• Title/Summary/Keyword: Derivative analysis

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Bioequivalence Test of Gabapentin 800 mg Tablets (가바펜틴 800밀리그람 정제의 생물학적동등성시험)

  • Kim, Se-Mi;Shin, Sae-Byeok;Kang, Hyun-Ah;Cho, Hea-Young;Lee, Yong-Bok
    • YAKHAK HOEJI
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    • v.52 no.4
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    • pp.299-305
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    • 2008
  • Gabapentin, 1-(aminomethyl) cyclohexaneacetic acid, is a amino acid derivative, and is clinically effective in the treatment of neuropathic pain and partial seizures of epilepsy as a complementary therapy. The purpose of the present study was to evaluate the bioequivalence of two gabapentin tablets, $Neurontin^{R}$ tablet 800 mg (Pfizer Pharmaceuticals Co., Ltd.) and Gabapenin tablet 800 mg (Hanmi Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with 0.06 M HCI dissolution media. Twenty six healthy male subjects, $23.85{\pm}2.24$ years in age and $69.40{\pm}11.11$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 800 mg as gabapentin was orally administered, blood samples were taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in the tested dissolution media. The pharmacokinetic parameters such as $AUC_{t}$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_{t}$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Neurontin^{R}$, were 1.28%, 0.63% and 0.62% for $AUC_{t}$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., $log0.9097{\sim}log1.1598$ and $log0.8919{\sim}log1.1262$ for $AUC_{t}$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Gabapenin tablet 800 mg was bioequivalent to $Neurontin^{R}$ tablet 800 mg.

Moisture Content Prediction Model Development for Major Domestic Wood Species Using Near Infrared Spectroscopy (근적외선 분광분석법을 이용한 국산 주요 수종의 섬유포화점 이하 함수율 예측 모델 개발)

  • Yang, Sang-Yun;Han, Yeonjung;Park, Jun-Ho;Chung, Hyunwoo;Eom, Chang-Deuk;Yeo, Hwanmyeong
    • Journal of the Korean Wood Science and Technology
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    • v.43 no.3
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    • pp.311-319
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    • 2015
  • Near infrared (NIR) reflectance spectroscopy was employed to develop moisture content prediction model of pitch pine (Pinus rigida), red pine (Pinus densiflora), Korean pine (Pinus koraiensis), yellow poplar (Liriodendron tulipifera) wood below fiber saturation point. NIR reflectance spectra of specimens ranging from 1000 nm to 2400 nm were acquired after humidifying specimens to reach several equilibrium moisture contents. To determine the optimal moisture contents prediction model, 5 mathematical preprocessing methods (moving average (smoothing point: 3), baseline, standard normal variate (SNV), mean normalization, Savitzky-Golay $2^{nd}$ derivatives (polynomial order: 3, smoothing point: 11)) were applied to reflectance spectra of each specimen as 8 combinations. After finishing mathematical preprocessings, partial least squares (PLS) regression analysis was performed to each modified spectra. Consequently, the mathematical preprocessing methods deriving optimal moisture content prediction were 1) moving average/SNV for pitch pine and red pine, 2) moving average/SNV/Savitzky-golay $2^{nd}$ derivatives for Korean pine and yellow poplar. Every model contained three principal components.

Liquid Phase Sintering and Electrical Properties of ZnO-Zn2BiVO6-Co3O4 Ceramics (ZnO-Zn2BiVO6-Co3O4 세라믹스의 액상소결과 전기적 특성)

  • Hong, Youn-Woo;Kim, You-Bi;Paik, Jong-Hoo;Cho, Jeong-Ho;Jeong, Young-Hun;Yun, Ji-Sun;Park, Woon-Ik
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.30 no.2
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    • pp.74-80
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    • 2017
  • This study focuses on the effects of doping $Zn_2BiVO_6$ and $Co_3O_4$ on the sintering and electrical properties of ZnO; where, ZZ consists of 0.5 mol% $Zn_2BiVO_6$ in ZnO, and ZZCo consists of 1/3 mol% $Co_3O_4$ in ZZ. As ZnO was sintered at about $800^{\circ}C$, the liquid phases, which are composed of $Zn_2BiVO_6$ and $Zn_2BiVO_6$-rich phases, were found to be segregated at the grain boundaries of sintered ZZ and ZZCo, respectively, which demonstrates that $V_o^{\cdot}$(0.33~0.36 eV) are formed as dominant defects according to the analysis of admittance spectroscopy. As $Co_3O_4$ is doped to ZZ, the resistivity of ZnO decreases to ~38%, while donor density ($N_d$), interface state density ($N_t$), and barrier height (${\Phi}_b$) increase twice higher than those of ZZ, according to C-V characteristics. This result harbingers that ZZCo and its derivative compositions will open the gate for ZnO to be applied as more progressive varistors in the future, as well as the advantageous opportunity of manufacturing ZnO chip varistors at lower sintering temperatures below $900^{\circ}C$.

