• Journal of Pharmaceutical Investigation
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• v.36 no.4
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• pp.253-262
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• 2006

This study was performed to investigate the effects of treatment for dermatitis using the herbal gel preparations. Scutellariae Radix(SR) and Zingiberis Rhizoma(ZR) were used for the purpose of herbal preparations. Baicalin, baicalein are the ingredients of SR, having biological effects like anti-inflammatory, anti-oxidative, anti-bacterial and antiallergic action. 6-Gingerol is one of the ingredients of ZR having biologicai effects like anti-inflammatory and analgesic action. The three types of hydrogels(SRE, SRH, SZH) were formulated with Carbopol 940, Labrasol, Triethanolamine etc. Baicalin was hydrolysed to baicalein by $\beta$-glucuronidase for the purpose to increase rate of skin permeation. Content of ingredients by HPLC determination, rate of skin permeation using Franz type diffusion cell, anti-oxidative activity for the free radical, hydroxyl radical, superoxide, anti-inflammatory by using carrageenan injection, efficacy on the dermatitis induced by 2,4-dinitro-chlorobenzene(DNCB) were experimented. Baicalein showed higher permeability than baicalin, so it is considered that baicalein was more suitable form than baicalin for transdermal absorption by its lipophilic property. In the anti-oxidative experiments, SZH gel was the most effective scavenging activity than the other gels in all experiments. In anti-inflammatory test, SRM and SZH gel more decreased edma rapidly than SRE gel. In case of using SZH gel, treatment period for the dermatitis was more declined than that of other gel groups. These results suggests that the SZH hydrogel could be suitable preparations for the treatment of dermatitis.

• Korean Journal of Environmental Agriculture
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• v.30 no.2
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• pp.196-201
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• 2011

BACKGROUND: Bioavailability enhancement by solubilization of lipophilic drugs in nano-emulsion has been reported and it may be useful in pharmaceutical and nutraceutical products. This study was performed to compare in vivo bioavailability of nano-emulsion formulation with that of the general product as control. METHODS AND RESULTS: The pharmacokinetics assessment of Vitamin A, D and E complex of nanoemulsion formulation (LaVita), in comparison to the general product, was performed in the male rat plasma by a single oral dose at 20 mL/kg body weight (n=3/group). For nano-emulsion formulation (LaVita), $C_{max}$ of vitamin A and E in plasma were much higher and the area under the curve (AUC) of vitamin A, D and E were 14-63% higher, and the half-life of vitamin E was 2-fold longer than the general product. According to statistical analysis, each $C_{max}$ of vitamin A, D & E was significantly higher (p<0.01, 0.05 and 0.01, respectively) than that of general product. Half-life of vitamin A was significantly higher (p<0.01) and AUC of vitamin A and D were also significantly higher than the general product. CONCLUSION(s): Considering significant increment of $C_{max}$ and AUC, LaVita made of nano-emulsion could be more effective the absorption rate and extent for bioavailability of vitamin A, D & E than those of general product.

• Journal of The Korean Society of Clinical Toxicology
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• v.13 no.1
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• pp.1-10
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• 2015

Purpose: The purpose of this study was to evaluate the usefulness of intravenous lipid emulsion as well as adverse events in acute poisoning patients. Methods: Literature was accessed through PubMed, EMBASE, Cochrane library, Web of science, and KoreaMed. All forms of literatures relevant to human use of intravenous lipid emulsion for acute poisoning were included. Cases reports or letters without description of clinical outcomes for each case were excluded. The literature search was conducted by two investigators in March, 2015, with publication language restricted to English and Korean. The effect, onset time, and adverse event of lipid emulsion and final outcome of each case were analyzed. Results: Eighty-one published articles were included, excluding articles whose title and abstract were not relevant to this study. No articles were classified as high level of evidence. Sixty-eight case reports were identified, consisting of 25 local anesthetics and 43 other drugs, such as tricyclic antidepressants and calcium channel blockers. Although most cases described significant clinical improvements, some of them showed no beneficial effect or worsening of clinical course. Several adverse events including hyperamylasemia and laboratory interference were reported. Conclusion: Although there were many case reports illustrating successful use of lipid for various drug poisonings, the effect cannot be estimated due to significant possibility of publication bias. Therefore, lipids might be considered in severe hemodynamic instability resulting from lipophilic drug poisoning, however further studies should follow to establish the use of lipid as the standard of care.

