• 제목/요약/키워드: Rebamipide

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Determination of rebamipide in human plasma by column-switching high- performance liqiud chromatography.

  • Koung, Joung-Sun;Park, Chang-Hun;Kim, Ho-Hyun;Lee, Hee-Joo;Beom, Han-Sang
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.278.2-278.2
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    • 2003
  • A column-switching semi-micro HPLC method with fluorescence detection was developed for the direct analysis of rebamipide in human plasma. Plasma was filtered through a 0.45 $\mu\textrm{m}$ membrane filter and 5 ${\mu}\ell$ of the filtrate was directly injected onto the pre-column. After elution of the plasma proteins to waste, the retained rebamipide and internal standard(ofloxacin) were transferred to a C18 semi-microcolumn (5$\mu\textrm{m}$, 150 ${\times}$2.0mm) where they were separated using acetonitrile-1.4% acetic acid (40:60, v/v) as mobile phase. (omitted)

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Effects of Small Molecular Antioxidants on Cerulein-induced Acute Pancreatitis in Rat

  • Choi, Joo-Young;Kim, Kyung-Hwan
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권5호
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    • pp.629-635
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    • 1998
  • It has been suggested that oxygen free radicals are involved in the initiation process of acute pancreatitis, although its pathogenesis is not clear. This study evaluates the roles of oxygen radicals and the effects of small molecular antioxidants (rebamipide, N-acetyl-cysteine, allopurinol, ${\beta}-carotene)$ on the development of cerulein-induced acute pancreatitis. Acute edematous pancreatitis was induced by the intravenous infusion of cerulein at supramaximal dose of 10 ${\mu}g/kg/hour$ for 3.5 hours. The effects of antioxidants, rebamipide (100 mg/kg, i.p.), N-acetyl-cysteine (200 mg/kg, i.v.), allopurinol (20 mg/kg/hour), ${\beta}-carotene$ (50 mg/kg, i.p.), were examined. Cerulein administration resulted in a significant increase in serum amylase activity and pancreatic malondialdehyde (MDA), but not glutathione peroxidase (GSHpx). The glutathione (GSH) content in pancreatic tissue decreased dramatically. Pretreatment of N-acetyl-cysteine significantly decreased the cerulein-induced hyperamylasemia and maintained GSH content in pancreas, but MDA was slightly decreased. In addition, N-acetyl-cysteine ameliorated histological damage. Allopurinol and ${\beta}-carotene$ attenuated cerulein-induced hyperamylasemia, but histologically there was no difference from control. These results indicate that oxygen free radicals play an important role in the initiation of experimental acute pancreatitis. N-acetyl-cysteine is an effective antioxidant that ameliorates the cerulein-induced acute pancreatitis, and the possible therapeutic application of antioxidants against acute pancreatitis needs a further evaluation.

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에탄올 유발 위점막 손상에 대한 황련 물 추출물의 방어효과 (Protective Effects of Coptidis Rhizoma on Ethanol-induced Gastric Ulcer in Mice)

  • 변준석
    • 동의생리병리학회지
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    • 제26권1호
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    • pp.67-73
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    • 2012
  • The exposure of gastric mucosa to ethanol produces acute ulcers mediated by inflammatory processes, hemorrhagic erosions and increase of reactive oxygen species. The purpose of this study was to assess the effects of Coptidis Rhizoma(CR) aqueous extracts on hydrochloride (HCl)/ethanol induced gastric ulcer in mice as compared with rebamipide (30 mg/kg) and ranitidine (100 mg/kg). Stomach ulcers were induced by oral ingestion of HCl/ethanol. CR extracts (125, 250 and 500 mg/kg) were orally administered, once a day for 7 continuous days, and 1 hr after last 7th treatment of CR extracts stomach ulcers were induced. Effects of CR extracts on HCl/ethanol-induced gastric ulcer were evaluated based on gross and microscopic observations with anti-oxidant activities. All three different dosages of CR extract significantly decreased HCl/ethanol-induced gastric ulcer compared with the HCl/ethanol control mice. CR extracts also strengthened the antioxidative defense systems - decreased the level of lipid peroxidation but increased the level of catalase, superoxide dismutase and nitrate/nitrite compared with the HCl/ethanol control. The effects of CR extract 500 mg/kg were similar to that of 30 mg/kg rebamipide, and CR extract 250 mg/kg showed similar anti-ulcer effects as compared with ranitidine 100 mg/kg. These results suggest that the gastroprotective effects of CR extracts on mice ulcer models can be attributed to its ameliorating effect on oxidative damages.

