• Title/Summary/Keyword: 약물농도

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Pharmacomkinetics of Roxithromycin after Intravenous Administration in Broilers (록시스로마이신의 정맥주사 후 육계에서의 약물동태학적 분석)

  • Lim Jong-Hwan;Park Byung-Kwon;Kim Myoung-Seok;Hwang Youn-Hwan;Yun Hyo-In
    • Journal of Veterinary Clinics
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    • v.23 no.2
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    • pp.87-90
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    • 2006
  • The aim of the present study was to investigate the disposition pharmacokinetics of roxithromycin in broilers. Roxithromycin was administered at a single dose of 20 mg/kg body weight by intravenous (i.v.) routes. Plasma concentrations of roxithromycin were determined by liquid chromatography/mass spectrometry. After a single i.v. dose plasma concentrations were best fitted to a two-compartment open model. The values of the pharmacokinetic parameters after i.v. administration were: elimination half-life = $5.83{\pm}1.79h$, mean residence time = $6.33{\pm}0.32h$, total body clearance = $0.55{\pm}0.15L/h/kg$, and volume of distribution at steady state = $3.47{\pm}0.84L/kg$. The pharmacokinetic interpretation of roxithromycin after i.v. administration revealed that the drug was well distributed throughout the body in broilers and slowly eliminated. More studies for the application of roxithromycin against poultry disease are needed to establish a suitable pharmaceutical formulation, propose optimum dosage regimens, investigate clinical efficacy and study the tolerability of repeated doses.

Development of PLGA Nanoparticles for Astrocyte-specific Delivery of Gene Therapy: A Review (별아교세포 선택적 유전자 치료전달을 위한 PLGA 나노입자 개발)

  • Shin, Hyo Jung;Lee, Ka Young;Kwon, Kisang;Kwon, O-Yu;Kim, Dong Woon
    • Journal of Life Science
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    • v.31 no.9
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    • pp.849-855
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    • 2021
  • Recently, as nanotechnology has been introduced and used in various fields, the development of new drugs has been accelerating. Nanoparticles have maintained blood drug concentration for extended periods of time with a single administration of the drug. The drug can then be selectively released only at the pathological site, thereby reducing side effects to other non-pathological sites. In addition, nanoparticles can be modified for selective target sites delivery for other specific diseases, with polymers being widely used in the manufacture of these nanoparticles. Poly (D,L-lactic-co-glycolic acid ) (PLGA) is one of the most extensively developed biodegradable polymers. PLGA is widely used in drug delivery for a variety of applications. It has also been approved by the FDA as a drug delivery system and is widely applied in controlled release formulations, such as in gene therapy treatments. PLGA nanoparticles have been developed as delivery systems with high efficiency to specific cell types by using passive and active targeting methods. After the development of a drug delivery system using PLGA nanoparticles, the drug is selectively delivered to the target site, and the effective blood concentration for extended periods of time is optimized according to the disease. In this review paper, we focus on ways to improve cell-specific treatment outcomes by examining the development of astrocyte selective nanoparticles based on PLGA nanomaterials for gene therapy.

Inhibitory Effects of Cabbage Juice and Cabbage-Mixed Juice on the Growth of AGS Human Gastric Cancer Cells and on HCl-Ethanol Induced Gastritis in Rats (양배추즙 및 양배추 혼합즙의 인체위암세포(AGS) 성장 억제효과와 HCl-Ethanol로 유발된 흰쥐의 항위염 효과)