Estimation of genetic parameter for carcass traits of commercial steers in Pyeongchang (평창지역 거세출하우 자료를 이용한 유전모수 추정)

  • Dang, Chang-Gwon;Kim, Hyeong-Cheol;Jang, Sun-Sik;Lee, Jeong-Mook;Hong, Yeong-Hun;Jeon, Gi-Jun;Yeon, Seong-Heum;Kang, Hee-Seol;Yang, Bo-Suk;Hong, Seong-Koo;Lee, Jun-Heon;Lee, Seung-Hwan
    • Korean Journal of Agricultural Science
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    • v.40 no.4
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    • pp.339-345
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    • 2013
  • The objective of this study was to establish genetic evaluation systems with carcass data collected by 68 individual farms from 2007 to 2011 in Pyeongchang area of Kangwon province. All the possible of environment effects were corrected by analysis of variance (ANOVA) to estimate more accurate genetic parameters. Heritabilities and genetic correlations were estimated from carcass data collected from Hanwoo steers(n=10,441) born in Pyeongchang region from 2005 to 2008. Traits evaluated included carcass weight (CWT), eye muscle area (EMA), back fat thickness (BF) and marbling score (MS). As for the mean value and standard deviation for carcass traits, CWT, EMA, BF and MS were 424.5, 92, 13.7 and 5.7. Parameters were estimated using a multiple trait animal model and derivative-free restricted maximum likelihood procedures. Estimated heritabilities for CWT, EMA, BF and MS were 0.30, 0.21, 0.42 and 0.42, respectively. Genetic correlation of CWT with EMA, BF and MS were estimated to 0.24, 0.36 and 0.07, respectively. Genetic correlation of EMA with BF and MS was -0.27 and 0.61, respectively.

Comparative Analysis of Benzylideneacetone-derived Compounds on Insect Immunosuppressive and Antimicrobial Activities (벤질리덴아세톤 유도 화합물들의 곤충면역반응 억제와 살균력 비교 분석)

  • Seo, Sam-Yeol;Chun, Won-Su;Hong, Yong-Pyo;Yi, Young-Keun;Kim, Yong-Gyun
    • Korean journal of applied entomology
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    • v.51 no.3
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    • pp.245-253
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    • 2012
  • Benzylinedeneacetone (BZA) is a bacterial metabolite which is synthesized by at least two entomopathogenic bacteria, namely Xenorhabdus nematophila and Photorhabdus temperata subsp. temperata. It has been shown to possess inhibitory effects on insect cellular and humoral immune responses as well as antimicrobial activities against various species of bacteria and fungi. However, its relatively high phytotoxicity, and nonsystematic effect have thus far prevented its development into an optimal pesticide. This study screened five different BZA derivatives in order to select an optimal compound, which would have relatively high solubility and low phytotoxicity while retaining sufficient degrees of the immunosuppressive and antimicrobial activities associated with BZA. Hydroxylation of the benzene ring of BZA was found to significantly suppress its immunosuppressive and antimicrobial activities. Transformation of the ketone of BZA by carboxylation also suppressed the inhibitory activities. However, a shortening of the aliphatic chain of BZA into acetate form (4-hydroxyphenylacetic acid: HPA) did not decrease the inhibitory activity. HPA also showed much less phytotoxicity against the hot pepper plant Capsicum annuum, when compared to BZA. This study identified an optimal BZA derivative, which exhibited relatively little phytotoxicity, but retained a high degree of inhibitory activity to suppress insect immune responses and antimicrobial activities against plant pathogens.

