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      • KCI등재

        타리비드 정(오플록사신 100㎎)에 대한 파비드 정의 생물학적동등성

        박완수,조성희,이헌우,임호택,홍성제,서성훈,류재환,이경태 한국약제학회 2005 Journal of Pharmaceutical Investigation Vol.35 No.1

        The purpose of the present study was designed to evaluate the bioequivalence of two ofloxacin tablets, Tarivid (Jell Pharm. Co., Ltd.) and Favid (ILHWA Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four normal male volunteers, 23.67±3.12 year in age and 68.50±7.23 kg in body weight, were divided into two groups and a randomized 2x2 cross-over study was employed. After four tablets containing 100 mg of ofloxacin were orally administered, blood was taken at predetermined time intervals and concentrations of ofloxacin in plasma were deter mined using HPLC. Pharmacokinetic parameters such as AUC_(t) and T_(max) were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed AUC_(t), and C_(max) and untransformed T_(max). There were no sequence effects between two formulations in these parameters. The 90% confidence intervals for the log transformed data were acceptance range of log 0.8 to log 1.25 (e.g., log 0.94-log 1.04 and log 0.90-log 1.07 for AUC_(t) and C_(max) respectively). The major parameters. AUC_(t) and C_(max) met the criteria of KDFA for bioequivalence indicating that Favid tablet is bioequivalent to Tarivid tablet.

      • SCOPUSKCI등재
      • SCOPUSKCI등재

        Bioequivalence Evaluation of Two brands of Cetirizine HCl 10 mg Tablets (Zyrix and Zyrtec) in Healthy Male Volunteers

        Im, Ho-Taek,Won, Jong-Hoen,Cho, Sung-Hee,Lee, Heon-Woo,Park, Wan-Su,Rew, Jae-Hwan,Lee, Kyung-Tae The Korean Society of Pharmaceutical Sciences and 2005 Journal of Pharmaceutical Investigation Vol.35 No.5

        The purpose of the present study was to evaluate the bioequivalence of two cetirizine HCl tablets, Zyrtec tablet (UCB Pharm. Co., Ltd. Korea, reference product) and Zyrix tablet (Kukje Pharm. Co., Ltd., Korea, test product), according to the guidelines of Korea Food and Drug Administration (KFDA). After adding an internal standard (diazepam), plasma samples were extracted using 1 mL of dichloromethane. Compounds extracted were analyzed by reverse-phase HPLC with ultra-violet detector. This method for determination cetirizine is proved accurate and reproducible with a limit of quantitation of 10 ng/mL in male plasma. Twenty-four healthy male Korean volunteers received each medicine at the cetirizine HCl dose of 10 mg in a $2{\times}2$ crossover study. There was a one-week wash out period between the doses. Plasma concentrations of cetirizine were monitored for over a period of 24 hr after the administration. AUC (the area under the plasma concentration-time curve) was calculated by the linear trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed AUC and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals for the log transformed data were acceptable range of log 0.8 to log 1.25 $(e.g.,\;log\;0.93-log\;1.08\;for\;AUC_{0-t},\;log\;0.91-log\;1.08\;for\;AUC_{0-{\infty}}\;and\;log\;1.01-log\;1.11\;for\;C_{max})$. The major parameters, AUC and $C_{max}$ met the criteria of KFDA for bioequivalence indicating that Zyrix tablet is bioequivalent to Zyrtec tablet.

      • SCIESCOPUSKCI등재

        생약복합제 SKI306X 의 랫드에 대한 4 주 경구 반복투여 독성연구

        김훈택(Hun Taek Kim),안재석(Jae Suk Ahn),정인호(In Ho Jeong),김택수(Taek Soo Kim),류근호(Keun Ho Ryu),임광진(Guang Jin Im),조용백(Yong Baik Cho),김대기(Dae Kee Kim),김환수(Hwan Su Kim),박광식(Kwang Sik Park),김기협(Key H . Kim),박병욱(P 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.1

        This study was performed to determine the subacute toxicities of SKI306X, an antiinflammatory herbal extract, in rats. SKI306X was administered orally to rats once a day for 4 weeks at doses of 0.3, 1.0, and 3.0 g/㎏/ day. Each group consisted of 20 male and 20 female rats, including 5 male and 5 female rats per group for an interim study at the end of 2-week administration and for a 2-week recovery study, respectively. Throughout the study, all rats survived and no adverse clinical signs were observed. Although male rats treated with high dose (3.0 g/㎏/day) of SKI306X showed slight loss of body weight (approximately 5%) in comparison with control animals during the administration period, their body weight loss was normally restored during the recovery period. No significant change was found in all hematological parameters of SKI306X-treated groups except for the decreased number of red blood cells in all female groups at the interim study. Statistically significant changes were observed in several blood enzyme levels of SKI306X-treated groups; however, most of these significant changes were within normal range and statistically significant values did not show dose-related responses. In SKI306X-treated groups, the absolute and relative weights of liver, heart, and stomach were statistically different from those of control group, but these differences disappeared at the end of recovery period and also drug-related gross and histopathological findings in these organs were not found. No other drug-related gross and histopathological findings were observed. It is concluded from the results of this study that non-toxic dose of SKI306X was estimated to be between 0.3 and 1.0 g/㎏/day and the maximum tolerated dose of SKI306X was assumed to be higher than 3.0 g/㎏/day.

