• 제목/요약/키워드: Half Life

검색결과 1,829건 처리시간 0.028초

Ketorolac Ester Enhancer-prodrugs: Preparation and Evaluation of Their Physicochemical Properties

  • Yun, Sung-Il;Kim, Jung-Sun;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • 제38권6호
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    • pp.405-412
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    • 2008
  • Six ester analogues of Ketorolac were synthesized as potential enhancer prodrugs for transdermal delivery. Solubility of these esters was determined in 10% propylene glycol (PG)/isotonic phosphate buffer (IPB) at room temperature while lipophilicity was obtained as partition coefficients (log P) and capacity factors (k') using HPLC. Stability of the prodrugs in skin extract and in plasma was investigated at $37^{\circ}C$. The lipophilicity of the potential prodrugs increased in proportion to their alkyl chain length. Good linear relationship between partition coefficients (log P) and capacity factors (log k') was observed ($R^2=0.9961$). All of the analogues were fairly stable but slowly degraded in IPB over a 12 hour period. However, their stability in skin extract and in plasma varied with most compounds gradually decomposing over a 12 hour period. Although unsaturation of the alkyl ester chain did not alter the over all lipophilicity of the compound, the half-life was significantly affected. In plasma, degradation of the esters was slower than in the skin extract, which is a desirable trait for enhancer-prodrugs. However, the overall hydrolysis in the skin extract needs to be facilitated for the development of an effective enhancer prodrug. The analogue with the shortest half life in the skin extract was the unsaturated C-12 analogue of 0.96 hr.

$\alpha$-아밀레이즈와 고정화된 글루코아밀레이즈를 이용한 전분의 액화 및 당화 (Liquefaction and Saccharification of Starch Using $\alpha$-Amylase and Immobilized Glucoamylase)

  • 안대희;장호남
    • 한국미생물·생명공학회지
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    • 제19권5호
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    • pp.497-503
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    • 1991
  • Packed bed column과 continuous stirred tank reactor에서 고정화된 glucoamylase의 catalytic activity를 비교하였다. Settling chamber를 이용한 연속애화, 당화 공정을 사용하여 액화된 전분으로부터 포도당을 연속적으로 생산하였다. . Chitin에 고정화된 glucoamylase에 의한 당화실험에 있어서는 dextrin의 농도가 100g/l일 때, 체류시간 20분 동안 20의 당화수율을 나타냈다.

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홍삼 첨가에 따른 쌀국수의 품질특성과 저장성 (Quality Characteristics and Shelf-life of Rice Noodles Prepared with Red Ginseng Powder )

  • 김은미
    • 한국조리학회지
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    • 제14권1호
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    • pp.161-169
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    • 2008
  • This study was performed to find out the quality characteristics of rice noodles by addition of red ginseng(0, 2, 6, 10%). The quality characteristics of the sample were estimated in terms of general composition, growth of microorganism and sensory evaluation. The results from this study were as follows. The protein, lipid and ash contents did not show significant difference in any of the groups. In dry rice noodles, moisture content significantly decreased in red ginseng groups but, in half-cooked rice noodles, moisture content significantly increased in 6 % and 10% red ginseng added groups(p<0.05). The microbial count showed less growth in red ginseng added groups after 3 months(p<0.05). According to sensory evaluation, surface color proved very good in the 10% red ginseng added group among the training panel while very good in the 2% red ginseng added group among consumers. Flavor was good in red ginseng added groups(p<0.05). Taste was very good in the 3% red ginseng added group. Appearance and overall quality were highest in the 2% and 6% red ginseng added groups(p<0.05). Therefore, rice noodles containing 2% or 6% red ginseng were most preferable and safe during 5 months and 6 days in dry and half-cooked noodles respectively.

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Pharmacokinetic Changes of Acebutolol after Orall Administration in Rabbits with Diabetes Mellitus Induced by Alloxan

