• 제목/요약/키워드: Half Life

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Urokinase Conjugated with Water-Soluble Dextran

  • 김남득;김현표;변시명;김성완
    • Bulletin of the Korean Chemical Society
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    • 제6권4호
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    • pp.210-214
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    • 1985
  • Urokinase, a plasminogen activator, was conjugated with dextran by the cyanogen bromide activation-coupling method. The resulting water-soluble conjugate was purified by gel permeation chromatography on Sephadex G-200. The maximal activity was obtained when the ratio of urokinase/dextran was 1/20 for the coupling. The final preparation showed 5 CTA units/mg conjugate, 300 CTA units/mg protein, 8.4 % activity retention, and 47 % protein retention. The urokinase-dextran conjugate had good thermal, pH and storage stabilities. In addition, it showed greater resistance to the inhibitory effect of human plasma than native urokinase. Also in vitro biological half-life of urokinase increased 40 times by this conjugation. In view of activity, excellent stability and increased half-life, the conjugate can be a potential fibrinolytic agent in an injectable form.

Health Promotion: An Emerging Strategy for Health Enhancement and Business Cost Savings in Korea

  • Donnell, Michael
    • 한국보건교육건강증진학회:학술대회논문집
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    • 한국보건교육건강증진학회 1999년도 3rd International Symposium
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    • pp.107-116
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    • 1999
  • .Half of deaths are caused by life-style related problems in developed nations. .Health promotion can improve life-style and health. .Improvements in life-style and health lead to savings in medical care core costs and enhancements in productivity. .Win-Win-Win-Win : Management, Labor, Employees and Government benefit

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Allometric analysis of tylosin tartrate pharmacokinetics in growing male turkeys

  • Pozniak, Blazej;Tikhomirov, Marta;Motykiewicz-Pers, Karolina;Bobrek, Kamila;Switala, Marcin
    • Journal of Veterinary Science
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    • 제21권3호
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    • pp.35.1-35.11
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    • 2020
  • Background: Despite common use of tylosin in turkeys, the pharmacokinetic (PK) data for this drug in turkeys is limited. Within a few months of growth, PK of drugs in turkeys undergoes changes that may decrease their efficacy due to variable internal exposure. Objectives: The objective of this study was to investigate the influence of age on the PK of a single intravenous (i.v.) and oral administration of tylosin to turkeys at a dose of 10 and 50 mg/kg, respectively. Methods: Plasma drug concentrations were measured using high-performance liquid chromatography with UV detection. The PK parameters were assessed by means of non-compartmental approach and were subjected to allometric analysis. Results: During a 2.5-month-long period of growth from 1.4 to 14.7 kg, the median value for area under the concentration-time curve after i.v. administration increased from 2.61 to 7.15 mg × h/L and the body clearance decreased from a median of 3.81 to 1.42 L/h/kg. Over the same time, the median elimination half-life increased from 1.03 to 2.96 h. For the oral administration a similar trend was noted but the differences were less pronounced. Bioavailability was variable (5.76%-21.59%) and age-independent. For both routes, the plasma concentration of the major tylosin metabolite, tylosin D, was minimal. Protein binding was age-independent and did not exceed 50%. Allometric analysis indicated a relatively poor predictivity of clearance, volume of distribution and elimination half-life for tylosin in turkeys. Conclusions: Age has a significant impact on tylosin PK in turkeys and dosage adjustment may be needed, particularly in young individuals.

강원도 및 경기도 소재 유류오염지역의 수질특성, 발현 생분해능과 오염물질 저감속도 (A Study on Groundwater Quality and Biodegradability at the Petroleum Contaminated Sites of Kangwon and Gyeonggi Provinces, Korea)

  • 최현미;이진용;박유철
    • 한국지하수토양환경학회지:지하수토양환경
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    • 제15권2호
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    • pp.24-33
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    • 2010
  • This study focused on the groundwater quality, biodegradability and attenuation rate at the petroleum contaminated sites of Kangwon and Gyeonggi Provinces, Korea. For groundwater quality, Kangwon site showed chemical compositions of $Ca-SO_4+Cl$, $Ca-HCO_3$ and $Na+K-HCO_3$ types, while Gyeonggi site showed chemical compositions of $Ca-SO_4$, $Ca-HCO_3$ and $Na-HCO_3$ types. $Na+K-HCO_3$ and $Na-HCO_3$ types were detected only in February. Among many biodegradation processes, the majority was attributed to biodegradation from denitrification in both area. In Kangwon site, biodegradation from denitrification occupied 63.5%, and in Gyeonggi site it was 39.45%. Biodegradation from the most efficient aerobic respiration occupied 7.12% in Kangwon site, while Gyeonggi site in it did 27.29%. Point attenuation rate of BTEX in Gyeonggi site (GW-22) was 0.0182 $day^{-1}$, half life of BTEX was 84 days, and thus 124 days (0.34 year) would be required to clean up this site. Mean of point attenuation rate of TPH in Kangwon site was 0.0088 $day^{-1}$, mean of half life was 257 days, and thus 462 days would be required to clean up the site. Mean of point attenuation rate of TPH in Gyeonggi site was 0.0387 $day^{-1}$, mean of half life was 55 days, and thus remediation time was calculated as 99 days.

