• Archives of Pharmacal Research
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• v.18 no.4
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• pp.219-223
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• 1995

Rectal absorption of opeprazole, a proton pump inhibitor, from suppositories was studied in rabbits. The suppositories were prepared by the conventional melting method with two types of bases, water-soluble polyethylene glycol (PEG) 4000 and oil-soluble Witepsol H15 bases, and administered intractally (ir) to rabbits at a dose of 10 mg omeprazole/kg. The plasma omeprazole concentration-time profiles of the two suppositories were compared with those following intravenous 9iv) administration of the same dose. There were no significant differences between the two suppositories in bioabailabilities and peak plasma concentrations $(C_{max})$. Bioavaiabilities and $C_{max}$ of PEG- and Witpsol suppositories were 30.3 and 33.9%, and 7.0 and $5.6\mug/ml$, resepectively. However, PEG suppository showed significantly (p<0.05) shorter time to reach peak plasma concentration $(T_{max})$ mean absorption time (MAT) and mean residence time in the plasma (MRT) than Witepsol suppository. The $T_{max}$ MRT nad MAT were 25.0, 83.0 and 38.5 min for PEG syppository, but were 90.0, 122.5 and 78.0 min for Wiepsol supposiotory, respectively. These differences between thw two suppositories could be explanined by the difference in the in vitro dissolution rates between the suppositories. The dissolution of omeprazole form PEG suppository was reportedly much faster than that from Witepsol suppository. It suggests that plasma profiles of omeprazole, especially $C_{max}$ MAT and MRT, could be controlled by modifying the in vitro dissolution rate of the drug from the suppositories. Above results suggest that rectal suppository is worth developing as an alternative dosage form of omeprazole to the conventional oral preparations which need sophisticated treatments, such as enterix coating, to prevent acid degradation of the drug in the stomach fluid.

• Journal of Veterinary Science
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• v.23 no.2
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• pp.19.1-19.9
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• 2022

Background: Gastric ulcer is one of the prevalent diseases in racehorses. However, it has not been recognized as important in Korea, and drugs used to treat gastric ulcers are included in the doping test list, so they are not allowed to be administered to racehorses in training. Objectives: This study was performed 1) to investigate the prevalence and the severity of gastric ulcers in Thoroughbred racehorses in Korea, 2) to confirm the therapeutic effect of ranitidine and omeprazole, and 3) to compare the efficacy between ranitidine and omeprazole. Methods: Forty-nine horses were randomly recruited, and gastroscopy was performed within two days after racing. Twelve horses with a sum grade of five or higher were randomly assigned to two treatment groups. Seven horses were administered ranitidine, and five horses were administered omeprazole. Follow-up gastroscopy was scheduled within one to five days after finishing the treatment. Results: The prevalence of gastric ulcer in Korean Thoroughbred racehorses after racing was 100%, and the grade was more severe in the non-glandular region than in the pyloric region. There was no correlation between the severity of gastric ulcer in the two regions. Omeprazole had a greater therapeutic effect than ranitidine. Conclusions: This study shows the importance of recognizing gastric ulcers as an important factor, and omeprazole as a possible treatment option in Korea, as it has been removed from the list of prohibited substances for racehorses. Thus, the use of omeprazole is currently recommended until one day before the race.

• The Korean Journal of Physiology and Pharmacology
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• v.5 no.4
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• pp.315-321
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• 2001

This study was aimed to evaluate the effects of quercetin and desferrioxamine on the development of the reflux esophagitis induced surgically, on gastric secretion and on lipid peroxidation which is a marker of oxidative stress. Omeprazole was used as a positive control drug. Omeprazole significantly and dose-dependently prevented the development of reflux esophagitis, but quercetin or desferrioxamine prevented only at high dose. Omeprazole significantly and dose-dependently inhibited the gastric acid secretion (gastric volume, pH and acid output), but quercetin or desferrioxamine did not inhibit. Malonyldialdehyde content, the end product of lipid peroxidation, increased significantly after the induction of reflux esophagitis. Omeprazole prevented lipid peroxidation. Quercetin and desferrioxamine inhibited the lipid peroxidation independent of their actions on gastric secretion. This result indicates that omeprazole confirmed preventing effect of rat reflux esophagitis, but quercetin and desferrioxamine inhibited esophagitis by reduction of lipid peroxidation irrespective of gastric acid secretion.