• YAKHAK HOEJI
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• v.45 no.6
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• pp.694-700
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• 2001

Synthetic pyrethroids are analysis of a natural chemical moiety, pyrethrin derived from the pyrethrum plant Chrysanthemum. The natural pyrethrin structure has been modified to be highly lipophilic and photostable, creating an effective pesticide and resulting in an increased presence in the environment. Worldwide, they are commonly used insecticides against ticks, mites, mosquitoes, and as treatment for human head lice and scabies. Therefore, human exposure to their compounds in extensive. Several studies on the effects of pyrethroids on thyroid hormone regulation, estrogen and androgen function have been reported and yet little has been done try assess their potential hormonal activities. Among humans, a pyrethroid compound was suggested to be the causal agent for gynecomastia in a group of Haitian men. The reports suggest that some pyrethroid compounds are capable of disrupting endocrine function. Therefore, we examined estrogenic/antiestrogenic potential of three pyrethroid insecticides, that is permethrin, allethrin and fenvalerate in human breast cancer cell and action mechanism mediated by the estrogen receptor. Fenvalerate showed weak estrogenic activity but aallethrin and permethrin showed no effect. In combination with high levels (10$^{-10}$ M, 10$^{-11}$ M) of 17$\beta$-estradiol and three synthetic pyrethroids inhibited cert proliferations in MCF7-BUS cell by 17$\beta$-estradiol. Whereas, fenvalerate increased cell proliferative activity at lower level of estradiol (10$^{-12}$ M, 10$^{-13}$ M). The relative affinities to the estrogen receptor were observed by allethrin and permethrin treatment, but not by fenvalerate. These results indicated that some of pyrethroid insecticides may modulate estrogen functions in human breast cancer cell. The action mechanisms of estrogen receptor mediated antiestrogenicity by allethrin and permethrin were postulated.

• Food Science and Preservation
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• v.11 no.4
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• pp.461-467
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• 2004

Antioxidant effect of traditional doenjang(TD) was reduced by increasing of maturation period. Methanol fractionate of TD matured for 1 year showed strong antioxidant effect against linoleic acid, following the order of hexane and water layer. Antioxidant effect in lipophilic and hydrophilic extracts of TD were gradually increased according to increasing maturation period, whereas their values or two extracts were lower than those or fractionates from TD. Hydrogen-scavenging effect in hydrophobic extract, methanol and butanol fractionates of TD were much higher than those of the other samples. Chloroform and ethylacetate fractionates were markedly lower in the range of $10.57{\sim}22.84\%\;and\;7.82{\sim}22.58\%$, respectively. Anticarcinogenic effect of extracts and fractionates from TD were higher in water fractionates for A549 cell (human lung carcinoma) and methanol fractionates fur MCF-7 cell (human breast adenocarcinoma). Especially, inhibitory effect for growth of cancer cell was increased by the increasing maturation period of TD.

• Journal of Pharmaceutical Investigation
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• v.26 no.1
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• pp.43-53
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• 1996

The objective of this study was to determine whether 4-phenylazobezyloxycarbonyl-Pro-Leu-Gly-Pro-D-Arg (Pz-peptide), an enhancer of hydrophilic solute permeability in the intestine, could elevate the paracellular permeability of hydrophilic drugs across cornea and conjunctiva in the rabbit. The in-vitro penetration of hydrophilic drugs (mannitol, atenolol) and lipophilic drug (propranolol) across the rabbit cornea and conjunctiva was studied either in the presence or absence of 3 mM Pz-peptide. Drug penetration was evaluated using the modified Ussing chamber. The conjunctiva was more permeable than the cornea to all drugs. Pz-peptide showed enhanced effects on the drug transport across cornea and conjunctiva in a concentration dependent manner. Effects or ion transport inhibitor on the mannitol penetration were then investigated. Mannitol penetration was not changed by serosal addition of $100\;{\mu}M$ ouabain, suggesting that $Na^+/K^+$ ion tranporter was not involved in the Pz-peptide induced elevation of paracellular drug permeability. Furthermore, effects of Pz-peptide and EDTA on the transport of atenolol and propranolol into the ocular tissues or blood circulation after its administration into both eyes were investigated. EDTA showed enhanced effect on propranolol transport into the ocular tissues, but Pz-peptide did not show significant difference. Systemic absorption of propranolol by the addition of EDTA or Pz-peptide was not changed. On the other hand, EDTA and Pz-peptide elavated the atenolol transport into the ocular tissues. The transport of atenolol into the blood circulation was also enhanced by the addition of EDTA, but no effect was observed by the addition of Pz-peptide. The above findings suggest that Pz-peptide would be used as an paracellular pathway enahncer of hydrophilic drugs into the eye, without affecting the systemic absortion of topically applied opthalmic drugs.

