• Title/Summary/Keyword: Antiulcer drug

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Antigastric and Antiulcerative Action of a New Proton Pump Inhibitor (IY-81233) (새로운 프로톤 펌프 억제제, IY-81233의 항위염과 항궤양작용)

  • Kim, Seung-Hee;Kim, Jeen;Kang, Seog-Youn;Lee, Song-Deuk;Hong, Sung-Gul;Kim, Dong-Yeun;Moon, A-Ree
    • Biomolecules & Therapeutics
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    • v.4 no.3
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    • pp.285-290
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    • 1996
  • This study was designed to determine the effect of newly synthesized antiulcer agent, 5-pyrrolyl-6-halo-2-(pyridyl-2-methylthio)benzimidazole derivatives (IY-81233), on various experimental ulcers and on the secretion of prostaglandin $E_2(PGE_2)$ into the gastric lumen of rat. IY-81233 was previously reported to have a strong inhibitory effect on $H^+/K^$-ATPase and on gastric acid secretion in rats. Oral administration of IY-81233 at concentrations of 0.2, 2.0, and 20 mg/kg inhibited gastric lesions and duodenal ulcer induced by indomethacin, HCI-ethanol, water-immersion stress, cysteamine, and acetic acid in a dose dependent manner. Their IC$IC_{50}$ values were 3.4, 1.4, 0.8, 1.3, and 1.2 mg/kg, respectively. These results indicate that IY-81233 is a potent antiulcer agent although it is slightly less potent than omeprazole in healing of gastritis and ulcers. The secretion of $PGE_2$ into gastric lumen was also investigated in relation to the cytoprotective effect by IY-81233 in rats. The $PGE_2$ level was not changed significantly by an oral administration of IY-81233, suggesting that IY-81233 has little effect on the gastric protection. Therefore, it can be concluded that IY-81233 exerts prominent antiulcer activity by suppressing gastric acid secretion via an inhibition of a proton pump and not by protecting the gastrointestinal mucosa against various ulcerative stimuli.

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Antiulcer Activity of Sida acuta Burm.

  • Malairajan, P.;Gopalakrishnan, Geetha;Narasimhan, S.;Veni, K. Jessi Kala
    • Natural Product Sciences
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    • v.12 no.3
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    • pp.150-152
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    • 2006
  • The ethanol extract of Sida acuta Burm. (ALSA) whole plant was studied for its anti-ulcer activity against aspirin plus pylorous ligation induced gastric ulcer, HCl-ethanol induced ulcer, and water immersion stress induced ulcer (WISIU) in rats. We found that ALSA at a dose of 300 mg/kg, (orally) markedly decrease the incidence of ulcers in the first two models. ALSA showed reduction in gastric volume, free acidity, and ulcer index (53.69%). It has not reduced the total acidity significantly and no significant change in pH. It also showed 55.14% gastro protective activity, wheres standard drug sucralfate showed 94.85%. WISIU showed protection index 24.4%, whereas standard drug omeprazole (OMEZ) showed protection index 100%.

Anti-ulcerogenic activity of virgin coconut oil contribute to the stomach health of humankind

  • Selverajah, Malarvili;Zakaria, Zainul Amiruddin;Long, Kamariah;Ahmad, Zuraini;Yaacob, Azhar;Somchit, Muhammad Nazrul
    • CELLMED
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    • v.6 no.2
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    • pp.11.1-11.7
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    • 2016
  • The aimed of the presence study was to determine the antiulcer potential of virgin coconut oil (VCO), either extracted by wet process (VCOA) or fermentation process (VCOB), and to compare their effectiveness against the copra oil (CO) using the HCl/ethanol-induced gastric ulcer model. Earlier, the oils underwent chemical analysis to determine the free fatty acids composition, physicochemical properties and anti-oxidant capability. In the antiulcer study, rats (n=6) were pre-treated orally for 7 consecutive days with distilled water (vehicle), 100 mg/kg ranitidine (positive group) or the respective oils (10, 50, and 100% concentration). One hour after the last test solutions administration on Day 7th, the animals were subjected to the gastric ulcer assay. Macroscopic and microscopic analyses were performed on the collected rat's stomachs. From the results obtained, the chemical analysis revealed i) the presence of high content of lauric acid followed by myristic acid and palmitic acid in all oils and; ii) the significant (*p< 0.05) different in anisidine- and peroxide-value, percentage of free fatty acid, total phenolic content and total antioxidant activity among the oils. The animal study demonstrated that all oil possess significant (*p< 0.05) antiulcer activity with VCOB being the most effective oil followed by VCOA and CO. The macroscopic observations were supported by the microscopic findings. Interestingly, all oils were more effective than 100 mg/kg ranitidine (reference drug). In conclusion, coconut oils exert remarkable antiulcer activity depending on their methods of extraction, possibly via the modulation of its antioxidant and anti-inflammatory activity.