  • Choi, Dong-Hyun;Bae, Hak-Yeon;Choi, Jun-Shik
    • Archives of Pharmacal Research
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    • 제26권6호
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    • pp.499-503
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    • 2003
  • Because physiological changes that potentially alter pharmacokinetics occurs in diabetes mellitus patients, pharamacokinetics of drugs used in the treatment of hypertension was studied using acebutolol as a model anti-hypertensive drug. Thus, the pharmacokinetics of acebutolol was investigated after oral administration of acebutolol (15 mg/kg) to control rabbits and rabbits with acute or chronic diabetes mellitus induced by alloxan. Kidney and liver functions were documented for acute and chronic diabetes mellitus groups based on plasma chemistry data. After oral administration of acebutolol to acute and chronic groups, the plasma concentrations appeared higher; As a result, area under the plasma concentration-time curve from time zero to time infinity10575 and 8668 $\mu g\cdot$ h/mL for acute and chronic group, respectively. In comparison, the area was apparently smaller in the control group (i.e., 7132 $\mu g\cdot$ h/mL). The half-life in acute groups was significantly prolonged 8.45 h compared with the half-life in the control group (i.e., 6.30 h). Alteration in acebutolol pharmacokinetics was more pronounced in the acute group as evidenced by the significantly higher values the area under the plasma concentration time curve, absorption rate constant and maximum plasma concentration compared with chronic or control group. Therefore, these observations indicate that acebutolol pharmacokinetics may be affected in patients with diabetes mellitus, especially in the early stage of the disease.

카페인 약리작용에 민감한 지원자와 둔감한 지원자 및 뚱뚱한 쥐와 마른 쥐에 대한 카페인 약물동태 비교 (Pharmacokinetics of Caffeine in Caffeine Sensitive and Non-Sensitive Volunteers, and in the Obses Rat and the Lean Rat)

  • 윤정옥;권광일
    • 약학회지
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    • 제37권4호
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    • pp.341-349
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    • 1993
  • To determine the reason of individual variation of the effect of caffeine, the absorption and the disposition of caffeine were studied in caffeine sensitive and caffeine nonsensitive volunteers. And also to study the effect of obesity on caffeine pharmacokinetics, the caffeine disposition in the obese rat and in the lean rat were investigated respectively. In result the caffeine sensitive group showed a longer terminal half-life of caffeine(7.35$\pm$0.71 hr : 5.49$\pm$0.73 hr) and a larger AUC (55.42$\pm$9.09 $\mu\textrm{g}$.$ml^{-1}$.hr:44.0$\pm$7.81$\mu\textrm{g}$.$ml^{-1}$.hr) than that of caffeine non-sensitive group without statistical significance. The obese rat showed a longer terminal half-life (3.47 hr : 2.31 hr) and a larger AUC(35.3 $\mu\textrm{g}$.$ml^{-1}$.hr:26.97$\mu\textrm{g}$.$ml^{-1}$.hr) than that of the lean rat. But there was no correlation in the amount of daily caffeine consumption and obesity. In conclusion, we suggest that the individual variation of the effect of caffeine are being caused from the individual differences of caffeine susceptibility or tolerance rather than the differences of the genetic metabolic capacity or metabolic tolerance.

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아테놀올의 체내동태에 대한 신장해의 영향 (Effect of Renal Failure on Pharmacokinetics of Atenolol in Rabbits)

  • 이종기;조삼상
    • 한국임상약학회지
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    • 제8권1호
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    • pp.23-28
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    • 1998
  • The pharmacokinetics of atenolol (25 mg/kg, i.v.) in the folate-induced renal failure rabbits was studied. Renal failure was induced by the i.v. injection of folate (50, 100, and 200 mg/kg). At folate dose of 100 and 200 mg/kg, the serum creatinine concentration (Scr) and blood urea nitrogen (BUN) increased significantly compared with control rabbits. Plasma concentrations and AUC of atenolol increased significantly at folate dose of 100 and 200 mg/kg. The elimination rate constant $(K_{el})$ and total body clearance $(CL_t)$ of atenolol decreased significantly, and half-life ($t_{1/2}$) and mean residence time (MRT) of atenolol increased significantly at folate dose of 100 and 200 mg/kg. The serum creatinine concentration $(S_{cr})$ correlated well (p<0.05) with half-life $(t_{1/2})$ and elimination rate constant $(K_{el})$ of atenolol, as well as BUN with AUC and total body clearance $(CL_t)$ of atenolol.

