• Biomolecules & Therapeutics
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• 제10권1호
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• pp.19-24
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• 2002

The effects of a newly synthesized $H^+/K^+$ ATPase inhibitor,1-(2-methyl-4-methoxypheny)-4-[(3-hy-droxypropyl)amino] -6-methyl-2,3-dihydropyrrolo (3,2-c) quinoline (DBM-819) , on the central nervous system, isolated smooth muscle, cardiovascular and digestive systems and renal function were investigated in various experimental animals. Oral administration of DBM-819 had no effect on the central nervous system except body temperature of mice slightly decreased at doses of 15 and 50 mg／kg. DBM-819 produced a moderate analgesic effect in acetic acid-induced writhing test in mice at 50 mg／kg (p.o.). In conscious rats, DBM-819 (15 and 50 mg／kg, p.o.) showed a slight increase in blood pressure and a small decrease in heart rate. DBM-819 had an significant effect on agonist-induced contraction of guinea pig ileum at $1.5{\times}10^{-5}g/ml.$ No significant effect of DBM-819 (5 and 15 mg／kg, i.p) on urinary volume or urinary excretion of $Na^+,\;K^+$ and Cl- was observed in rats. DBM-819 had no significant effect on intestinal transport of a semisolid meal in mice at 15 and 50 mg／kg (p.o.). These findings suggest that DBM-819 exerts no significant pharmacological effects on the central nervous system and renal function at 15 mg／kg (p.o.), but produces some effects on the smooth muscle and circulatory system.

• BMB Reports
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• 제52권4호
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• pp.271-276
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• 2019

Zingerone (ZGR), a phenolic alkanone isolated from ginger, has been reported to possess pharmacological activities such as anti-inflammatory and anti-apoptotic effects. This study was initiated to determine whether ZGR could modulate renal functional damage in a mouse model of sepsis and to elucidate the underlying mechanisms. The potential of ZGR treatment to reduce renal damage induced by cecal ligation and puncture (CLP) surgery in mice was measured by assessment of serum creatinine, blood urea nitrogen (BUN), lipid peroxidation, total glutathione, glutathione peroxidase activity, catalase activity, and superoxide dismutase activity. Treatment with ZGR resulted in elevated plasma levels of BUN and creatinine, and of protein in urine in mice with CLP-induced renal damage. Moreover, ZGR inhibited nuclear $factor-{\kappa}B$ activation and reduced the induction of nitric oxide synthase and excessive production of nitric acid. ZGR treatment also reduced the plasma levels of interleukin-6 and tumor necrosis $factor-{\alpha}$, reduced lethality due to CLP-induced sepsis, increased lipid peroxidation, and markedly enhanced the antioxidant defense system by restoring the levels of superoxide dismutase, glutathione peroxidase, and catalase in kidney tissues. Our study showed renal suppressive effects of zingerone in a mouse model of sepsis, suggesting that ZGR protects mice against sepsis-triggered renal injury.

• KSBB Journal
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• 제25권3호
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• pp.297-302
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• 2010

Ketoprofen is one of the propionic acid class of nonsteroidal anti-inflammatory drug with analgesic and antipyretic effects. The most common side effects from ketoprofen after oral administration are gastrointestinal irritation, diarrhea, abdominal pain and retention of fluid. Ketoprofen was formulated as water-soluble gels to reduce these side effects. To increase the skin permeability of ketoprofen, microsphere containing ketoprofen was prepared with chitosan and ploy-$\varepsilon$-caprolactone. And then prepared microsphere was manufactured as an adhesive hydrogel with polyvinylpyrrolidone K-25, polyethylene glycol 4000, and various permeation enhancers. The flux and permeability of ketoprofen were evaluated. As the concentration of tween 80 and enhancers increased, the flux of ketroprofen was accelerated. Also the permeation rate was facilitated by enhancers, but did not affect the lag time. From these results, the adhesive hydrogel using microsphere could be a good delivery system for ketoprofen to improve the skin permeation.

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.107-112
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• 2001

In order to reduce the systemic side effects and gastrointestinal irritation after its oral adminitration, ketoprofen was formulated as water-soluble packs. The effects of fatty acids and fatty alcohols on the penetration of ketoprofen through excised rat skins were evaluated. The role of stratum corneum as a protective barrier was also investigated. Fatty acids and fatty alcohols were generally effective in promoting ketoprofen penetration. The flux of ketoprofen through rat skin was maximized when oleic acid or lauryl alcohol was used as an enhancer. As the concentration of fatty acids and fatty alcohols varied from 0% to 10%, the amounts of ketoprofen penetrated were in direct proportion to that of fatty acids but those had no relationship with that of fatty alcohols. The penetration of ketoprofen through stripped skin was enhanced compared to normal skin irrespective of enhancer type, which indicated that the action site of enhancers would be stratum corneum.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
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• pp.100-100
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• 2003

