• Title/Summary/Keyword: Half Life

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Urokinase Conjugated with Water-Soluble Dextran

  • Kim Nam Deuk;Kim Hyun-Pyo;Byun Si Myung;Kim Sung Wan
    • Bulletin of the Korean Chemical Society
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    • v.6 no.4
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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
    • Proceedings of The Korean Society of Health Promotion Conference
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    • 1999.07a
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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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    • v.21 no.3
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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.

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

  • Choi, Hyun-Mi;Lee, Jin-Yong;Park, Yu-Chul
    • Journal of Soil and Groundwater Environment
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    • v.15 no.2
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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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    • v.16 no.8
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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.

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

  • Lee, Young-Deuk;Lee, Hae-Keun;Park, Young-Sun
    • Korean Journal of Environmental Agriculture
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    • v.2 no.2
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    • pp.59-64
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    • 1983
  • A study was undertaken to investigate the persistence of 2,4-D and MCPP in two different Suweon soils under field conditions. MCPP was extracted from soil with aqueous calcium hydroxide solution and then derivatized to pentafluorobenzyl ester to enhance the electron capture sensitivity. Total recovery of MCPP from soil was 85.6% and the detection limit for 20g sample was 0.02 ppm. Ethyl ester of 2,4-D applied to soil was rapidly hydrolysed to 2,4-D with the half-life of less than 1 day. Half-life of total 2,4-D ethyl ester, including 2,4-D, incorporated into soils at a rate of 0.045 ㎏ a.i./10a was $4{\sim}7$ days and that of under laboratory conditions was $7{\sim}8$ days. Half-life of MCPP applied at a rate of 0.25㎏ a.i./10a under field conditions was $9{\sim}12$ days and that of under laboratory conditions was $12{\sim}23$ days.

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

  • Kye, Young-Sik;Jeong, Keunhong;Kim, Dongwook
    • Applied Chemistry for Engineering
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    • v.31 no.5
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    • pp.475-480
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    • 2020
  • Chelates synthesized with Cu(II) ion and lactic acid or chitosan were applied to the hydrolysis of organophosphate simulant, DFP (diisopropyl fluorophosphate). Under the homogeneous reaction condition, Cu(II)-lactic acid chelate hydrolyzed DFP with the half life time of 37.1 min. Cu(II)-LMWS chitosan chelate was synthesized with 1 kDa molecular weight of chitosan, which showed low solubility, and then crystallized. The half life time for hydrolyzing DFP using Cu(II)-LMWS chitosan was 32.9 h indicating that the reaction rate is enhanced as much as 16 times more than that of using 18 kDa chitosan-Cu(II) complex. Under the homogeneous reaction condition, the half life time of Cu(II)-LMWS chitosan was 8.75 h. Therefore, we found out that the solubility of Cu(II)-LMWS chitosan makes the difference in the reaction rate as much as 4 times.

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

  • Kim, Hong-Ryul
    • Journal of the Korean Society for information Management
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    • v.32 no.4
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    • pp.7-27
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    • 2015
  • This study is to analyze impact factor, self-citation, immediacy index and cited half-life through citation analysis of scholarly journals of LIS field in Korea. This study was analysed the 9,329 references cited in Korean scholarly journal of LIS field. As a result, it analyzed that the articles of Korean LIS journal among the cited references in scholarly journal of LIS field in Korea is very insignificant. In other words, the percentage of citations was observed 19.1% in Journal of Korean Library and Information Science Society (KSLIS), 20.2% in Journal of the Korean Society for Library and Information Science (KLISS), 17.0% in Journal of the Korean Society for Information Management (KOSIM), 18.8% in Korean Biblia Society for Library and Information Science (KBIBLIA). Also, the cited half-life was analysed 5.87 years in KSLIS, 5.40 years in KLISS, 4.25 years in KOSIM, 3.57 years in KBIBLIA. And Impact factor has been found to be very low compared to journals of other fields.

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

  • Cho, Hoon;Chung, Yong-Seog
    • Archives of Pharmacal Research
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    • v.27 no.6
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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.

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

  • Choi, Jun Shik;Kim, Jin;Baek, Chae Sun;Do, Nam Yong;Kim, Sung Hwan;Park, Young Jin
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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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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