• Title/Summary/Keyword: new drug

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Drug-Drug Interactions : Mood Stabilizers and Anti-Anxiety Drugs (약물상호작용 : 기분안정제와 항불안제)

  • Kim, Young Hoon;Rhee, Jung Goo
    • Korean Journal of Biological Psychiatry
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    • v.7 no.1
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    • pp.34-45
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    • 2000
  • Pharmacotherapy of bipolar disorder is a rapidly evolving field. Mood stabilizers and anticonvulsants have varying biochemical profiles which may predispose them to different adverse effects and drug-drug interactions. Several of the new anticonvulsants appear less likely to have the problems with drug-drug interaction. To provide more effective combination pharmacotherapies, clinicians should be allowed to anticipate and avoid pharmacokinetic and pharmacodynamic drug-drug interactions. We reviewed the role of cytochrome P450 isozymes in the metabolism of the drugs and their interactions. The drug-drug interactions of several classes of drugs which used as mood stabilizers and new anticonvulsants, some of which may have psychotropic profiles, are discussed mainly in this article. Finally, potential pharmacokinetic interactions between the benzodiazepines and other coadministered drugs are discussed briefly.

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Drug Target Protein Prediction using SVM (SVM을 사용한 약물 표적 단백질 예측)

  • Jung, Hwie-Sung;Hyun, Bo-Ra;Jung, Suk-Hoon;Jang, Woo-Hyuk;Han, Dong-Soo
    • Proceedings of the Korean Information Science Society Conference
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    • 2007.10b
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    • pp.17-21
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    • 2007
  • Drug discovery is a long process with a low rate of successful new therapeutic discovery regardless of the advances in information technologies. Identification of candidate proteins is an essential step for the drug discovery and it usually requires considerable time and efforts in the drug discovery. The drug discovery is not a logical, but a fortuitous process. Nevertheless, considerable amount of information on drugs are accumulated in UniProt, NCBI, or DrugBank. As a result, it has become possible to try to devise new computational methods classifying drug target candidates extracting the common features of known drug target proteins. In this paper, we devise a method for drug target protein classification by using weighted feature summation and Support Vector Machine. According to our evaluation, the method is revealed to show moderate accuracy $85{\sim}90%$. This indicates that if the devised method is used appropriately, it can contribute in reducing the time and cost of the drug discovery process, particularly in identifying new drug target proteins.

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Detection Characteristics of PSL and TL Methods in Spices Irradiated with Different Radiation Sources (조사선원에 따른 향신료의 PSL과 TL 검지 특성)

  • Kim, Kyu-Heon;Kwak, Ji-Young;Kim, Jung-Ki;Hwang, Cho-Rong;Lee, Jae-Hwang;Park, Yong-Chjun;Kim, Jae-I;Jo, Tae-Yong;Lee, Hwa-Jung;Lee, Sang-Jae;Han, Sang-Bae
    • Journal of Radiation Industry
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    • v.7 no.1
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    • pp.15-21
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    • 2013
  • The detection characteristics of irradiated spices were investigated depending on radiation sources and doses by photostimulated luminescence (PSL) and Thermoluminescence (TL). 6 kinds of spices (turmeric, onion powder, red pepper, basil, parsley, black pepper) were irradiated at 0 to 10 kGy under ambient conditions by both a $^{60}Co$ gamma irradiator and an electron beam (EB) accelerator, respectively. The PSL analysis showed negative results for non-irradiated spices, while irradiated spices gave intermediate and positive value, which presented the limited potential of PSL technique. In TL measurement, TL glow curves on non-irradiated samples appeared at about $300^{\circ}C$ with low intensity. All irradiated samples were easily distinguishable through radiation-specific strong TL glow curves with maximum peak in range of $150{\sim}200^{\circ}C$. TL ratio ($TL_1/TL_2$) obtained by a re-irradiation step could verify the detection result of $TL_1$ glow curves, showing ratios lower than 0.1 in the non-irradiated sample and higher than 0.1 in irradiated ones. Therefore, in PSL measurement, the identification of irradiated spices showed more clear results in electron beam irradiated samples. TL analysis showed obvious difference between non-irradiated and irradiated samples in gamma ray and electron beam irradiated samples.