Breast Cancer Association with CYP1A2 Activity and Gene Polymorphisms - a Preliminary Case-control Study in Tunisia

  • Ayari, I;Arnaud, MJ;Mani, A;Pavanello, S;Saguem, S
    • Asian Pacific Journal of Cancer Prevention
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    • 제16권8호
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    • pp.3559-3563
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    • 2015
  • The aim of the present study was to evaluate the relative contribution of CYP1A2 isoforms (-3860 G/A, -2467T/delT and -163C/A) in control subjects and breast cancer patients to the metabolism of caffeine in human liver. Restriction fragment length polymorphism analysis of PCR-amplified Fragments (PCR-RFLP) was used for the genotyping of CYP1A2 SNPs and HPLC allowed the phenotyping through the measurement of CYP1A2 activity using the 17X + 13X + 37X/137X urinary metabolite ratio (CMR) and plasma caffeine half life (T1/2). The CYP1A2 -3860A genotype was associated with a decreased risk of breast cancer. In contrast, distributions of the CYP1A2 -2467T/delT or -2467delT/delT and -163A/C or A/A genotypes among breast cancer patients and controls were similar. When the genotype and phenotype relationship was measured by comparing the mean CMR ratios and caffeine half life within the genotype groups between subjects and breast cancer patients, there were no significant differences except for -3860 A, most of them being homozygous for the -3860 G/G SNP and had a significant higher mean CMR ratio and half life than those with -3860 G/A (P=0.02). The results of this preliminary study show a significant association between CP1A2 -3860 G variant and CYP1A2 phenotype which must be confirmed by further large-size case-control studies.

토양중(土壤中) 2,4-D와 MCPP의 잔류특성(殘留特性) (Persistence of 2,4-D and MCPP in Soil)

  • 이영득;이해근;박영선
    • 한국환경농학회지
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    • 제2권2호
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    • pp.59-64
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    • 1983
  • 수원소재(水原所在) 2개토양(個土壤)에서 2,4-D ethyl ester 및 MCPP의 토양중(土壤中) 잔유소장(殘油消長)을 조사(調査)한 결과(結果)는 다음과 같다. 1) 살포(撒布)한 2,4-D ethyl ester는 토양중(土壤中)에서 신속(迅速)히 가수분해(加水分解)되어 2,4-D를 생성(生成)하였다. 2) 포장조건하(圃場條件下)에서 2,4-D 잔유분(殘留分)을 포함한 총(總) 2,4-D ethyl ester의 반감기(半減期)는 $4{\sim}7$일(日)이었으며 실험실(實驗室) 조건하(條件下)에서는 다소 긴 $4{\sim}7$일(日)이었다. 3) 포장조건하(圃場條件下)에서의 토양중(土壤中) MCPP의 반감기(半減期)는 $9{\sim}12$일(日)이었고 실험실(實驗室) 조건하(條件下)에서는 다소 긴 $12{\sim}23$일(日)의 반감기(半減期)를 보였다.

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Cu(II)-Lactic Acid와 Cu(II)-LMWS-Chitosan 착물의 DFP 가수분해반응 연구 (Hydrolysis of DFP Using Cu(II)-Lactic Acid and Cu(II)-LMWS-Chitosan Chelates)

  • 계영식;정근홍;김동욱
    • 공업화학
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    • 제31권5호
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    • pp.475-480
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    • 2020
  • Lactic acid와 키토산을 Cu(II) 이온과 반응시켜 합성한 착물을 사용하여 유기인 유사 독성물질인 DFP (Diisopropyl fluorophosphate) 분해반응에 적용하였다. Cu(II)-lactic acid 착물의 경우 homogeneous 상태에서 분해반응 반감기가 37. 1 min으로 분해성능이 우수하였다. 1 kDa 저분자량 수용성 키토산으로 합성한 Cu(II)-LMWS chitosan 착물은 결정화 후에는 용해도가 낮아 heterogeneous 한 상태에서 분해반응이 진행되었으며 그 반감기는 32.9 h이었다. 이 결과는 기존에 연구된 18 kDa 키토산 Cu(II)착물의 분해반응속도보다 약 16배 정도 증가된 것이다. Cu(II)-LMWS chitosan 착물을 결정화하지 않고 homogeneous한 상태로 진행한 분해반응에서는 반감기가 8.75 h로 용해도에 따라 약 4배의 차이를 확인할 수 있었다.

