• Proceedings of the PSK Conference
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• 2001.10a
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• pp.282.2-282.2
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• 2001

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.281.1-281.1
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• 2001

• Journal of Ginseng Research
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• v.43 no.3
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• pp.460-474
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• 2019

Background: Ginsenoside compound K (CK) is a promising drug candidate for rheumatoid arthritis. This study examined the impact of polymorphisms in NR1I2, adenosine triphosphate-binding cassette (ABC) transporter genes on the pharmacokinetics of CK in healthy Chinese individuals. Methods: Forty-two targeted variants in seven genes were genotyped in 54 participants using Sequenom MassARRAY system to investigate their association with major pharmacokinetic parameters of CK and its metabolite 20(S)-protopanaxadiol (PPD). Subsequently, molecular docking was simulated using the AutoDock Vina program. Results: ABCC4 rs1751034 TT and rs1189437 TT were associated with increased exposure of CK and decreased exposure of 20(S)-PPD, whereas CFTR rs4148688 heterozygous carriers had the lowest maximum concentration ($C_{max}$) of CK. The area under the curve from zero to the time of the last quantifiable concentration ($AUC_{last}$) of CK was decreased in NR1I2 rs1464602 and rs2472682 homozygous carriers, while $C_{max}$ was significantly reduced only in rs2472682. ABCC4 rs1151471 and CFTR rs2283054 influenced the pharmacokinetics of 20(S)-PPD. In addition, several variations in ABCC2, ABCC4, CFTR, and NR1I2 had minor effects on the pharmacokinetics of CK. Quality of the best homology model of multidrug resistance protein 4 (MRP4) was assessed, and the ligand interaction plot showed the mode of interaction of CK with different MRP4 residues. Conlusion: ABCC4 rs1751034 and rs1189437 affected the pharmacokinetics of both CK and 20(S)-PPD. NR1I2 rs1464602 and rs2472682 were only associated with the pharmacokinetics of CK. Thus, these hereditary variances could partly explain the interindividual differences in the pharmacokinetics of CK.

• 한국임상약학회:학술대회논문집
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• 2007.12a
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• pp.185-186
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• 2007

• Korean Journal of Clinical Pharmacy
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• v.22 no.1
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• pp.21-29
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• 2012

Modern biologics are biotechnology-derived therapeutics, including recombinant therapeutic proteins like monoclonal antibodies, cytokines and tissue growth factors. Although the pharmacokinetics of therapeutic biologics should be evaluated based on the same general principles as small molecules, careful considerations should be given to bioanalytics and pharmacokinetics when designing pharmacokinetic studies of biologics during their drug development, due to their different physicochemical properties compared with small molecules. The aim of this study was to develop a draft guidance on pharmacokinetic studies of therapeutic biologics in clinical studies. All the elements outlined in the current Food and Drug Administration (FDA), European Medicinal Agency (EMEA), and International Conference on Harmonisation (ICH) guidelines and regulations, and the related literatures previously published were searched and evaluated. In this draft guidance, the specific problems related to the pharmacokinetics of therapeutic biologics that need special consideration during drug development process were addressed, and differences in pharmacokinetic characteristics between biologics and small molecules affecting the content of the development programme were presented.

• Archives of Pharmacal Research
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• v.21 no.6
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• pp.753-758
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• 1998

Sixteen novel 2-substituted acetyl amino-5-alkyl-1,3,4-thiadiazol were synthesized and screened for their pharmacological activities. A few of the compounds namely 11, 12 and 16 showed anti-inflammatory activities comparable to phenylbutazone. Compound 12 also showed significan non-specific spasmolytic activity. Diuretic activity of compound 15 at a dose level of 90mg/kg p.o. was two fold higher compared to 50mg/kg p.o. of furosemide. Comparable diuresis was aso produced by compounds 9, 10, and 16.

• Korean Journal of Clinical Pharmacy
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• v.11 no.2
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• pp.57-61
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• 2001

The effect of circadian rhythm on the pharmacokinetics of acebutolol was studied in rabbits administered intravenous 5 mg/kg dose of acebutolol at 09:00 in the morning (a.m) and 22:00 in the evening (p.m). A significant effect of circadian rhythm of pbarmacokinetic parameters as a function of time of day was noted in rabbits, showing lower total body clearance (CLt), higher plasma concentration and the area under the plasma concentration time curve (AUC) when acebutolol was given in the evening. The plasma concentration of acebutolol was increased significantly (p<0.05) at 12-24 hr after dosing in the evening. The AUC was greater in the evening $(111\%)$ than that in the morning and $CL_t$, was higher when acebutolol was given in the morning ($1.12\pm0.24$ ml/hr) versus in the evening ($1.01\pm0.22$ ml/hr), but those were not significant. Therefore, It is reasonable to consider individual circadian rhythm for effective dosage regimen of acebutolol in clinical chronotherapeutics.

• The Korean Journal of Physiology and Pharmacology
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• v.15 no.2
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• pp.67-81
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• 2011

Epilepsy is a chronic disease occurring in approximately 1.0% of the world's population. About 30% of the epileptic patients treated with availably antiepileptic drugs (AEDs) continue to have seizures and are considered therapy-resistant or refractory patients. The ultimate goal for the use of AEDs is complete cessation of seizures without side effects. Because of a narrow therapeutic index of AEDs, a complete understanding of its clinical pharmacokinetics is essential for understanding of the pharmacodynamics of these drugs. These drug concentrations in biological fluids serve as surrogate markers and can be used to guide or target drug dosing. Because early studies demonstrated clinical and/or electroencephalographic correlations with serum concentrations of several AEDs, It has been almost 50 years since clinicians started using plasma concentrations of AEDs to optimize pharmacotherapy in patients with epilepsy. Therefore, validated analytical method for concentrations of AEDs in biological fluids is a necessity in order to explore pharmacokinetics, bioequivalence and TDM in various clinical situations. There are hundreds of published articles on the analysis of specific AEDs by a wide variety of analytical methods in biological samples have appears over the past decade. This review intends to provide an updated, concise overview on the modern method development for monitoring AEDs for pharmacokinetic studies, bioequivalence and therapeutic drug monitoring.

• Korean Journal of Clinical Pharmacy
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• v.20 no.1
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• pp.50-55
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• 2010

Cefetamet pivoxil is a prodrug of cefetamet possessing a broad spectrum of activity against many aerobic gram-positive and -negative organisms. Although many literatures in abroad had introduced its pharmacokinetics about two decays ago, no data have been revealed in Korean subjects. Therefore, this study was aimed to investigate the pharmacokinetics of cefetamet following a single oral administration of cefetamet pivoxil in Korean healthy volunteers. After an overnight fast, a tablet of cefetamet pivoxil (500 mg) was given to eight volunteers, and blood samples were serially taken up to 12 h. Plasma concentrations of cefetamet were determined by HPLC with UV detection. Cefetamet reached the peak concentration ($2.0{\pm}1.3\;{\mu}g/ml$) at $3.0{\pm}0.8$ h, and mono-exponentially decayed at a half-life of $2.6{\pm}0.9$ h. Three volunteers represented very low systemic exposure compared to the others, which provided very large inter-individual variation in Cmax, and AUC. The present results were discussed and reviewed with the previously published data, and a couple of points are suggested for clinical trials of this drug in Korean subject including bioequivalence study.

• 대한임상약리학회:학술대회논문집
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• 2002.12a
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• pp.8-8
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• 2002