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테크네슘-99엠 트리카보닐 시스테인의 제조 및 생물학적 특성 평가
장범수,박경배,윤효인,Jang, Beom-su,Park, Kyung-bae,Yun, Hyo-in 대한수의학회 2004 大韓獸醫學會誌 Vol.44 No.1
This paper describes the development of $^{99m}Tc$ tricarbonyl cysteine as potential renal function diagnostic radiopharmaceutical and evaluation of its biological characteristics using experimental animals. l-Cysteine was labeled efficiently with $^{99m}Tc$ tricarbonyl precursor $([^{99m}Tc(CO)_3(H_2O)_3)]^{+})$ under 30 min heating at ${75^{\circ}C}$. Labeling yield and stability were analyzed by high performance liquid chromatography (HPLC). The biodistribution property of $^{99m}Tc$ tricarbonyl cysteine in mice and its dynamic imaging profiles in rabbits were carried out. To investigate the excretion mechanism of $^{99m}Tc$ tricarbonyl cysteine, tubular transport inhibition test with probenecid was adopted. $^{99m}Tc$ tricarbonyl cysteine was obtained with a high labeling yield under the moderate condition. The results of biodistribution experiments of $^{99m}Tc$ tricarbonyl cysteine in ICR mice at 3 and 90 min provided that $^{99m}Tc$ tricarbonyl cysteine was very highly accumulated in the kidney and bladder, thereby almost 99% of $^{99m}Tc$ tricarbonyl cysteine was excreted within 90 min post injection. The same results were confirmed by the whole body dynamic images for 30 minutes and static images in rabbits at given time intervals after injection. Renogram of $^{99m}Tc$ tricarbonyl cysteine in rabbits showed that its $T_{max}$ and $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine were $2.33{\pm}0.56$ and $4.30{\pm}0.79$ min, respectively. The $T_{max}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was $2.30{\pm}0.17$ min, whereas $T_{1/2}$ of that with probenecid pretreatment was $17.0{\pm}32.47$ min. $T_{1/2}$ of $^{99m}Tc$ tricarbonyl cysteine with probenecid pretreatment was significantly different, as compared to the result without probenecid (p<0.0001). The results showed that the excretion of $^{99m}Tc$ tricarbonyl cysteine was extremely affected by probenecid. Therefore, $^{99m}Tc$ tricarbonyl cysteine was rapidly excreted from the kidney principally by the tubular secretion.
형광유도체화법을 이용한 Moxidectin 정량 및 피하주사 후 돼지에서의 잔류 연구
장범수,임종환,박병권,김민규,윤효인,Jang, Beom-su,Lim, Jong-hwan,Park, Byung-kwon,Kim, Min-Kyu,Yun, Hyo-in 대한수의학회 2004 大韓獸醫學會誌 Vol.44 No.1
We established a new method to analyze moxidectin using high performance liquid chromatography(HPLC) with fluorescence derivatization in order to obtain its residual profiles in biological samples. Recovery of moxidectin in tissue was 62% at 10 ppb. Average detection reproducibility in terms of coefficience variation was 4.47% at 0.32 to 10 ppb. Residual of moxidectin was studied in 44 Yorkshire-Landrace mixed bred male pigs administered subcutaneously 0, 200, or $800{\mu}g/kg$ body weight (BW) Residual profiles of moxdectin in blood, muscle, liver, kidney and fat of pigs were described. The concentration of the moxidectin in liver after administration of moxidectin was the highest among the tissues examined. Moxidectin in liver after administration of moxidectin as $200{\mu}g/kg$ BW was declined from $10.0{\pm}3.7ng/g$ at 10 day post administration to $0.5{\pm}0.3ng/g$ level at 40 day post administration. Residual levels of moxidectin in all samples were estimated to fall below the limit of quantitation (0.32 ng/ml) after 50 day after treatment of $200{\mu}g/kg$. Moxidectin showed no abnormal observations in all the clinical findings at any concentrations under these experimental conditions. In conclusion, this analysis method by HPLC after fluorescence derivatization was very effective for the detection of moxidectin in biological samples. We suggest that 50-day is safe enough for the withdrawal time of moxidectin in pigs, following the recommendation dose by the manufacturer.
은나노입자의 방사성 동위원소 운반체 적용 유효성 검증 연구
장범수,이주상,박해준,김화정,박상현 한국방사선산업학회 2011 방사선산업학회지 Vol.5 No.3
In this study, an Ag-polyaniline-silica (Ag-PANI-silica) nanoparticle was evaluated asa radioisotope carrier. An Ag-PANI-silica nanoparticle was incubated in the 125I solution for aduration of 24 hr to test its radioisotope absorptivity. During the incubation, radioactivity of thenanoparticle was measured at 3, 6, 12, and 24 hr. After a 24 hr incubation, 125I-Ag-PANI-silicananoparticle was incubated in a fresh saline for a duration of 48 hr to check its stability. Additionally,the 125I-Ag-PANI-silica nanoparticle was injected to the ICR mouse to investigate its in-vivodistribution characteristics. The 125I absorption yield of the Ag-PANI-silica nanoparticle was higherthan 95% after a 6 hr incubation period in the 125I solution. And 125I-Ag-PANI-silica was stablefor 48 hr at 80% yield at room temperature. The SPECT/CT image of a mouse that received 125IAg-PANI-silica complex showed that the 125I-Ag-PANI-silica complex was distributed in the lung,stomach and thyroid at 30 min post injection. From these results, the Ag-PANI-silica nanoparticlehas good radio-iodine carrying property and can be applicable for the purpose of diagnosis andtherapy.
수용성 키토산의 SD 랫드에 대한 4 주 반복 경구 투여 독성시험
장범수,임종환,윤효인,Jang, Beom-su,Lim, Jong-hwan,Yun, Hyo-in 대한수의학회 2003 大韓獸醫學會誌 Vol.43 No.2
Chitosan is known to have antibacterial, antitumorogenic, hypolipidemic and immunopotentiating activities, hence finding diverse uses as a component in varying functional foodstuffs. However, some investigators reported it caused mineral absoiption inhibition and excess coagulation. From the chemical viewpoint, conventional chitosans are high-molecule polymers lacking water solubility, which could be related with their possible toxicity. A newly developed low- molecule water soluble chitosan is thought to have low toxicity compared to conventional chitosans. But no investigation was carried out to evaluate its toxicity. In this study, a 28-day subacute oral toxicity study of the water-soluble chitosan was performed in Sprague-Dawley rats of both sexes. Each 36 male and female rats were orally administered with 500, 1,000 and 2,000 mg/kg/day for 28 consecutive days, respectively. Clinical parameters (growth rate, feed and water consumption, daily inspection, urine analysis) during the 28 days indicated the water-soluble chitosan did not induce any abnonnal changes. There were no abnormal findings due to the administration of the test substance in gross and microscopic findings. We had not found alteration in absolute and relative organ weight between the control and treated groups, with only exception in the liver but lacking dose-dependency. The results of hematology and serum biochemistry examination revealed that no treatment related changes were between control and all dose groups. In conclusion, it was suggested that subacute toxicity of the water-soluble chitosan was low and the no-observed adverse effect level was considered to be over 2,000 mg/kg in rats.