국내 문헌정보학분야 학술지의 상호인용관계 분석 (Citation Analysis of Scholarly Journals of Library & Information Science Field in Korea)

  • 김홍렬
    • 정보관리학회지
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    • 제32권4호
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    • pp.7-27
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    • 2015
  • 본 연구는 국내 문헌정보학분야 유력 학술지간의 상호 인용관계를 바탕으로 영향지수, 즉시성지수, 피인용반감기, 자기인용비율을 밝히고자 하였다. 이를 위하여 2014년에 발행된 국내 문헌정보학 분야 학술지 4종의 학술논문 252건에서 인용한 인용문헌 9,329건을 대상으로 분석하였다. 그 결과 국내 주요 학술지의 인용문헌 비율은 한국도서관 정보학회지가 20.2%, 한국문헌정보학회지 19.1%, 한국비블리아학회지 18.8%, 정보관리학회지 17.0%의 순으로 나타나 국내 학술논문 생산에 주요 학술지 논문의 활용이 미미한 것으로 분석되었다. 또한 피인용반감기는 정보관리학회지가 4.25년, 한국문헌정보학회지가 5.87년, 한국도서관 정보학회지가 5.40년, 한국비블리아학회지가 3.57년으로 나타나 비교적 최신논문을 인용하고 있었으며, 영향력 지수는 0.47~0.67로 나타나 타 주제 분야 학술지에 비해 낮은 지수를 보였다.

Water Soluble Cyclosporine Monomethoxy Poly(ethyleneglycol) Conjugates as Potential Prod rugs

  • Cho, Hoon;Chung, Yong-Seog
    • Archives of Pharmacal Research
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    • 제27권6호
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    • pp.662-669
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    • 2004
  • The highly water-soluble monomethoxypoly(ethyleneglycol) (mPEG) prod rugs of cyciosporin A(CsA) were synthesized. These prod rugs were prepared by initially preparing intermediate in the form of carbonate at the 3'-positions of CsA with chloromethyl chloroformate, in the pres-ence of a base to provide a 3'-carbonated CsA intermediate. Reaction of the CsA intermediate with mPEG derivative in the presence of a base provides the desired water-soluble prod rugs. As a model, we chose molecular weight 5 kDa mPEG in the reaction with CsA to give water soluble prodrugs. To prove that the prod rug is decomposed in the body to produce CsA, the enzymatic hydrolysis test was conducted using human liver homogenate at $37^{\circ}C$. The prodrug was decomposed in human liver homogenate to produce the active material, CsA, and the hydrolysis half-life ($t_{1/2}$) of the prodrug, KI-306 was 2.2 minutes at $37^{\circ}C$. However, a demon-stration of non-enzymatic conversion in pH 7.4 phosphate buffer was provided by the fact that the half-life ($t_{1/2}$) is 21 hours at 37$^{\circ}C$. The hydrolysis test in rat whole blood was also conducted. The hydrolysis was seen with half-life ($t_{1/2}$) of about 9.9, 65.0, 14.2, 3.4, 2.1 9.5, and 1.6 minutes for KI-306, 309, 312, 313, 315, 316, and 317, respectively. This is the ideal for CsA prodrug. The pharmacokinetic study of the prodrug, KI-306, in comparison to the commer-cial product (Sandimmune Neoral Solution) was also carried out after single oral dose. Each rat received 7 mg/kg of CsA equivalent dose. Especially, the prodrug KI-306 exhibits higher AUC and $C_{max}$ than the conventional Neoral. The AUC and $C_{max}$ were increased nearly 1.5 fold. The kinetic value was also seen with $T_{max}$ of about 1.43 and 2.44 hours for KI-306 and Neoral, respectively.

계절리듬이 겐타마이신의 약물동태에 미치는 영향 (The Effect of Seasonal Rhythm on the Gentamicin Pharmacokinetics in Healthy Volunteers)

  • 최준식;김진;백채선;도남용;김성환;박영진
    • 한국임상약학회지
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    • 제8권2호
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    • pp.89-94
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    • 1998
  • Seasonal rhythmic changes in gentamicin pharmacokinetics was evaluated in 10 healthy male volunteers after single intravenous 80 mg administration of gentamicin at 9:00 a.m. during summer and winter. The mean terminal half-life and AUC of gentamicin were $3.56\pm0.14\;hr\;and\;25.03\pm2.84\;{\mu}g/ml{\cdot}hr$ in winter and $3.08\pm0.41\;hr\;and\;21.84\pm2.51\;{\mu}g/ml{\cdot}hr$ in summer. The mean total body clearance $(CL_t)$ and elimination rate constant $(k_{10})$ of gentamicin was $3.17\pm0.43\;L/hr,\;0.458\pm0.06\;hr^{-1}\;in\;winter\;and\;3.66\pm0.45\;L/hr,\;0.561\pm0.07\;hr^{-1}$ in summer, The mean volumn of distribution $(V_{dss})$ of gentamicin at steady state was $12.65\pm1.09$L in winter and $12.39\pm1.25$ L in summer. Serum concentrations of gentamicin in winter were increased significantly during 4-8 hr (p<0.05) compared to those of gentamicin in summer. The elimination rate constant $(k_{10})$ of gentamicin in winter was decreased significantly $(p<0.05)$ compared to that of gentamicin in summer. The mean volume of distribution at steady state $(V_{dss})$, AUC, mean total body clearance ($CL_t$) and terminal half-life of gentamicin in the winter were increased but were not significant. The mean intrasubject fluctuations in terminal half-life, AUC and $CL_t$ between winter and summer were 8.2, 11.0 and $6.0\%$ respectively.

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