• Proceedings of the Korean Society of Veterinary Clinics Conference
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• 2009.04a
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• pp.229-229
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• 2009

• Archives of Pharmacal Research
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• v.28 no.10
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• pp.1196-1202
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• 2005

Omeprazole (OMP) is a proton pump inhibitor used as an oral treatment for acid-related gastrointestinal disorders. In the liver, it is primarily metabolized by cytochrome P-450 (CYP450) isoenzymes such as CYP2C19 and CYP3A4. 5-Hyroxyomeprazole (5-OHOMP) and omeprazole sulfone (OMP-SFN) are the two major metabolites of OMP in human. Cimetidine (CMT) inhibits the breakdown of drugs metabolized by CYP450 and reduces, the clearance of coad-ministered drug resulted from both the CMT binding to CYP450 and the decreased hepatic blood flow due to CMT. Phenobarbital (PB) induces drug metabolism in laboratory animals and human. PB induction mainly involves mammalian CYP forms in gene families 2B and 3A. PB has been widely used as a prototype inducer for biochemical investigations of drug metabolism and the enzymes catalyzing this metabolism, as well as for genetic, pharmacological, and toxicological investigations. In order to investigate the influence of CMT and PB on the metabolite kinetics of OMP, we intravenously administered OMP (30 mg/kg) to rats intraperitoneally pretreated with normal saline (5 mL/kg), CMT (100 mg/kg) or PB (75 mg/kg) once a day for four days, and compared the pharmacokinetic parameters of OMP. The systemic clearance ($CL_{t}$) of OMP was significantly (p<0.05) decreased in CMT-pretreated rats and significantly (p<0.05) increased in PB-pretreated rats. These results indicate that CMT inhibits the OMP metabolism due to both decreased hepatic blood flow and inhibited enzyme activity of CYP2C19 and 3A4 and that PB increases the OMP metabolism due to stimulation of the liver blood flow and/or bile flow, due not to induction of the enzyme activity of CYP3A4.

• Journal of Pharmacopuncture
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• v.22 no.1
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• pp.49-54
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• 2019

Objective: Antibiotic resistance is a global health problem and threatens health of societies. These problems have led to a search for alternative approaches such as combination therapy. The aim of the present study was to investigate the effect of caffeine and omeprazole in combination with gentamicin or ciprofloxacin against standard and clinically resistant isolates of Staphylococcus aureus and Escherichia coli. Methods: The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of different agents against bacterial strains were determined. The interaction of non- antibiotic drugs with gentamicin and ciprofloxacin was studied in vitro using a checkerboard method and calculating fraction inhibitory concentration index (FICI). Verapamil as efflux pump inhibitor was used to evaluate the possible mechanism of bacterial resistance to antibiotics. Results: The MIC and MBC values of gentamicin against bacterial strains were in the range of $20-80{\mu}g/ml$ and $40-200{\mu}g/ml$, respectively. Caffeine and omeprazole had no intrinsic inhibitory activity against tested microorganisms. However, upon combination of caffeine with antibiotics, the synergistic effects were observed. Verapamil was able to reduce the MIC values of gentamicin (4 folds) only in some bacterial strains. Conclusion: These findings indicated that caffeine was effective in removing bacterial infection caused by S. aureus and E. coli. The relevant mechanisms of antibiotic resistance were not related to the drug efflux.

• Pediatric Gastroenterology, Hepatology & Nutrition
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• v.5 no.1
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• pp.19-25
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• 2002