Effect of Solar Irradiances on Growth and Pigmentation of Antarctic Red Algae, Kallymenia antarctica and Palmaria decipiens

  • Han, Tae-Jun;Han, Young-Seok;Lee, Min-Soo;Park, Jin-Hee;Cho, Man-Gi;Koo, Jae-Gun;Kang, Sung-Ho
    • Ocean and Polar Research
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    • v.25 no.4
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    • pp.427-435
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    • 2003
  • Growth and pigment responses to different levels of solar radiation with or without ultraviolet (UV)-B component $({\lambda}=280-315nm)$ were investigated in Antarctic rhodophytes, Kallymenia antarctica and Palmaria decipiens, collected around King George Island during the summer of 2000. In K. antarctica specific growth rate, based on thallus area or fresh weight, decreased with increasing solar irradiances while P. decipiens were relatively insensitive to the effects of light. It is noticeable that the presence or absence of UV-B had no significant effect on growth for either species. However, K. antarctica showed a more pronounced reduction in chlorophyll (Chl a) concentrations at higher irradiances in the presence of UV-B. In P. decipiens, Chl a concentrations did not differ despite radiation level fluctuations being lower albeit than initial measurements. Thallus thickness was greater in K. antarctica than in P. decipiens. There were higher relative amounts of UV-absorbing pigments (UVAPs) in P. decipiens than in K, antarctica. The single absorbance peak obtained from the methanol extracts was resolved into three (316,332 and 346nm) in K. antarctica and four peaks (315,326,333 and 349 nm) in Palmaria as a result of the fourth-derivative. After 7 days exposure to solar radiation, the amount of UVAPs in K. antarctica was significantly reduced to a similar degree at all light levels, whereas that of P. decipiens remained unchanged except at 5% of surface irradiance. High performance liquid chromatography (HPLC) analysis of purified extracts indicated that P. decipiens possesses porphyra-334 in addition to three other mycosporine-like anlino acids (MAAs; asterina-330, palythine, shinorine), which are commonly present in K. antarctica. Significantly lower tolerance of K. antarctica to high levels of solar radiation may be connected with its usual absence in the eulittoral, while the active growth and elastic pigment responses of P. decipiens over a wide range of solar irradiance levels up to full sunlight seems to correspond well with its wide vertical distribution from rock pools down to 25-30m.

Bioequivalence of Azela Tablet to Azeptin Tablet (Azelastine Hydrochloride 1 mg) (아젭틴 정(염산아젤라스틴 1 mg)에 대한 아젤라 정의 생물학적 동등성)

  • Cho, Hea-Young;Yun, Ji-Hun;Seo, Yu-Lee;Oh, In-Joon;Lee, Sung-Kwan;Moon, Jai-Dong;Lee, Yong-Bok
    • Journal of Pharmaceutical Investigation
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    • v.31 no.1
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    • pp.57-62
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    • 2001
  • Azelastine, a phthalazinone derivative, is an antiallergic agent which demonstrates histamine $H_1-receptor$ antagonist activity and also inhibits histamine release from mast cells following antigen and non-antigen stimuli. Thus, azelastine may be useful in the management of both asthma and allergic disorders. The purpose of the present study was to evaluate the bioequivalence of two azelastine hydrochloride tablets, $Azeptin^{TM}$ (Bu Kwang Pharmaceutical Co., Ltd.) and $Azela^{TM}$ (Kyung Dong Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Eighteen normal male volunteers, $22.44{\pm}2.01$ years in age and $61.99{\pm}6.18\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After two tablets containing 1 mg of azelastine hydrochloride per tablet were orally administered, blood was taken at predetermined time intervals and the concentrations of azelastine in serum were determined using HPLC with fluorescence detector. Pharmacokinetic parameters such as $AUC_t$, $C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_t$, $C_{max}\;and\;T_{max}$ between two tablets were -6.45%, -2.60% and -7.14%, respectively, when calculated against the $Azeptin^{TM}$ tablet. The powers $(1-{\beta})$ for $AUC_t\;and\;C_{max}$ were 96.65% and 88.47%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.05$ and $1-{\beta}=0.8$ were less than 20% (e.g., 14.40% and 17.65% for $AUC_t\;and\;C_{max}$, respectively). The 90% confidence intervals were within ${\pm}20%$ (e.g., $-14.87{\sim}1.97$ and $-12.92{\sim}7.72$ for $AUC_t\;and\;C_{max}$, respectively). Two parameters met the criteria of KFDA for bioequivalence, indicating that $Azela^{TM]$ tablet is bioequivalent to $Azeptin^{TM}$ tablet.

