• Title/Summary/Keyword: Half Life

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Effects of feed intake and water hardness on fluralaner pharmacokinetics in layer chickens

  • Sari, Ataman Bilge;Gunes, Yigit;Anlas, Ceren;Alkan, Fulya Ustun;Guncum, Enes;Ustuner, Oya;Bakirel, Tulay
    • Journal of Veterinary Science
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    • v.23 no.5
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    • pp.64.1-64.9
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    • 2022
  • Background: Fluralaner is a novel drug belonging to the isoxazoline class that acts on external parasites of domestic animals. It is used systemically via drinking water, especially against red poultry mite in layer chickens. Fluralaner is frequently used in layers infected with D. gallinae. However, no study to date has investigated the effects of feed intake and water hardness. Objectives: This study aimed to investigate the effects of variable water hardness and feed intake on the pharmacokinetic profile of fluralaner. Methods: Layer chickens were divided into four groups (n = 8): fed + purified water (Group 1), feed restricted + purified water (Group 2), feed restricted + hard water (Group 3), and feed restricted + soft water (Group 4). After administering a single dose of the drug with drinking water, the blood samples were collected for 21 days. Fluralaner concentrations in plasma samples were determined by liquid chromatography/tandem mass spectrometry. The maximum plasma concentration (Cmax), time to reach maximum plasma concentration (tmax), area under the concentration-time curve values (AUC0-21d), half-life (t1/2), and other pharmacokinetic parameters were calculated. Results: Although the highest maximum plasma concentration (Cmax) was determined in Group 1 (fed + purified water), no statistically significant difference was found in the Cmax, tmax, t1/2, MRT0-inf_obs, Vz/Fobs, and Cl/F_obs parameters between the experimental groups. Conclusions: It was concluded that the feed intake or water hardness did not change the pharmacokinetic profile of fluralaner in layer chickens. Therefore, fluralaner could be used before or after feeding with the varying water hardness in poultry industry.

Biodistribution and pharmacokinetic evaluation of Korean Red Ginseng components using radioisotopes in a rat model

  • Sung-Won Kim;Byung-Cheol Han;Seung-Ho So;Chang-Kyun Han;Gyo In;Chae-Kyu Park;Sun Hee Hyun
    • Journal of Ginseng Research
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    • v.47 no.1
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    • pp.74-80
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    • 2023
  • Background: Although many studies have evaluated the efficacy and pharmacokinetics of Korean Red Ginseng (KRG) components (Rg1, Rb1, Rg3, Rd, etc.), few have examined the in vivo pharmacokinetics of the radiolabeled components. This study investigated the pharmacokinetics of ginsenosides and their metabolite compound K (CK), 20(s)-protopanaxadiol (PPD), and 20(s)-protopanaxatriol (PPT) using radioisotopes in rat oral administration. Methods: Sprague-Dawley rats were dosed orally once with 10 mg/kg of the tritium(3H) radiolabeled samples, and then the blood was collected from the tail vein after 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 24, 48, 96, and 168 h. Radioactivity in the organs, feces, urine, and carcass was determined using a liquid scintillation counter (LSC) and a bio-imaging analyzer system (BAS). Results and conclusion: After oral administration, as the 3H-labeled ginsenosides were converted to metabolites, Cmax and half-life increased, and Tmax decreased. Interestingly, Rb1 and CK showed similar values, and after a single oral administration of components, the cumulative excretion ratio of urine and feces was 88.9%-92.4%. Although most KRG components were excreted within 96-168 h of administration, small amounts of components were detected in almost all tissues and mainly distributed to the liver except for the digestive tract when observed through autoradiography. This study demonstrated that KRG components were distributed to various organs in the rats. Further studies could be conducted to prove the bioavailability and transmission of KRG components to confirm the mechanism of KRG efficacy.

