• Title/Summary/Keyword: Half Life

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Permeability of a Capsaicin Derivative $[{14}^C]DA-5018$ to Blood-Brain Barrier Corrected with HPLC Method

  • Kang, Young-Sook;Kim, Jong-Mi
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.165-172
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    • 1999
  • In the present work , the transport mechanism of a capsaicin derivative, DA-5018, through blood-brain barrier (BBB) has been investigated to evaluate the feasibility of potential drug development. The result of pharmacokinetic parameters obtained from the intravenous injection of plasma volume marker,$[3^H]RSA$ and $[{14}^C]DA-5018$, indicated that both AUC, area under the plasma concentration curve and VD, volume of distribution in brain of $[3^H]RSA$ agreed with those reported ($1620{\pm}10 $percentage injected dose minute per milliliter (%IDmin/ml) and $12.0{\pm}0.1{\mu}l/g$, respectively). Elimination half-life and AUC of $[{14}^C]DA-5018$is corrected by the PHLC analysis, 19.6$\pm$1.2 min and 7.69$\pm$0.85% IDmin/ml, respectively. The metabolic rate of $[{14}^C]DA-5018$was very rapid. The blood-brain barrier permeability surface area (PS) product of $[{14}^C]DA-5018$ was calculated to be 0.24$\pm$0.05 $\mu$l/min/g. The result of internal carotid artery perfusion and capillary depletion suggested that [14C]DA-5018 pass through BBB with the time increasingly. Investigation of transport mechanism of $[{14}^C]DA-5018$ using agonist and antagonist suggested that vanilloid (capsaicin) receptor did not exist in the BBB, and nutrient carrier system in the BBB has no effect on the transport of DA-5018. In conclusion, despite the fact that penetration of DA-5018 through BBB is significant, the intact drug found in the brain tissue is small because of a rapid metabolism. Therefore, for the central analgesic effect of DA-5018, the method to increase the metabolic stability in plasma and the brain permeability should be considered.

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HPLC Determination of Tolperisone in Human Plasma

  • Bae Jung-Woo;Park Young-Seo;Sohn Uy-Dong;Myung Chang-Sun;Ryu Byung-Kwon;Jang Choon-Gon;Lee Seok-Yong
    • Archives of Pharmacal Research
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    • v.29 no.4
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    • pp.339-342
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    • 2006
  • A simple high performance liquid chromatographic (HPLC) method was developed for the determination of tolperisone in human plasma. Tolperisone and internal standard (chlorphenesin) were isolated from 1 mL of plasma using 8 mL of dichlormethane. The organic phase was collected and evaporated under nitrogen gas. The residue was then reconstituted with 300 mL aliquot of mobile phase and a 100 mL aliquot was injected onto the $C_{18}$ reverse-phased column. The mobile phase, $45\%$ methanol containing $1\%$ glacial acetic acid and $0.05\%$ 1-hexanesulfonic acid was run at a flow rate of 1 mL/min. The column effluent was monitored using UV detector at 260 nm. The retention times for tolperisone and the internal standard were approximately 7.1 and 8.4 min, respectively. The standard curve was linear with minimal intra-day and inter-day variability. The quantification limit of tolperisone in human plasma was 10 ng/ mL. The proposed method has been applied to the determination of pharmacokinetic profile of tolperisone in Koreans. The T max of tolperisone in Koreans $(0.94{\pm}0.42\;h)$ was not significantly differ from that reported in Europeans (0.5-1 h), but the mean half-life in Koreans $(1.14{\pm}0.27\;h)$ was shorter than that in Europeans $(2.56{\pm}0.2\;h)$. The proposed HPLC method is simple, accurate, reproducible and suitable for pharmacokinetic study of tolperisone.