We have reported that oral administration of Saiko-Ka-Ryukotsu-Borei-To (SRB), a traditional Chinese formulation, inhibited the intimal thickening in carotid artery after balloon injury in cholesterol-fed rats. To elucidate its mechanism, the effects of SRB on migration and proliferation of vascular smooth muscle cell (VSMC) were examined in vivo and in vitro. We have reported that oral administration of Saiko-ka-Ryukotsu-Borei-To (SRB), a traditional Chinese formulation, inhibited the intimal thickening in carotid artery after balloon injury in cholesterol-fed rats. To elucidate its mechanism, the effects of SRB on migration and proliferation of vascular smooth muscle cell (VSMC) were examined in vivo and in vitro.

• Journal of Pharmaceutical Investigation
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• 제4권1_2호
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• pp.19-24
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• 1974

The comparative studies were made on the analgesic antipyretic effects of aminopyrine used individually and combined with parasympathetic agents (atropine sulfate). The analgesic antipyretic effects were eximined by Writhing's method to the experimental groups(mouse), and the following effects were found : 1) The active intensity of aminopyrine by it's oral administration combined with atropine sulfate is as follows. Amiinopyrine 80 mg/kg combided with Atropine sulfate 0.005 mg/kg=Aminopyrine 100 mg/kg 2) The most active range of intensity of Atropine sulfate(adjuvant) by it's oral administration is as follows. Atropine sulfate $0.004{\sim}0.005\;mg/kg$.

• Journal of Pharmaceutical Investigation
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• 제17권1호
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• pp.15-21
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• 1987

Effects of phenobarbital pretreatment on the pharmacokinetics of enterohepatic recirculating griseofulvin were investigated by comparing normal to bile duct cannulated rats and also the effects of enhanced endogeneous bile flow on the absorption of griseofulvin were studied by means of in situ recirculation method in phenobarbital-pretreated rats. Phenobarbital was administered orally for five days at the dose of 75 mg/kg/day. The influence of phenobarbital pretreatment on the absorption rate constant, area under the plasma concentration-time curve, maximum plasma concentration of orally administered griseofulvin was not found in bile duct cannulated rats. Decreased absorption clearance and apparent partition coefficient of griseofulvin in accordance with the amount of endogeneous bile juice seemed to be due to the decrease of thermodynamic activity of griseofulvin as bile forms the micelle with griseofulvin.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.1-7
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• 1995

IY-80843, N[2-(2-methoxyphenyl)ethyl]-N'-[4-(lmidazole-4-yl)phenyl] formamidine, is a new potent $H_2-receptor$ anagonist. The potential secondary pharmacologic effects of this agent, on the central nervous and cardiovascular systems were studied. IY-80843 caused ptosis, suppression of locomotion, hypotehrmia, prolongation of sleeping time and hypotensive effects in mice, rats and dogs. These results suggest that IY-80843 affects the funcition of the central nervous and cardiovascular systems in a dose-dependent manner.

• Clinical and Experimental Pediatrics
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• 제64권12호
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• pp.642-651
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• 2021

Background: Infantile colic (IC) is excessive crying in otherwise healthy children. Despite vast research efforts, its etiology remains unknown. Purpose: Most treatments for IC carry various side effects. The collection of evidence may inform researchers of new strategies for the management and treatment of IC as well as new clues for understanding its pathogenesis. This review and meta-analysis aimed to evaluate the efficacy and possible mechanisms of probiotics for mananaging IC. Methods: Ten papers met the study inclusion and exclusion criteria, and the meta-analysis was conducted using Review Manager (RevMan) software and a random-effects model. Results: This meta-analysis revealed that probiotics are effective for treating infantile colic, while the review showed that this efficacy may be due to their anti-inflammatory effects. Conclusion: Probiotics may be an important treatment option for managing infantile colic due to their anti-inflammatory properties.

• Journal of Pharmaceutical Investigation
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• 제15권2호
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• pp.63-72
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• 1985

Analgesic, anticonvulsive, sedative and antipyretic actions of Yangkyuksanwhatang which is composed of nine crude drugs including Rehmanniae Radix, and its effects on isolated ileum and blood vessel were investigated. The results of the studies were summerized as follows; 1. Analgesic and antipyretic effects were observed. 2. Suppressive actions were not shown on the convulsion induced by strychnine, but significant effects were noted on the convulsion induced by picrotoxin. 3. A prolongation of anesthetic time induced by pentobarbital sodium was significantly observed. 4. Relaxing actions were noted on the ileum of mice, and also, same effects were recognized on the contraction of the ileum due to acetylcholine chloride and barium chloride. 5. The expansion of blood vessels by relaxation of smooth muscle and hypotensive effects were noted.