Recent progress of enzyme cleavable linker in antibody-drug conjugates: sulfatase and phosphatase

  • Sushil K. Dwivedi;Abhinav Bhise;Rajkumar Subramani;Jeongsoo Yoo
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.1
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    • pp.33-40
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    • 2021
  • Recently, antibody-drug conjugates (ADCs) are used to deliver efficient cytotoxic payloads selectively in cancer cells. In the designing of an ADC, the antibody is connected to a toxic payload via a covalent linker, which helps to solubilizes the typical hydrophobic payload as well as stabilizes the linkage over circulation. The development of the linkers for the antibody drug conjugate is still in demand. Initially, the acid, disulfide, and cathepsin-sensitive ADCs attracted considerable attention for the delivery of a potent cytotoxic payload but suffer from instability in human and mouse plasma with a short half-life. In addition, It also suffer from a solubility issue that induces aggregation, which is the major problem in their development. ADCs associated with sulfatase and phosphatase cleavable linker are highly soluble due to the anionic nature of sulfate and phosphate groups. The ADCs also showed high stability in human and mouse plasma. Therefore, to overcome these limitations, sulfatase and phosphatase cleavable linkers were developed. This review focuses on the recently reported advantages of sulfatase and phosphatase cleavable linkers for ADCs.

A relationship of healthy eating status and body composition in Korean adults by their constitution type: A cross-sectional study (우리나라 성인의 사상체질에 따른 식생활 상태와 신체구성의 상관성에 관한 단면분석연구)

  • Kim, Jieun;Jeong, Kyoungsik;Baek, Younghwa;Lee, Siwoo
    • Journal of Sasang Constitutional Medicine
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    • v.34 no.1
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    • pp.46-57
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    • 2022
  • Background Adherence to healthy diet acts as a key role to modify sedentary lifestyle in real life setting. Constitution type of traditional Korean medicine has been prediagnosed to risk factors of cardiometabolic diseases. This study aims to evaluate the associations between body composition and healthy eating status in Korean adults by their constitution type. Methods Of 4046 participants from Korean Medicine Daejeon Citizen Cohort study, Korean Medicine Daejeon Citizen Cohort (KDCC) study were included for analysis. Demographic, health-related behaviors and Korean Medicine (KM) type were surveyed based on a general health-related questionnaire. Anthropometric measurements and dietary factors by using Korean Healthy Eating Index (KHEI) were assessed only in the half of the original participants. Results 50.8% of Taeeum was observed from eligible 1967 participants (66.7%, women). The highest KHEI score was observed in soyang group (52.0±0.3, p=0.006) compared to other two groups. In taeeum group, lower appendicular skeletal muscle mass (ASM)(%)(Taeeum: 38.7±0.1 vs. Soeum/Soyang: 39.2±0.1, p < 0.05), and higher percent of body fat (PBF)(%) (Taeeum: 32.9±0.2 vs. Soeum/Soyang: 29.0±0.2, p < 0.05) by the lowest tertile (T1) of the KHEI score, respectively. When the KHEI score increased by 1 point in taeeum group, a positive relationship was observed, which increased by 0.015% of ASM, however, a negatively related to in which body fat mass (BFM) decreased by 0.022 kg and PBF decreased by 0.024%. Conclusion Customized nutritional management is required that could help maintaining physical health and diet by their constitution type.

Study of Simultaneous Counting of Thyroid Uptake with Quantitative Analysis of Thyroid Scans (갑상샘 스캔 정량분석을 통한 갑상샘 섭취율 동시계측법 연구)

  • Jung-Soo Kim;Geun-Woo Kim
    • Journal of radiological science and technology
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    • v.46 no.5
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    • pp.401-408
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    • 2023
  • Thyroid uptake measurements can be subject to measurement errors due to the scoping and positioning of the thyroid gland. To compensate for these limitations, the clinical utility of the thyroid simultaneous counting method as an alternative to thyroid uptake measurement was analyzed and evaluated experimentally through quantitative analysis of images acquired after thyroid scanning. Experimental data were obtained using a Gamma camera (GE infinia), a thyroid uptake system (KOROID 1), and a thyroid neck phantom. Based on the thyroid uptake rate of 1-5% according to the protocol of thyroid scan test (99mTcO4 - , 370 MBq) in normal results, 99mTcO4 - was set in the range of 3.7-18.5 MBq (Matrix: 256×256, Scan time: 1 min, collimator: pin hole, phantom-collimator distances: 7 cm). The acquired images were corrected for the attenuation of isotopes due to the set-up time and half-life by applying the Auto Region of interest (ROI) drawing system, and the significance of the experimental results was evaluated by Multiple linear regression analysis (SPSS, ver. 22, IBM). The thyroid uptake rate showed a significant correlation between the dose and the measured counts when using the thyroid uptake system equipment. Meanwhile, the quantitative analysis counts of phantom images using Gamma camera also showed a significant correlation. Thus confirmed that the correlation between these two experiments was statistically significant (P<0.05). The simultaneous counting protocol, which indirectly measures thyroid uptake from thyroid scans, is likely to be clinically relevant if complemented by additional studies with different variables in patients with thyroid disease.