Transient Neonatal Diabetes Mellitus Managed with Continuous Subcutaneous Insulin Infusion (CSII) and Continuous Glucose Monitoring

  • Kim, Min Soo;Kim, Sung Eun;Lee, Na Yeong;Kim, Seul Ki;Kim, Shin Hee;Cho, Won Kyoung;Cho, Kyoung Soon;Jung, Min Ho;Suh, Byung-Kyu;Ahn, Moon Bae
    • Neonatal Medicine
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    • v.28 no.1
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    • pp.41-47
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    • 2021
  • Neonatal diabetes mellitus can be categorized as transient, permanent, or syndromic, and approximately half of the cases are transient. We present a case involving a term newborn who showed overt progression of transient neonatal diabetes mellitus, with complete remission within 6 months. On the second day of life, the patient presented with tachypnea, hyperglycemia, and decreased serum levels of C-peptide and insulin. Continuous subcutaneous infusion of insulin and continuous glucose monitoring were well tolerated. The patient showed a normal growth pattern, with no hyperglycemic or hypoglycemic episodes at 6 months of age. As it is rare and often asymptomatic, hyperglycemia may be attributed to various factors, including intrauterine environment, perinatal stress, and diverse genetic background. Therefore, consistent blood glucose monitoring and prompt early insulin therapy are crucial for any term newborns with persistent hyperglycemia, to prevent further diabetic complications. Moreover, continuous subcutaneous insulin infusion and the utilization of continuous glucose monitoring devices are the most effective and practical management strategies.

A Survey on Clinical Practice Patterns of Patients with Cancer at Korean Medical Hospitals for Korean Medicine Cancer Registry (한의 암 레지스트리 연구를 위한 암 환자의 한방병원 진료현황에 대한 전문가집단 설문조사)

  • Yoon, Jee-Hyun;Park, Su Bin;Kim, Eun Hye;Lee, Jee Young;Yoon, Seong Woo
    • Journal of Korean Traditional Oncology
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    • v.26 no.1
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    • pp.17-27
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    • 2021
  • Objective: This study aimed to evaluate which information of cancer patients should be collected for the Korean medicine cancer registry in order to assess the efficacy and safety of Korean medicine (KM) treatment and to identify Korean medical prognostic predictors. Methods: A total of fifteen Korean medical specialists completed an online survey questionnaire including items about general characteristics of cancer patients and clinical practice patterns. Results: The four main types of cancer at Korean medical hospitals were breast, lung, stomach, and colorectal cancer. The majority of patients with cancer at Korean medical hospitals were in the advanced or metastatic stage (50.0%). The prominent purposes of KM treatment were to alleviate cancer-related symptoms, reduce the side effects of conventional therapy, and improve quality of life. The major options for treatment were traditional herbal medicine (THM), acupuncture, moxibustion, thermotherapy, pharmacoacupuncture, and meditation, with THM being the most frequently used (35.7%). Almost all Korean medical specialists (93.9%) used syndrome differentiation in clinical practice and identified over half the cancer patients as deficiency syndrome (57.2%). Conclusion: Physicians considered the primary goal of KM treatment for cancer patients to be symptom management since advanced or metastatic stage patients were the majority at Korean medical hospitals. THM were the most common treatment option and syndrome differentiation was used by almost all physicians. Further research is needed to monitor and ensure optimal KM treatment for patients with cancer.

Heteroexpression and Functional Characterization of Glucose 6-Phosphate Dehydrogenase from Industrial Aspergillus oryzae