• Archives of Pharmacal Research
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• v.18 no.3
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• pp.141-145
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• 1995

Omeprazole, a proton pump inhibitor, was given intravenously (iv), orally (po), intraperitoneally (ip), hepatoportalvenously (pv), and intrarectally (ir) to rats at a dose of 72mg/kg in order to investigate the bioavailability of the drug, The extent of bioavailabilities of omeprazole administered through pv, ip, po, and ir routes were 88.5, 79.4, 40,8, and 38.7%, respectively. Pharmacokinetic analysis in this study and literatures (Regardh et al., 1985 : Watanabe et al., 1994) implied significant dose-dependency in hepatic first-pass metabolism, clearance and distribution, and acidic degradation in gastric fluid. The high bioavailability from the pv administration (88.5%) means that only 11.5% of dose was extracted by the first-pass metabolism through the liver at this dose (72 mg/kg). The low bioavailability from the oral administration (40.8%) in spite of minor hepatic first-pass extraction indicates low transport of the drug from GI lumen to portal vein. From the literature (Pilbrant and Cederberg, 1985), acidic degradation in gastric fluid was considered to be the major cause of the low transport. Thus, enteric coating of oral preparations would enhance the oral bioavailability substantially. The bioavailability of the drug from the rectal route, in which acidic degradation and hepatic first-pass metabolism may not occur, was low (38.7%) but comparable to that from the oral route (40.8 %) indicating poor transport across the rectal membrane. In this case, addition of an appropriate absorption enhancer would improve the bioavailability. Rectal route seems to be an possible alternative to the conventional oral route for omeprazole administration.

• Korean Journal of Clinical Pharmacy
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• v.10 no.2
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• pp.68-73
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• 2000

The bioequivalence of two omeprazole preparations was evaluated following their oral administration to 16 normal volunteers. The test product was 'Ulpro tablet' made by Boryung Pharmaceutical Co. and the reference was 'Losec capsule' made by Yuhan Corp. After one capsule or tablet containing 20 mg omeprazole was administered, blood was taken at predetermined time intervals and the concentration of the drug in plasma was determined with an HPLC method. AUC and $C_{max}$ were determined and analyzed statistically for the evaluation of bioequivalence of the two products. The differences in AUC and $C_max$ between two products were $0.45\%\;and\;2.83\%$, respectively. The powers for AUC and $C_{max}\;were\;89.2\%\;and\;>90\%$, respectively. Confidence intervals were within $20\%$ for AVC and $C_{max}$All of these parameters met the criteria of KFDA for bioequivalence, indicating that 'Ulpro tablet' is bioequivalent to 'Losee capsule.'

• The Journal of Internal Korean Medicine
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• v.34 no.2
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• pp.165-177
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• 2013

Objectives : The object of this study was to observe the protective effects of 8 types of individual herbal components of Yijintang-gamibang, on the reflux esophagitis (RE) in rats as compared with omeprazole. Methods : Each 100 mg/kg individual herbal component was orally pretreated, at 1 hr before and 6 hrs after pylorus and forestomach ligation, the changes on the esophageal lesion areas, gastric volumes, acid and pepsin outputs, antioxidant effects, esophageal total hexose and sialic acid contents were observed with changes on the esophageal histopathology. The results were compared with an omeprazole 10 mg/kg treated group. Results : Pylorus and forestomach ligation-induced RE were inhibited by treatment of all 8 herbal components and omeprazole except for Pinella Rhizoma and Massa Meicata Fermentata, in order of Atractylodis Rhizoma, Citri Pericarpium, omeprazole, Glycyrrhizae Radix, Hordei Fructus Germiniatus, Holelen and Citri Pericarpium, as compared with RE control. Pinella Rhizoma and Massa Meicata Fermentata did not show any favorable protective effects against RE nor antioxidant effects in the present study. Conclusions : The main active herbal components showing favorable protective effects on RE of Yijintang-gamibang mediated by antioxidant effects, were Atractylodis Rhizoma, Citri Pericarpium, Glycyrrhizae Radix, Hordei Fructus Germiniatus, Holelen and Citri Pericarpium. Furthermore Atractylodis Rhizoma and Citri Pericarpium showed more favorable protective effects as compared with omeprazole, therefore, it is expected that Atractylodis Rhizoma and Citri Pericarpium have potential as new alternatives or safe therapeutics against RE.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.227-237
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• 1995