General Pharmacological Properties of YJA20379-2, a New Antiulcer Agent

  • Lee, Eun-Bang;Cho, Sung-Ig;Cheon, Seon-Ah;Chang, Man-Sik;Kim, Kyu-Bong;Woo, Tae-Wook;Chung, Young-Kuk
    • Archives of Pharmacal Research
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    • v.23 no.1
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    • pp.72-78
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    • 2000
  • The general pharmacological properties of YJA20379-1 2-dimethylamino-4,5-dihydrothiazolo[4,5:3,4]pyridol[1,2-a]benzoimidazole, a novel proton pump inhibitor with antiulcer activities were investigated in mice, rats, guinea pigs and rabbits. YJA20379-2 at oral doses of 50, 100 and 200 mg/kg did not affect the general behaviour, hexobarbital hypnosis and motor coordination in mice. The drug did not have analgesic or anticonvulsant action at 200 mg/kg. Locomotor activity and body temperature were not influenced at 100 mg/kg. At a concentration up to 2{\times}10^{-4} g/ml$, YJA20379-2 did not produce any contraction or relaxation of isolated preparations, such as the rat fundus, the guinea pig ileum and the rat uterus, and did not antagonize the contractile response to several spasmogens, such as histamine, acetylcholine, serotonin and oxytocin. At dosages up to 200 mg/kg p.o. YJA20379-2 did not affect the pupil size of mice. Intestinal propulsion of mice was not affected up to 200 mg/kg p.o. and the drug did not affect urinary excretion at 100 mg/kg p.o. These results indicate that at dosages up to 100 gm/kg p.o. YJA20379-2 was found not to affect this pharmacological profile. However, at 200 mg/kg the drug lowered body temperature and showed decreased in locomotor activity and urine volume.

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Metabolism of YH1885 by Rat, Dog, Monkey and Human Liver S9 Fractions

  • Kim, Eun-Joo;Roh, Jung-Koo;Green, Carol
    • Biomolecules & Therapeutics
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    • v.6 no.3
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    • pp.283-288
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    • 1998
  • YH 1885 (5,6-dimethyl -2-(4-fluorophenylamino)-4-(1-methyl -1,2,3,4-tetrahydroisoquinolin -2- yl) pyrimidine hydrochloride) was developed as an antiulcer drug. The objective of this study was to examine a comparative metabolism of YH1885 in rat, dog, monkey and human liver tissues and to determine the metabolite profiles produced by the four species. YH1885 was metabolized by liver 59 fractions from all four species. Control incubations containing 59 fraction but no cofactors, contained essentially no metabolites. Metabolism of YH1885 apparently became saturated in the concentration range studied because the % of YH 1885 metabolized decreased with increasing drug concentration for all four species. Six to nine metabolite peaks were detected in the incubations and the particular profile of metabolites varied with species. The total amount of metabolites formed by liver microsomes from human and monkey were less than microsomes from rat or dog. The major metabolite peak formed by rat liver 597actions fluted near the solvent front on the HPLC or remained at the origin in TLC, indicating that it contained one or more polar metabolites. Dog liver 59 fractions incubations contained four major metabolites that each accounted for about 15 to 20 % of the total radioactivity at the low concentration of YH1885. The metabolite profiles of YH1885 appeared to be similar in incubations with rhesus monkey and human liver 59 fraction. The amount of metabolites formed by rhesus monkey liver preparations was greater than that of human liver that contained prominent metabolite peaks with approximate relative retention time of 0.14 and 0.43.

