• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.235-235
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• 1996

1. 초산 writhing법에서 DA-5018, morphine, capsaicin 및 acetaminophen의 E $D_{50}$ 은 각각 0.1, 0.3, 1.4 및 45.4 mg/kg이었으며, formalin법에서 DA-5018과 morphine의 E $D_{50}$은 0.17과 4.3 mg/kg이었다. Randall-Selitto법에서 DA-5018, morphine, capsaicin 및 acetaminophen의 E $D_{50}$은 0.66, 3.9, 4.2 및 643 mg/kg이었다. Tail flick법에서 DA-5018, morphine 및 capsaicin의 E $D_{50}$ 은 2.0, 2.6 및 14.2 mg/kg이었고 hot plate법에서 DA-5018과 capsaicin의 E $D_{50}$은 1.7 및 26.5mg/kg이었다. 그러나 열자극에 의한 동통모델에서 acetaminophen은 진통효과가 없었다. 2. Streptozotocin유발 당뇨랫드에 DA-5018 0.2, 0.5 및 1.0mg/kg 또는 capsaicin 10 mg/kg 투여시 1, 3, 7 일째에서 각각 유의성있는 동통역치의 증가를 나타내었으나 ketoprofen(10 mg/kg) 및 desipramin(10 mg/kg) 투여시는 동통역치의 유의성있는 증가가 나타내지 않았다. 관절염 동통모델에서 DA-5018, ketoprofen 및 capsaicin을 투여한 후 7일째에 동통역치를 2배 증가시키는 용량은 각각 0.66, 3.76 및 17.38 mg/kg이었다. 3. 이상의 결과로부터 DA-5018은 morphine 및 capsaicin에 비해 동등 이상의 효력을 갖고 있으며, 비스테로이드성 진통제보다 효능이 우수함을 확인하였다.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.313-319
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• 2002

Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at $37^{\circ}C$. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from thε partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at $37^{\circ}C$. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers testεd, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation ratε achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.

• Polymer(Korea)
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• v.27 no.6
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• pp.536-541
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• 2003

Unsaturated poly(3-hydroxyalkanoate) (UPHA) was biosynthesized and the properties of drug delivery using the polymer matrix were investigated. The biosynthesis of UPHA was carried out by pH-stat fed batch fermentation of Pseudomonas oleovorans (ATCC 29347) grown solely with 10-undecenoic acid as a carbon source. The physical and chemical properties of the biosynethesized UPHA were characterized using NMR, FT-IR, GPC and DSC. The drug release experiments were carried out using HPLC with a diffusion cell fur the release amount of ketoprofen as model drug. The effects of crosslinking degree, patch thickness, and enhancer on the drug release were studied. The drug release rate was linearly decreased and consistent with increased crosslinking degree of the polymer matrix. The duration of drug release was enhanced by the Increased patch thickness. The drug release rate was increased with increased amount of propylene gylcol as an enhancer.

• Journal of Environmental Analysis, Health and Toxicology
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• v.21 no.4
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• pp.243-251
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• 2018

Pharmaceuticals in wastewater effluents have been recognized as emerging pollutants threatening freshwater organisms. To extend understanding for bioaccumulation and toxicity in those organisms, information on biotransformation products (or metabolites) and their metabolic pathway are crucial. The aim of the present study is to identify and elucidate metabolites of pharmaceuticals formed in exposed organisms using suspect and nontarget screening approach using LC-HRMS. As the target pharmaceuticals, carbamazepine, ketoprofen, metoprolol, propranolol, and verapamil were selected whereas Daphnia magna and Gammarus pulex were used as test organisms. After 24h exposure, metabolites formed in the organisms were identified using LC-HRMS. The structures of metabolites were elucidated via analysis of MS/MS fragment pattern and the comparison with fragment database. As the results, a total of 10 metabolites were identified for 5 parent compounds (C253/C356 for carbamazepine, K211 for ketoprofen, M256 for metoprolol, P218/P276/P306 for propranolol, V196/V291/V441 for verapamil). Among them, the presence of C253 and V291 was confirmed using standard materials. Most of the identified metabolites were formed through oxidative reactions such as hydroxylation, N-demethylation, and dealkylation. Cysteine conjugation (phase II reaction) metabolite (C356) for carbamazepine was found in daphnia. The metabolic pathway of verapamil showed similar metabolic pathways and metabolic pathways for both species. Although the toxicological information on the identified metabolites could not be confirmed, the molecular structure information of the proposed metabolites can be used for future evaluation and prediction of toxicity.

• Advances in nano research
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• v.16 no.1
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• pp.41-52
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• 2024

In this study, rare-earth orthoferrites LnFeO₃ were synthesized using a facile hydrothermal reaction and their visible-light-induced photo-Fenton degradation of organics was optimized through Ln variation (Ln = La, Pr, or Gd). The morphological, structural, and chemical characteristics of as-prepared samples were examined in detail by using different methods, including XRD, SEM, TEM, XPS, etc. On the other side, under visible light illumination, the photo-Fenton-like catalytic activities of LnFeO₃ were assessed in terms of the removal of selected organic models, i.e., pharmaceuticals (ketoprofen and tetracycline) and dyes (rhodamine B and methyl orange). As compared with PrFeO₃ or GdFeO₃, the sample of LaFeO₃ displayed more structural distortion, larger specific surface area, and narrower band gap, resulting in its higher photo-Fenton-like catalytic activity toward the degradation of organics. In organic-containing solution, in which the initial solution pH = 5, catalyst dosage = 1 g/L and H₂O₂ concentration = 10 mM, 98.2% of rhodamine B, 31.1% of methyl orange, 67.7% of ketoprofen, or 96.4% of tetracycline was removed after 90-min exposure to simulated visible light. Our findings revealed that variation of Ln site on rare-earth orthoferrites was an effective strategy for optimizing their organic removal via visible-light-induced photo-Fenton reaction.

