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혈소판 응집 억제제의 효과 측정법에 대한 고찰과 지원자에서 Triflusal의 혈소판 응집 억제능 평가
이병요,장힘찬,백인환,윤휘열,권광일 충남대학교 약학대학 의약품개발연구소 2010 藥學論文集 Vol.25 No.-
The anti-platelet agent is a member of a class of pharmaceuticals that decreases platelet aggregation and inhibits thrombus formation. They are effective in the arterial circulation and widely used in primary and secondary prevention of thrombotic cerebrovascular or cardiovascular disease. As a method for estimating the effects of anti-platelet agent, platelet aggregation was conventionally measured using the optical method or the impedance method. Several alternate methods currently in development or recently developed were considered, including luminescence method, flow cytometry, laser-light scattering method, and Verify Now-P2Y12 assay. Principles, advantages, and disadvantages of the optical method, impedance method, and the other alternate platelet aggregation methods were discussed in this report. 15 human volunteers were recruited for the evaluation of the efficacy of triflusal using the optical method. After the oral administration of a single dose of 900mg, 15 subjects received eight doses administered at 24-hour intervals of 600mg triflusal. Using platelet rich-plasma from above subjects, we performed baseline platelet aggregation test induced by adenosine diphosphate(ADP), collagen, and arachidonic acid. The results of platelet aggregation test after triflusal administration were compared with the baseline study. Triflusal significantly inhibited platelet aggregation induced by ADP (33.0±21.3%) and arachidonic acid (99.1±1.2%), respectively. Therefore, we concluded that anti-platelet aggregation effect of triflusal can be studied successfully with the optical method. Each of the platelet aggregation methods has value for evaluating the effects by various mechanisms of the anti-platelet agents. The ideal method for estimating the platelet aggregation as it relates to safety and efficacy in patients treated with anti-platelet agents will need to be determined in clinical trials.
국내외 현황 파악을 통한 국내 소아용 의약품의 안전성.유효성 평가제도 개선 방안
이병요,이수진,권광일 충남대학교 약학대학 의약품개발연구소 2013 藥學論文集 Vol.28 No.-
Recently it has been noticed that pharmacokinetics / Pharmacodynamic (PK/PD) properties of drug in the pediatric population are different from those in adults. Clinical trials that considering age-specific properties and characteristics should be performed and safety and efficacy are established based on the clinical trials. FDA and EMEAs exists in developed countries especially America and Europe due to which there are proper guidelines for pediatric patients. However, in Korea, there doesn’t exist any guidelines and the study is focused regarding it. This study aimed to analyze the current state of safety and efficacy assessment of pediatric drug by foreingn drug regulatory agencies and suggest the regulatory methods for Korea based on FDA and EMEA guidelines and regulatory. MEDLINE and foreign drug regulatory agency database were extensively searched to obtain scientific research articles, guidance, regulations and pediatric drug review reports on foreign pediatric drug evaluation system.
Afloqualone의 LC/MS/MS분석과 건강한 성인 지원자에 대한 약물동태 연구
이서판,이병요,윤휘열,이은주,권광일 충남대학교 약학대학 의약품개발연구소 2008 藥學論文集 Vol.23 No.-
Afloqualone is a centrally acting muscle relaxant that inhibits mono- and polysynaptic reflexes. The purpose of this study was to estimate the pharmacokinetic parameters of afloqualone in healthy volunteers. The pharmacokinetics of afloqualone tablet was examined on 24 healthy volunteers who received a single oral dose(20 Bg) of each preparation in the fasting state. Blood samples were ten at 0, 0.5, 1, 1.5 2 3 4 6 8 10, 12 and 24 hr after drug administration. Blood concentrations of afloqualone were determined using a liquid chromatography tandem mass spectrometry(LC/MS/MS) systems. A two compartment model was used to explain the pharmacokinetic properties of afloqualone. The pharmacokinetic parameters were calculated with model independent(AUC, C_max, T_max, CL_t, V/F) and model dependent(K_ei, K_a, K_cp, K_pc, t_1/2) Pharmacokinetic analysis using WinNonlin program. The estimated means of AUC_0-24hours, C_max, T_max CL_t and V/F were 148.99 ± 127.39 ng·hi/ml 35.11 ± 56.62 ng/ml, 1.81 士 1.34 hr, 189.01 士 79.67 L/hr and 848.61 ± 567.06 L, respectively. The model dependent parameters(K_ei, K_a, K_cp, K_pc, t_1/2) were 0.14 ± 0.18 hr^(-1), 11.64 ± 30.03 hr^(-1), 0.34 ± 0.39 hr^(-1), 0.1 ± 0.16 hr^(-1) and 10.56 ± 4.30 hr, respectively. In conclusion a two compartment model was best described the pharmacokinetic behavior of afloqualone in healthy human.