Chemoprevention of Helicobacter pylori-associated Gastric Carcinogenesis in a Mouse Model; Is It Possible?

  • Hahm, Ki-Baik;Song, Young-Joon;Oh, Tae-Young;Lee, Jeong-Sang;Surh, Young-Joon;Kim, Young-Bae;Yoo, Byung-Moo;Kim, Jin-Hong;Ha, Sang-Uk;Nahm, Ki-Taik;Kim, Myung-Wook;Kim, Dae-Yong;Cho, Sung-Won
    • BMB Reports
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    • 제36권1호
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    • pp.82-94
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    • 2003
  • Although debates still exist whether Helicobacter pylori infection is really class I carcinogen or not, H. pylori has been known to provoke precancerous lesions like gastric adenoma and chronic atrophic gastritis with intestinal metaplasia as well as gastric cancer. Chronic persistent, uncontrolled gastric inflammations are possible basis for ensuing gastric carcinogenesis and H. pylori infection increased COX-2 expressions, which might be the one of the mechanisms leading to gastric cancer. To know the implication of long-term treatment of antiinflammatory drugs, rebamipide or nimesulide, on H. pylori-associated gastric carcinogenesis, we infected C57BL/6 mice with H. pylori, especially after MNU administration to promote carcinogenesis and the effects of the long-term administration of rebamipide or nimesulide were evaluated. C57BL/6 mice were sacrificed 50 weeks after H. pylori infection. Colonization rates of H. pylori, degree of gastric inflammation and other pathological changes including atrophic gastritis and metaplasia, serum levels and mRNA transcripts of various mouse cytokines and chemokines, and NF-${\kappa}B$ binding activities, and finally the presence of gastric adenocarcinoma were compared between H. pylori infected group (HP), and H. pylori infected group administered with long-term rebamipide containing pellet diets (HPR) or nimesulide mixed pellets (HPN). Gastric mucosal expressions of ICAM-1, HCAM, MMP, and transcriptional regulations of NF-${\kappa}B$ binding were all significantly decreased in HPR group than in HP group. Multi-probe RNase protection assay showed the significantly decreased mRNA levels of apoptosis related genes and various cytokines genes like IFN-$\gamma$, RANTES, TNF-$\alpha$, TNFR p75, IL-$1{\beta}$ in HPR group. In the experiment designed to provoke gastric cancer through MNU treatment with H. pylori infection, the incidence of gastric carcinoma was not changed between HP and HPR group, but significantly decreased in HPN group, suggesting the chemoprevention of H. pylori-associated gastric carcinogenesis by COX-2 inhibition. Long-term administration of antiinflammatory drugs should be considered in the treatment of H. pylori since they showed the molecular and biologic advantages with possible chemopreventive effect against H. pylori-associated gastric carcinogenesis. If the final concrete proof showing the causal relationship between H. pylori infection and gastric carcinogenesis could be obtained, that will shed new light on chemoprevention of gastric cancer, that is, that gastric/cancer could be prevented through either the eradication of H. pylori or lessening the inflammation provoked by H. pylori infection in high risk group.

Protective Effect of Liriodendrin Isolated from Kalopanax pictus against Gastric Injury