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A Case Report of Drug-Induced Parkinsonism Treated with Jodeung-san and Electro-acupuncture at GB34 (조등산(Diaoteng-san, Choto-san, 釣藤散)과 GB34(陽陵泉) 전침치료를 활용한 약인성파킨슨증후군 환자의 증례 1례)

  • Kim, Eun-ji;Song, Ho-joon;Kim, Hyun-ho;Han, Yang-hee;Leem, Jung-tae
    • The Journal of Internal Korean Medicine
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    • v.38 no.5
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    • pp.600-609
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    • 2017
  • Drug-induced Parkinsonism is the most frequently observed type among the cases of secondary Parkinsonism. Besides typical parkinsonian symptoms, such as tremor, rigidity and bradykinesia, drug-induced Parkinsonism manifests with additional simultaneous symptoms like orobuccolingual dyskinesia, mixed type of tremor (resting, action), and symmetry of expressions. We present a case of drug-induced Parkinsonism, affected by taking the antiulcer drug cimetidine. Jodeung-san extract (Choto-san, Tsumura Co. 10) was administered for 7 days and acupuncture (electronic, auricular, pharmacopuncture) was conducted 3 times. The clinical outcomes were then evaluated through the patient's global impression of change, visual analogue scale, and Hoehn and Yahr stage. After the treatment, the clinical features, such as tremor and orobuccolingual dyskinesia, disappeared. The combination of Jodeung-san and electro-acupuncture at GB34 could therefore be a remedy for the patients with drug-induced Parkinsonism.

Traditional uses, phytochemistry and pharmacological profile of Bambusa arudinacea Retz

  • Soni, Vishal;Jha, Arvind Kumar;Dwivedi, Jaya;Soni, Priyanka
    • CELLMED
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    • v.3 no.3
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    • pp.20.1-20.6
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    • 2013
  • Bambusa arundinacea family Graminae, is one of the precious plant resources of the earth. It has played a significant role in human civilization since ancient times. It is tall sized tree growing throughout India, moist parts of India. It also occurs in Sri Lanka, Malaya, Peru and Myanmar. The different parts of this plant contain silica, cholin, betain, cynogenetic glycosides, albuminoids, oxalic acid, reducing sugar, resins, waxes, benzoic acid, arginine, cysteine, histidine, niacin, riboflavin, thiamine, protein, gluteline, contains lysine, methionine, betain, cholin, proteolytic enzyme, nuclease, urease. Various parts of this plant such as leaf, root, shoot and seed possess anti-inflammatory, antiulcer, anti-diabetic, anti-oxidant, anthelmintic, antifertility, antibacterial, insectisidal, antiarthritic, vessele protection etc. This review mainly focuses on the traditional, phytochemical and pharmacological information of Bambusa arundinacea.

Trends on the Curtailment of Drug Expenditure Before and After the Seperation between Prescription and Dispensing in General Hospitals By Drug Types (의약분업 전후 일부 종합병원의 약제종류별 약제비 삭감추이)

  • Lee, Sun-Hee;Jo, Heui-Sug;Lee, Hye-Jean
    • Korea Journal of Hospital Management
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    • v.8 no.2
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    • pp.93-110
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    • 2003
  • Fiscal crisis in the medical insurance has put the pressure upon hospitals by increasing the rate of curtailment, since the implementation of the separation between prescription and dispensing of Drug. The purpose of this study is to analyze the curtailment for antibiotics, injected drug and other drugs expenditure before and after the system of separation between prescribing and dispensing. Data were gathered from 13 general hospitals and used for analysis of trends on antibiotics and injected drug expenditure, and curtailment in 2000-2001 at three months intervals. The results were as follows; The curtailment rate of antibiotics expenditure has been increased in outpatient and inpatient since 2000. The curtailed antibiotics cost and injected drug cost in outpatient under the prescription within the hospital and in inpatient increased. The ratios of curtailment versus expenditure had increased in antibiotics, injected drugs, anticancer drugs, antiulcer drugs, albumine, antiinflammatory drugs. These results suggest that claim review system in social health insurance were over-focused mainly to control the cost and it might to impede the validity of claim review function in health insurance system. Therefore, it's needed to develope the scientific and reasonable parameter & criteria for claim review of drug expenditure.

