• YAKHAK HOEJI
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• v.38 no.3
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• pp.250-264
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• 1994

Omeprazole(OMZ)-cholestyramine(CHL) and various OMZ-Dowex resin complexes were prepared by reaction between OMZ and activated resins in 0.1N NaOH solution. And their physical properties were tested by means of infrared(IR), differential scaning caloimeter(DSC), X-ray diffraction. Chemical stability of OMZ-CHL was increased markedly compared with OMZ and the decomposition of OMZ-CHL followed the pseudo first-order kinetics and the rate constants were $2.743{\times}10^{-4}/day$ at $20^{\circ}C$, $7.83{\times}10^{-3}day^{-1}$ under 80% RH and $1.68{\times}10^{-2}day^{-1}$ under UV radiation, respectively. On the other hand, the rate constants of OMZ were $2.996{\times}10^{-4}day^{-1}$ at $20^{\circ}C$, $1.17{\times}10^{-2}day^{-1}$ under 85% RH, and $4.07{\times}10^{-2}day^{-1}$ under UV radiation, respectively. The rates of dissolution of OMZ-CHL bulk and OMZ-CHL tablet were 100% and more than 85% in 15 minutes, respectively, which were increased than OMZ base and OMZ-tablet. In the acute toxicological test, the value of oral $LD_{50}$(mouse) was 4.608 g/kg. OMZ-CHL was pelletized using lactose, polyethyle neglycol(PEG), D-sorbitol, Avicel PH 101, sodium laurylsulfate and polyvinylpyrrolidone(PVP) K-30, and enteric coated with HPMCP, Myvacet, acetone, ethanol and cetanol, of which dissolution rate was found to be more than 85% in 10 minutes. From the above results, it was found that OMZ-CHL is a useful means for development of new oral dosage forms of OMZ.

• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.2
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• pp.198-204
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• 1994

This study was carried out to investigate the effect of the feeding mixture of linesed oil, rich in n-3 PUFA and the sunflower seed oil, rich in n-6 PUFA on the lipid metabolism in the dietary hypprlidemic rats. After male Sprague-Dawley rats were induced hyperlipidemia by feeding the diet containing lard, butter, and cholesterol for 3 weeks, then they were fed with the diet containing lard 3.0% and butter 12.0% for control, the mixture in different proportion of both linseed oil and sunflower seed oil, and antihyperlipidemic durgs for 2 weeks. Analysis of the lipid component and the fatty acid composition of the liver showed following results. Concentration s of the total cholesterol and phospholipid in liver were significantly higher in group 2 (olive oil 12.0%) and lower in the other groups than in the control group, especially lower in groups 3 (cholestyramine 2.0%) and 9 (sunflower seed oil 12.0%) . Concentration of triglyceride was lower in the other groups except group 4 (liparoid), especially lowe rin group 9 than in the control group. In the fatty acid composition of liver lipids, C18:2 was the major fatty acid. Contents of n-6 PUFA increased , while those of n-3 PUFA decreased in groups composition of the test lipids. From the data on concentration s of total cholesterol. Phospholipid and triglyceride in liver, we concluded that the feeding mixed with 3.0% lard and 12.0 % sunflower seed oil were most effective for the improvement of the live lipids. The fatty acid composition in liver lipids were affected by the fatty acid composition of the test lipids.

• Journal of The Korean Society of Clinical Toxicology
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• v.1 no.1
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• pp.47-50
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• 2003

Endosulfan, one of organochlorine insecticides, is $\gamma$-aminobutyric acid (GABA) antagonist. In sufficient dose, this pesticide lower the seizure threshold and produce CNS stimulation, with resultant seizures, respiratory failure, and death. In patients with endosulfan intoxication, the first manifestation of toxicity is largely a generalized seizure without prodromal signs or symptoms. So the management of airway and seizure control are essential for survival and prognosis of intoxicated patients. We report two cases of acute endosulfan poisoning who manifest 'status epilepticus' similarly, but have different prognosis.

