• 대한한방내과학회지
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• 제37권3호
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• pp.495-507
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• 2016

Objectives: This study was designed to investigate the effects of Jwa Kum-Whan (JKW) on reflux esophagitis in rats.Methods: Forty rats were divided into five groups: a sham group (with no medication and only treated with ventrotoby); a group with reflux esophagitis (RE); a pantoprazole group (treated with 30 mg/kg pantoprazole per day for two weeks); a JKW280 group (treated with 280 mg/kg JKW per day for two weeks); and a JKW560 group (treated with 560 mg/kg JKW per day for 2 weeks). All rats fasted for 24 hrs and then were induced with RE by the oral administration of indomethacin and by a pylorus and forestomach ligation operation. After 8 hrs, the rats were sacrificed. We measured body weight, gastric juice pH, gastric volume, antioxidant activity, and cytokine and made a histologic examination of the esophagus and the stomach.Results: The weights of the rats in each group were not significantly different. The gastric juice pH significantly increased in the JKW560 group and the pantoprazole group compared with the RE group. Gastric volume significantly decreased in the JKW560 group compared with the RE group and the pantoprazole group. SOD activities significantly increased in the JKW280 and JKW560 groups compared with the RE group. Catalase activities significantly increased in the pantoprazole group and the JKW560 group compared with the RE group. TNF-α significantly decreased in the JKW280 and JKW560 groups compared with the RE group. IL-6 significantly decreased in the pantoprazole group and the JKW280 and JKW560 groups compared with the RE group. Histologic examination of the esophagus and the stomach showed significant improvements in the pantoprazole, JKW280, and JKW560 groups compared with the RE group.Conclusion: Based on these results, it is concluded that JKW can prevent reflux esophagitis.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.169-170
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• 2002

It has been well known for the stereoselectivity in pharmacodynamic effects of many xenobiotics including therapeutic agents, which have lead to the development of enantiomer drugs. Compared to pharmacodynamic stereoselectivity, stereoselective pharmacokinetics of each enantiomer has not been seriously considered in the development of enantiomer drugs although many reports have been demonstrated the stereoselective absorption and metabolism of racemic drug (e.g verapamil). (omitted)

• Asian Pacific Journal of Cancer Prevention
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• 제16권14호
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• pp.6089-6092
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• 2015

Background: The prevalence of metronidazole-resistant H. pylori is almost 50% in Thailand which severely limits the use of this drug for eradication therapy. The aims of this study were to evaluate the efficacy and safety profiles of 7-day bismuth-based quadruple therapy including metronidazole as an initial treatment for H. pylori infection in a high metronidazole resistance area. Materials and Methods: This study was performed at Thammasat University Hospital and King Chulalongkorn Memorial Hospital during January 2009 to October 2010. Patients with non-ulcer dyspepsia (NUD) with active H. pylori infection were assigned to receive seven days of quadruple therapy (pantoprazole 40 mg bid, bismuth subsalicylate 1,048 mg bid, amoxicillin 1 gm bid and metronidazole 400 mg tid). H. pylori infection was defined as positive H. pylori culture or two positive tests (rapid urease test and histology). Antibiotic susceptibility test for metronidazole by Epsilometer test (E-test) was performed in all positive cultures. At least four weeks after treatment, $^{13}C$ urea breath test ($^{13}C-UBT$) was performed to confirm H. pylori eradication. Results: A total of 114 patients were enrolled in this study, 50 males and 64 females with a mean age of 49.8 years. All 114 patients had a diagnosis of NUD. Overall eradication as confirmed by negative $^{13}C-UBT$ was achieved in 94 out of 114 patients (82.5%). 44 patients had positive cultures and success for E-test. In vitro metronidazole resistance was observed in 22/44 (50%) patients. Eradication rate in patients with metronidazole resistant strains was 16/22 (72.7%) and 20/22 (90.1%) with metronidazole sensitive strains (72.7% vs 90.1%, p-value=0.12; OR=3.75 [95%CI=0.6-31.5]). Minor adverse reactions included nausea, bitter taste, diarrhea and black stools but none of the patients dropped out from the study. Conclusions: Initial treatment with 7-day bismuth-based quadruple therapy including metronidazole, amoxycillin and pantoprazole is highly effective and well tolerated for metronidazole-sensitive H. pylori infections. However, the efficacy markedly decline with metronidazole resistance. Longer duration of this regimen might be required to improve the eradication rate and larger multi-center studies are needed to confirm this hypothesis.

• 대한기관식도과학회지
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• 제9권1호
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• pp.60-66
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• 2003