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Pharmacological Test for a Combined Products Containing Sucralfate as a Suspended Antiulcer drug.

  • Kang, Seog-Youn;Kim, Seung-Hee;Jung, Sook-Young;Lee, Song-Deuk
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1995.04a
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    • pp.93-93
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    • 1995
  • The three combined products were prepared as suspended solutions composed of various ratio of Sucralfate, Hydrotalcite and Neusilin, into which 30% ethanol extracts of Machili cortex, and of Atractylodis rhizoma were added. The efficacy for these products was examined in vivo using a pyrous ligation method in rats. The influence of these products on the intestinal motility was also examined in mice. In all experimental setting, the antisecretory effect of the combined treatment was more pronounced than that of each drug alone. The combined treatment consisted of Sucralfate, Hydrotalcite, Neusilin ratios of 2:2:1 produced the highest inhibitory effect for the gastric secretion. The intestinal motility was not influenced significantly by the treatment of all experimental setting. The above results revealed that the therapeutic dose of Sucralfate, Hydrotalcite, Neusilin given in combination showed a synergistic effect for the inhibition of gastric secretion and little side effect on the intestinal motility. Therefore, the combined product with Sucralfate, Hydrotalcite, Neusilin ratio of 2:2:1 is recommended for the useful drug to heal the gastrointestinal diseases with no side effect on the intestinal motility.

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Evaluation of the gastroprotective effects of 20 (S)-ginsenoside Rg3 on gastric ulcer models in mice

  • Zhang, Kai;Liu, Ying;Wang, Cuizhu;Li, Jiannan;Xiong, Lingxin;Wang, Zhenzhou;Liu, Jinping;Li, Pingya
    • Journal of Ginseng Research
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    • v.43 no.4
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    • pp.550-561
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    • 2019
  • Background: Gastric ulcer (GU) is a common gastrointestinal disease that can be induced by many factors. Finding an effective treatment method that contains fewer side effects is important. 20 (S)-ginsenoside Rg3 is a kind of protopanaxadiol and has shown superior antiinflammatory and antioxidant effects in many studies, especially cancer studies. In this study, we examined the treatment efficacy of 20 (S)-ginsenoside Rg3 on GU. Methods: Three kinds of GU models, including an alcohol GU model, a pylorus-ligated GU model, and an acetic acid GU model, were used. Mouse endothelin-1 (ET-1) and nitric oxide (NO) levels in blood and epidermal growth factor (EGF), superoxide dismutase, and NO levels in gastric mucosa were evaluated. Hematoxylin and eosin staining of gastric mucosa and immunohistochemical staining of ET-1, inducible nitric oxide synthase (NOS2), and epidermal growth factor receptors were studied. Ulcer index (UI) scores and UI ratios were also analyzed to demonstrate the GU conditions in different groups. Furthermore, Glide XP from $Schr{\ddot{o}}dinger$ was used for molecular docking to clarify the interactions between 20 (S)-ginsenoside Rg3 and EGF and NOS2. Results: 20 (S)-ginsenoside Rg3 significantly decreased the UI scores and UI ratios in all the three GU models, and it demonstrated antiulcer effects by decreasing the ET-1 and NOS2 levels and increasing the NO, superoxide dismutase, EGF, and epidermal growth factor receptor levels. In addition, high-dose 20 (S)-ginsenoside Rg3 showed satisfactory gastric mucosa protection effects. Conclusion: 20 (S)-ginsenoside Rg3 can inhibit the formation of GU and may be a potential therapeutic agent for GU.