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Analysis of anatoxin-a in aqueous and cyanobacterial samples from korean lakes by liquid chromatography with fluorescence detection (액체크로마토그래피-형광검출법에 의한 호소시료의 아나톡신-a 분석)

  • Lee, In-Jung;Lee, Chul-Gu;Heo, Seong-Nam;Lee, Jae-Gwan
    • Analytical Science and Technology
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    • v.24 no.3
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    • pp.225-230
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    • 2011
  • Anatoxin-a is a cyanobacterial neurotoxin with a high toxicity produced by Anabaena, Aphanizomenon and Oscillatoria. Water bloom, formed by Anabaena has been occurring frequently in Lake Yeongchun. It is need to develop a sensitive method for determination of anatoxin-a to control potential hazard in raw water resources. In this study, we developed a highly sensitive analytical method of anatoxin-a using solid phase extraction (SPE) and high performance liquid chromatography (HPLC) with fluorescence detection. Anatoxin-a was converted into a highly fluorescent derivative using 4-fuoro-7-nitro-2,1,3-benzoxadiazole (NBF-F). The method was evaluated in terms of linearity of calibration curve, recovery and repeatability, and the adequate values were obtained. The method detection limit was $0.034\;{\mu}g/g$ and $0.022\;{\mu}g/L$ for algal and water samples, respectively. The concentrations of anatoxin-a were measured in algal and water samples from Lake Andong, Yeongchun and Daechung and ranged from $0.135\;{\mu}g/g$ to $10.979\;{\mu}g/g$ in algal samples and not detected in water samples.

Nitration of 3,7,9,11-Tetraoxo-2,4,6,8,10-pentaaza[3.3.3]propellane (3,7,9,11-테트라옥소-2,4,6,8,10-펜타아자[3.3.3]프로펠레인의 니트로화 반응)

  • Shin, Moonyong;Ha, Tae-Hwan;Chung, Kyoo-Hyun;Kim, Jin Seuk;Kim, Young Gyu
    • Applied Chemistry for Engineering
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    • v.25 no.2
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    • pp.188-192
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    • 2014
  • Until now, there has been much efforts for the development of polycyclic molecules as high energy materials because of their high density and potential energy. However, there were only a few reports on the development of highly N-substituted polycyclic compounds due to difficulties of the synthesis. We have designed pentaazapropellanes as new high energy materials and we have recently reported unsubstituted 3,7,9,11-tetraoxo-2,4,6,8,10-pentaaza[3.3.3]propellane (TOPAP) 2 as a new skeleton for high energy materials. Herein, the nitration of TOPAP 2 was reported for the first time. Thus, 2,6-dinitro-3,7,9,11-ttraoxo-2,4,6,8,10-pentaaza[3.3.3]propellane (2,6-DNTOPAP) 5C, which is a new nitro derivative of TOPAP 2, was obtained up to 82% yield by the reaction of $NO_2BF_4$ and anhydrous $HNO_3$. The structure of 5C was determined by spectroscopic analysis.

Determination of alkylphenol ethoxylate in water by high performance liquid chromatography/electrospray ionization/mass spectrometry (HPLC/ESI/MS를 이용한 물 중의 알킬페놀에톡실레이트 분석)

  • Lee, Jeongae;Park, Song-Ja;Chung, Bong Chul
    • Analytical Science and Technology
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    • v.17 no.3
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    • pp.263-270
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    • 2004
  • A method is described for the analysis of short-chain alkylphenol ethoxylates (APEOs), 4-octylphenol-di-ethoxylate (OP2EO) and 4-nonylphenol-di-ethoxylate (NP2EO), in drinking water or wastewater using reversed phase high-performance liquid chromatography with electrospray ionization mass spectrometry. The solvent system was water and methanol containing $10{\mu}M$ trifluoroacetic acid as an ionization solvent. We acidified 1 L of water samples to less than pH 2 with concentrated $H_2SO_4$ and loaded onto Sep-Pak $C_{18}$, and eluted with acetone. The calibration of OP2EO and NP2EO was performed for the concentration range from 20 to 500 ng/L and the correlation coefficients were 0.999 and 0.990, respectively. The limits of detection were 20 ng/L (OP2EO) and 50 ng/L (NP2EO) at a signal-to-noise ratio of 3. Accuracy and precision of this analytical method were 85.8 ~ 122.1% and 8.2 ~ 18.8%, respectively. The proposed method allowed a sensitive and rapid detection of OP2EO and NP2EO and it could be applied for monitoring of APEOs from environmental samples.