• Title/Summary/Keyword: mepirizole

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Effect of Baegi-eum (BGU) on mepirizole-induced gastrointestinal tissue injury in rabbit (배기음(排氣飮)이 Mepirizole에 의해 유발된 토끼의 위장관 손상에 미치는 영향)

  • Kim, Woo-Hwan;Kim, Won-Ill
    • The Journal of Internal Korean Medicine
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    • v.22 no.1
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    • pp.21-27
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    • 2001
  • 목적 : 본 연구는 배기음(排氣飮)이 토끼의 위장관내에서 화학물질에 의해 유발된 장관의 궤양에 유효한 효과를 발휘할 수 있는지를 검증하기 위한 실험이다. 방법 : 토끼 5마리를 한 군으로 하여 정상군과 체중 1kg당 200mg 분량의 mepirizole을 경구 투여한 군과 100mg/kg의 배기음(排氣飮)(경구투여)과 800Units/kg 분량의 catalase(정맥주사)를 mepirizole을 경구투여하기 2시간 전에 각각 전처치한 군으로 나누었다. Mepirizole을 경구 투여한 후 각각 24hr와 48hr에 토끼를 희생시켜 위장, 십이지장부의 궤양성 병변을 관찰하였다. 결과 : Mepirizole을 경구투여하여 위장 및 십이지장 기부의 궤양성 병변이 유발되었다. 배기음(排氣飮)(경구투여)과 catalase(정맥주사)를 전처치하였을 경우 궤양의 크기가 현저하게 줄어들었다. Mepirizole은 십이지장 점막에서 지질의 과산화를 증가시키는데 이는 수산화기와 관련되어 있음을 시사한다. 배기음(排氣飮)과 catalase를 전처치함으로써 mepirizole에 의해 유발된 지질의 과산화가 현저하게 억제되었다. 형태학상의 연구에서도 mepirizole의 처치에 의한 십이지장의 손상과 배기음(排氣飮)에 의한 방지효과가 나타났다. 결론 : 이러한 결과들로 볼 때 반응성산소기는 mepirizole에 의해 유발된 위장관 궤양의 병리변화 형성에 주요한 영향을 미치며 배기음(排氣飮)이 항산화작용을 통해 궤양의 형성을 억제하는 역할을 하고 있음을 나타낸다. 따라서 본 연구는 배기음(排氣飮)이 반응성산소기에 의해 매개된 인체 위장관질환에 치료적 역할을 할 수 있음을 제시하고 있다.

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Experimental Studies on the Effect of Gamibaegi-eum

  • Kim Won-Ill
    • The Journal of Korean Medicine
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    • v.25 no.4
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    • pp.61-78
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    • 2004
  • Objective : This study was undertaken to determine whether Gamibaegi-eum (BGU) in vitro and in vivo exerts a beneficial effect against cell injury induced by reactive oxygen species (ROS) in the human intestine. Methods : Effects of BGU in vitro on cell injury were examined using Caco-2 cells, cultured human intestinal cell line. Exposure of cells to H₂O₂ induced increases in the loss of cell viability in a time and dose-dependent fashion. Results : BGU prevented H₂O₂-induced cell death and its effect was dose-dependent over a concentration range of 0.05­1%. H₂O₂-induced cell death was prevented by catalase, the hydrogen peroxide scavenger enzyme, and deferoxamine, the iron chelator. However, the potent antioxidant DPPD did not affect H₂O₂-induced cell death. H₂O₂ increased lipid peroxidation, which was inhibited by BGU and DPPD. H₂O₂ caused DNA damage in a dose-dependent manner, which was prevented by BGU, catalase, and deferoxamine, but not DPPD. BGU restored ATP depletion induced by H₂O₂. BGU inhibited generation of superoxide and H₂O₂ and scavenged directly H₂O₂. Oral administration of mepirizole in vivo at a dose of 200mg/kg resulted in ulcer lesions in the stomach and the proximal duodenum. Pretreatment of BGU(0.1%/kg, orally) and catalase (800Units/kg, i.v.) significantly decreased the size of ulcers. Mepirizole increased lipid peroxidation in the mucosa of the duodenum, suggesting an involvement of ROS. Pretreatment of BGU and catalase significantly inhibited lipid peroxidation induced by mepirizole. Morphological studies showed that mepirizole treatment causes duodenal injury and its effect is prevented by BGU. Conclusion : These results indicate that BGU exerts a protective effect against cell injury in vitro and in vivo through antioxidant action. The present study suggests that BGU may playa therapeutic role in the treatment of human gastrointestinal diseases mediated by ROS.

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Development of spherical crystallization technique and its application to pharmaceutical systems

  • Kawashima, Yoshiaki
    • Archives of Pharmacal Research
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    • v.7 no.2
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    • pp.145-151
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    • 1984
  • A novel agglomeration technique, termed "Spherical Crystallization Process", which can transform directly the fine crystals produced in the crystallization or the reaction process into a spherical shape was developed. By this technique, needle like crystals such as salicylic acid were transformed into free flowing and directly compressible agglomerates. Sphericaly agglomerated aminophyline crystals were obtained directly from the reaction system, which could reduce the preparation processes, e. g. synthesis, crystallization and agglomeration, into only one step. Sodium theophyline monohydrate agglomerates were prepared by salting out, the rate process of which was described by a first order kinetics. Agglomerated crystals of ndw complex of indo-methacin-mepirizole were prepare with this technique; an improved therapeutic effect of the resultant crystals was expected. expected.

