• Journal of Pharmaceutical Investigation
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• 제41권2호
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• pp.67-73
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• 2011

Ion exchange resins can be one of the good carriers for sustained drug release. However, the sustained release may not be enough only with themselves and hence film coating with rate controlling polymers can be applied to have a further effect on the drug release. Due to the environmental and economic issues of organic solvent for the polymer coating, aqueous polymeric systems were selected to develop dosage forms. Among the many aqueous polymeric dispersions for the film coating, EC (ethylcellulose) based polymers such as Aquacoat$^{(R)}$ ECD and Surelease$^{(R)}$ were evaluated.A fluid-bed coating was applied as a processing method. The drug release rate was quite dependent on the coating level so the release rate could be modified easily by changing different levels of the coating. The drug release rate in the Aquacoat$^{(R)}$ coated resin particles was strongly dependent on curing, which is a thermal treatment to make homogeneous films and circumvent drug release changes during storage. After dissolution test using the compressed tablets in which the coated resin particles are contained, inhomogeneous coating and even pores could be observed showing that the mechanical properties of EC were not resistant to granulation and compaction process. However, when tablets were prepared in different batches, the release profiles were almost identical showing the feasibility of the coated resin particle as incorporated into the tablet formulation.

• Archives of Pharmacal Research
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• 제26권11호
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• pp.892-897
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• 2003

Anticancer drugs have serious side effects arising from their poor malignant cells selectivity, Since insulin receptors highly express on the cytomembrane of some kind of tumor cells, using insulin as the vector was expected to reduce serious side effects of the drugs. The objective of this study was to evaluate the tumor targeting effect of the newly synthesized mitoxantrone-insulin conjugate (MIT-INS) with the drug loading of 11.68%. In vitro stability trials showed MIT-INS were stable in buffers with different pH (2-8) at $37^{\circ}C$ within 120 h (less than 3% of free MIT released), and were also stable in mouse plasma within 48 h (less than 1 % of free MIT released). In vivo study on tumor-bearing mice showed that, compared with MIT [75.92 $\mu g \cdot$ h/g of the area under the concentration-time curve (AUC) and 86.85 h of mean residence time (MRT)], the conjugates had better tumor-targeting efficiency with enhanced tumor AUC of 126.53 1l9 h/g and MTR of 151.95 h. The conjugate had much lower toxicity to most other tissues with targeting indexes ($TI^c$) no larger than 0.3 besides good tumor targeting efficiency with $TI^c$ of 1.67. The results suggest the feasibility to promote the curative effect in ca.ncer chemotherapy by using insulin as the vector of anti-cancer drugs.

• Mass Spectrometry Letters
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• 제7권4호
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• pp.106-110
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• 2016

Ginseng, a traditional herbal drug, has been used in Eastern Asia for more than 2000 years. Various ginsenosides, which are the major bioactive components of ginseng products, have been shown to exert numerous beneficial effects on the human body when co-administered with drugs. However, this may give rise to ginsenoside-drug interactions, which is an important research consideration. In this study, acassette assay was performed the inhibitory effects of 12 ginsenosides on seven cytochrome P450 (CYP) isoforms in human liver microsomes (HLMs) using LC-MS/MS to predict the herb-drug interaction. After incubation of the 12 ginsenosides with seven cocktail CYP probes, the generated specific metabolites were quantified by LC-MS/MS to determine their activities. Ginsenoside Rb1 and F2 showed strong selective inhibitory effect on CYP2C9-catalyzed diclofenac 4'-hydroxylation and CYP2B6-catalyzed bupropion hydroxylation, respectively. Ginsenosides Rd showed weak inhibitory effect on the activities of CYP2B6, 2C9, 2C19, 2D6, 3A4, and compound K, while ginsenoside Rg3 showed weak inhibitory effects on CYP2B6. Other ginsenosides, Rc, Rf, Rg1, Rh1, Rf, and Re did not show significant inhibitory effects on the activities of the seven CYPs in HLM. Owing to the poor absorption of ginsenosides after oral administration in vivo, ginsenosides may not have significant side effects caused by interaction with other drugs.

• 한국임상약학회지
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• 제24권2호
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• pp.126-134
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• 2014

Purpose: This study was aimed to examine the financial effect of 2-tiered copayment system on annual expenditure of pharmacy benefit in the National Health Insurance (NHI) of Korea, focusing on oral antidiabetic medications. Methods: 284 oral antidiabetic products with 14 different active single ingredients listed in the National Formulary of NHI (August 2009) were assigned to tier 1 or tier 2 according to the selected criteria. 10 different combinations of coinsurance rates were selected to estimate the changes in drug expenditure cost of NHI. Results: The annual drug cost was estimated based on the drug price per unit listed in the National Formulary and the used amount of products in 2009 from the IMS Health data of Korea. In the combinations of coinsurance rate of 20% for tier 1 and 40% for tier 2, the total annual drug cost was estimated to be reduced by 1.3% in the case of no change of generic and original drug consumptions, and to be reduced by 4.3% in the case of 10% increased generic drug consumptions. Conclusion: The tiered copayment system with optimal coinsurance rates appears to be a potential strategy to reduce the financial burden of NHI in Korea by promoting the use of generic products.

