J.;Ryu, H.;Choi, H.S.;Ryu, S.Y.;Im, S.Y.;Kim, K.M. 113.2
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Ko, K.H.;Lee, W.J.;Shin, C.Y.;Rhu, J.R;Yoo, B.K.;Park, K.H.;Choi, J.W.;Jang, E.S.;Min, H.W. 114.2
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Jung, H.K.;Park, M.S.;Lee, J.J.;Park, H.S.;Kim, J.W.;Eom, M.O.;Han, E.S.;Jeong, S.H.;Oh, H.Y. 127.1
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Kim, H.J.;Hong, J.T.;Nam, K.T.;Park, K.S.;Ryu, S.R.;Lee, J.K.;Ahn, K.S.;Kim, J.H.;Cho, D.H. 129.3
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Kang, Chan-Sun;Park, Bo-Kyung;Park, Seung-Hee;Park, Sang-Aeh;Park, Myoeng-Sin;Kang, Myoeng-Hee;Hong, Chong-Hee;Kim, Sung-Il;Han, Sang-Bum;Jang, Seung-Jae 136.2
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Kim, Young-Ock;Park, Ju-Young;Joe, Kum-Ho;Lee, Kang-Hyun;Suk, Kyoung-Ho;Kim, Sun-Yeou;Kim, Ho-Cheol 141.2
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Kwak, J.;Hwang, S.W.;Jung, J.;Cho, H.W.;Shin, J.E.;Shon, J.M.;Oh, Y.K.;Hong, Y.M.;Lee, S.Y. 142.2
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Park, J.H.;Chung, H.J.;Kim, J.H.;Chung, S.T.;Kim, J.H.;Cho, E.D.;Kim, Y.O.;Kim, H.S.;Kim, D.S. 143.2
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Soo, Chun-Kyung;Sam, Keum-Young;Su, Han-Seong;Joung, Seo-Hyo;Lee, Jee-Woo;Joon, Surh-Young 150.1
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Yoon, J.W.;Ahn, S.H.;Shin, S.K.;Hong, S.Y.;Lee, H.Y.;Zee, O.P.;Lee, K.R.;Han, J.W.;Lee, H.W. 150.2
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Jew, S.S.;Yoo, C.H.;Kim, H.M.;Mook-Jung, I.H.;Jung, M.W.;Park, H.S.;Jung, Y.H.;Kim, H.D.;Park, H.G. 160.2
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Park, Yong-Kyu;Baek, Nam-Joon;Lee, Sook-Ja;Lee, Jae-Yeol;Yang, Beom-Seok;Park, Ho-Koom;Lee, Yong-Sup 162.1
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Koo, Kang-Yong;Jung, Shin-Kye;Ho, Yoo-Kyung;Kim, Dong-Chan;Jae, Seo-Kyung;Lee, Kyung-Seok;Park, Ran-Hee;Kim, Dong-Jin;Park, Sang-Woo 167.3
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Jin Cheng Hua;Lee, M.J.;Kang, H.O.;Kim, D.K.;Moon, H.I.;Lee, K.R.;Chung, K.H.;Zee, O.P.;Jung, Y.H. 170.2
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Kang, S.S.;Kim, J.S.;Son, K.H.;Chang, H.W.;Kim, H.P.;Yoo, S.W.;Byun, J.H.;Han, S.J.;Xu, Y.N. 174.3
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Park, J.C.;Park, J.G.;Hur, J.M.;Park, S.J.;Park, K.Y.;Shin, D.Y.;Kim, M.S.;Miyashiro H.;Yokozawa T.;Haltori M. 183.2
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Park, J.C.;Hur, J.M;Lee, J.H.;Sung, N.J;Baek, N.I;Kim, M.S.;Park, J.G.;Kim, H.J.;Park, J.W. 189.3
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Kim, H.S.;Lee, S.D.;Park, D.W;Kim, M.J.;Jin, J.S.;Jung, K.S.;Yang, S.J.;Jung, H.Y.;Jang, S.J. 202.2
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Lee, S.H.;Kang, C.S.;Park, B.K.;Park, S.H.;Park, S.A.;Park, M.S.;Kang, M.H.;Hong, C.H.;Park, M.H. 208.2
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Park, S.U.;Ryu, S.Y.;Jung, N.P.;Song, S.O.;Park, E.J.;Kim, K.H.;Park, S.H.;Kim, J.E.;Lee, C.O. 210.2
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