Although there is a wide range of diseases caused by gastric acid reflux and the number of cases is on the rise, it is difficult for the laryngologist to make the correct diagnosis. The treatment for laryngopharyngeal reflux can be grouped into 3 categories - changes in lifestyle, medication, and surgery. The medication used to treat laryngopharyngeal reflux are prokinetic agents and acid supressive agents such as antacids, H2 blockers, and PPIs(Proton pump inhibitor). Rabeprazole sodium($Pariet^{\circledR}$) is a newly developed agent belonging to the PPI group, but in contrast with the existing drugs such as omeprazole, lansoprazole, pantoprazole, has a low dependency on CYP2C19 during the metabolic cycle. Thus, it is known to have a quick but fixed antiacid effect and less individual differences. We analyzed 2166 patients from 32 hospitals who were prescribed $Pariet^{\circledR}$ from May, 2001 to April, 2002. The patients were divided into 4 groups according to the duration of treatment - Group 1: 1-14 days, Group 2: 15-28 days, group 3: 29-56 days, Group 4: more than 56 days. The cases were then analyzed for improvement of 8 symptoms(heart bum, regurgitation, chronic cough, hoarseness, globus sensation, chronic throat clearing, sore throat, and dysphagia), improvement on laryngoscope, usefulness to the doctor, and complication development. Of the total of 2116 patients, 1627(75.1%) cases showed at least 50% improvement of symptoms and the amount of improvement increased according to the duration of medical treatment. Most of the patients showed objective improvement on the laryngoscope, with 32.9% showing significant improvement and 38.7% showing moderate improvement. 37.6% of the doctors questioned replied that $Pariet^{\circledR}$ was very useful and 50.3% said it was useful, showing that most were satisfied with the treatment results. The complications known to develop after taking PPI are headache, nausea, diarrhea, abdominal pain, constipation, dizziness, fatigue, and of these, only a small percentage of the patients complained of mild headache. $Pariet^{\circledR}$ has shown to be a relatively safe and effective drug for the treatment of laryngopharyngeal reflux.

• 대한기관식도과학회:학술대회논문집
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• 대한기관식도과학회 2002년도 제2차 추계학술대회
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• pp.9-9
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• 2002

이비인후과 영역에 있어서 위산 역류에 의한 질환의 진단은 쉽지 않고 분명하지 않은 점이 많지만, 병변의 영향은 광범위하며, 실제로 역류에 의한 증상을 가지고 내원하는 환자도 증가하는 추세이다. 인후두역류질환의 치료는 크게 생활습관의 변경, 약물복용, 항역류수술로 나눌 수 있으며, 사용약제는 크게 두 부류로 나누는데, 제산제, H2 수용체 차단제, PPI(Proton Pump Inhibitor) 제제와 같은 산억제 약물군과 Prokinetic 약물군이다. Rabeprazole sodium(Pariet(R))은 PPI 제제에 해당하는 약제로 기존의 omeprazole, lansoprazole, pantoprazole과는 달리 대사 과정 중 CYP2C19에 대한 의존도가 낮아, 개체 간 차이가 적고 빠르고 일정하게 산분비 억제 효과를 나타내는 것으로 알려져 있은 약물이다. 2001년 5월부터 2002년 4월까지 32개 병원에서 Pariet(R) 를 복용한 2166명의 환자를 대상으로 분석하였다. 복용기간에 따라 4군(1군;1-14일, 2군;15-28일, 3군;29-56일, 4군:57일 이상)으로 나누었으며, 8가지 증상(Heart burn, Regurgitation, Chronic cough, Hoarseness, Globus sensation, Chronic throat clearing, Sore throat, Dysphagia)에 대한 호전 여부 및 후두내시경상 개선 정도, 의사에 의한 유용도 평가, 부작용 발생 여부에 대해 연구하였다. 증상개선율 50%이상을 치료 반응군으로 했을때 전체 2166명중 1627명(75.1%)에서 증상의 호전을 보았으며, 이는 복용기간이 길수록 증가하였다. 후두 내시경상 개선 정도는 현저한 개선이 32.9%, 중등도 개선이 38.7%로 대부분 환자에서 객관적인 병변의 호전을 보였으며, 유용도 평가에서는 매우 유용이 37.6%, 유용이 50.3%로 치료효과에 대한 만족도도 높은 것을 알수 있었다. PPI 제제의 부작용으로 보고되고 있는 두통, 오심, 설사, 복통. 변비, 어지럼증. 피곤 중. 소수의 환자가 두통을 호소하였으나, 그다지 심각한 정도는 아니었다. 인후두역류증 치료제로서 Pariet(R) 는 비교적 안전하고 효과가 높은 약물임이 임상 연구 결과 밝혀졌기에 보고하는 바이다.

• 분석과학
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• 제32권5호
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• pp.185-195
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• 2019

Over the past decades, chiral switch of the proton pump inhibitors (PPIs) has been received widespread attention in therapeutic advantages as well as pharmaceutical analysis. In present study, the influence of cyclodextrins (CDs) on the chiral separation of four common PPIs (lansoprazole, omeprazole, pantoprazole, and rabeprazole) was investigated. The results demonstrated that capillary electrophoresis (CE) with dual CDs as a chiral selector system is a possible and promising method for the enantioseparation of these PPIs. Rabeprazole, which is the most challenging and acid-labile candidate among four PPIs, was selected for further development of the technique. To optimize CE condition, the effects of capillary parameters and background electrolytes on the enantioseparation were investigated. Finally, the best chiral separation was acheived by using sulfobutyl ether-${\beta}$-CD, and ${\gamma}$-CD as dual chiral selectors. The developed CE method not only provided the effective chiral separation but also showed the good stability of rabeprazole. The proposed method was successfully validated according to the International Conference on Harmonization guideline and effectively applied to determine rabeprazole enantiomers in commercial rabeprazole tablets, with recoveries ranging from 97.17 % to 103.29 % of the label content.