Purpose: The triple therapy with proton pump inhibitor (PPI) has been recognized as the treatment of choice in Helicobacter pylori (H. pylori) infection in adults. However, the effect of triple therapy with omeprazole, amoxicillin and clarithromycin (OAC) on eradication of H. pylori infection in children has not been established yet. This study was performed to evaluate the efficacy of OAC triple therapy and to compare the effect of one-week with two-week therapy on H. pylori eradication. Methods: From July 1998 to July 2000, 34 children with upper gastrointestinal symptoms, who underwent upper gastrointestinal endoscopy with biopsy at entry and 4 or more weeks after therapy, were enrolled in this study. H. pylori infection was assessed by CLO test and histologic examination (Hematoxylin-Eosin stain or Alcian yellow stain) with biopsy specimens. The regimen consisted of omeprazole (0.7 mg/kg/day), amoxicillin (50 mg/kg/day), and clarithromycin (25 mg/kg/day) for 1 week (n=21) or 2 weeks (n=13). Eradication of H. pylori was determined after the termination of treatment by the CLO test and histologic examination. Results: One-week treatment group consisted of 21 children (11 male, 10 female) with a mean age of $9.5{\pm}3.0$ years. Two-week group consisted of 13 children (4 male, 9 female) with a mean age of $9.9{\pm}4.0$ years. The endoscopic diagnoses included nodular gastritis in 19 cases, superficial gastritis in 7 cases, gastric ulcer in 4 cases, purpuric duodenitis in 2 cases, and normal in 2 cases. H. pylori was eradicated in 28 of total 34 children (82.4%). In 1-week group, H. pylori was eradicated in 17 of 21 children (81%). In 2-week group, H. pylori was eradicated in 11 of 13 children (84.6%). In remaining 6 cases in whom H. pylori had not been eradicated with OAC regimen, H. pylori infection persisted despite of the treatment with additional drugs such as colloidal bismuth subcitrate ($Denol^{(R)}$) and metronidazole. Conclusion: In this study, eradication rate of H. pylori with OAC regimen was 82.4%, and the triple therapy would be highly effective as primary treatment. However, there was no significant difference in the eradication rate between the 1-week and 2-week treatment group (P=0.785).

• Journal of Pharmaceutical Investigation
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• v.22 no.4
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• pp.281-287
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• 1992

Omeprazole (OMZ) is very unstable in acidic solution, which selectively inhibit the release of the gastric juice in the gastric mucosa, In order to stabilize (OMZ) in oral solid dosage form, the enteric-coated microcapsules and compression-coated OMZ tablets containing lysine or arginine as stabilizer were prepared and their dissolution and stability test were performed. The haif life of OMZ microcapsules containing arginine was 194 days at $30^{\circ}C$ and OMZ was completely released in 60 min. The half-lives of enteric coated and non-coated compression-coated OMZ tablets with lysine were 292 and 95 days at $30^{\circ}C$, respectively. The half-lives of enteric coated and non-coated compression-coated tablets with arginine were 1752 and 293 days at $30^{\circ}C$, respectively, and OMZ were released completely in 20 min in the 2nd fluid of K.P.VI. Consequently, the enteric-coated compression-coated OMZ tablets with arginine as stabilizer provided a good formulation for oral solid dosage form.

• The Korean Journal of Physiology and Pharmacology
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• v.17 no.5
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• pp.411-415
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• 2013

In this study, we investigated the protective action of glucuronopyranoside flavonoids (QGC, AGC, LGC) on gastritis in rats. QGC, AGC and omeprazole decreased the gastric volume significantly, and each $ID_{50}$ was 0.75, 0.54 and 8.5 mg/kg, respectively, thus the order of potency was AGC, QGC and omeprazole. They also decreased acid output, and each $ID_{50}$ was 7.81, 0.58 and 6.71 mg/kg, respectively, thus the order of potency was AGC, omeprazole and QGC. They inhibited gastritis induced by indomethacin, and it recovered significantly by increasing the GSH levels in gastritis. The gastric MPO activity in the gastritis group increased more than in the normal group. QGC, LGC, or AGC administration reduced moderately the MPO activity in a dose-dependent manner. This study demonstrated that AGC, QGC, or LGC showed potent efficacy on the gastritis, by preventing oxidative stress. These results suggest that QGC, AGC, or LGC have gastroprotective effect in rats.