Efavirenz, indinavir, lopinavir, ritonavir의 LC-MS/MS를 이용한 동시 정량법
채정우,배경진,백인환,서정원,이병요,이은주,남진경,강원구,권광일 충남대학교 약학대학 의약품개발연구소 2009 藥學論文集 Vol.24 No.-
Efavirenz indinavir and kaleta (co-formulation of lopinavir and ritonavir) are important antiretroviral drugs which have been proved to be human immunodeficiency virus (HIV) protease inhibitors and reduced the morbidity and mortality associated with HIV-1 infection. A brief and fast high performance liquid chromatography coupled with electrospray mass spectrometry (LC-MS/MS, API 4000) method for the determination of 4 anti-retroviral agents (efavirenz, lopinavir, indinavir, ritonavir) in human plasma was developed and validated. A simple protein precipitation method was used on 100μl of human plasma. And internal standard solution (10 ng/ml methaqualone) 1ml and reconstitution solution (MeOH) 1ml were added. After vortexing for 30 s and centrifuging at 13,200rpm for 10min, 2μl of supernatant was injected into the column (XTerra MS C_(18) column, 2.1mm × 50mm 3.5㎛ particle size). The mobile phase consisted of MeOH and 0.1% formic acid in water (80:20 , v/v). The chromatogram was run for 1.5 min at a flow rate of 300μl/min. A triple quadrupole mass spectrometer was operated in a positive ion mode (lopinavir, indinavir, ritonavir) and negative mode (efavirenz), simultaneously and multiple reaction monitoring (MRM) was used for drug quantification. The precursor-to-product ion transitions of m/z 316→69 (efavirenz) and 629→447 (lopinavir) and 614→421 (indinavir) and 721→296 (ritonavir)were used to measure and quantify the analyte. The limit of quantitation (LOQ) was 50 ng/ml (efavirenz, indinavir, ritonavir) and 100 ng/ml (lopinavir). The weighted (l/y²) calibration curve was linear over human plasma range 50∼5000ng/ml (efavirenz), 100∼20000ng/ml (lopinavir), 50∼10000ng/ml (indinavir), 50∼2000ng/ml (ritonavir), correlation coefficient(r²) of 4 antiretroviral agents were higher than 0.998. Accuracies and intra-run precisions ranged within 86.60 and 113.29%, 1.06 and 11.16% for all 4 drugs analysed. This analytical method used to determine these drugs was fast and easy to perform, with minimal sample preparation, and without compromising precision and accuracy. The developed method was successful to determine antiretroviral agents in human plasma, and proved suitable for clinical pharmacokinetic study.
폐질환 치료제의 효율적인 신약개발을 위한 생체표지자 및 대리결과 변수
서정원(Jeong-Won Seo),이병요(Byung-Yo Lee),채정우(Jung-Woo Chae),손추영(Chu-Young Son),강원구(Wonku Kang),채한정(Han-Jung Chae),권광일(Kwang-il Kwon) 대한약학회 2010 약학회지 Vol.54 No.2
Biomarkers are likely to be important in the study of various pulmonary diseases for many reasons. Research efforts in developing biomarkers and surrogate endpoints of lung diseases have resulted in the identification of new risk factors and novel drug targets, as well as the establishment of treatment guidelines. Government agencies, academic research institutions, diagnostic industries, and pharmaceutical companies all recognize the importance of biomarkers in new drug development and advancing therapies to improve public health. In drug development, biomarkers are used to evaluate early signals of efficacy and safety, to select dose, and to identify the target population. Identification of suitable end points not only would help investigators design appropriate clinical trials but would assist clinicians in caring for this patient population. Though the area of pulmonology has received much attention in the past decades, it still lags behind with regard to the development of biomarkers, particularly those of health effects and susceptibility. This review critically summarized several biomarker researches such as Evaluation of COPD Longitudinally to Identify Predictive Surrogate End-points (ECLIPSE) study with objectives of identifying the parameters that predict disease progression of COPD, as well as biomarkers that may serve as surrogate end-points.