Development of Large-sized Propane Engine for Emission Reduction of Construction Machinery (건설기계의 배출가스 저감을 위한 대형 프로판 전용 엔진 개발)

  • Yongrae Kim;Cheolwoong Park;Hyungjun Jang;Young Choi;Moonyong Jeong;Myunghoon Han;Donghoon Jeong
    • Journal of the Korean Institute of Gas
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    • v.27 no.3
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    • pp.91-97
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    • 2023
  • Aging construction machinery and vehicles with old diesel engines usually have a long life span, so they continue to emit harmful emissions. Therefore, replacing these older diesel engines with engines that meet the latest emisstion standard is expected to help improve air quality, and engines with propane fuels, which are easily available at construction sites, can be an appropriate alternative. In this study, a propane fueled engine was developed based on a 6.8-liter CNG engine, and technologies such as gas injectors, exhaust gas recirculation (EGR), and enhanced catalysts were applied. As a result, nitrogen oxides achieved half of the emission performance at the Stage-V level, the latest emission standard, while securing diesel engine output and torque in the same class.

Determination of Hydroperoxyl/superoxide Anion Radical (HO2·/O2·-) Concentration in the Decomposition of Ozone Using a Kinetic Method

  • Kwon, Bum-Gun;Lee, Jai H.
    • Bulletin of the Korean Chemical Society
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    • v.27 no.11
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    • pp.1785-1790
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    • 2006
  • A novel kinetic method for determination of $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ in ozone decomposition in water is described. In this study, potential interferences of $O_3$ and the hydroxyl radicals, $^{\cdot}OH_{(O3)}$, are suppressed by $HSO_3{^-}/SO_3{^{2-}}$. $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ formed in ozone decomposition reduces $Fe^{3+}$-EDTA into $Fe^{2+}$-EDTA and subsequently the well-known Fenton-like (FL) reaction of $H_2O_2$ and $Fe^{2+}$-EDTA produces the hydroxyl radicals, $^{\cdot}OH_{(FL)}$. Benzoic acid (BA) scavenges $^{\cdot}OH_{(FL)}$ to produce OHBA, which are analyzed by fluorescence detection (${\lambda}_{ex}=320nm$ and ${\lambda}_{ex}=400nm$). The concentration of $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ in ozone decomposition has been determined by the novel kinetic method using the experimentally determined half-life ($t_{1/2}$). The steady-state concentration of $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ is proportional to the $O_3$ concentration at a given pH. However, the steady-state concentration of $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ in ozone decomposition is inversely proportional to pH values. This pH dependence is due to significant loss of $O_2{^{{\cdot}-}}$ by $O_3$ at higher pH conditions. The steady-state concentrations of $HO_2{^{\cdot}}/O_2{^{{\cdot}-}}$ are in the range of $2.49({\pm}0.10){\times}10^{-9}M(pH=4.17){\sim}3.01({\pm}0.07){\times}10^{-10}M(pH=7.59)$ at $[O_3]_o=60{\mu}M$.

A rare ginsenoside compound K (CK) induces apoptosis for breast cancer cells

  • Seun Eui Kim;Myoung-Hoon Lee;Hye-Myoung Jang;Wan-Taek Im;Joontaik Lee;Sang-Hwan Kim;Gwang Joo Jeon
    • Journal of Animal Reproduction and Biotechnology
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    • v.38 no.3
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    • pp.167-176
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    • 2023
  • Background: A breast cancer is the second leading cause of cancer death in women worldwide and among different types of breast cancers, triple-negative breast cancer (TNBC) has a poor prognosis. Methods: We investigated the potential of ginsenoside compound K (CK), an active ingredient in the bio-transformed ginsenoside, to be used as a therapeutic ingredient by examining the effects of CK on cell proliferation, apoptosis, and cancer-related gene expressions in breast cancer cells. Results: From the results of treating MCF-7, an ER and PR-positive breast cancer cells, and MDA-MB-231 (TNBC) with CK at a concentration of 0-100 µM, the half maximal inhibitory concentration (IC50) values for each cell were 52.17 µM and 29.88 µM, respectively. And also, it was confirmed that cell migration was inhibited above the IC50 concentration. In addition, fluorescence analysis of Apoptosis/Necrosis showed that CK induced apoptosis rather than necrosis of breast cancer cells. Through qPCR, it was confirmed that the expression of genes related to apoptosis and cell cycle arrest was increased in CK-treated breast cancer cells, and it acted more effectively on TNBC. However, the expression of genes related to tumor invasion and metastasis is also increased, so it is necessary to consider the timing of application of CK as a potential therapeutic anticancer compound. Conclusions: CK showed a stronger inhibitory effect in TNBC with poor prognosis but considering the high tumor invasion and metastasis-related gene expression, the timing of application of CK should be considered.

