• Title/Summary/Keyword: Cmax

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Analysis of Ethnic Differences in Physician's Desk Reference (Physician's Desk Reference에 나타난 인종차이 분석)

  • Kim, Eun Jung;Lee, Kyung Eun;Gwak, Hye Sun
    • Korean Journal of Clinical Pharmacy
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    • v.23 no.2
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    • pp.123-128
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    • 2013
  • Purpose: The aim of study was to investigate the racial or ethnic differences in FDA-approved medications. Methods: Data on racial-based differences of drugs in PDR (Physician's Desk Reference) were analyzed by searching with keywords, "ETHNIC" and "RACE". Results: There were descriptions related to "ETHNIC" in product directions of 53 cases and "RACE" in 266 cases in 2010 PDR. After excluding 30 cases of duplicates, 289 cases were shown of which 28 cases were verified to demonstrate racial or ethnic differences. Drug category showing the higher racial or ethnic differences was cardiovascular drugs (7), followed by alimentary tract and metabolism drugs (6), nervous system drugs (5), and antineoplastic and immunomodulating agents (3). Pharmacokinetic differences between race and ethnicity were observed most frequently; differences in AUC or Cmax showed in 15 drugs and clearance differences in 7 drugs. Conclusions: This study identified the racial differences in medication usage in PDR. Therefore, the results can contribute to safe use of medication in real clinical settings in regards to the racial or ethnic differences.

새로운 Quinolone 항균제(Q-35)의 제 1 상 임상 연구

  • 임동석;이경훈;장인진;신상구;이명묵;김의종;김진규;권준수
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.189-189
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    • 1994
  • Q-35의 일회 및 반복투여 연구결과, 자타학 증상은 단지반복투여 피험자에서 중등도의 두통(1예)과 설사(3예)가 관찰되었으나 이들 설사증례는 장내 세균총 검사상 복감염에 의한 것이 아니었다. Q-35 투여 후 Q-EEG 및 평행기능의 장애 등은 관찰되지 않았으며 임상화학 검사상 반복투여 3예에서 SGOT, SGPT의 경미한 상승을 보였으나 이러한 변화는 정상 범위내에서의 변화이었다. Q-35의 반복투여에 따라 투약 3일에서 8일에 걸처 장내세균총은 일부 호기성 및 혐기성 세균총의 감소를 보였으나 투약종료 10일 후에는 투약전 상태로 회복되었다. Q-35는 투여량의 약 70 % 가 24시간 뇨중으로 배설되었으며 일회 및 반복투여의 결과 용량의존적인 동태양상은 관찰할 수 없었다. 50 mg에서 400 mg까지 일회 투여시 5.6-7.1 시간의 혈장반감기를 보였으며, 반복투여 시험에서는 평균 5.6 $\pm$ 0.7 시간의 반감기를 보였다. Q-35는 타액내로 신속히 이행되었으며 타액내 AUC는 혈장 AUC의 약 75 %에 해당하였고, 식사에 의해 약간의 흡수속도지연(Cmax 0.4 시간지연)과 공복시에 비해 82 %의 상대적 생체이용율을 보였다.

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Experimental Study on Compaction Effect of Hydraulic Fill Soils (실내실험을 통한 수중 매립토의 다짐효과 분석)

  • Lee, Haeng-Woo;Chang, Pyoung-Wuck;Chang, Woong-Hee;Bong, Tae-Ho
    • Proceedings of the Korean Geotechical Society Conference
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    • 2006.03a
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    • pp.301-310
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    • 2006
  • A series of laboratory tests was carried out for analyzing compaction characteristics of hydraulic fill soils(or hydraulically filled soils). Hydraulic fill soils were settled down by the weight of soil particle itself in water and consolidated by the extraction of water from the soil structures. Water content and dry unit weight were observed as the depth of sedimentation and consolidation soil. It was found from the result that the optimum water content $(W_{cpt})$ of the maximum unit weight$(\gamma_{dmax})$ is higher than that of laboratory compaction test(KS F 2312 A method). It was due to difference in compaction energy and compaction effect between two methods. And the maximum dry unit of hydraulic fill soil is smaller than that of laboratory compaction test. Especially in terms of compaction effect, the maximum relative compaction degrees$(R_{cmax})$ of Seamangum dredged sand, river sand and mixed sand, half and half of dredged and river sands, were 85%, 91% and 86%, respectively. It means that the compaction effect can be $85\sim91%$ of the maximum unit weight in laboratory compaction test.