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Effect of Recombinant Human Epidermal Growth Factor(DWP 401) on Gastric Secretion and Ulcers in Rats (재조합 인간 상피세포 성장인자(DWP 401)의 흰쥐 위액분비 및 궤양에의 작용)

  • Lee, Eun-Bang;Cheon, Seon-A;Lee, Eun-Sim;Kim, Ok-Gyeong
    • YAKHAK HOEJI
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    • v.40 no.4
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    • pp.456-461
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    • 1996
  • The effects of human epidermal growth factor(EGF) which was produced by recombinant DNA technique was investigated on gastric secretion, gastric lesion and ulcer models in rats. The EGF showed significant inhibition of secretion of gastric juice and total acid output, at 0.4mg/kg, id and also inhibited Shay ulceration at 0.4mg/kg, id in rats. The lesion induced by absolute ethanol was significantly reduced by oral administration of EGF at 0.4mg/kg. Likewise, EGF caused significant inhibition of indomethacin induced gastric ulcer at oral doses of 0.2 and 0.4mg/kg. The EGF produced dose-dependent inhibition of gastric ulcer induced by acidified aspirin, but showed no significant inhibition at oral doses of 0.1, 0.2 and 0.4mg/kg. The chronic gastric ulcer induced by injection of 20% acetic acid solution was significantly reduced by oral doses of 0.1 and 0.4mg/kg of EGF. Duodenal ulcer induced by mepirizole was dose-dependently inhibited by oral doses of 0.1, 0.2 and 0.4mg/kg of EGF. These data suggest that EGF possesses pronounced inhibitory action in gastric ulcer and duodenal ulcer of rats.

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Biochemical and Pharmacological Properties of a New Proton Pump Inhibitor, 2-Amino-4,5-dihydropyrido[1,2-a]thiazolo [5,4-g] benzimidazole (YJA20379-5)

  • Sohn, Sang-Kwon;Chang, Man-Sik;Chung, Young-Kuk;Kim, Kyu-Bong;Woo, Tae-Wook;Kim, Sung-Gyu;Choi, Wahn-Soo
    • Archives of Pharmacal Research
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    • v.21 no.3
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    • pp.241-247
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    • 1998
  • This study was designed to determine biochemical and pharmacological properties of a newly synthesized benzimidazole derivative, 2-amino-4, 5-dihydropyrido [1, 2-a] thiazolo [5, 4-g] benzimidazole (YJA20379-5) in vitro and in vivo. In the leaky membrane vesicles of pig gastric mucosa, YJA20379-5 inhibited the $K^+$-stimulated $H^+$, $K^+$-ATPase activity in a concentration- and time-dependent manner, with $IC_{50}$ values being $43{\mu}\textrm{M}$ and $43{\mu}\textrm{M}$ at pH 6.4 and 7.4, respectively. YJA20379-5, given intraduodenally, had a potent inhibitory effect on the gastric acid secretion in pylorus-ligated rats. The $ED_{50}$ value for acid secretion was 15.4 mg/kg. YJA20379-5, administered orally, also suppressed gastric damages induced by water-immersion stress, indomethacin and ethanol, and duodenal damage induced by mepirizole in rats; the $ED_{50}$ values were 17.6, 4.7, 3.0 and 18.7 mg/kg, respectively. Furthermore, repeated oral administration of YJA20379-5 accelerated the spontaneous healing of acetic acid-induced gastric ulcers in rats. It is concluded that the a-ntisecretory activity of YJA20379-5 appears to be associated with inhibition of $H^+$, $K^+$-ATPase, while its antigastric and antiduodenal lesion activities are primarily related to the antisecretory effect.

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Effect of Antacids, Aceglutamide Aluminium or Their Combination on Acute and Chronic Ulcer Models in Rats (흰쥐의 급만성궤양모델에서 제산제와 Aceglutamide aluminium의 병용효과)

  • Jang, Byeong-Su;Yeom, Je-Ho;Kang, Jin-Suk;Yu, Young-Hyo;Park, Myung-Hwan;Kim, Woon-Ja;Chun, Sun-A;Kim, Sang-Mee;Lee, Eun-Bang
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.496-503
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    • 1994
  • The combined products of antacids(AM) composed of aluminium hydroxide, magnesium hydroxide, and simethicone with a ratio of 1 : 1 : 0.1 and aceglutamide aluminium(AGA) were assayed for the antiulcer activity. The effect of the antacids(AM) in concurrent treatment with AGA was studied in acute gastric lesion induced by Shay's method, stress, ethanol, and indomethacin, in chronic gastric ulcers induced by acetic acid, and in duodenal ulcer induced by mepirizole. In all experimental models, the combined treatment of AM and AGA in the ratio of 2.3:1 showed significant potentiation in inhibition against acute gastric and duodenal ulcer and revealed a significant potentiation of the healing of chronic gastric ulcer.

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