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A Study for Establishment of High Dose Radioiodine Therapy Patients' Release Standard

  • Park, Hoon-Hee;Kim, Hyun-Soo;Dong, Kyung-Rae
    • 대한디지털의료영상학회논문지
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    • 제13권4호
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    • pp.153-156
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    • 2011
  • This study, which is proceeded in the department of nuclear medicine, aims at preventing unnecessary radiation exposure to the patients and the people near the patients by understanding and presenting the realities about the isolating period for the high dose radioiodine patients after total thyroidectomy in the 7 general hospitals in metropolitan area. Theoretically, the physical half-life of the high dose radioiodine is 8 days. Radioiodine lower than 100 mCi usually is eliminated all in 2 days 1 night considering the biological half-life and the amount of excreting radioiodine The hospitalization standard of the patients treated with high-dose radioiodine therapy has been established according to the fact above. Investigation of the data and questionnaire from the hospital have proven that some hospitals didn't even measure the acceptable dose because of the faith in the vague data. Besides, the some of those inevitably let the readmitting patients exceeding the acceptable dose be in the general ward, not in the isolation ward, because the number of the isolation rooms is relatively smaller than the patients. Thus, we want to contribute that patients understand the realities and the hospitals consider the relevant problem actively so that the problem will be settled by this journal.

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Measurements of $^{224}Ra\;and\;^{223}Ra$ in the Nakdong River estuary and the South Sea of Korea

  • Hwang, Dong-Woon;Kim, Gue-Buem;Yang, Han-Soeb
    • Journal of the korean society of oceanography
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    • 제38권2호
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    • pp.80-86
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    • 2003
  • The horizontal distributions of $^{224}Ra$ (half life=3.4 days) and $^{223}Ra$ (half life=11.3 days) were measured in surface seawaters of the Nakdong River estuary and the South Sea of Korea in April and October 2002. In order to determine these short-lived Ra isotopes, we used a delayed coincidence counter which is much more rapid and accurate than traditional methods. In an estuarine mixing zone (salinity, ~l6 ppt), the activities of $^{224}Ra\;and\;^{223}Ra$ were much greater than what would be expected from a mixture of freshwater and seawater in the Nakdong River estuary. This excess Ra may be a result of Ra desorption from fresh sediments originating from the river upstream. However, in the more open areas of the Nakdong River estuary (salinity>30 ppt) and the South Sea of Korea, $^{224}Ra\;and\;^{^{223}Ra$ activities decreased exponentially as a function of distance offshore. Using the decrease of $^{223}Ra$ with distance offshore in the South Sea of Korea, we estimated the apparent horizontal eddy diffusivities. The apparent eddy diffusion coefficients in South Sea of Korea are calculated to be approximately $3500-8000\;\textrm{m}^2/sec$.

CJ-11668, a new selective and potent cox-2 inhibitor, has long-acting pharmacokinetic profiles

  • Park, Hyun-Jung;Kang, Hye-Jung;Chung, Young-Mee;Chun, Hyung-Ok;Hong, Kwang-Hee;Kim, Il-Hwan;Kim, Taek-Rho;Noh, Hyun-Jung;Kim, Deog-Yeor
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.88.1-88.1
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    • 2003
  • CJ-11668 is a new potent and selective COX-2 inhibitor (IC$\sub$50/ COX-2 65nM; COX-l/COX-2 ratio 770). The pharmacokinetic profile of CJ-11668 (20 mg/kg, p.o.) in the rat was characterized by high bioavailability (90%) and long plasma half-life (11.7 hr) with low clearance (0.4 L/hr/kg). In the dog, the PK profiles (2 mg/kg, p.o.) also showed long plasma half-life (l7.9hr) with low clearance (0.5 L/hr/kg), and the bioavalability of 60%. The inhibition of CJ-11668 infive different cytochrome P450 isozymes (1A2, 2C9, 2C19, 2D6 and 3A4) was determined in vitro and had observed no significant effect. (omitted)

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The rapid synthetic strategy of [11C]PIB via disposable column cartridge purification

  • Jihye Lee;Yansheng Li;Sang-Yoon Lee;Tatsuo Ido
    • 대한방사성의약품학회지
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    • 제6권2호
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    • pp.69-74
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    • 2020
  • PIB is the first amyloid plaque PET image tracer reported for the first time in 2003, and is considered to be the best and is still being utilized due to its very high uptake and kinetic properties. Initially, it was synthesized by radioisotope labeling using a precursor containing a methoxy methyl protection group, but now it is synthesized using a 6-OH precursor that can be easily synthesized in one step using [11C]methyl triflate. Carbon-11 has several limitations in clinical studies using PET because its half-life is as short as 20 minutes. In this study, in order to overcome the difficulty of this half-life, a rapid method using Sep-Pak was adopted instead of HPLC purification to significantly reduce the burden of the purification process and attempted synthesis. As a result, the synthesis time was shortened by more than 50%, and the yield of the final compound was higher than the previous result and showed relatively high specific radioactivity, confirming that it is a strategic method with high applicability for various precursors having primary amines.