• 대한약침학회지
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• 제12권2호
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• pp.51-66
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• 2009

Objective : Functional dyspepsia is a prevalent disease. It impedes subjective quality of life. The purpose of this research is to examine the equivalent effect of herb drug medicine treatment(H-D)and Over the Counter(OTC) for functional dyspepsia. Method : In this controlled study, we compared herb drug medicine(H-D) with Over the Counter(OTC) of functional dyspepsia. 30 volunteers who satisfied the requirements were enrolled in study. Severity of dyspepsia was measured by Nepean Dyspepsia Index(NDI-K) before and after treatments. Result : The results are summarized as follows. 1. In Herb drug medicine and Over the Counter groups, total key symptoms score of after treatment were significantly decreased and improve rate of key symptoms was higher than before treatment, but there were no statistical significance between two groups. 2. In Herb drug medicine and Over the Counter groups, each symptoms score of after treatment were significantly decreased and improve rate of key symptoms was higher than before treatment, but there were no statistical significance between two groups. 3. In Herb drug medicine and Over the Counter groups, quality of life score of after treatment were significantly decreased and improve rate of key symptoms was higher than before treatment, but there were no statistical significance between two groups. Conclusion : Herb drug medicine treatment(H-D) is effective to improve the symptoms and quality of life in patients with functional dyspepsia.

• Mass Spectrometry Letters
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• 제12권2호
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• pp.53-58
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• 2021

Previous in vitro studies have demonstrated that ginsenoside Rc inhibits UGT1A9, but there are no available data to indicate that ginsenoside Rc inhibits UGT1A9 in vivo. The effect of single and repeated intravenous injection of ginsenoside Rc was evaluated on the pharmacokinetics of mycophenolic acid. After injection of ginsenoside Rc (5 mg/kg for one day or 3 mg/kg for five days), 2-mg mycophenolic acid was intravenously injected, and the pharmacokinetics of mycophenolic acid and mycophenolic acid-β-glucuronide were determined. Concentrations of mycophenolic acid and its metabolite from rat plasma were analyzed using a liquid chromatography-triple quadrupole mass spectrometry. Single or repeated pretreatment with ginsenoside Rc had no significant effects on the pharmacokinetics of mycophenolic acid (P > 0.05): The mean difference in maximum plasma concentration (C_max) and area under the concentration-time curve (AUC_inf) were within 0.83- and 0.62-fold, respectively, compared with those in the absence of the ginsenoside Rc. These results indicate that ginsenoside Rc has a negligible effect on the disposition of mycophenolic acid in vivo despite in vitro findings indicating that ginsenoside Rc is a selective UGT1A9 inhibitor. As a result, ginsenoside Rc has little possibility of interacting with drugs that are metabolized by UGT1A9, including mycophenolic acid.

• Natural Product Sciences
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• 제11권4호
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• pp.189-192
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• 2005

Anti-amnestic activities of Korean red ginseng (Ginseng Radix Rubra) and Crude drug-combined preparations (RGCDP-1, RGCDP-2, and RGCDP-3) were evaluated by the animal experiment. RGCDP-1 and RGCDP-2 were prepared based on Korean folk prescriptions, 'Chongmyongtang' and 'Guibitang', respectively, while RGCDP-3, by a combination of both. Among the three preparations, RGCDP-3 was found to show the most potent anti-amnestic activity as evaluated by the passive avoidance test with mice, indicating synergistic action by combined effect of RGCDP-1 and RGCDP-2.

• Archives of Pharmacal Research
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• 제9권2호
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• pp.87-91
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• 1986

In attempt to develop a drug delivery system using serum albumin microspheres, bovine serum albumin microspheres containing antitumar agent. Cytarabine, were prepared. The shape, surface characteristics, size distribution, behavior of in vivo distribution, drug release behavior, and degradation of albumin microsphers in animal liver issue homogenate and proteolytic enzyme were investigated. The shape of albumin microspheres was spherical and the surface was smooth and compact. The size distribution of the albumin microspheres was effected by dispertion forces during emulsification and albumin concentration. Distribution of albumin microspheres after imtravenous administration in rabbit was achieved immediately. In vitro, albumin microsphere matrix was so hard that it retained most of cytarabine except initial burst during the first 10 minutes, and the level of drug release during the initial burst was affected by heating temperature, drug/albumin microsphere matrix was so hard that it retained most of cytarabine except initial burst during the first 10 minutes, and the level of drug release during the initial burst was affected by heating temperature, drug/albumin concentration ratio and size distribution. After drug release test, the morphology of albumin microspheres was not changed. Albumin microsphere matrix was degraded by the animal liver issue homogenate and proteolytic enzyme. The degree of degradation was affected by heating temperature.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Molecular and Cellular Response to Toxic Substances
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• pp.143-143
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• 2002

Capsaicin (8-methyl-N-vanillyl-6-nonenamide), a pungent ingredient of hot chili peppers, has been reported to possess substantial anticarcinogenic and antimutagenic activities. In our previous study, we found that capsaicin (100 ${\mu}$M) induced significant inhibition of matrix metalloproteinase-2 activity by gelatin zymography, and that capsaicin (i.p., 2.5mg/kg) inhibited development of lung colonization (58%) in experimental lung metastasis assay.(omitted)

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Molecular and Cellular Response to Toxic Substances
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• pp.162-162
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• 2002

There has been many findings of natural, environmental or manufactered nonsteroidal substances shown to have estrogenic activity. Since estrogens affect reproduction and cellular development to cause disease in people or animals, chronic exposure may have a major impact on health.(omitted)