• Journal of Physiology & Pathology in Korean Medicine
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• v.17 no.3
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• pp.672-676
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• 2003

To investigate the effect of acupuncture on Zusanli (ST 36) in this study, gastrin level of serum by radioimmunoassay was measured at 1, 3, 6 weeks in rats. In other groups, 1 mg/day omeprazole was administered for 1, 3, 6 weeks. Omeprazole increased significantly gastrin level of serum at 1, 3, 6 weeks in a time dependent manner. Acupuncture applied to the ST 36 acupoint decreased at 1, 3, 6 weeks. Furthermore, acupuncture applied to other acupoint, Yanglinquan (GB 34) did not produced significant effect. When the common peroneal nerve was dissected, acupuncture of ST 36 produced the change of gastrin level. These data suggest that acupuncture decreased gastrin level of serum in point specific way and that effect was not related with surrounding nerve.

• Journal of Physiology & Pathology in Korean Medicine
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• v.23 no.5
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• pp.1073-1079
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• 2009

The object of this study was to observe the protective effects of Yijin-tang-gamibang (YJGMB), Yijin-tang has been traditionally used as Korean medicine for treating various digestive diseases. The study showed that it is effective on reflux esophagitis induced by pylorus and forestomach ligation in rats. Three different dosages of Yijin-tang-gamibang extracts, 300, 150 and 75 mg/kg, were once orally administered 1 hour before pylorus ligation. 6 groups, each of 8 rats per group were used in the present study. The results were compared with Omeprazole, antioxidant and proton pump inhibitor, 30 mg/kg treated group. Yijin-tang-gamibang extracts 300 mg/kg were showed similar or slightly lower effects as compared with 30 mg/kg of omeprazole in the present study. Detail mechanism studies should be conduced in future with the efficacy tests of individual herbal composition of Yijin-tang-gamibang and the screening of the biological active compounds in herbs.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.132-132
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• 1995

OMPED의 결합비는 1:1 몰비로 복합체가 형성됨을 확인하였다. 수용액중(pH 7.0)에서 OMP는 분해속도 k=1.542$\times$$10^{-2}$$hr^{-1}$, shelf life=6.81hr 이었고 OMPED는 k=2.088$\times$$10^{-4}$$hr^{-1}$, shelf life=502.8hr이며 중성은 물론 약산성에서 안정하였다. HPMCP로 장용피한 OMPED pellet은 산저항성이 완벽하고 용출속도가 양호하였으며, OMPED 정제에서는 CAP로 코팅한 정제가 가장 큰 AUC값을 나타내었다. Witepsol H-15 기제를 사용한 각 좌제의 생체이용율은 OMPED 좌제가 86.53 $\mu\textrm{g}$ㆍmin/$m\ell$ 로서 OMP 좌제 61.9 $\mu\textrm{g}$ㆍmin/$m\ell$ 및 OMP-$\beta$-CD 좌제 68.8 $\mu\textrm{g}$ㆍmin/$m\ell$이다.

• Macromolecular Research
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• v.11 no.4
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• pp.283-290
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• 2003

Organic drugs including aspirin, omeprazole, and naproxen with three different levels of octanol/water partition coefficient were examined for their release behavior from the amphiphilic PCL-b-PEO-b-PCL (PCEC) matrix. Scanning electron micrograph (SEM) of PCEC illustrated a well defined two-phase morphology consisted of dispersed poly(ethylene oxide) (PEO) domain and continuous polycaprolactone (PCL) phase. Differential scanning calorimetry (DSC) and X-ray diffractometry (XRD) experiments veri tied that three model drugs are dissolved as a molecular dispersion in PCEC matrix. The release of hydrophilic aspirin closely followed the water absorption profile of the matrix indicating that its major fraction is present in PEO domain. However, substantial amount of aspirin present in less hydrophilic region displayed discontinuous biphasic release pattern. In the case of omeprazole with intermediate hydrophobicity consistent release behavior was observed for a period of 24 hrs after the rapid liberation of ca. 10% of the drug presumably partitioned in PEO phase. It was ascribed to the fact that the progressive hydration of PCEC matrix gradually increased the chance of drug/water exposure to compensate the exhaustion of device. Naproxen with the highest octanol/water distribution coefficient among three model drugs exhibited a limited release of 35% for 24 hrs. Finally, hydroxypropyl methylcellulose phthalate (HPMCP)/PCEC blend matrix demonstrated an accelerated and quantitative release of hydrophobic naproxen by generating high porosity and thereby expanding polymer/water interface.