  • Hong, Ye-Ji;Kim, Seong Yoon;Han, Jaegab;Lim, Yaung-Iee;Park, Kun-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.42 no.5
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    • pp.682-689
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    • 2013
  • This study determined the effects of cabbage juice and cabbage-mixed juices on the growth of AGS human gastric cancer cells and their anti-gastritic effects on HCl-ethanol induced gastritis in SD rats. Cabbage juice showed the highest growth inhibition on AGS gastric cancer cells in vitro (42%), compared with chlorella (20%) and kale juice (21%). However, cabbage-chlorella and cabbage-kale juice mixtures (at a 7:3 ratio) showed synergistic effects (57% and 65% inhibitory effects, respectively) on the gastric cancer cells. Inflammatory genes (iNOS, COX-2, TNF-${\alpha}$ and IL-$1{\beta}$) were significantly down-regulated in the mixed juices. Tests of DPPH radical scavenging activity and acid-neutralizing capacity with the mixed juices also showed this trend, as cabbage-chlorella and cabbage-kale mixed juices showed synergistic effects compared to cabbage juice alone. The inhibition rate of acute gastritis induced by HCl-ethanol in rats was 46% with high amounts of cabbage (CH; 800 mg/kg), 71% with high amounts of cabbage and chlorella (CChH; 800 mg/kg), 74% with high amounts of cabbage and kale (CKH; 800 mg/kg), and 75% with cimetidine (positive control) compared with the control. In addition, rates with CChH and CKH showed decreasing gastric secretions with increasing pH. These results show that cabbage juice and cabbage-mixed juices, especially with chlorella or kale, exhibit remarkable anti-gastritic effects and can be administered for a long period for the prevention and treatment of gastric cancer and gastritis.

Pharmacokinetics of oxolinic acid in cultured olive flounder Paralichthys olivaceus by oral administration, injection and dipping (Oxolinic acid의 경구투여, 주사 및 약욕에 따른 넙치, Paralichthys olivaceus 체내 약물동태학적 특성)

  • Jung, Sung-Hee;Choi, Dong-Lim;Kim, Jin-Woo;Jo, Mi-Ra;Jee, Bo-Young;Seo, Jung-Soo
    • Journal of fish pathology
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    • v.22 no.2
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    • pp.125-135
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    • 2009
  • The pharmacokinetic properties of oxolinic acid (OA) were studied after oral administration, intraperitoneal injection and dipping to cultured olive flounder, Paralichthys olivaceus (average 90 g, $23{\pm}1{^{\circ}C}$). Plasma samples were taken at 3, 5, 10, 15, 24, 30, 48, 96 and 144 h post-dose. In oral dosage at 15, 30 and 60 ㎎/㎏, the peak plasma concentrations of OA, which attained at 10~15 h post-dose, were 1.92, 2.45 and 3.72 $\mu{g}/m\ell$, respectively. In intraperitoneal injection with 10 and 20 ㎎/㎏, the peak plasma concentrations of OA, which attained at 10 h post-dose, were 4.1 and 4.8 $\mu{g}/m\ell$, respectively. In dipping in 30 and 50 ppm for 1 h, peak concentrations were observed at 5 h and 30 h post-dose, were 0.22 and 0.38 $\mu{g}/m\ell$, respectively. The kinetic profile of absorption, distribution and elimination of OA in plasma were analyzed fitting to a one-compartment model by WinNonlin program. Calculated parameters for a single oral dosage of 15, 30 and 60 ㎎/㎏, respectively, were: AUC (the area under the concentration-time curve)=70.93, 120.0 and 141.86 $\mu{g}$ $h/m\ell$ $T_{max}$ (time for maximum concentration)=16.22, 20.39 and 17.33 h; $C_{max}$ (maximum concentration)=���D1.61, 2.40 and 3.01 $\mu{g}/m\ell$. Following intraperitoneal injection of 10 and 20 ㎎/㎏, these parameters were AUC=184.7 and 315.92 $\mu{g}$ $h/m\ell$ $T_{max}$=5.91 and 6.26 h; $C_{max}$=4.19 and 4.45 $\mu{g}/m\ell$. Following dipping at 30 and 50 ppm, these parameters were AUC=17.58 and 21.69 $\mu{g}$ $h/m\ell$ $T_{max}$=19.08 and 31.43 h; $C_{max}$x=0.22 and 0.25 $\mu{g}/m\ell$.

