• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-1
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• pp.90-90
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• 2003

I describe here a novel and promising approach to drug discovery that involves the identification and assembly of drug-like fragments to afford lead compounds. This approach is attractive for a number of reasons. First, the productive assembly of two weakly bound fragments, even fragments with independent dissociation constants in the low mM range, can potentially afford ligands with sub-micromolar affinities for their targets. (omitted)

• Environmental Analysis Health and Toxicology
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• 제31권
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• pp.16.1-16.9
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• 2016

Objectives Banha-sasim-tang (BST), which consists of seven different herbs, is one of the most popular herbal formulae for treating gastrointestinal disorders in Eastern Asia. The commonly used herbal medicine is often co-administered with other therapeutic drugs, which raises the possibility of herb-drug interactions and may modify the clinical safety profile of therapeutic drugs. Methods We investigated the potential herb-drug interactions between BST extract and midazolam (MDZ) in mice. The area under the plasma concentration-time curve (AUC) of MDZ and 1'-hydroxymidazolam (1'-OH-MDZ) was evaluated for both oral and intraperitoneal administration of MDZ, following oral administration of BST (0.5 and 1 g/kg). Results It was found that the AUC of MDZ and 1'-OH-MDZ was lower in case of oral administration of MDZ. Administration of BST extract was not associated with hepatic cytochrome P450 activity. BST extract induced a strong reduction in pH and it has been reported that oral mucosal absorption of MDZ is lower at low pH. The decreased absorption rate of MDZ might be caused by the ingredients of BST and may not be related to other factors such as increased excretion of MDZ by P-glycoprotein. Conclusions The altered pharmacokinetics of midazolam caused by co-administration with BST in vivo could be attributed to a decrease in pH and subsequent reduction of MDZ absorption rate.

• 한국임상약학회지
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• 제23권4호
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• pp.316-321
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• 2013

Purpose: Atorvastatin, a HMG-CoA reductase inhibitor is widely prescribed in hyperlipidemic patients and telmisartan, an angiotensin receptor blocker is frequently used in the treatment of hypertension. Both drugs are substrates of organic anion transporting polypeptide (OATP) expressed in basolateral membrane in the liver, and undergo high first pass metabolism. Therefore, OATP-mediated hepatic uptake is important for disposition and metabolism of these drugs. The present study was designed to investigate the pharmacokinetic interactions between atorvastatin and telmisartan in rats. Method: Young adult SD rats were divided into three groups (n=6, each) and atorvastatin (10 mg/kg) and telmisartan (4 mg/kg) were orally given alone and together. Heparinized blood was serially taken and plasma concentrations of both drugs were measured using HPLC-MS/MS. Pharmacokinetic parameters of two drugs were calculated. Results: No significant pharmacokinetic change was found except a delay of time to peak of telmisartan when administered with atorvastatin. Each drug at the present dosage seemed to be insufficient to alter the pharmacokinetic parameters of its counterpart drug. Conclusion: Conclusively, co-administration of atorvastatin and telmisartan may lead to negligible clinical consequences.

• Archives of Pharmacal Research
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• 제4권2호
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• pp.99-107
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• 1981

To investigate the protein binding characteristics of ibuprofenlysine, the effects of drub conentration, pH, ionic strength and protein concentration on the binding of drug to protein concentration on the binding of drug to protein were studied by fluorescence probe method. The conformational change of protein was investigated by circular dichroism (CD) measurement. As the concentration of drug increases, the association constant decreases. These may be due to complex formation of the probe and drug, or the interaction of the protein-probe complex and drug. The association constant for ibuprofenlysine increased with increasing protein concentration. These finding suggest a sharing of one ibuprofenlysine molecule by more than one protein molecule in the binding. The binding between ibuprofenlysine and protein was dependent on pH and ionic strength. It seems that both hydrophobic binding and some electrostatic forces are involved in the binding of ibuprofenlysing to protein.