Detection Limit of a NaI(Tl) Survey Meter to Measure 131I Accumulation in Thyroid Glands of Children after a Nuclear Power Plant Accident

  • Takahiro Kitajima;Michiaki Kai
    • Journal of Radiation Protection and Research
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    • v.48 no.3
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    • pp.131-143
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    • 2023
  • Background: This study examined the detection limit of thyroid screening monitoring conducted at the time of the Fukushima Daiichi Nuclear Power Plant (FDNPP) accident in 2011 using a Monte Carlo simulation. Materials and Methods: We calculated the detection limit of a NaI(Tl) survey meter to measure 131I accumulation in the thyroid gland of children. Mathematical phantoms of 1- and 5-year-old children were developed in the simulation of the Particle and Heavy Ion Transport code System code. Contamination of the body surface with eight radionuclides found after the FDNPP accident was assumed to have been deposited on the neck and shoulder area. Results and Discussion: The detection limit was calculated as a function of ambient dose rate. In the case of 40 Bq/cm2 contamination on the body surface of the neck, the present simulations showed that residual thyroid radioactivity corresponding to thyroid dose of 100 mSv can be detected within 21 days after intake at the ambient dose rate of 0.2 µSv/hr and within 11 days in the case of 2.0 µSv/hr. When a time constant of 10 seconds was used at the dose rate of 0.2 µSv/hr, the estimated survey meter output error was 5%. Evaluation of the effect of individual differences in the location of the thyroid gland confirmed that the measured value would decrease by approximately 6% for a height difference of ±1 cm and increase by approximately 65% for a depth of 1 cm. Conclusion: In the event of a nuclear disaster, simple measurements carried out using a NaI(Tl) scintillation survey meter remain effective for assessing 131I intake. However, it should be noted that the presence of short-half-life radioactive materials on the body surface affects the detection limit.

Clinical and radiographic characteristics of pycnodysostosis: A systematic review

  • Amanda Katarinny Goes Gonzaga;Carla Samily de Oliveira Costa;Hannah Gil de Farias Morais;Brazm da Fonseca Neto;Leao Pereira Pinto;Wagner Ranier Maciel Dantas;Patricia Teixeira de Oliveira;Daniela Pita de Melo
    • Imaging Science in Dentistry
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    • v.54 no.1
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    • pp.13-24
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    • 2024
  • Purpose: Pycnodysostosis (PYCD), an autosomal recessive syndrome, is characterized by an imbalance in bone remodeling that produces various clinical and radiographic craniofacial manifestations. This review represents a systematic examination of these manifestations, as well as oral features associated with PYCD. Materials and Methods: A systematic review was conducted across 8 databases from February to March 2023. The search strategy focused on studies reporting cases of PYCD that examined the clinical and radiographic craniofacial and oral characteristics associated with this syndrome. Results: The review included 84 studies, encompassing a total of 179 cases of PYCD. More than half of the patients were female (55.3%), and the mean age was 14.7 years. Parental consanguinity was reported in 51.4% of the cases. The most common craniofacial clinical manifestation was a prominent nose, observed in 57.5% of cases. Radiographically, the most frequently reported craniofacial characteristics included the presence of an obtuse mandibular angle (84.3%) and frontal cranial bosses(82.1%). Clinical and radiographic examinations revealed oral alterations, with micrognathia present in 62.6% of patients and malocclusion in 59.2%. Among dental anomalies, tooth agenesis was the most commonly reported, affecting 15.6% of patients. Conclusion: Understanding the clinical and radiographic craniofacial features of PYCD is crucial for dental professionals. This knowledge enables these clinicians to devise effective treatment plans and improve patient quality of life.