• Biomolecules & Therapeutics
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• 제25권6호
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• pp.648-658
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• 2017

7-O-Succinyl macrolactin A (SMA) exerts several pharmacological effects including anti-bacterial, anti-inflammation, and anti-cancer activities. Recently, SMA has been extensively evaluated as an anti-cancer drug. Thus, the objectives of the present study were to characterise the pharmacokinetics of SMA via both non-compartmental and compartmental analysis in mice, rats, and dogs, and to derive an appropriate first-in-man dose based on allometric scaling of the animal data. The time courses of plasma SMA concentrations after intravenous administration to rats and dogs were analysed retrospectively, as were data collected after intraperitoneal SMA injection in mice. Pharmacokinetic parameters were estimated via both noncompartmental and compartmental analysis, and were correlated with body weight and/or the potential maximum life-span. The clearance and distribution volume of SMA in humans were predicted, and a first-in-man dose proposed. A two-compartment model best described the time courses of SMA plasma concentrations after a saturation elimination process was applied to fit the dataset obtained from rats. Incorporation of the maximum potential life-span during allometric scaling was required to improve the estimation of human clearance. The SMA clearance and the distribution volume in the steady state, in a 70-kg adult male, were estimated to be 30.6 L/h and 19.5 L, respectively. To meet the area under the curve (AUC) required for anti-tumour activity, a dose of 100 mg (~1.5 mg/kg) was finally proposed as the first dose for a 70-kg human. Although toxicological profiles derived from non-clinical studies must be considered before any final decision is made, our work will facilitate clinical studies on SMA.

• 분석과학
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• 제34권2호
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• pp.37-45
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• 2021

A rapid and simple LC-MS/MS analytical method in determining Jaspine B has been developed and validated in rat plasma. The standard curve value was 25 - 5000 ng/mL and the linearity, inter-day and intra-day accuracy and precision were within 15.0 % of relative standard deviation (RSD). The mean recoveries of Jaspine B ranged from 87.5 % to 91.2 % with less than 3.70 % RSD and the matrix effects ranged from 91.1 % to 108.2 % with less than 2.6 % RSD. The validated LC-MS/MS analytical method of Jaspine B was successfully applied to investigate the dose-escalated pharmacokinetic study of Jaspine B in rats following an intravenous injection of Jaspine B at a dose range of 1 - 10 mg/kg. The initial plasma concentrations and area under plasma concentration curves showed a good correlation with intravenous Jaspine B dose, indicating the dose independent pharmacokinetics of Jaspine B in rats. In conclusion, this analytical method for Jaspine B can be easily applied in the bioanalysis and pharmacokinetic studies of Jaspine B, including its administration at multiple therapeutic doses, or for making pharmacokinetic comparisons for the oral formulations of Jaspine B in small experimental animals as well as in vivo pharmacokinetic-pharmacodynamic correlation studies.

• 동의생리병리학회지
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• 제18권3호
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• pp.874-879
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• 2004

Alakaline phosphatase (ALP)- or horseradish peroxidase (HRP)-antibody conjugate was used frequently on the immunological detection methods such as enzyme-linked immunosobent assay (ELISA), immunobolt, immunohistochemistry. The classical enzyme-antibody coupling method by one-step (direction) injection of glutaraldehyde bring into being disadvantage such as low sensitivity of antigen detection because of homopolymers. This study was modified with the dialysis glutaraldehyde method to provide simple coupling through E-amino residues present in most protein. The dialysis glutaraldehyde coupling effects were better than the classical one-step glutaraldehyde injection in antigen detection of ELISA and immunobolt. Optimal dose of the dialysis glutaraldehyde solution was 0.10-0.25 %. This results suggest that the dialysis glutaraldehyde coupling method can readily applied to antigen detection of in vitro and in vivo.

• Biomolecules & Therapeutics
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• 제1권2호
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• pp.280-283
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• 1993

Single subcutaneous injection to SD rats of both sexes was performed to investigate the acute toxicity of new skin allergy-remedy ointment, Banaron. Banaron is composed of lidocaine hydrochloride, chloro-pheniramine maleate, prednisolone acetate, chlorohexidine hydrochloride, methyl salicylate, 1-menthol and d-camphor. The results were as fellows. $LD_{50}$, /TEX> values of Banaron were 8373.6 mg/kg for male and 8260.1 mg/kg for females. Death occurred within 24 hours after administration at doses up to 6600 mg/kg. The main cause of deaths seemed to be respiratory disturbance. General symptoms decreased of activity and respiratory rate, salivation, tremor and loss of consciousness which were commonly observed by some survived animals and all dead animals. No significant gross findings of internal organs and body weight changes in treatment groups in comparison with these of control group were observed at the maximum dose levels in Banaron.

