• 제목/요약/키워드: Drug Dose

검색결과 1,564건 처리시간 0.024초

HepaRG 세포를 이용한 Bosentan 약물의 CYP450 효소활성 측정 (Measurement of CYP450 Enzymes Activity of Bosentan in HepaRG Cell)

  • 한경문;정정아;신지순;차혜진;배영지;김현욱;김영훈;성원근;강호일
    • 약학회지
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    • 제58권4호
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    • pp.255-261
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    • 2014
  • Poly-pharmacy has been on the rise because of aging of population and chronic disease. Most of drug metabolism happens in the liver by CYP isozymes and the metabolism by CYP450 enzymes. The Cytochrome P450 (CYP) is a superfamily of enzymes that catalyzes the oxidations of many endogenous and exogenous compounds. Primary human Hepatocytes (HH) are considered as the gold standard model for In vitro drug interaction studies. However, there are several limitations (cost, limited life span) for using HH cells. HepaRG cells are being used as a possible alternative. HepaRG cells were cultured in William E medium containing the positive control inducers (1A2: 10, 25, 50 ${\mu}M$ omeprazole, 2C9 and 2C19: 10 ${\mu}M$ rifampin, 3A4: 10, 25, 50 ${\mu}M$ rifampin) at $37^{\circ}C$, 5 % $CO_2$ in a humidified atmosphere. This study was to evaluate the induction of CYP isozymes (1A2, 2C9, 2C19 and 3A4) using LC-MS/MS. We evaluated the potential induction ability of Bosentan, as a drug of pulmonary artery hypertension, in HepaRG cells. For reference, dose of the Bosentan is determined to the basis of the $C_{max}$ (835 mg/ml) value. The enzyme activity demonstrated that CYP2C9 and 3A4 were induced up to 20 times by Bosentan. Like as In vivo, the enzyme activity of CYP2C9 and CYP3A4 is significantly induced in a dose-dependent by Bosentan.

친수성고분자 매트릭스의 Naproxen 제어방출에 관한 연구 (A Study on the Controlled Release of Naproxen from Hydrophilic Polymer Matrix)

  • 김종국;조은실
    • 약학회지
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    • 제31권1호
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    • pp.25-32
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    • 1987
  • The effect of loading dose, plasticiser and PVA molecular weight on naproxen release from hydrophilic polymer matrix was examined. Hydrophilic polymer matrix was prepared with PVA and PVP by adding glycerine as plasticiser. The release of naproxen from polymer matrix was determined in phosphate buffer medium. The release rate of naproxen from the polymer matrix increased as drug loading dose and plasticiser percentage increased. Raproxen released from the polymer matrix showed the time square root kinetics. Without changing the release-pattern, the release rate of naproxen could not be changed by varying molecular weight of PVA. Linearly released time range increased as drug loading dose increased, whereas decreased as plasticiser percentage increased up to 30%.

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Enantioselective Determination of Cetirizine in Human Urine by HPLC

  • Choi, Sun-Ok;Lee, Seok-Ho;Kong, Hak-Soo;Kim, Eun-Jung;Parkchoo, Hae-Young
    • Archives of Pharmacal Research
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    • 제23권2호
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    • pp.178-181
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    • 2000
  • In order to study the simultaneous determination of (+)- and (-)-cetirizine in human urine we have developed a chiral separation method by HPLC. A chiral stationary phase of $\alpha$$_1$-acidglycoprotein, the AGP-CSP was used to separate the enantiomers. The pH of the phosphate buffer, as well as the content of the organic modifier in the mobile phase, markedly affected the chromatographic separation of (+)- and (-)-cetirizine. A mobile phase of 10 m㏖/1 phosphate buffer (pH 7.0)-acetonitrile (95 : 5, v/v) was used for the urine assays. Ultraviolet absorption was monitored at 230nm and roxatidine was employed as the internal standard for quantification. (+)-Cetirizine, (-)-cetirizine and the internal standard were eluted at retention times of 12, 16, and 32 mins, respectively. The detection limit for cetirizine enantiomers was 400 ng/$m\ell$ of urine. A pharmacokinetic study was conducted with the help of 5 healthy female volunteers who were administered with a single oral dose of racemic cetirizine (20 mg). The peak area ratios provided by the cetirizine enantiomers were linear(r>0.997) over a concentration range of 2.5-200 ${\mu}g/ml$. The peak of the excreted cetirizine enantiomers appeared in the urine sample during the period of 1-2 hrs following the administration of the oral dose. The excreted level of (+)-cetirizine was slightly higher than (-)-cetirizine but the difference was not statistically significant. However, this method appears to have applications for enantioselective pharmacokinetic studies of racemic drugs.