Omeprazole(OMP) complexes such as inclusion complexes of OMP with $hydroxypropyl-{\beta}-cyclodextrin$(HPCD) and ${\beta}-cyclodextrin({\beta}-CD)$, OMP-cholestyramine(CHL) and OMP-ethylenediamine(OMP-ED) were prepared, respectively. The partition coefficients in Witepsol H-15 /pH 7.4 phosphate buffer solution of OMP complexes$(OMP-HPCD;\;3.69{\pm}0.26,\;OMP-{\beta}-CD;\;4.08{\pm}0.21,\;OMP-CHL;\;4.36{\pm}0.25\;and\;omeprazole\;sodium(OMP-Na);\;3.64{\pm}0.37)$ were higher than that of OMP $(2.66{\pm}0.47)$. OMP was not completely dissolved until even 3 hrs, but all the OMP complexes studied were released about 100% in 20 min. The rectal suppositories containing OMP or each above OMP complex were prepared using Witepsol H-15 base, and their dissolution and stability were examined, and pharmacokinetic study were investigated after their rectal administrations to the rabbits. While the suppository containing OMP was released only less than 60% in 150 min, $OMP-{\beta}-CD$, OMP-CHL, OMP-Na and OMP-ED suppositories were all released about 65% in 20 min. Especially, OMP-HPCD suppository released OMP about 70% in 10 min. All the additives such as sodium laurylsulfate, eglumine, arginine and PVP increased drug release from OMP-HPCD suppository to some extent. The decomposition rate constants of OMP in the suppositories were $9.117{\times}10^{-3}\;day^{-l}$ for OMP suppository, $2.121{\times}10^{-2}$ for OMP-HPCD, $1.607{\times}10^{-2}$ for $OMP-{\beta}-CD$, $9.26{\times}10^{-3}$ for OMP-Na, $6.769{\times}10^{-3}$ for OMP-CHL and $5.58{\times}10^{-3}\;day^{-l}$ for OMP-ED suppository, respectively. Additives such as arginine, eglumine and ED had some stabilizing effect for OMP-HPCD, OMP-CHL and OMP-Na suppositories, respectively. After 6 month-storage at $30^{\circ}C$, 75% RH, OMP-CHL suppository was most stable. The values of Tmax for OMP-HPCD and OMP-Na suppositories were $11.7{\pm}2.36\;and\;11.4{\pm}2.56\;min$, respectively. The values of Cmax for OMP-HPCD and OMP-CHL suppository were $2.31\;{\mu}g/ml\;(p<0.01)\;and\;1.89\;{\mu}g/ml\;p<0.01)$, respectively. The values of AUC for OMP and $OMP-{\beta}-CD$ suppository were $61.9{\pm}25.79\;and\;68.6{\pm}29.48\;{\mu}g\;{\cdot}\;min/ml$, and the corresponding values for OMP-HPCD and OMP-CHL were $106.1{\pm}43.16\;(p<0.05)\;and\;127.3{\pm}42.52\;{\mu}g\;{\cdot}\;min/ml(p<0.01)$, respectively. The above results indicate the OMP-HPCD and OMP-CHL suppositories have the excellent bioavailabilties in vivo study.

• Pediatric Gastroenterology, Hepatology & Nutrition
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• v.3 no.1
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• pp.23-29
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• 2000

Purpose: It has recently been recognized that Helicobacter pylori (H. pylori) is an important factor in the pathogenesis of recurrent abdominal pain (RAP) in children. But, the best treatment for H. pylori infection is still unsettled. This study was performed to evaluate the efficacy of 2 weeks dual therapy with proton pump inhibitor (PPI) and amoxicillin for children with H. pylori infection associated with RAP. Method: Our study included 24 children with RAP who were H. pylori positive assessed by CLO test and histologic examination (silver stain). We used the regimen consisted of PPI (omeprazole, 0.7 mg/kg/day) and amoxicillin (50 mg/kg/day) for 2 weeks to eradicate H. pylori. Eradication of H. pylori was determined 4 weeks after the termination of treatment using the CLO test and histologic examination. Results: The endoscopic diagnoses of patients were nodular gastritis in 11 cases, superficial gastritis in 7 cases, peptic ulcer in 4 cases and normal finding in 2 cases. H. pylori was eradicated in 12 cases by omeprazole and amoxicillin dual therapy for 2 weeks and the eradication rate was 50%. In 4 of 12 children in whom H. pylori had not been eradicated with that regimen, we successfully eradicated H. pylori with other regimens of which 2 or 3 drugs among omeprazole, amoxicillin, clarithromycin, colloidal bismuth subcitrate ($Denol^{(R)}$) and metronidazole were used. Conclusion: The dual therapy with PPI and amoxicillin for 2 weeks had no clear advantage over other regimens for the eradication of H. pylori infection in children. We concluded that the combi-nation of PPI and amoxicillin for 2 weeks is not so good for H. pylori eradication as other commonly used regimens.

• YAKHAK HOEJI
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• v.44 no.1
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• pp.16-21
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• 2000

Peptic ulcer is involved with Helicobacter pylori infection and antibiotic regimens are primary treatments. An optimal therapeutic regimen for eradication of Helicobacter pylori remains uncertain due to variable efficacy. The objectives of this study were to evaluate the efficacy of omeprazole based antibiotic regimens in bacterial eradication, healing of peptic ulcer and to identify factors affecting efficacy. Seventy-seven patients were enrolled in the prospective, open-trial from November 1997 to Setember 1998. H. pylori infection was identified with endoscopy, H. pylori stain and rapid urease test. The first group (OAC7) received omeprazole 20 mg twice daily for 4 weeks which were the same schedule for all, amoxicillin and clarithromycin 500 mg three times daily for 1 week; the second group (OAC14), for 2 weeks on the same regimen as the first; and the last group (OACD) has taken bismuth in addition to the OAC7 regimen for 1 week. Eradication of H. pylori and healing of peptic ulcer were evaluated with endoscopy and tests for H. pylori before and after treatments. There were no significant differences in eradication rates; 77% in OAC7, 76% in OAC14, 81% in OACD (p=0.935) and healing rates; 82% in OAC7, 71% in OAC14, 95% in OACD (p=0.179), respectively. Compliance had an relationship with eradication rates significantly among regimens (p=0.049). Twenty three cases (29%) complained of the minor side effects. In conclusion, OAC7 was better in convenience of dosing schedule and showed fewer side effects with shorter duration and lower cost while There were no significant differences in efficacy among regimens.

• 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.