• YAKHAK HOEJI
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• v.37 no.4
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• pp.331-340
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• 1993

Inclusion complex of omeprazole(OMZ) with hydroxypropyl-$\beta$-cyclodextrin(HP-$\beta$-CD) was prepared by freeze-drying method. The complexation was confirmed by means of UV, CD, IR, DSC, XRD and $^{1}$H-NMR spectra. The benzimidazole moiety of OMZ might be found to be included into the cavity of HP-$\beta$-CD and the inclusion complex appeared to be $A_{L}$ type. The stoichiometric ratio of OMZ : HP-$\beta$-CD was found to be 1:1, and the stability constants of the inclusion complex by solubility and UV method were about 34 and 45 M$^{-1}$, respectively. The dissolution of OMZ was significantly enhanced from powder and. yablet of OMZ-HP-$\beta$-CD complex when compared to those of OMZ alone, and oil-to-water partition coefficient of OMZ-HP-$\beta$-CD complex was significantly higher than that of OMZ alone. Therefore, it was expected that the bioavailability of OMZ could be improved markedly by inclusion complexation of OMZ with HP-$\beta$-CD.

• The Korean Journal of Physiology and Pharmacology
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• v.16 no.6
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• pp.455-462
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• 2012

This study was designed to determine the protective effect of Rumex Aquaticus Herba extracts containing quercetin-3-${\beta}$ -D-glucuronopyranoside (ECQ) on experimental reflux esophagitis. Reflux esophagitis was induced by surgical procedure. The rats were divided into seven groups, namely normal group, control group, ECQ (1, 3, 10, 30 mg/kg) group and omeprazole (30 mg/kg) group. ECQ and omeprazole groups received intraduodenal administration. The Rats were starved for 24 hours before the experiments, but were freely allowed to drink water. ECQ group attenuated the gross esophagitis significantly compared to that treated with omeprazole in a dose-dependent manner. ECQ decreased the volume of gastric juice and increased the gastric pH, which are similar to those of omeprazole group. In addition, ECQ inhibited the acid output effectively in reflux esophagitis. Significantly increased amounts of malondialdehyde (MDA), myeloperoxidase (MPO) activity and the mucosal depletion of reduced glutathione (GSH) were observed in the reflux esophagitis. ECQ administration attenuated the decrement of the GSH levels and affected the MDA levels and MPO activity. These results suggest that the ECQ has a protective effect which may be attributed to its multiple effects including anti-secretory, anti-oxidative and anti-inflammatory actions on reflux esophagitis in rats.

• Korean Journal of Clinical Pharmacy
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• v.7 no.1
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• pp.40-44
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• 1997

Helicobacter pylori(HP) has been implicated as the cause of acute and chronic gastritis, peptic ulcer, and gastric carcinoma. To date the most successful treatment in eradicating HP is known to be the combination of two or more antibiotics with an anti-ulcer drug. In this study, in vitro antimicrobial activity against two was assessed, when proton pump inhibitors (PPIs), omeprazole and lansoprazole, were added to antibiotics at different concentrations. The assays in the absence of PPIs gave minimum inhibitory concentration(MIC) value of 0.63 mg/l for amoxicillin, 4 mg/l for tetracycline, 0.08 mg/l for clarithromycin and 0.16 mg/l for azithromycin. At the concentrations of 125 mg/l, 25 mg/1 and 0.5 mg/l of omeprazole, and the concentrations of 31.25 mg/l, 6.25 mg/l and 1 mg/l of lansoprazole, the MICs of clarithromycin and azithromycin were reduced by $50\%$. Also, lansoprazole at the highest concentration 31.25 mg/l reduced the MIC of amoxicillin by $50\%$, and omeprazole at the highest concentration of 125 mg/l reduced the MIC of tetracycline by $50\%$. In conclusion, the in vitro combination of PPIs and antibiotics led to improvement in the MIC of antibiotics against HP associated gastric disease.