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Pharmacogenomics in Drug Discovery and Development

  • Ahn, Chul
    • Genomics & Informatics
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    • 제5권2호
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    • pp.41-45
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    • 2007
  • Pharmacogenomics is the study that examines how genetic variations affect the ways in which people respond to drugs. The ways people respond to drugs are complex traits that are influenced by many different genes. Pharmacogenomics intends to develop rational means of optimizing drug therapy, with respect to the patients' genotype, to maximize efficacy with minimal adverse drug reactions. Pharmacogenomics has the potential to revolutionize the practice of medicine, and promises to usher in an area of personalized medicine, in which drugs and drug combinations are optimized for each individual's unique genetic makeup. Indeed, pharmacogenomics is exploited as an essential step for target discovery and drug development in the pharmaceutical industry. The goal of the personalized medicine is to get the right dose of the right drug to the right patient at the right time. In this article, we will review the use of pharmacogenomics in drug discovery and development.

어류 약물정보시스템의 구현 및 응용 (Implementation and Application of Fish Drug Information System)

  • 김해란;박계화;조혁현;정희택
    • 한국전자통신학회논문지
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    • 제2권2호
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    • pp.92-98
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    • 2007
  • 수산용 의약품의 목록을 데이터베이스 화 한 어류약물정보시스템엔 상품명, 대상어종, 유효성분, 제조회사명, 적응증(질병) 등 약물에 대한 다양한 자료와 제조회사정보, 식품의 기준 및 규격에 관한 자료가 들어있다. 또한 추후에는 어류 질병에 대한 상세 자료를 데이터베이스 화 한 어류질병정보시스템을 구축할 것이다. 따라서 약물정보시스템과 질병정보시스템을 근간으로 한 어류질병판별시스템에서 질병 판정 후 치료에 필요한 처방전 발행과 약품 주문 등에 응용 활용할 것을 제안한다.

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우리나라의 두부 엑스선검사에서의 환자선량 권고량 (A Study for Establishment of Diagnostic Reference Level of Patient Dose in Skull Radiography)

  • 이정은;정진백;이현구;임천일;손혜경;진현미;김병우;양현규;김혁주;김동섭;이광용
    • Journal of Radiation Protection and Research
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    • 제35권3호
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    • pp.111-116
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    • 2010
  • 진단을 위한 엑스선검사는 의료분야에서 전리방사선을 가장 많이 사용하고 있으며 인공 방사선피폭중 가장 높은 비율을 차지하고 있다. 우리나라에서도 진단 엑스선검사에 의한 의료피폭은 전체 방사선 피폭 중 17.4%를 차지하고 있으며 인공방사선피폭 중에서는 92%를 차지하고 있다. 두부진단을 위한 엑스선 촬영 횟수도 2007년의 경우에는 111,567건으로서 2004년 이후 매년 3% 정도의 증가 추세를 나타내고 있다. 따라서 환자선량 권고량을 국내의료기관 실정에 맞도록 설정하여 두부촬영시 환자가 받는 방사선량을 줄이고 환자의 방사선 방어를 최적화 하는 것이 필요하다. 본 논문에서는 전국 114개 의료기관에서의 두부 촬영시 피폭되는 방사선량을 인체팬텀과 유리선량계를 사용하여 측정하고 환자선량권고량(DRL, Diagnostic Reference Level)을 확립하였다. 이 결과에 따라 두부 후전면 촬영에서의 환자선량 권고량은 2.23 mGy이며, 이는 세계보건기구, 국제원자력기구 등 국제기구가 권고하는 선량 5 mGy 보다 낮았으며, 두부 측면찰영에서의 환자선량 권고량인 1.87 mGy는 국제기구가 권고하는 선량 3mG 보다 낮았다.

Unit Dose Drug Distribution System의 도입을 통한 투약시스템의 질 향상 평가 (Evaluation of Quality Improvement in Inpatient's Medication System through the Implementation of Unit Dose Drug Distribution System)

  • 이인향;이순실;이병구;최원자;홍성선
    • 한국의료질향상학회지
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    • 제8권1호
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    • pp.22-42
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    • 2001
  • Background : A study comparing unit dose drug distribution system(UDS) versus traditional drug distribution system(TDS) was conducted in Seoul National University Hospital. The objectives of this study were to identify safer drug distribution system and to measure the efficiency of both systems in utilizing nursing and pharmacist's time. Methods : The study was designed to compare the data on medication errors, nursing time and pharmacists' time before and after implementation of the UDS in the internal medicine and otorhinolaryngology care units. The data on actual medications administered to patients were obtained by a disguised observer during the study period. The data collected were then compared with the physicians' orders to determine the rate of medication errors. In addition, using ten-minute interval work-sampling method nursing and pharmacists' time were measured. Results : About 6% of medications were administered incorrectly in the TDS, in comparison to 1.6% in the UDS. The rate of medication error decreased significantly in the UDS compared with the TDS. Mean times spent on medication-related activities by nurses were 34.1% in the TDS and 28.5% in the UDS. In the internal medicine care unit, nursing time associated with medications decreased significantly after the implementation of the UDS, but the reduction in medication-related nursing time in the otorhinolaryngology care unit was not significant. Pharmacist's medication-related work activities, increased from 2% in the TDS to 20% in the UDS. Pharmacist's time spent on therapy-related activities increased significantly. Conclusion : The rate of medication errors in the UDS decreased significantly compared with the TDS. Time spent on medication-related activities decreased for nurses while it increased for pharmacists. In summary, the UDS was estimated to be safer and to utilize of pharmacists' and nursing time more efficiently than the TDS.