      • SCISCIESCOPUS

        Microsuspension of fatty acid esters of entecavir for parenteral sustained delivery

        Ho, Myoung Jin,Lee, Dae Ro,Im, Sung Hyun,Yoon, Jeong A.,Shin, Chang Yong,Kim, Hyun Jung,Jang, Sun Woo,Choi, Young Wook,Han, Young Taek,Kang, Myung Joo Elsevier 2018 International journal of pharmaceutics Vol.543 No.1

        <P><B>Abstract</B></P> <P>Entecavir (EV), an anti-viral agent for hepatitis B infection, should be administered under fasted state, as intestinal absorption of this hydrophilic compound is markedly decreased under post-prandial conditions. Herein, in order to improve therapeutic adherence, a parenteral sustained delivery system was constructed, by synthesizing water-insoluble ester prodrugs of the nucleotide analogous with fatty acids. EV-3-palmitate (named EV-P), exhibited the lowest solubility in phosphate buffered saline (pH 7.4, 1.1 μg/ml), with extended release profile compared with EV, EV-3-myristate, and EV-3-stearate, was selected as a candidate to formulate drug suspension. The crystalline suspension was fabricated using anti-solvent crystallization technique, with a mean particle size of 7.7 μm. After subcutaneous (SC) injection in beagle dogs (0.43 mg/kg as EV), the plasma concentrations of EV were markedly protracted with lowered maximum plasma concentration (<I>C</I> <SUB>max</SUB>, 4.7 ng/ml), extended time required to reach <I>C</I> <SUB>max</SUB> (<I>T</I> <SUB>max</SUB>, 9.0 days), and lengthened elimination half-life (<I>T</I> <SUB>1/2,</SUB> 129.3 h) compared with those after oral administration (0.0154 mg/kg, <I>C</I> <SUB>max</SUB>, 15.4 ng/ml; <I>T</I> <SUB>max</SUB>, 0.01 days; <I>T</I> <SUB>1/2</SUB>, 4.1 h). The systemic exposure of the lipidic prodrug was below 0.1% compared with that of EV following SC injection, denoting that EV-P was rapidly converted into the parent compound in blood. Therefore, SC delivery of EV-P microsuspension can be an alternative to oral EV therapy, offering prolonged pharmacokinetic profile after single injection.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

      • SCISCIESCOPUS

        Defect Chemistry of Highly Defective La<sub>0.1</sub>Sr<sub>0.9</sub>Co<sub>0.8</sub>Fe<sub>0.2</sub>O<sub>3-δ</sub> by Considering Oxygen Interstitials

        Im, Ha-Ni,Singh, Bhupendra,Hong, Jae-Woon,Kim, In-Ho,Lee, Kang Taek,Song, Sun-Ju The Electrochemical Society 2016 Journal of the Electrochemical Society Vol.163 No.14

        <P>In case of highly defective perovskite oxides such as La0.1Sr0.9Co0.8Fe0.2O3-delta (LSCF1982), the ionic defect has been in question by suggesting direct oxygen ion diffusion by considering lattice oxygen site as an interstitial rather than an oxygen vacancy. In the present study, the thermomigration of ionic defect species was measured by ionic thermopower measurement to provide strong evidence of interstitial diffusion and the defect structure was further analyzed in terms of effectively negatively charged oxygen interstitial as a charge-compensating defect against hole. Two kinds of holes-delocalized and localized at B-site cations; were investigated by defect chemical analysis. From the conductivity analysis based on the non-stoichiometry results, the contributions of delocalized holes, localized hole at Co site, localized hole at Fe site, and localized hole moving from Co site to Fe site were successfully separated, and it was observed that the hopping reaction involving hole localized at Co is dominant in conductivity mechanism. The measurement of electronic thermopower further confirms the involvement of two different types of holes in p-type conduction. (C) 2016 The Electrochemical Society. All rights reserved.</P>

      • SCISCIESCOPUS

        Description of Fimbriimonas ginsengisoli gen. nov., sp. nov. within the Fimbriimonadia class nov., of the phylum Armatimonadetes.