  • Sohn, Yoon Ah;Hwang, Seon A;Lee, Sun Yi;Hwang, In Young;Kim, Sun Whoe;Kim, So Yeon;Moon, Aree;Lee, Yong Soo;Kim, Young Ho;Kang, Keum Jee;Jeong, Choon Sik
    • Biomolecules & Therapeutics
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    • 제23권1호
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    • pp.53-59
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    • 2015
  • In this study, we investigated the inhibitory activities on gastritis and gastric ulcer using liriodendrin which is a constituent isolated from Kalopanax pictus. To elucidate its abilities to prevent gastric injury, we measured the quantity of prostaglandin $E_2$ ($PGE_2$) as the protective factor, and we assessed inhibition of activities related to excessive gastric acid be notorious for aggressive factor and inhibition of Helicobacter pylori (H. pylori) colonization known as a cause of chronic gastritis, gastric ulcer, and gastric cancer. Liriodendrin exhibited higher $PGE_2$ level than rebamipide used as a positive control group at the dose of $500{\mu}M$. It was also exhibited acid-neutralizing capacity (10.3%) and $H^+/K^+$-ATPase inhibition of 42.6% ($500{\mu}M$). In pylorus-ligated rats, liriodendrin showed lower volume of gastric juice ($4.38{\pm}2.14ml$), slightly higher pH ($1.53{\pm}0.41$), and smaller total acid output ($0.47{\pm}0.3mEq/4hrs$) than the control group. Furthermore liriodendrin inhibited colonization of H. pylori effectively. In vivo test, liriodendrin significantly inhibited both of HCl/EtOH-induced gastritis (46.9 %) and indomethacin-induced gastric ulcer (46.1%). From these results, we suggest that liriodendrin could be utilized for the treatment and/or protection of gastritis and gastric ulcer.

Effects of Antioxidants on the Gamma-Radiation Damage of the Cultured Vascular Smooth Mucle Cells of Rat Aorta

  • Lee, Jong-Doo;Choi, Hyoung-Chul;Kang, Young-Jin;Kim, Myung-Se;Lee, Kwang-Youn
    • The Korean Journal of Physiology and Pharmacology
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    • 제11권5호
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    • pp.189-195
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    • 2007
  • To study the protective effects of antioxidants on the radiation damages of the cells, vascular smooth muscle cells(VSMC) from thoracic aorta of Sprague-Dawley rats were cultured and irradiated with gamma-ray. Cell viability was measured by direct cell counting and MTT assay, and flow cytometry was performed to measure fractional distributions of the cells. Gamma-ray irradiation inhibited cell proliferations accompanied with decreased G1 phase and increased S- and G2/M phases, and the maximum effects were observed at 1500 or 2000 cGy. Submaximal concentrations of antioxidants, such as allopurinol, vitamin C, N-acetylcycteine(NAC), lipoic acid, dihydrolipoic acid and rebamipide tended to increase the cell viability suppressed by low dose of radiation(500 cGy), and enalapril and vitamin E increased it significantly. Allopurinol, vitamin E, NAC, lipoic acid, captopril and enalapril significantly increased G1 phase. Allopurinol and vitamin E tended to increase c-Myc expression, detected by Western blot, that was reduced by the radiation, and enalapril increased it significantly. The cell viability and c-Myc expression were highly correlated(r=0.97) with each other. These results suggest that antioxidants, especially enalapril and vitamin E, recover the viability of VSMC from gamma-radiation injury, through a mechanism which includes increase of c-Myc protein expression.

합성의약품으로 호전되지 않은 소화기 증상 환자(KCD K-코드)에 대한 반하사심탕 제제 병용의 효과 : 후향적 차트 분석 (Effectiveness of Additional Administration of a Banha-sasim-tang Formulation to Patients with Gastrointestinal Symptoms (KCD K-code) Not Improved by Western Medicines: A Retrospective Chart Review)

  • 김철현;김광호;이영웅;강선이;강건희
    • 대한한방내과학회지
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    • 제42권6호
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    • pp.1349-1355
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    • 2021
  • Objectives: The aim of this study was to evaluate the effectiveness of additional administration of Banha-sasim-tang formulation to patients with gastrointestinal symptoms that did not improve with Western medicines. Methods: The patients who met the inclusion and exclusion criteria were analyzed retrospectively. A paired t-test was performed on the Nepean Dyspepsia Index-Korean version (NDI-K) scores before and after administering the Banha-sasim-tang formulation. Results: A total of 27 subjects were included. The mean duration of taking the Banha-sasim-tang formulation was 15.6±3.1 days. The most commonly used Western medicine before taking the Banha-sasim-tang formulation was rebamipide. The means of the NDI-K score were 57.4±21.8 before administering Banha-sasim-tang formulation and 34.9±16.5 after administration, and the difference was statistically significant (p<0.0001). No serious side effects were encountered while taking the Banha-sasim-tang formulation. Conclusions: For patients whose gastrointestinal symptoms do not improve with Western medicines, additional administration of Banha-sasim-tang formulation may be an option. However, as this study is a retrospective chart review, prospective, large-scale, double-blind studies are needed in the future.