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Pharmacokinetics of Cyclosporine in Rabbits with Carbon Tetrachloride and Bile Duct Ligation-induced Hepatic Disorder (사염화탄소 및 담도폐쇄 유발 간장장애 가토에서 싸이크로스포린의 약물동태)

  • Choi, Jun-Shik;Choi, Byong-Chul;Burm, Jin-Pil
    • YAKHAK HOEJI
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    • v.42 no.2
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    • pp.181-186
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    • 1998
  • This study was attempted to investigate the pharmacokinetics of cyclosporine (10mg/kg, oral) in rabbits with $CCI_4$ and bile duct ligation-induced hepatic disorder. The area under the curve (AUC) of blood cyclosporine concentration versus time was significantly increased ($CCI_4$-induced hepatic disorder. Elimination rate constant (Kel) was significantly decreased (p<0.05, p<0.01) in rabbits with $CCI_4$ and bile duct ligation-induced hepatic disorder. Volume of distribution (Vdss) and total body clearance (CLtot) were significantly decreased (p<0.01) in rabbits with $CCI_4$-induced hepatic disorder. But Vdss was significantly increased (p4-induced hepatic disorder were 874ng/ml and 2.71 hr, respectively. Cmax and Tmax values in rabbits with bile duct ligation were 105ng/ml and 2.834 hr, respectively. From results of this experiment. It is desirable to do therapeutic drug monitoring of cyclosporine for effective treatment when the cyclosporine is administered to patients with liver disorder m clinical practice.

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LC-MS/MS Assay Validation for a New Immune Modulator, JHL45, and its Major Metabolite in Plasma: Application to Pharmacokinetic Studies in Rats

  • Baek, In-Hwan;Chae, Jung-Woo;Song, Gyu-Yong;Kwon, Kwang-Il
    • Bulletin of the Korean Chemical Society
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    • v.30 no.11
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    • pp.2631-2636
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    • 2009
  • JHL45, a novel immune modulator for anti-atopic dermatitis and allergic airway disease, was synthesized from decursin isolated from Angelica gigas. In order to conduct a pharmacokinetic study of JHL45, an analytical method, ideally one that uses a minimal amount of biological sample must first be validated. In this study, a HPLC-MS/MS method was developed and validated for the quantification of JHL45 and its major metabolite, (+)-decursinol, from 10 ${\mu}L$ of rat plasma. JHL45 was stable under the analysis conditions, and intra- and inter-day accuracies exceeded 90.06%, with a precision variability ${\leq}$ 13.16% for each analyte. The mean values for Cmax, AUC8h, half-life of JHL45 in rats after intravenous administration of 5 mg/kg JHL45 were 24.59 μg/mL, 10.02 ${\mu}g{\cdot}h/mL$, and 1.88 h, respectively. The validated method herein will be useful for further pharmacokinetic studies of JHL45, as well as in preclinical and clinical phases.

Drug Interaction between Flavone and Paclitaxel in Rats (프라본과 파크리탁셀과의 약물상호작용)

  • 최준식;이진환
    • YAKHAK HOEJI
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    • v.47 no.2
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    • pp.98-103
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    • 2003
  • The purpose of this study was to investigate the effect of flavone (20 mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel (40 mg/kg) orally coadministered in rats. The plasma concentration of paclitaxel in combination with flavone was increased significantly (coadministration p<0.05, pretreatment p<0.0l) compared to that of control. Area under the plasma concentration-time curve (AVC) of paclitaxel with flavone was significantly (coadministration p<0.05, pretreatment p<0.0l) higher than that of control. Peak concentration (Cmax) of paclitaxel with flavone were significantly increased (coadministration p<0.05, pretreatment p<0.01) compared to that of control. Time to peak concentration (Tmax) of paclitaxel with flavone decreased significantly (p<0.05) than that of control. The total body clearance (CLt) and elimination rate constant ($\beta$) of paclitaxel with flavone were significantly reduced (p<0.05) compared to those of control. Half-life (t$_{1}$2/) of paclitaxel with flavone was significantly prolonged (p<0.05) compared to that of control. Based on these results, it might be concluded that flavone may enhance bioavailability of paclitaxel through the inhibition of cytochrome P450 and P-glycoprotein, which are engaged in paclitaxel absorption and metabolism in liver and gastrogintestinal mucosa, respectively.

Pharmacokinetics of Cefetamet Pivoxil in Korean Healthy Subject (건강한 한국 성인에서 세페타메트 피복실의 약물동태)

  • Noh, Keum-Han;Kang, Won-Ku
    • 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.