• Archives of Pharmacal Research
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• v.9 no.1
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• pp.49-54
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• 1986

Effect of sodium taurodeoxycholate (TDC) infused intravenously on the pharmacokinetics of methylene blue (MB) was studied in the rat to investigate the role of ion-pair complexation in the body on drug elimination and disposition. Distribution volume (Vd) of MB was increased significantly (p< 0.05) by TDC infusion. Considering together with the fact that apparent partition coefficient (APC) of MB between phosphate buffer (pH 7.4) and n-octanol was increased markedly by TDC, the increase in Vd seemed to be the result of decreased polarity of MB by ion-pair formation with TDC. But total body clearance (CLt) and biliary excretion clearance (CLbil) of MB were not increased significantly by TDC.

• 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.

• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.1
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• pp.31-37
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• 1994

This study was carried out to investigate the effect of the feeding mixture of linseed oil, rich in n-3 PUFA and the sunflower seed oil, rich in n-6 PUFA on the lipid metabolism in the dietary hyperlipidemic rats. After male Sprague-Dawley rats were induced hyperlipidemia by feeding the diet containing lard, butter and cholesterol for 3 weeks, then they were fed with the diet containing lard 3 .0% and butter 12.0% for control, the mixture in different proportion of both linseed oil and sunflower seed oil and antihyperlipidemic drugs for 2 weeks. Analysis of the fatty acid composition of the serum lipoprotein fractions showed following results. In the fatty acid composition of serum lipoprotein , the proportion of C18:2 was dominant in all fractions, C20:5 in LDL and HDL fraction and C22:6 in chylomicron fraction. The ratio of n-3P/n-6P tended to increase gradually as it of the test lipid increased in groups 5 to 9 group and was affected by the fatty acid composition of the test lipids.

• Journal of the Korean Society of Food Science and Nutrition
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• v.23 no.2
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• pp.205-211
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• 1994

This study was carried out to investigate the effect of the feeding mixture of linseed oil, rich in n-6 PUFA on the lipid metabolism in the dietary hyperlipidemic rats. After male Sprague-Dawley rats were induced hyperlipidemia by feeding the diet containing lard, butter and cholesterol for 3 weeks. then they were fed with the diet containing lard 3.0% and butter 12.0% for control, the mixture in different proportion of both linseed oil and sunflower seed oil, and antihyperlipidemic drugs for 2 weeks. Analysis of the fatty acid composition of the brain and heart lipids showed following results. In the fatty acid composition of brain lipids, C20:4 and C22:6 were the major fatty acids but showed little difference among the groups. In the fatty acid of heart lipids,C18:2 was the major fatty acid. The proportion of C20:4 decreased gradually as n-3P/n-6P ratio of the test lipids increased in groups 5 (linseed oil 12.0%) to 9 (sunflower seed oil 12.0%) while the proportion of C22:6 was not affected by the fatty acid composition of the test lipids.

• BMB Reports
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• v.30 no.5
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• pp.370-377
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• 1997

A novel assay method is described for rapid quantitation of reaction rate of sterol ${\Delta}^7$-reductase (${\Delta}^7$-SR) which catalyzes reduction of the ${\Delta}^7$-double bond of sterols. Of six different organ tissues-liver, small intestine, brain, lung, kidney, and testis-. ${\Delta}^7$-SR activity was detected only in liver (2.30 nmol/min/mg protein) and testis (0.11 nmol/min/mg protein). Using a newly developed method which employs diet-induced enzyme proteins and ergosterol as substrate, we assessed both kinetics ($K_m=210\;{\mu}M$, $V_{max}=1.93\;nmol/min/mg$) and inhibition of the rat hepatic ${\Delta}^7$-SR against well-studied cholesterol lowering agents such as triparanol ($IC_{50}=16\;{\mu}M$). 3-$\beta$-[2-(diethylamino)ethoxy]androst-5-en-17-one (U18666A) ($IC_{50}=5.2\;{\mu}M$), and trans-1.4-bis(2-chlorobenzylaminomethyl)cyclohexane dihydrochloride (AY-9944) ($IC_{50}=0.25\;{\mu}M$). Of the three well-known AY-9944-sensitive cholesterogenic enzymes (i.e., ${\Delta}^7$-SR, sterol ${\Delta}^8$-isomerase, and sterol ${\Delta}^14$-reductase). ${\Delta}^7$-SR was found to be the most sensitive enzyme with a noncompetitive inhibition of this compound ($K_i=0.109\;{\mu}M$). Substrate specificity studies of the microsomal ${\Delta}^7$-SR indicate that the relative reaction rate for 7-dehydrocholesterol and ergosterol are 5.6-fold and 1.6-fold higher than that for lathosterol. ${\Delta}^7$-SR activity was also modulated by feeding rats a diet supplemented with 0.5% ergosterol (>2.6-fold) in addition to 5.0% cholestyramine plus 0.1% lovastatin ($\simeq$5.0-fold). Finally, microsomal ${\Delta}^7$-SR was solubilized by 1.5% 3-[3-(cholamidopropyl)-dimethylammonio]-1-propanesulfonate (CHAPS) and enriched on PEG (0~10%) precipitation, which should be suitable for further purification of the enzyme.

