• Archives of Pharmacal Research
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• v.22 no.1
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• pp.86-88
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• 1999

An advance d and sensitive high-performance liquid chromatographic (HPLC) method for determination of omeparzole in human plasma has been developed. After omeprazole was extracted from plasma with diethylether, the organic phase was transferred to another tube and trapped back with 0.1 N NaOH solution. The alkaline aqueous layer was injected into a reversed-phase C8 column. Lansoprazole was used as an internal standard. The mobile phase consisted of 30% of acetonitrile and 70% of 0.2 M $ KH_{2}PO_{4}$, pH 7.0. Recoveries of the analytes and internal standard were >75.48%. The coefficients of variation of intra- and inter-day assay were <5.78 and 4.59% for plasma samples. The detection limit in plasma was 2 ng/ml. The clinical applicability of this assay method was evaluated by determining plasma concentration-time courses of the respective analytes in 24 healthy volunteers after oral administration 40 mg of omeprazole. The present assay is considered to be simple, accurate, economical and suitable for the study of the kinetic disposition of omeprazole in the body.

• Korean Journal of Clinical Pharmacy
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• v.11 no.1
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• pp.13-18
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• 2001

Omeprazole is usually administered as encapsulated enteric-coated granules and enteric-coated tablets because of its acid-labile nature. For children and patients who can not swallow, it can be mixed with water or other liquid after a capsule is opened or a tablet is crushed. This study was performed to compare omeprazole liquid formulations of tablet and capsule Omeprazole 20 mg capsule containing enteric coated granules was opened and 20 mg entric-coated tablet was ground to be mixed with sodium bicarbonate solution, orange juice or water. Each liquid formulation was poured into dissolution tester, mixed with first solution (artificial gastric juice; pH 1.2) for two hours, then with second solution (artifical enteric juice; pH 6.8) for thirty minutes. pH was measured periodically for two and half hours. Samples were drawn periodically, mixed with lansoprazole as an internal standard, and injected to HPLC. As results, pH of sodium bicarbonate solution of omeprazole was significantly higher than that of orange juice or water in first solution (6.2-7.4 vs. 1.2, p<0.005). At 150 min, concentrations of omeprazole in three diluents with granules and in sodium bicarbonate solution of tablet powder sustained significantly higher than in other solution of tablet powder (p<0.001). In conclusion, enteric-coated granules from capsule with three diluents and powder from tablet in sodium bicarbonate solution was stable during dissolution test, which would be appropriate and recommended for patient who can not swallow solid preparations.

• Korean Journal of Bronchoesophagology
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• v.9 no.1
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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.

• Proceedings of the KOR-BRONCHOESO Conference
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• 2002.12a
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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.

• Analytical Science and Technology
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• v.32 no.5
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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.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.22
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• pp.9909-9913
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• 2014

Background: Helicobacter pylori (H. pylori) remains an important cause of gastric cancer and peptic ulcer disease worldwide. Treatment of H. pylori infection is one of the effective ways to prevent gastric cancer. However, standard triple therapy for H. pylori eradication is no longer effective in many countries, including Thailand. This study was designed to evaluate the efficacy of adding bismuth and probiotic to standard triple therapy for H. pylori eradication. Materials and Methods: In this prospective single center study, H. pylori infected gastritis patients were randomized to receive 7- or 14-day standard triple therapy plus bismuth with probiotic or placebo. Treatment regimen consisted of 30 mg lansoprazole twice daily, 1 g amoxicillin twice daily, 1 g clarithromycin MR once daily and 1,048mg bismuth subsalicylate twice daily. Probiotic bacteria composed of Bifidobacterium lactis, Lactobacillus acidophilus and Lactobacillus paracasei. Placebo was conventional drinking yogurt without probiotic. CYP2C19 genotyping and antibiotic susceptibility tests were also done. H pylori eradication was defined as a negative $^{13}C$-urea breath test at least 2 weeks after completion of treatment. Results: One hundred subjects were enrolled (25 each to 7- and 14-day regimens with probiotic or placebo). Antibiotic susceptibility tests showed 36.7% metronidazole and 1.1% clarithromycin resistance. CYP2C19 genotyping revealed 40.8%, 49% and 10.2% were rapid, intermediate and poor metabolizers, respectively. The eradication rates of 7- or 14 regimens with probiotics were 100%. Regarding adverse events, the incidence of bitter taste was significantly lower in the 7- day regimen with the probiotic group compared with 7- day regimen with placebo (40% vs. 64%; p=0.04). Conclusions: The 7-day standard triple therapy plus bismuth and probiotic can provide an excellent cure rate of H. pylori (100%) in areas with low clarithromycin resistance such as Thailand, regardless of CYP2C19 genotype. Adding a probiotic also reduced treatment-related adverse events.