Pharmacokinetic Characteristics of Oral Clonazepam in Korean (한국인에서의 경구용 클로나제팜의 약물동력학적 특성)

  • 정지훈;유대식;박준홍;이석용;손의동
    • YAKHAK HOEJI
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    • v.48 no.5
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    • pp.278-284
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    • 2004
  • In order to determine the bioavailability of c1onazepam, an anxiolytic drug, a simple, rapid and sensitive HPLC analysis was developed in healthy Korean volunteers. The analysis system was validated in specificity, accuracy, precision and linearity. The analysis condition we established was 2.58 min and 5 ng/$m\ell$ in retention time and limit of quantitation of c1onazepam, respectively, using reverse-phase C18 column connected to UV detector. Quantitation was performed at 235 nm wave length with p-hydroxybenzoic acid ethyl ester as internal standard. The method involved a simple extraction. In order to study blood level profiles as a function of time, eight volunteers were enrolled and orally took 6 mg clonazepam once. The blood samples were collected from 0 to 120 h after the drug administration. Mean AUC and Cmax value were 1028.17$\pm$568.165 (ng/$m\ell$$.$hr) and 41.25$\pm$10.82 (ng/$m\ell$), respectively. And mean Tmax and T$_{1}$2/ value were 1.08$\pm$0.42 (hr) and 30.78$\pm$3.26 (hr). From the results we determine the pharmacokinetic characteristics of clonazepam in Korean people using a newly developed and useful HPLC method.

The Impact of Drug Interactions with Tyrosine Kinase Inhibitors on Adverse Event Development based on the changes of drug concentration level: Meta-analysis (Tyrosine Kinase 억제제와의 약물 상호작용이 약물 혈중농도 변화에 따라 부작용 발생에 미치는 영향: 메타분석 연구)

  • JinAh Hwang;Heeyoung Lee
    • Korean Journal of Clinical Pharmacy
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    • v.34 no.1
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    • pp.71-78
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    • 2024
  • Background: Oral cancer drugs, particularly tyrosine kinase inhibitors (TKIs), are increasingly popular due to their convenience. However, they pose challenges like drug interactions, especially with medications like azole antifungals. While the FDA provides some guidance, more detailed information is needed to manage these interactions effectively. A meta-analysis was conducted to understand the impact of interactions between TKIs and azole antifungals on adverse events during clinical studies. Methods: A meta-analysis followed PRISMA guidelines. Data from PubMed, EMBASE, and references were searched until November 30, 2021. Inclusion criteria encompassed studies on TKI-antifungal interactions in English. Study selection and quality assessment were conducted by two independent investigators. Results: Out of 158 articles, 11 were selected for analysis. Combination therapy showed a slight increase in adverse events but was not statistically significant (OR 1.02, 95% CI 0.49-2.13, p=0.95). AUC and Cmax fold changes did not significantly impact adverse event development. Both itraconazole and ketoconazole showed no significant difference in adverse event development compared to TKI alone. Conclusions: Study finds TKI-DDI not significantly linked to AE increase; azole antifungal types not related to AE. Future DDI research crucial for drug development.

Mode of Action of Water Soluble β-Glucan from Oat (Avena sativa) on Calorie Restriction Effect In-Vitro and In-Vivo Animal Models (In-Vitro, In-Vivo 동물모델에서 귀리 유래 수용성 베타-글루칸의 칼로리 제한 효과 작용기전 규명)

  • Kang, Hanna;Kim, Se-Chan;Kang, Yong Soo;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.30 no.6
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    • pp.1222-1228
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    • 2017
  • In the current study, we investigated the inhibitory activity of water soluble ${\beta}-glucan$ from oat (Avena sativa) against various digestive enzymes such as ${\alpha}-glucosidase$, sucrase, maltase and glucoamylase. Inhibition of these enzymes involved in the absorption of disaccharide can significantly decrease the post-prandial increase of blood glucose level after a mixed carbohydrate diet. The ${\beta}-glucan$ had the highest documented rate of small intestinal sucrase inhibitory activity (2.83 mg/mL, $IC_{50}$) relevant for potentially managing post-prandial hyperglycemia. Furthermore, we evaluated the effects of ${\beta}-glucan$ on the level of post-prandial blood glucose in animal model. The post-prandial blood glucose levels were tested two hours after sucrose/starch administration, with and without ${\beta}-glucan$ (100, and 500 mg/kg-body weight). The maximum blood glucose levels (Cmax) of ${\beta}-glucan$ administration group were decreased by about 23% (from $219.06{\pm}27.82$ to $190.44{\pm}13.18$, p<0.05) and 10% (from $182.44{\pm}13.77$ to $165.64{\pm}10.59$, p<0.01) in starch and sucrose loading test, respectively, when compared to control in pharmacodynamics study. The ${\beta}-Glucan$ administration significantly lowered the mean, maximum, and minimum level of post-prandial blood glucose at 30 min after meal. In view of the foregoing, it is felt that our findings suggest that ${\beta}-glucan$ from oat serves to reduce post-prandial blood glucose rise secondary to slower absorption of glucose in the small intestine, via carbohydrate hydrolyzing enzymes inhibition.