  • Guo, Hongwei;Han, Jinyao;Wu, Jingjing;Chen, Hongwen
    • Journal of Microbiology and Biotechnology
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    • v.29 no.4
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    • pp.577-586
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    • 2019
  • The engineered Aspergillus oryzae has a high NADPH demand for xylose utilization and overproduction of target metabolites. Glucose-6-phosphate dehydrogenase (G6PDH, E.C. 1.1.1.49) is one of two key enzymes in the oxidative part of the pentose phosphate pathway, and is also the main enzyme involved in NADPH regeneration. The open reading frame and cDNA of the putative A. oryzae G6PDH (AoG6PDH) were obtained, followed by heterogeneous expression in Escherichia coli and purification as a his6-tagged protein. The purified protein was characterized to be in possession of G6PDH activity with a molecular mass of 118.0 kDa. The enzyme displayed maximal activity at pH 7.5 and the optimal temperature was $50^{\circ}C$. This enzyme also had a half-life of 33.3 min at $40^{\circ}C$. Kinetics assay showed that AoG6PDH was strictly dependent on $NADP^+$ ($K_m=6.3{\mu}M$, $k_{cat}=1000.0s^{-1}$, $k_{cat}/K_m=158.7s^{-1}{\cdot}{\mu}M^{-1}$) as cofactor. The $K_m$ and $k_{cat}/K_m$ values of glucose-6-phosphate were $109.7s^{-1}{\cdot}{\mu}M^{-1}$ and $9.1s^{-1}{\cdot}{\mu}M^{-1}$ respectively. Initial velocity and product inhibition analyses indicated the catalytic reaction followed a two-substrate, steady-state, ordered BiBi mechanism, where $NADP^+$ was the first substrate bound to the enzyme and NADPH was the second product released from the catalytic complex. The established kinetic model could be applied in further regulation of the pentose phosphate pathway and NADPH regeneration of A. oryzae to improve its xylose utilization and yields of valued metabolites.

Reliability and Validity of an Instrument Assessing Spiritual Needs of Families of Terminal Cancer Patients (말기 환자 가족 영적요구 측정도구의 신뢰도 및 타당도 검증)

  • Kang, Kyung-Ah;Choi, Youngsim;Kim, Yejean
    • Journal of Hospice and Palliative Care
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    • v.21 no.4
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    • pp.144-151
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    • 2018
  • Purpose: The purpose of this study was to test the reliability and validity of an instrument that measures spiritual needs of families of terminal cancer patients. Methods: This methodological study was processed as follows: 1) The preliminary 26 items were developed based a conceptual framework of spiritual needs of families of patients with cancer. 2) The content was validated by an expert panel (Three nursing professors and five hospice nursing specialists). 3) The instrument was validated by a survey (n=111). 4) Twenty-six items were selected and used for the final version of the scale. Results: Three factors were extracted through factor analysis: 'relationship with God/Acceptance of dying', 'recovery of relationship/hope and peace', and 'meaning and purpose of life'. These factors explained 61.088% of the total variance. Cronbach's alpha and Guttman split-half coefficient of the 26 items were 0.944 and 0.826 respectively. Conclusion: This scale was identified as a valid and reliable tool. Therefore, the scale is useful in assessing spiritual needs of families of terminal cancer patients in the field of hospice and palliative care.

The exfoliation of irradiated nuclear graphite by treatment with organic solvent: A proposal for its recycling

  • Capone, Mauro;Cherubini, Nadia;Cozzella, Maria Letizia;Dodaro, Alessandro;Guarcini, Tiziana
    • Nuclear Engineering and Technology
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    • v.51 no.4
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    • pp.1037-1040
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    • 2019
  • For the past 50 years, graphite has been widely used as a moderator, reflector and fuel matrix in different kinds of gas-cooled reactors. Resulting in approximately 250,000 metric tons of irradiated graphite waste. One of the most significant long-lived radioisotope from graphite reactors is carbon-14 ($^{14}C$) with a half-life of 5730 years, this makes it a huge concern for deep geologic disposal of nuclear graphite (NG). Considering the lifecycle of NG a number of waste management options have been developed, mainly focused on the achievement the radiological requirements for disposal. The existing approaches for recycling depend on the cost to be economically viable. In this new study, an affordable process to remove $^{14}C$ has been proposed using samples taken from the Nuclear Power Plant in Latina (Italy) which have been used to investigate the capability of organic and inorganic solvents in removing $^{14}C$ from exfoliated nuclear graphite, with the aim to design a practicable approach to obtain graphite for recycling or/and safety disposed as L& LLW.