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.19-29
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• 1995

The study was carried out to develop useful formulation for omeprazole(OMP) through OMP-ethylendiamine complex(OMPED), and the pharmaceutical properties of formula were tested to find out the difference in vivo behaviors of formulations between the free and complexed OMP. Oral and suppository dosage forms were also formulated and the dissolution profiles and pharmacokinetic parameters were measured to observe the difference in bioavailability between the free and complex form, and the correlation between dissolution rate and bioavailability was evaluated. The results are summarized as follows; In the case of formulation for oral administration, the release of OMP from enteric OMPED pellets was found satisfactory to the requirement standard and no decomposition of OMP in the pellets was found in acidic solution. Therefore the enteric OMPED pellets are anticipated to be a stable formulation. The release of OMP from OMPED tablet with chitosan as excipient and coated with cellulose acetate phthalate was found to be significantly retarded. The results of bioavailability test for OMP and OMPED tablets with lactose-excipient showed that the AUC value of OMP tablet was $116.89\;{\mu}g\;{\cdot}\;min/ml$, that of OMPED tablet was $161.10\;{\mu}g\;{\cdot}\;min/ml$, respectively. The reason why was thought that OMP decomposes more readily in body than OMPED, and the AUC of the tablet with chitosan-excipient and coated with cellulose acetate phthalate was most enhanced. In the case of bioavailability for suppositories with OMP, $OMP-{\beta}\;-cyclodextrin$ complex and OMPED, the AUC of OMPED suppository was most increased. From the above results, it is thought that the more stable and bioavailable oral or rectal dosage forms could be developed by using the OMPED as a potential OMP complex.

• The Journal of Korean Medicine
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• v.31 no.5
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• pp.64-81
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• 2010

Objectives: The object of this study was to observe the suppressive effects of Yijintang-gamibang (YJGMB), Yijintang being traditionally used in the Korean Medicine for treating various digestive diseases, on the rat reflux esophagitis (RE) as compared with omeprazole, a well-known proton pump inhibitor. Methods: Three different dosages of YJGMB, 50, 100 and 200 mg/kg, were orally pretreated once a day for 28 days before pylorus and forestomach ligation. Seven groups of 8 rats each were used in the study. Six hrs after pylorus and forestomach ligation, changes to the stomach and esophagus lesion areas, gastric volumes, acid and pepsin outputs, invasive lesion percentages, fundic mucosa, esophageal submucosa and total thicknesses were measured by histomorphometry. The results were compared with omeprazole 10 and 30 mg/kg treated groups in which the effects on RE were already confirmed. Results: As results of pylorus and forestomach ligation, marked increases of esophageal and gastric mucosa lesion areas, gastric volumes, acid outputs, pepsin outputs were observed with histopathological changes of RE, such as hemorrhages, ulcerative lesions and edematous changes on the esophageal and fundic mucosa. However, these pylorus and forestomach ligation induced RE were dose-dependently inhibited by treatment of 50, 100 and 200 mg/kg of YJGMB. YJGMB 50 mg/kg showed similar suppressive effects as 30 mg/kg of omeprazole, but more favorable effects were observed as compared with omeprazole 10 mg/kg. Conclusion: The results suggest that YJGMB showed favorable suppressive effects on the RE induced by pylorus and forestomach ligation. It is therefore expected that YJGMB will show favorable effects on RE as corresponds to the suggestion of traditional Korean medicine. However, more detailed mechanism studies should be conducted in future with the screening of the biological active chemical compounds in herbs.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.3
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• pp.416-425
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• 2010

The object of this study was to observe the protective effects of Yijin-tang-gamibang (YJGMB), Yijin-tang has been traditionally used in the 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 YJGMB extracts, 200, 100 and 50 mg/kg, were orally pretreated, once a day for 28 days before pylorus and forestomach ligation. Seven 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 and 10 mg/kg treated group. YJGMB 200 mg/kg were showed similar protective effects as compared with 30 mg/kg of omeprazole but more favorable effects were observed in 200, 100 and 50 mg/kg of all YJGMB treated rats as compared with omeprazole 10 mg/kg in the present study. In addition, YJGMB 200 mg/kg were showed more favorable antioxidant effects as compared with 30 mg/kg of omeprazole in the present study. Detail mechanism studies should be conduced in future with the screening of the biological active chemical compounds in herbs.