• Journal of Pharmaceutical Investigation
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• 제24권1호
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• pp.33-40
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• 1994

In order to develop a broad-spectrum veterinary anthelmintic, a combined preparation of nitroxynil and levamisole was formulated for subcutaneous injection. The preformulation studies on solubilization, physicochemical stability and toxicity of combined preparation were performed. The combined preparation of nitroxynil-N-ethylglucamine and levamisole base could be solubilized up to 50.3%(w/v) of active ingredient concentration in propylene glycol/water system. Injectable solutions were most stable at $4^{\circ}C$. Local toxicities such as flare and edema were not shown when the usual dose of the combined preparation was injected subcutaneously to the rats.

• 전자공학회논문지A
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• 제30A권2호
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• pp.36-45
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• 1993

The n-channel MOSFETs with gate-$n^{-}$S/D overlapped structure have been fabricated by ITLDD(inverse-T gate lightly doped drain) technology. The gate length(L$_{mask}$) was 0.8$\mu$m. The degradation effects of hot carriers injected into the gate oxide were analyzed in terms of threshold voltage, transconductance and drain current variations. The degradation dependences on the gate voltage and drain voltage were characterized. The devices with higher n-concentration showed higher resistivity against the hot carrier injection. As the results of investigating the lifetime of the device, the lifetime showed longer than 10 years at V$_{d}$ = 5V for the overlapped devices with the implantation of an phosphorus dose of 5$\times$10$^{13}$ cm$^{-2}$ and an energy of 80 keV in the n$^{-}$resion.

• 설비공학논문집
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• 제15권4호
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• pp.261-267
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• 2003

The present study investigates the fire suppression characteristics using a water mist fire suppression system. Numerical simulations of fire suppression with water mist are performed with considering the interaction of fire plume and water droplet, droplet evaporation, and combustion of pool fire. The predicted temperature fields of smoke layer are compared with that of measured data. Numerical results agree with the experimental results within 5$^{\circ}C$ in the case without water mist In the case of fire suppression with water mist, numerical results dose not predict well lot temperature field in the gradual cooling region after water mist injection. But the predicted results of initial fire suppression are in good agreement with that of measured data. The reason of the discrepancy between predicted and measured data is due to the variation of turning rate during the injection of water mist. The effect of burning rate on the fire suppression is left as future study.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1995년도 춘계학술대회
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• pp.119-119
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• 1995

This study was performed to evaluate the general toxicity of novel Pt(II) complexes, (KHPC-002: [Pt(trans-1-dach) (DPPE)].2NO$_3$, KHPC-005: [Pt(cis-dach)(DPPE)].2NO$_3$ and KHPC-006: [Pt(cis-dach)(DPPP)]. 2NO$_3$). In the acute toxicity study in rats, three dosing groups of Sprague-Dawley male rats in each compounds were given a single intraperitoneal injection of KHPC-002, KHPC-005 and KHPC-006. In order to compare the toxic effects of these novel Pt(II) complexes with those of cisplatin, one group Sprague-Dawley male rats were given 7mg/kg i.p injection of cisplatin. Body weights showed dose-related decrease in all treatment groups when compared wi th the control group.

• Journal of Pharmaceutical Investigation
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• 제6권3호
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• pp.70-76
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• 1976

Pharmacological studies on the water extracts of Sambbcus latipnna var. coreana have confirmed that there are: 1) Remarkable sedative actions in preteated mice with C.N.B (caffeine and sodium benzoate) by the administration of intraperitoneal injection. 2) Antihypertensive actions in rabbits intraperitoneally injected with the extract, and as antihypertensive components, rutin, and crystal A (m.p. $250{\sim}254^{\circ}$, Liberman-Buchard's reaction, positive) were isolated from Sambucus latipinna var. coreana. 3) Marked diuretic actions in mice intramuscular injection with the dose of 600mg/kg.

• 대한수의학회지
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• 제10권2호
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• pp.21-51
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• 1970

Series of experiments were conducted to determine lethal does of X-ray and Neutron on Toxoplasma gondii. strain RH and IRI. As well morphological changes of Toxoplasma gondii irradiated or not were compared by use of electron microscope. The pathogenicity test of the irradiated and nonirradiated Toxoplasma gondii was made in mice guinea-pigs, rabbits and pigs: The letahl dose of X-ray and Neutron on RH and IRI strain and the growth rate between two strains after irradiation were shown little differences. Morphological changes were not observed until 18th passage was made. After then, the growth rate was decreased apparently, and atrophied forms were frequently observed in electron microscope. Survival time of animals inoculated with irradiated strain was longer than that of animals giving non-irradiated strain, and Toxoplasma gondii were isolated from all the dead animals. But it is of interest that pigs survived after injection of Toxoplasma gondii remained health and much attempts were failed toisolate Toxplasma gondii remained health and much attempts were slaughtered them. Animals were succumbed after injection of Toxoplasma gondii without any relationship with serum titers. (HA antibody).