Stabilization and Drug Release of Water/Oil/Water Multiple Emulsions : Effect of Glucose in the Outer Aqueous Phase on Osmotic Pressure Reduction (Water/Oil/Water 다중유화의 안정성과 약물 방출: 외부 수상에 포함된 글루코즈에 의한 삼투압 조절 효과)

  • Yoo, Youngtai;Lim, Eun-Jung;Kim, Tae-Yoon;Kim, Dong-Chul
    • Applied Chemistry for Engineering
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    • v.8 no.5
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    • pp.715-721
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    • 1997
  • W/O/W multiple emulsions were prepared comprising $MgSO_4$ in the inner aqueous phase as a model drug. The stability and drug release behavior of the multiple emulsions were studied using optical microscopy, viscometry and conductometry. Glucose was introduced in the outer aqueous phase to reduce the osmotic pressure gradient across the oil layer arising from the localization of drug molecules in the inner water phase. It was found that the presence of glucose was effective in stabilization of the multiple emulsions and in control of the release rate of drug more evidently when oil phase was partially hydrophilized with cetostearyl alcohol. This may be attributed to the fact that the migration of water accompanying the hydrophilic surfactant to the inner water phase was limited under a reduced osmotic pressure gradient and thereby slow down the destabilization of the oil/inner water interface.

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Release Characteristics of Silver Sulfadiazine from Dextran-based Polymeric Matrices (Dextran을 기초로 한 고분자 Matrix로 부터의 Silver Sulfadiazine의 방출 특성)

  • Na, Jae-Woon;Park, Yung-Hoon;Kim, Sung-Hyun;Kim, Sun-Il
    • Applied Chemistry for Engineering
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    • v.7 no.4
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    • pp.735-742
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    • 1996
  • Polymeric matrices were prepared with dextran and silver sulfadiazine by adding glycerine as a plasticiser. Namely, the release rate of the drug from the polymeric matrix formulations in dissolved phases was determined in a phosphate buffer solution. The results were as follows : The drug release time was delayed as drug loading contents increased, whereas it decreased as the glycerine concentration increased. The drug release time was not changed with varying the molecular weight of the dextran. The apparent release rate constant (k) increased as the composition of silver sulfadiazine and glycerine was increased. But the apparent release rate constant (k) was not changed with increasing molecular weight of the dextran.

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Effect of Other Medications on the Stability of Omeprazole in Aqueous Solution for the Peptic Ulcer Disease (소화성궤양시 병용약물이 수용액 중의 오메프라졸 안정성에 미치는 영향)

  • Lee, Young-Jae;Whang, Wan-Kyunn;Cho, Seong-Wan
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.10 no.11
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    • pp.3494-3499
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    • 2009
  • The stability of omeprazole in the aqueous solutions containing loxoprofen or Sodium bicarbonate was examined at room temperature. Loxoprofen or Sodium bicarbonate (60 mg) was added to omeprazole (600 ${\mu}g$/ml) solution to check the stability profile. Then, the solution was kept at room temperature for 80 hours. The concentration was assayed at each concentration by stability-indicating High performance liquid chromatography (HPLC) method. Aliquots of the solution were withdrawn at specified time intervals and assayed by chromatographic analysis for intact omeprazole. The relation between omeprazole concentration and peak area was linear from 5 to 160 ${\mu}g$/ml. The analysis method was precise with relative standard deviation (% RSD) no greater than 3.05 %. The remaining percentage-time curves revealed that omeprazole was degraded rapidly as functions of time and temperature following pseudo first-order kinetics. In conclusion, the stability of omeprazole was significantly affected by liquid solutions mixed with alkalizer (Sodium carbonate) or the NSAIDs (loxoprofen).

Evaluation of Cytotoxic Properties of Tea Polyphenols in Intestinal Cells Treated with Over-the-counter Drugs (녹차 폴리페놀 성분과 일반 의약품의 상호작용에 의한 장관계 세포 독성 평가)

  • Choi, Hyun-A;Kim, Mi-Ri;Hong, Jung-Il
    • Korean Journal of Food Science and Technology
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    • v.43 no.5
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    • pp.641-647
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    • 2011
  • Polyphenols in green tea are biologically active and may interact with commonly-consumed over-the-counter (OTC) drugs in the body. In this study, modulation of cytotoxicity of polyphenon 60 (PPE, tea polyphenol mixture) with co-treatment of several OTC drugs, including ibuprofen (Ibu), acetaminophen (AAP), and aspirin was investigated in intestinal cells. PPE showed more potent cytotoxic effects on colon cancer HCT 116 cells than on normal intestinal INT 407 cells. Ibu had the strongest cytotoxic effects on both cell types. Cytotoxicity of PPE on HCT 116 and INT 407 cells was not markedly altered by co-treated OTC drugs. Cytotoxicity of the OTC drugs was not affected by PPE. When HCT 116 cells were incubated with AAP before or after PPE treatment, cytotoxicity was slightly enhanced more than their additive effect. The present study may provide basic information of possible toxicity due to interaction of the polyphenols and the OTC drugs.