• Journal of Pharmaceutical Investigation
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• v.23 no.3
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• pp.127-132
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• 1993

The effect of omeprazole (OPZ) suppository on rat rectal mucosa was investigated microscopically. The suppository was prepared with Witepsol H15 base by molding method. Rectal irritation was evaluated according to defined pathological features. The suppository produced a slight damage to the rectal mucosa at 1 hr after the interectal administration, which was almost completely recovered within 24 hr. The damage was not due to OPZ but due to suppository base, Witepsol H15, itself, since Witepsol H15 suppository without OPZ produced the same damage. Therefore, it was concluded that OPZ itself has no rectal mucosa-irritating effect and thus can be developed as a suppository dosage form without any further toxicity problems.

• YAKHAK HOEJI
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• v.37 no.5
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• pp.427-436
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• 1993

The pharmacokinetics and relationship between in vitro dissolution and in vivo fraction absorbed were investigated after intravenous(iv) injection of omeprazole(OMZ), oral administration of OMZ capsules and rectal administration of 8 types of suppositories. The plasma concentration of OMZ (C$_{p}$)-time (t) curve after iv. administration fitted a two-compartment open model and the equation which best fitted the pharmacokinetics of OMZ was $C_{p}$ = 13.936 $e^{-8.78t}$+2.973 $e^{-0.716t}$. The bioavailabilities of OMZ in Witepsol H15 base (Supp-2) and PEG 4000 base (Supp-6) suppositories were 40.7% and 33.4%, respectively, which are higher(p<0.001) than 13% of oral administration of capsule. The avoidance fractions of the first-pass metabolism for Supp-2 and Supp-6 suppositiories were 31.8% and 23.4%, respectively, suggesting that the rectal application of OMZ may be a more adequate route of administration than oral one.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.458-461
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• 1994

A new high-performance liquid chromatographic method with column switching has been onto a Bondapak phenyl/corsil $(37-50{\;}{\mu}m)$ precolumn and polar plasma components were washed with 0.06 M borate burffer. After valve switching, the concentrated drug were eluted in the back-flush mode and separated on a ${\mu}-Bondapak$ C18 column with acetonitrilke-phosphate buffer as the mobile phae. The method showed excellent precision, accuracy and speed with detection limit of $0.01{\;}{\mug}/ml^{-1}$. Total analysis time per smaple was less than 20 min and the coefficients of variation for intra and inter-assay were less than 5.635. This method has been successfully applied to plasma smaples from eats after oral administration of omeprazole.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.4
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• pp.714-719
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• 2002

To examine effects of Whadamcheongwha-tang(WDCWT) extract, the mice investigated the gastrin and histamine secreting cells of the stomach by immunohistochemical method, and the lymphocytes of the spleen and thymus by flow cytometry after the oral administration of WDCWT extract(0.2ml/day) and omeprazole (1mg/day) for 7, 14 and 21 days. The result are as follows; 1. When WDCWT extract was administrated for 7 days, in result, gastrin secreting cells were unchanged. When omeprazole was administrated for 7 and 14 days, gastrin secreting cells were slightly increased than that of normal control group. When WDCWT extract was administrated for 21 days, in result, gastrin secreting cells were significantly increased 1.9 times than that of normal control group. When omeprazole was administrated for 21 days, gastrin secreting cells were increased 1.96 times than that of normal control group. 2. When WDCWT extract and omeprazole were administrated for 7 days, in result, histamine secreting cells were unchanged. When WDCWT extract was administrated for 21 days, in result, histamine secreting cells were significantly increased 1.9 times more than that of normal control group. When omeprazole was administrated for 21 days, in result, histamine secreting cells were increased 2.1 times compared with normal control group. 3. When WDCWT extract administrated for 7, 14 and 21 days, in result, splenic Band T lymphocytes, especially T/sub H/ lymphocytes were significantly increased compared with normal control group, and thymic T/sub H/ lymphocytes were also increased in WDCWT administrated group for 14 days. The results suggest that WDCWT extract inhibit a gastric acid secretion in mice stomach, and is useful in the treatment of the hyperacidity and gastric ulcer.