• 한국생물공학회:학술대회논문집
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• 2003.04a
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• pp.506-510
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• 2003

SMB(simulated moving bed) chromatography system has been developed to realize continuous separation and save solvent consumption for binary mixture in especial. The parameters of SMB chromatography system can be calculated from mass balance equations of true moving bed chromatography, and they are used in design of 6-column SMB chromatography. We can separate S-ketoprofen enantiomer as a raffinate product in 85% of purity and 0.3mg/ml using assembled SMB chromatography system.

• Journal of Veterinary Clinics
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• v.16 no.2
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• pp.443-447
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• 1999

전지 파행을 호소하여 의뢰된 약 2개월령의 진도개 암캐에서 비대성골이영양증이 진단되었다. 내원 2일 전부터 파행과 침울 증상을 보인 이 개의 이학적인 검사 결과 grade II/IV 정도의 좌측 전지파행이 관찰되었으며, 좌측과 우측의 앞발목관절의 미약한 종대가 인정되었다. 좌측발목관절을 촉진한 결과 요골과 척골의 골단부위를 촉진할 때 심한 통증을 호소하였으며, 우측 앞발목관절의 촉진에서도 미약한 통증이 인정되었다. 좌측과 우측 앞발목관절의 x-ray 검사에서 양측 전지 원위 요골 및 척골의 성장절 바로 위쪽 골간단에 성장절과 나란히 존재하는 불규칙한 방사선투과성의 선이 관찰되었고, 이 부위의 바로 아래쪽과 위쪽에는 방사선투과성이 감소되어 있었다. 이상의 결과 비대성골이영양증으로 진단되었다. ketoprofen과 amoxicillin을 투여하고, 운동을 철저히 제한한 결과 이 개의 증상은 빠르게 호전되었으며, 치료 2일 후 파행증상이 완전히 소실되었고, 증상이 재발되지 않았다. 이 보고에서는 진도개에 발생한 비대성골이영양증을 처음으로 소개하면서 이 질환으로 원인, 진단 및 치료에 대해 문헌적으로 고찰되었다.

• YAKHAK HOEJI
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• v.30 no.4
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• pp.180-184
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• 1986

Such carboxyl drugs as mefenamic acid, alclofenac, ketoprofen, cicloxilic acid and tolfenainic acid in rat plasma were determined by the gas chromatography flame photometric detector (GC-FPD). After methylthiomethyl (MTM) esterification with MTM-chloride in 1, 8-diazabicyclo [5.4.0] undec-7-ene (DBU) catalyst, determination of these drugs by this method was tried and compared with that by the GC-flame ionization detector (FID) method in respect to sensitivity and effect of inteferences. The results showed it was possible to analyze with accuracy by this method because of specificity of the FPD, although these drugs were not separated from interferences in plasma on GC column. The GC-FPD method was more sensitive than GC-FID method and the minimum detectable amount of monocarboxylic drugs on 3%, QF-1 column was about 15fmol/injection.

• KSBB Journal
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• v.14 no.3
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• pp.273-278
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• 1999

The molecularly imprinted polymers(MIPs) synthesized at various polymerization conditions were examined as ibuprofen receptors in terms of binding characteristics. The 4-vinylpyridine polymers had 1.2 times higher adsorption capability for (S)-(+)-ibuprofen than the methacrylic acid polymers. The methacrylic acid polymers synthesized by UV radiation had 1.9 times higher selectivity for (S)-(+)-ibuprofen compared to those by thermal initiation. Effects of various solvents for binding were also examined in this research. According to the Scatchard analysis, the (S)-(+)-ibuprofen artificial receptors had two different kinds of binding sites for (S)-(+)-ibuprofen while having only single kind of binding site for ketoprofen. The binding sites of (S)-(+)-ibuprofen, n were calculated as 4.3~4.9 $\mu$mol/g and the dissociation constants, $K_D$ were 0.68 mM for the specific binding.

• Biomolecules & Therapeutics
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• v.19 no.1
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• pp.109-117
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• 2011

In this work, we have investigated the effect of polyoxyethylene alkyl ester nonionic surfactants on percutaneous permeation enhancement of a model drug, ketoprofen. We also investigated the mechanism involved in the enhancement using impedance and solubility measurement. Three groups of nonionic surfactants with different ethylene oxide content were studied. The permeation results showed that all surfactants enhanced the percutaneous absorption, irrespective of the molecular weight. The permeation results from PEG-45 monostearate (PEGMS45) were rather unexpected. Impedance and solubility results indicate that the mechanism involved in the enhancement of permeation by PEG-10 monooleate (PEGMO10) and PEGMS45 is rather different. The results from PEGMS45 suggest that it could be a potential candidate as a skin penetration enhancer with high molecular weight, which may poses less skin irritation and systemic side effect than the smaller surfactant molecules. Overall, this work provided some useful information on percutaneous transport enhancement and the mechanistic insights involved in skin permeation for these nonionic surfactants.