High Throughput Screening for Natural Products to Find Biologically Active Compounds : Natural Products versus Combinatorial Chemistry

  • Sankawa, Ushio
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.11a
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    • pp.47-50
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    • 1997
  • Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

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Patient compliance with drug treatment - new perspectives on an old problem

  • Kruse W.
    • 대한예방의학회:학술대회논문집
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    • 1994.02b
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    • pp.332-335
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    • 1994
  • Compared to other variables being considered in therapeutics, patient compliance has long been given minor attention although it affects every aspect of medical care; Limited methodology of compliance measurement, in particular, has hampered major progress in research, and pre-conceptions have been reiterated. However, there is a recent surge in interest derived from new data revealed by reliable methods, i.g. continuous medication (compliance) monitoring. The visualization of dynamics in drug regimen compliance over time offers unique opportunities, both to scientific drug evaluation and therapeutics in medical practice. New perspectives related to the descriptive and explanatory side of the problem are outlined by giving examples from various therapeutic fields.

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Determination of N-nitrosodimethylamine in zidovudine using high performance liquid chromatography-tandem mass spectrometry

  • Yujin Lim;Aelim Kim;Yong-Moon Lee;Hwangeui Cho
    • Analytical Science and Technology
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    • v.36 no.6
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    • pp.281-290
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    • 2023
  • Zidovudine is an antiretroviral agent prescribed for the prevention and treatment of human immunodeficiency virus/acquired immune deficiency syndrome (HIV/AIDS). It is typically recommended to be used in combination with other antiretroviral drugs. Zidovudine has the potential to generate N-nitrosodimethylamine (NDMA) in the presence of dimethylamine and nitrite salt under acidic reaction conditions during the drug manufacturing process. NDMA is a potent human carcinogen that may be detected in drug substances or drug products. An analytical method was developed to determine NDMA in pharmaceuticals including zidovudine using high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS). The analysis involved reversed-phase chromatography on a Kinetex F5 column with a mobile phase comprising water-acetonitrile mixtures. The detection of positively charged ions was conducted using atmospheric pressure chemical ionization (APCI). The calibration curve demonstrated excellent linearity (r = 0.9997) across the range of 1-50 ng/mL with a highly sensitive limit of detection (LOD) at 0.3 ng/mL. The developed method underwent thorough validation for specificity, linearity, accuracy, precision, robustness, and system suitability. This sensitive and specific analytical method was applied for detecting NDMA in zidovudine drug substance and its formulation currently available in the market, indicating its suitability for drug quality management purposes.

Studies on the Applications of PSL, TL and ESR Methods for the Detection of Dried Fruits and Mushrooms (PSL, TL 및 ESR 분석에 의한 건조과일류 및 버섯류에 대한 검지 특성 연구)

  • Kim, Kyu-Heon;Son, Jin-Hyok;Kang, Yoon-Jung;Park, Hye-Young;Hwang, Cho-Rong;Kim, Jae-I;Lee, Kang-Bong;Jo, Tae-Yong;Eom, Mi-Ok;Park, Sue-Nie;Seong, Rack Seon;Jang, Young-Mi;Lee, Jae-Hwang;Park, Yong-Chjun;Lee, Hwa-Jung;Lee, Sang-Jae;Han, Sang-Bae
    • Journal of Radiation Industry
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    • v.7 no.1
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    • pp.7-14
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    • 2013
  • In this study, we investigated the applicability of the photostimulated luminescence (PSL), thermoluminescence (TL) and electron spin resonance (ESR) methods for various foods. The analysed samples consist of 11 items including dried fruits (6 items) and mushrooms (5 items). To compare between non-irradiated and irradiated food, all samples were irradiated with $^{60}Co$ gamma-ray source. In PSL study, the photon counts of all the unirradiated sample were identified negative (lower than 700). The photon counts irradiated (1, 5, 10 kGy) dried date-palm, dried jujube and mushrooms (Auricularia auricula, Phellinus linteus and Sarcodon aspratus) showed positive (higher than 5,000) and the results for the other samples were negative or intermediate (>700 and >5,000). In TL analysis most of items can be applicable to detect irradiated foods because of showing TL ratio above 0.1. The glow curves by TL method were estimated in the range of $150{\sim}250^{\circ}C$ in irradiated samples. In ESR measurements, the intensity of ESR signal (single-line) increased as the dose of irradiation increased. In particular, the specific ESR signals of irradiation-induced radical were detected in dried papaya, dried date-palm, dried banana, dried pineapple and S. aspratus. According to the results, PSL, TL and ESR methods were successfully applied to detect the irradiated foods. It is concluded that PSL, TL and ESR methods are suitable for detection of irradiated samples and a combined method is recommendable for enhancing the reliability of detection results.