        Im, Wan-Taek,Hu, Zi-Ye,Kim, Kyoung-Ho,Rhee, Sung-Keun,Meng, Han,Lee, Sung-Taik,Quan, Zhe-Xue N.V. Swets en Zeitlinger 2012 Antonie van Leeuwenhoek Vol.102 No.2

        <P>Strain Gsoil 348(T) was isolated from a ginseng field soil sample by selecting micro-colonies from one-fifth strength modified R2A agar medium after a long incubation period. 16S rRNA gene sequence analysis indicated that the strain is related to members of the phylum Armatimonadetes (formerly called candidate phylum OP10). Strain Gsoil 348(T) is mesophilic, strictly aerobic, non-motile and rod-shaped. It only grows in low nutrient media. The major respiratory quinones are menaquinones MK-11 and MK-10, and the main fatty acids are iso-C(15:0), iso-C(17:0), C(16:0) and C(16:1) ω11c. The G+C content is 61.4 mol%. The 16S rRNA gene sequences in public databases belonging to the phylum Armatimonadetes were clustered here into 6 groups. Five of these groups constituted a coherent cluster distinct from the sequences of other phyla in phylogenetic trees that were constructed using multiple-outgroup sequences from 49 different phyla. On the basis of polyphasic taxonomic analyses, it is proposed that strain Gsoil 348(T) (= KACC 14959(T) = JCM 17079(T)) should be placed in Fimbriimonas ginsengisoli gen. nov., sp. nov., as the cultured representative of the Fimbriimonadia class. nov., corresponding with Group 4 of the phylum Armatimonadetes.</P>

      • Dexmedetomidine Inhibits Voltage-Gated Sodium Channels via <i>α</i> 2-Adrenoceptors in Trigeminal Ganglion Neurons

        Im, Sang-Taek,Jo, Youn Yi,Han, Gayoung,Jo, Hyun Jung,Kim, Yong Ho,Park, Chul-Kyu Hindawi 2018 Mediators of inflammation Vol.2018 No.-

        <P>Dexmedetomidine, an <I>α</I>2-adrenoceptor agonist, is widely used as a sedative and analgesic agent in a number of clinical applications. However, little is known about the mechanism by which it exerts its analgesic effects on the trigeminal system. Two types of voltage-gated sodium channels, Na<SUB>v</SUB>1.7 and Na<SUB>v</SUB>1.8, as well as <I>α</I>2-adrenoceptors are expressed in primary sensory neurons of the trigeminal ganglion (TG). Using whole-cell patch-clamp recordings, we investigated the effects of dexmedetomidine on voltage-gated sodium channel currents (<I>I</I><SUB>Na</SUB>) via <I>α</I>2-adrenoceptors in dissociated, small-sized TG neurons. Dexmedetomidine caused a concentration-dependent inhibition of <I>I</I><SUB>Na</SUB> in small-sized TG neurons. <I>I</I><SUB>Na</SUB> inhibition by dexmedetomidine was blocked by yohimbine, a competitive <I>α</I>2-adrenoceptor antagonist. Dexmedetomidine-induced inhibition of <I>I</I><SUB>Na</SUB> was mediated by G protein-coupled receptors (GPCRs) as this effect was blocked by intracellular perfusion with the G protein inhibitor GDP<I>β</I>-S. Our results suggest that the <I>I</I><SUB>Na</SUB> inhibition in small-sized TG neurons, mediated by the activation of Gi/o protein-coupled <I>α</I>2-adrenoceptors, might contribute to the analgesic effects of dexmedetomidine in the trigeminal system. Therefore, these new findings highlight a potential novel target for analgesic drugs in the orofacial region.</P>

      • Design and <i>in vivo</i> evaluation of entecavir-3-palmitate microcrystals for subcutaneous sustained delivery

        Ho, Myoung Jin,Lee, Dae Ro,Im, Sung Hyun,Yoon, Jeong A,Shin, Chang Yong,Kim, Hyun Jung,Jang, Sun Woo,Choi, Young Wook,Han, Young Taek,Kang, Myung Joo Elsevier 2018 European journal of pharmaceutics and biopharmaceu Vol.130 No.-

        <P><B>Abstract</B></P> <P>The objectives of this study were to formulate microcrystals of entecavir-3-palmiate (EV-P), a palmitic acid ester of entecavir (EV), and evaluate the influence of particle size on its pharmacokinetic behavior following subcutaneous (SC) injection. Systemic toxicity and local tolerability of the hepatitis B anti-viral suspension were further evaluated in normal rats. EV-P microcrystals possessing median diameters of 2.1, 6.3, and 12.7 µm were fabricated using anti-solvent crystallization technique with polysorbate 20 and polyethylene glycol 4000 as steric stabilizer. Dissolution rate of EV-P microcrystals was controlled by adjusting the particle size, under sink condition. Pharmacokinetic profiles of 2.1 µm-sized and 6.3 µm-sized EV-P microcrystals were quite comparable (1.44 mg/kg as EV), over 46 days in rats. The absorption rate and extent of EV after SC injection of 12.7 µm-sized microcrystals were significantly retarded, due to its slower dissolution rate in aqueous media. No single-dose systemic toxicity was observed after SC injection of high dose of EV-P microcrystal suspension (30–300 mg/kg as EV). The microcrystals were tolerable in the injected site, showing mild inflammatory responses at a dose of 30 mg/kg. Therefore, the novel microcrystal system with median particle size of below 6.3 µm is expected to be a unique long-acting system of the anti-viral agent, improving patient’s compliance with chronic disease.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

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