Effect of Cimetidine on Pharmacokinetics of Theophylline in Healthy Korean Volunteers (건강한 한국인 자원자에서 theophylline 약동학에 미치는 Cimetidine의 효과)

  • Kwon, Jun-Tack;Chai, Seok;Sohn, Dong-Ryul;Yom, Yoon-Ki;Kim, Hyung-Ki
    • Korean Journal of Clinical Pharmacy
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    • v.17 no.1
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    • pp.13-18
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    • 2007
  • The purpose of the present study was to investigate the effect of cimetidine on theophylline pharmacokinetics in Korean healthy normal subjects. Eight subjects were enrolled and open label, two period cross-over study was conducted without significant drug related adverse reactions. Cimetidine seemed that significantly inhibited the metabolism of theophylline, oral clearance decreased significantly when cimetidine was coadministered. Coadministered cimetidine increased $AUC_t$ and $C_{max}$ of theophylline. All subjects were genotyped using PCR-RFLP methods to evaluate the differences in metabolic capacity in accordance with CYP1A2 genotypes, but no mutant genotype was found. This suggests that metabolic capacities were not significantly affected by CYP1A2 genotypes among subjects. In conclusion, disposition of theophylline was significantly affected by coadministered cimetidine. Further evaluation with well-designed drug interaction study in accordance with various genotype of CYP1A2 is needed.

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Haemophilus K-12균주로부터 황산전이효소의 분리정제

  • 김동현;김병택;이남수
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.257-257
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    • 1994
  • 생쥐의 장내세균으로 부터 황산전이 반응을 촉매하는 효소인 sulfotransferase를 생산하는 균주를 분리하였으며 동정결과 Haemophilus속 균주로 확인되어 Haemophilus K-12라 명명하였다. 균의 성장과 효소활성과의 관계를 보면 균은 10시간에서 완전히 성장하였으며 효소활성도 이와 비례하였다. Haemophilus K-12의 배지조성에 따른 sulfotransferase의 생산성을 Brain Heart Infusion 배지에서의 생산성과 비교해보면 탄소원으로는 sucrose가 0.2%농도에서 584%로 가장 좋았으며 질소원으로는 yeast extract가 266%로 가장 좋았다. 공여체로 PNS를 최종농도 1mM로 하여 배지에 첨가하였을때 212%로 가장 높은 효소증가를 보였다. 2가금속이온에 의한 효소증가는 현저하지 않았으며 $Mn^{2+}$이 107%로 가장 높았고$Zn^{2+}$와 EDTA에 의해서는 저해를 받았다. 이상의 결과를 종합하여 균배양을 위한 이상적인 배지조성을 sucrose 0.2%, yeast extract 1%, $Na_2$HPO$_4$ 0.25%, NaCl 0.5%로 결정하였다. 결정된 최적배지에 균을 10L 배양하여 초음파 처리, 원심분리한 것을 70 % ammonium sulfate fractionation, DEAE-cellulose column chromatography를 2회, Hydroxyapatite column chromatography, chromatdfocusing column chromatography, Silica PAE column chromatography, Sephacryl S-300 superfine column chromatography를 행한결과 specific activity가 6.76 umoie/min/mg protein인 효소액을 얻었으며 homogeneous enzyme였다. 이렇게 해서 얻은 효소를 이용하여 수용체 기질 특이성을 측정한 결과 1-naphthol이 phenol을 100%로 하였을 때 233%로 가장 좋았으며 Eubacterium A-44 sulfotransferase의 좋은 기질이었던 p-acetaminophenol, tyramine, 9-phenanthrol은 좋은 기질이 되지 못했다. 이상의 결과로 미루어 보아Haemophilus K-12 sulfotransferase는 지금까지 보고된 bacterial sulfotrasferase와는 다른 효소로 사려되며 효소반응기전의 규명이 이루어지면 산업적 응용이 가능할것으로 사료된다.

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