Pharmacokinetic and Bioequivalence Study of Zolpidem Tartate in Healthy Volunteers

  • Park, Jun-Sung;Myung, Ja-Hye;Wang, Hun-Sik;Koo, Ja-Seong;Cho, Won-Kyung;Cha, Kwang-Ho;Park, Hee-Jun;Kim, Min-So;Kim, Jeong-Soo;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.41 no.3
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    • pp.191-196
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    • 2011
  • In this study simple and sensitive high performance liquid chromatographic method using a commercially available column, was developed and validated for the determination of zolpidem tartrate in human plasma. The developed method with suitable validation was applied to a bioequivalence study of two different kinds of zolpidem tartrate. Two different formulations containing 10 mg of zolpidem tartate (CAS : 99294-93-6) were compared in 24 healthy male volunteers in order to compare the bioavailability and prove the bioequivalence. The study was performed in an open, single dose randomized, 2-sequence, cross-over design in 24 healthy male volunteers with a one-week washout period. Blood samples for pharmacokinetic profiling were drawn at selected times during 12 h. The mean $AUC_{0-12h}$, $C_{max}$, $T_{max}$ and $T_{1/2}$ were $676.6{\pm}223.4$ $ng{\cdot}h{\cdot}mL^{-1}$, $177.4{\pm}34.2$ $ng{\cdot}mL^{-1}$, and $0.8{\pm}0.4$ and $3.5{\pm}2.1$, respectively, for the test formulations, and $640.7{\pm}186.6$ $ng{\cdot}h{\cdot}mL^{-1}$, $193.0{\pm}64.5$ $ng{\cdot}mL^{-1}$, and $0.9{\pm}0.4$ and $2.7{\pm}0.9$, respectively, for the reference formulation. Both primary target parameters $AUC_{0-12h}$ and $C_{max}$ were log-transformed and tested parametrically by analysis of variance (ANOVA). 90% confidence intervals of $AUC_{0-12h}$ and $C_{max}$ were in the range of acceptable limits of bioequivalence (80-125%). Based on these results, the two formulations of zolpidem tartate are considered to be bioequivalent.

Learnings from Generic Substitution in US and Suggestions to Korean Food and Drug Administration

  • Yoo, Bong-Kyu
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.91-92
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    • 2003
  • Virtually every state in US has adopted laws and regulations that mandate the generic substitution of brand-named prescription drugs in order to reduce sky-rocketing drug costs. In the late 1970s, many state governments began to recognize the need of generic substitution and requested Food and Drug Administration (FDA) to consult with this issue. FDA did consult which drugs were interchangeable each other based upon the available scientific and experimental evidences given to the agency along with New Drug Application (NDA) and Abbreviated New Drug Application (ANDA). (omitted)

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Pseudoreceptor: Concept and an Overview

  • Kothandan, Gugan;Madhavan, Thirumurthy;Gadhe, Changdev G.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.3 no.3
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    • pp.162-167
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    • 2010
  • A pseudoreceptor combines structure-based and ligand-based techniques to represent a unifying concept for both receptor mapping and ligand matching. In this molecular modeling approach, there are opportunities to construct the pseudoreceptor models using a set of small molecules. To build a reliable pseudoreceptor model, we need a set of ligand molecules with known affinity (biological activity) to generate 3D bioactive conformation for each of these ligand molecules. Several software packages are available to generate a pseudoreceptor model and this can provide an entry point for structure based drug discovery in cases where receptor structure information is not available. In this review, we presented the concept of pseudoreceptor, as well as discussed about various software packages available to generate a pseudoreceptor model.