• 대한약학회:학술대회논문집
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• 대한약학회 2005년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.131-132
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• 2005

• 대한약학회:학술대회논문집
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• 대한약학회 2005년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.137-139
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• 2005

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2002년도 창립10주년기념 및 국립독성연구원 의약품동등성평가부서 신설기념 국재학술대회:생물학적 동등성과 의약품 개발 전략을 위한 국제심포지움
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• pp.147-150
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• 2002

• 대한본초학회지
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• 제33권6호
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• pp.9-18
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• 2018

Objective : Many patients take antihypertensive drugs as well as herbal medicines at the same time in order to treat other symptoms or to keep their well-being. In this study, interactions between herbal medicines and synthetic antihypertensive drugs were analyzed. Methods : To investigate the interaction between herbal medicines and synthetic antihypertensive drugs, three electronic databases, including OASIS, Mediline and Sciencedirect were searched. Experimental and clinical studies on the interaction between herbal medicines and antihypertensive drugs were independently reviewed and included. Results : Analyzing selected studies, twenty herbs were found to interact with antihypertensive drugs. Herbs found to increase the antihypertensive effect were Panax ginseng, Carthamus tinctorius, Magnolia officinalis, Silybum marianum, Scutellaria baicalensis, Schisandra chinensis, Sophora flavescens, Piper nigrum, Curcuma longa, Ginkgo biloba, Juncus effuses and Hydrastis canadensis. In contrast, Commiphora myrrha, Rhodiola rosea, Hypericum perforatum, Eurycoma longifolia, and Daturae metel were found to inhibit the antihypertensive effect. Stephania tetrandra could increase or decrease the effect depending on the type of antihypertensive drug. Epedria sínica was suspected of pharmacodynamic interaction with antihypertensive drug. Glycyrrhiza uralensis has been reported to have serious side effects in combination with antihypertensive drugs. Conclusion : These results imply that when used in combination with herbal medicines and synthetic antihypertensive drugs, proper doses and herbs which are to avoid need to be informed to the patients. Despite concerns about interactions between herbal medicines and synthetic drugs, related research is very limited. More systematic researches are needed to give information on patient safety as well as to guide clinical practice.

• 한국임상약학회지
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• 제23권2호
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• pp.129-136
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• 2013

Objectives: Among many new drugs that are under investigation with intent to treat cancer, oral kinase inhibitors are proven to be effective in numerous clinical trials and easy to administer. Due to these advantages the use of oral kinase inhibitors is increasing. Oral kinase inhibitors are metabolized by CYP450 which can result either increase of adverse effect or decrease of drug effect by drug interaction when used concurrently with other agents. In this research, the medication records of patients on oral kinase inhibitors from Oct. 2010 to Nov. 2011 were reviewed to investigate potential drug interactions. Methods: From Oct. 2010 to Nov. 2011, cancer patients in Inha University Hospital who took oral kinase inhibitors more than once were included. The patients' medication records were reviewed to list out concurrent medications that have interaction potential with oral kinase inhibitors, the frequency of concurrent use, and the severity of interaction result using Micromedex$^{(R)}$ and Lexicomp-online$^{(R)}$ as references. Results: As a result, 90 cases of drug with interaction potential were prescribed by Micromedex$^{(R)}$ and 179 cases by Lexicomp-online$^{(R)}$ data. In case of severity, 33.3% by Micromedex$^{(R)}$ and 26.3% by Lexicomp-online$^{(R)}$ were categorized as Major and 65.6% by Micromedex$^{(R)}$ and 72.6% by Lexicomp-online$^{(R)}$ as Moderate. The number of adverse events was 92 cases which 58.7% were on skin and 19.6% on Gastro-intestinal tract. Conclusions: Considerable number of drug with interaction potential was used though each oral kinase inhibitors showed differences in extent. Hence there exists the risk of drug interaction in patients taking oral kinase inhibitors with other drugs.

• 한국임상약학회지
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• 제20권2호
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• pp.99-106
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• 2010

Drugs mostly represent an efficacy or an adverse effect according to their dosage and/or plasma concentrations. Therefore, to investigate the pharmacokinetic behavior of drugs including herbal medicines is necessary both to maximize the drug action and to minimize the adverse effect. To date, pharmacokinetic studies of herbal medicines have been conducted by some experts in this field on the bases of science and knowledge in Korea. On the other hand, in advanced countries, a typical series of pharmacokinetic studies has been conducted by using a harmonized guidance established. Consequently, an administrative support on these studies has to be needed in Korea as well. This study aimed to establish a draft guidance on pharmacokinetic studies of herbal medicines in non-clinical and clinical studies. Literatures previously published as well as guidances in the US, Europe and Japan were summarized for the present guidance. Effect of herbal medicines was listed on the proteins in charge of drug metabolism and transportation, as well as on the pharmacokinetics of chemical drugs. The present suggestion might be helpful to proceed pharmacokinetic studies of herbal medicines efficiently, and further polish should be needed in terms of an administrative point of view.