• Clinical Endoscopy
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• v.56 no.2
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• pp.194-202
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• 2023

Background/Aims: Endoscopic therapy for neoplastic Barrett's esophagus (BE) has become the standard of care over the past two decades. In clinical practice, we regularly encounter patients who fail to achieve complete squamous epithelialization of the esophagus. Although the therapeutic strategies in the individual stages of BE, dysplasia, and esophageal adenocarcinoma are well studied and largely standardized, the problem of inadequate healing after endoscopic therapy is only marginally considered. This study aimed to shed light on the variables influencing inadequate wound healing after endoscopic therapy and the effect of bile acid sequestrants (BAS) on healing. Methods: Retrospective analysis of endoscopically treated neoplastic BE in a single referral center. Results: In 12.1% out of 627 patients, insufficient healing was present 8 to 12 weeks after previous endoscopic therapy. The average follow-up duration was 38.8±18.4 months. Complete healing was achieved in 13 patients already after intensifying proton pump inhibitor therapy. Out of 48 patients under BAS, 29 patients (60.4%) showed complete healing. An additional eight patients (16.7%) improved, but only partial healing was achieved. Eleven (22.9%) patients showed no response to BAS augmented therapy. Conclusions: In cases of insufficient healing even under exhaustion of proton pump inhibitors, treatment with BAS can be an option as an ultimate healing attempt.

• Journal of the Korean Society of Food Science and Nutrition
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• v.22 no.5
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• pp.517-523
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• 1993

This study was designed to observe the efforts of the feeding Platycodon grandiflorum, Codonopsis ianceolata, perilla oil and safflower oil on the improvement of the lipids in the serum and liver of dietary hypercholes-terolemic rats. Experimental groups mixed with 5% cellulose+10% lard (group 1, control group), 2% cholestyramine＋10% lard (group 2), 5% C. Ianceolata+10％ perilla oil (group3). 5％ P. grandiflorum＋10% perilla oil(group 4), 5% C. ianceolata+10% safflower oil(group 5) and 5% P. grandiflorum＋10% safflower oil (group 6) were administered to the male rats of the Sprague Dawley for 3 weeks. Concentrations of total cholesterol in serum were significantly lower in the all experimental groups (2~6 groups) than in the control group, and particularly, the lowest in the group 2 and 6. Concentrations of HDL-cholesterol in serum were remarkably higher in the groups 2 and 4. The ratio of HDL-cholesterol to total cholesterol was the highest in the group 2. Atherosclerotic index was lower in the groups 2, 4 and 6. Concentrations of LDL, phospholipid and triglyceride in serum were remarkably lower in the all experimental groups than in the control group, and particularly, lower in the groups 2, 4 and 6. Concentrations of free cholesterol and cholesteryl ester in serum were significantly lower in the all experimental groups than in the control group, and particularly, the lowest in the group 2. Concentrations of glucose in blood were the lowest in the group 2. And groups 3 and 5 were slgnificantly lower. Contents of total cholesterol and triglyceride in liver were significantly lower in the all experimental groups than in the control group, and particularlyr the lowest in the groups 2 and 3. Phospholipid content was showed little differenre among groups but the lowest in the group 2. From the above research, the feeding 5% Platycodon grandiflorum＋10% perilla oil and 5% Platycodon grandiflorum＋10% safflower oil were effective on the improvement of the lipid compositions in serum and liver.