• Journal of Korean Society of Environmental Engineers
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• v.35 no.8
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• pp.579-585
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• 2013

Persistent Organic Pollutants (POPs) are chemical substances which persist in the environment, bioaccumulate through the food web, and pose a risk of causing adverse effects to human health and the environment. POPs are thermally stable, highly lipophilic and water-insoluble compounds which can induce various toxic influences including immunotoxicty, carcinogenicity adverse effects on reproduction, development and endocrine fuctions. Polybrominated diphenyl ethers or PBDEs, are organobromine compounds that are used as flame retardant. Because of their toxicity and persistence, the industrial production of some PBDEs is restricted under the Stockholm Convention, a treaty to control and phase out major POPs. In this study, PBDEs was measured in various site of Sihwa industrial complex to investigate concentration distribution of POPs. The levels of PBDEs in house dust samples were 0.722~44.024 ng/g-dry. In PBDEs congener, BDE-209 was relatively higher in the all sites. The concentration of BDE-209 measured over 80.0% of total PBDEs. In various site, high molecular PBDEs homologues are measured higher than low molecular.

• Archives of Pharmacal Research
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• v.10 no.4
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• pp.212-218
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• 1987

Intact brain cell aggregates were dissociated from adult rat brains without cerebellum using a sieving technique. This proparation was used to elucidate the binding characteristics of agonist to muscarinic acetylcholine receptors (mAchR) in brain. Incubation of cells with carbamylcholine (carbachol) was shown agonist-induced receptor down-regulation depending on the concentration of agonist, not depending on the incubation time. This effect of carbachol was due to a reduction in the maximal binding capacity ($B_{max}$) to the mAchR without decreasing the affinity of the remaining receptors in incubation at 37.deg.C but was not apparent inincubation at $15^{\circ}}C$In addition, it was abolished when the receptors were blocked by atropine. The decline in ($^3H$)N-methylscopolamine (($^3H$)NMS) binding induced by agonist was reflected as a significant reduction in the receptor density with no change in receptor affinity, suggesting that 'true' receptor down-regulation takes place. Moreover, when the receptors were labeled with the lipophilic antagonist ($^3H$) quinuclidinyl benzilate (($^3H$) QNB) insted of the hydrophilic ligand ($^3H$)NMS, the magnitude of the observed receptor down-regulation was significantly lower in case of the former than the latter. This suggested that exposure of intact brain cells to muscarinic agonists might induce a slight degree of accumulation of receptors in intracellular sites before the receptors are actually degraded.

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.83-88
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• 2003

KR-984055 is a new oral cephalosporin antibiotic with activity against both gram-positive and gram-negative bacteria. Lipophilic ester-type prodrugs of KR-984055, i.e., KR-999001 and KR-999002, have been synthesized in an attempt to increase the oral bioavailability of this broad-spectrum antibiotic agent. In this study we determined the oral bioavailability of KR-984055 and its prodrugs in the rat, and evaluated the pharmacokinetic model that best describes the plasma concentration behavior following single intravenous (IV) and oral single dose. In addition, concentrations in plasma as well as biliary and urinary recovery of KR-984055 were determined. Also, protein binding of KR-984055 in plasma was examined in vitro. The degree of protein binding of KR-984055 was in the range of 92.09~94.77%. KR-984055 exhibited poor oral bioavailability (7.02$\pm$1.58%). The observed oral bioavailabilities of KR-984055 from KR-999001 and KR-999002 were 38.77$\pm$2.81 % and 39.81$\pm$5.25%, respectively. These data were calculated from the levels of free KR-984055 in plasma. Oral KR-999001 and KR-999002 were not recovered from plasma, suggesting that it was readily cleaved to free KR-984055. KR-999001 and KR-999002 appear to be an efficient oral prod rug of KR-984055 that deserved further clinical evaluation in human.

• Journal of the Korean Chemical Society
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• v.46 no.5
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• pp.407-411
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• 2002

A method to determine lead ion in aqueous media using an optical sensor loaded on a fluorescent optode membrane incoporating a metal ion-selective ionophore, a proton-selective chromoionophore and lipophilic anionic sites has been studied. The effects of pH and thickness of membrane on the fluorescence intensity were investigated. The effects of foreign ions such as $Na^+$, $K^+$, $Mn^{2+}$ and $Zn^{2+}$ on the determination of lead ion were also studied. The linear range in the calibration curve for the determination of lead ion was found to be 5.0${\times}10^-7$ to 5.0${\times}$$10^-3$M and the correlation coefficient in this range was -0.99107 under the optimal experimental conditions. The relative standard deviation of the blank signals was 3.0% and the detection limit of lead ion was 5.0${\times}$$10^-9$M.