A Study on Development of Early Childhood Teacher's Guidance Efficacy Scale (유아교사의 생활지도 효능감 척도개발 연구)

  • Choi, Yeun Hwa
    • Korean Journal of Child Education & Care
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    • v.19 no.2
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    • pp.165-176
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    • 2019
  • Objective: The purpose of this study is to develop a measure of the Early Childhood Teacher's Guidance Efficacy Scale based on guidance and teacher-efficacy theory. Methods: This subjects were 243 teachers in Seoul and Gyeonggi-do. Results: An exploratory factor analysis was conducted on the data collected of 4 factors, namely, guidance efficacy for problem behavior, children understanding, home-connected, basic life habits. In addition, there are significant positive correlations between the sub-area score and the overall in the early childhood teacher's guidance efficacy scale(r = .26 ~ .72, p < .001). Internal consistency and split-half reliability of each sub scale were reasonably accept. Conclusion/Implications: 'The guidance efficacy scale for early childhood teachers' developed in this study is an appropriate tool. Therefore, the developed scale can become a useful tool to measure the overall guidance efficacy level of early childhood teachers.

Purification and Characterization of Metalloprotease from Serratia marcescens PPB-26 and Its Application for Detergent Additive

  • Thakur, Shikha;Sharma, Nirmal Kant;Thakur, Neerja;Bhalla, Tek Chand
    • Microbiology and Biotechnology Letters
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    • v.47 no.2
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    • pp.259-268
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    • 2019
  • In this study, the extracellular metalloprotease from Serratia marcescens PPB-26 was purified to homogeneity via ethanol fractionation and DEAE-cellulose column chromatography. Thus, a 3.8-fold purification was achieved with a 20% yield and specific activity of 76.2 U/mg. The purified protease was a 50-kDa monomer whose optimum pH and temperature for activity were 7.5 and $30^{\circ}C$ respectively; however, it was found to remain active in the 5-9 pH range and up to $40^{\circ}C$ for 6 h. The protease had a half-life of 15 days at $4^{\circ}C$, an optimum reaction time of 10 min, and an optimum substrate (casein) concentration of 0.25%. Furthermore, the Michaelis constant ($K_m$) and reaction velocity ($V_{max}$) of the protease were calculated to be 0.28% and $111.11{\mu}moles/(min{\cdot}mg)^{-1}$, respectively. The protease was stable when subjected to metal ions (2 mM), showing increased activity with most (especially $CoCl_2$ and $MgSO_4$ (30.54% increase)). It was also stable when exposed to oxidizing agents, bleaching agents, and detergents (5% v/v for 60 min). It retained 93% of its activity in non-ionic detergents (Tween-20, Tween-80, and Triton X-100). Moreover, wash performance analysis in commercial detergents (Ariel and Tide) showed that not only was the protease capable of protein stain removal, but also reduced cleaning time by 80% when added to detergents. Thus, the Serratia marcescens PPB-26 metalloprotease appears to be a promising new candidate as a laundry additive in the detergent industry.

Effect of Gamma Rays Emitted by the 99mTc on the CT Image (99mTc에서 방출되는 감마선이 CT 영상에 미치는 영향)

  • Park, Jae-Yoon;Lee, Yong-Ki
    • Journal of the Korean Society of Radiology
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    • v.13 no.2
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    • pp.169-174
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    • 2019
  • This study examines the changes that $^{99m}Tc$ causes to CT(Computed Tomography) images quantitatively when CT scans were continuously performed using $^{99m}Tc$. With the use of the CT, $^{99m}Tc$ 740MBq was injected into the Resolution Phantom and Water Phantom, and the tube voltage was changed with 80 kVp and 120 kVp, scanning before and after the injection. The result indicate, by comparing the Signal Intensity according to the presence or absence of the $^{99m}Tc$ injection with the tube voltage of 120 kVp and 80 kVp, a decrease of 0.173 and 0.241 was observed respectively and the spatial resolution increase of 0.090 and 0.109 was observed respectively. The order of the test should be considered because the gamma rays of the radiopharmaceutical used in the nuclear medicine test do not affect the CT while the effective half-life of the radiopharmaceuticals should be considered for the CT scan to reduce the influence of the gamma rays emitted after the nuclear medicine test, with the possibility to reduce the difference of the results.