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팔선초 물 추출물의 면역자극 및 항종양 활성 (Immunostimulant and Anti-Tumor Activity of Crude Extracts of Galium aparine L.)

  • 윤택준;이창권;박태규;이광호
    • 생약학회지
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    • 제36권4호통권143호
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    • pp.332-337
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    • 2005
  • We here demonstrate the evidence of increased anti-tumor and immunostimulating activities of crude extracts (GAL) from Galium. aparine L. In experimental lung metastasis of colon26-M3.1 carcinoma or B16-BL6 melanoma cells, prophylactically intravenous (i.v) administration of GAL significantly inhibited lung metastasis in a dose-dependant manner. In an in vitro cytotoxicity analysis, GAL at the concentration up to $500\;{\mu}g/ml$ did not affect the growth of B16-BL6 melanoma cells. In contrast, GAL showed the enhancement of splenocyte proliferating activity in a dose-dependent manner. Peritoneal macrophages stimulated with GAL produced various cytokines such as $1L-1{\beta},\;TNF-{\alpha},\;IFN-{\gamma}$ and IL-12. These data suggest that GAL has an antitumor activity to inhibit tumor metastasis, and its antitumor effects is associated with activation of nonspecific immnune related cells.

Cardiovascular effect of epinephrine in endodontic microsurgery: a review

  • Jang, Youngjune;Kim, Euiseong
    • Restorative Dentistry and Endodontics
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    • 제38권4호
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    • pp.187-193
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    • 2013
  • Epinephrine is one of the most widely-used vasoconstrictors in dental treatment including endodontic microsurgery. However, the systemic safety of epinephrine has been in debate for many years because of its potential risk to cause cardiovascular complications. The purpose of this review was to assess the cardiovascular effect of epinephrine use in endodontic microsurgery. Endodontic microsurgery directly applies epinephrine into the bone cavity, and the amount is reported to be much larger than other dental surgeries. Moreover, when considering that systemic potency of intraosseous application is reported to be comparable to intravenous application, the systemic influence of epinephrine could be increased in endodontic microsurgery. Besides, pre-existing cardiovascular complications or drug interactions can enhance its systemic influence, resulting in increased susceptibility to cardiovascular complications. Although clinical studies have not reported significant complications for patients without severe systemic complications, many epinephrine-induced emergency cases are warning the cardiovascular risk related with pre-existing systemic disease or drug interactions. Epinephrine is a dose-sensitive drug, and its hypersensitivity reaction can be fatal to patients when it is related to cardiovascular complications. Therefore, clinicians should recognize the risk, and the usage of pre-operative patient evaluation, dose control and patient monitoring are required to ensure patient's safety during endodontic microsurgery.

위내체류를 목적으로 한 알부민 가교 PVP 하이드로겔의 팽윤특성 (Albumin-Crosslinked PVP Hydrogel as a Gastric Retention Platform)

  • 심창구;여소현
    • Journal of Pharmaceutical Investigation
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    • 제23권3호
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    • pp.145-153
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    • 1993
  • Retaining a drug in the stomach by some means is sometimes necessary to extend the G1 absorption time of the drug more than 6-8 hrs. Hydrogel has often been examined for its feasibility as a dosage form, so called platform, that could be retained in the stomach due to its excellent swelling properties in the gastric fluid. In this study, polyvinylpyrrolidone (PVP) hydrogel crosslinked by albumin or acrylated albumin was synthesized in a tablet form and evaluated for its possibility as the platform. The synthesis of the hydrogel was performed by $^{60}Co\;{\gamma}-ray$ irradiation of N-vinyl-2-pyrrolidone (monomer) in the presence of a crosslinking agent: aqueous solution of albumin or acrylated albumin. Synthetic conditions such as radiation dose, dose rate and concentration of crosslinking agent were varied in order to optimize the swelling and mechanical properties of the hydrogels. Degree of swelling of albumin-crosslinked PVP (Al-PVP) was highly dependent on radiation dose, dose rate and albumin concentration: it was decreased as they increased. On the other hand, that of acrylated albumin-crosslinked PVP (Acryl-PVP) was almost independent on them except dose rate: it was decreased as the radiation dose rate increased. The compressive strength of the two hydrogels was decreased as the dose rate increased. Digestion of both PVP in artificial gastric fluid containing pepsin was delayed by the ${\gamma}-ray$ irradiation. In conclusion, Al-PVP and Acry-PVP with diverse swelling and mechanical properties could be obtained by controlling synthetic conditions, mainly the irradiation dose rate.

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