• 환경생물
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• 제20권2호
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• pp.101-108
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• 2002

Benthic organisms dwell in sediment-water interface that contains significant amount of organic and inorganic contaminants. Their feeding behavior is highly related with sediment itself and pore water in the sediments, especially in ease of deposit feeder (i.e. polychaete, amphipod). The acid volatile sulfide (AVS) is one of the important binding phases of sediment-bound metals in addition to organic matter and Fe and Mn oxide fractions in sediments, particularly in anoxic sediments. The AVS model is a powerful tool to predict metal bioavailability and bioaccumulation in benthic organisms considering SEM/AVS mole ratios in surficial sediments. However, several biogeochemical factors must be considered to use AVS model in the sediment-bound metal bioavailability.

• 한국지하수토양환경학회:학술대회논문집
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• 한국지하수토양환경학회 1998년도 공동 심포지엄 및 추계학술발표회
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• pp.137-141
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• 1998

A chemical has been aging in soil environment is more less bioavailable than freshly added chemical. The amount of bioavailability of the aged chemical is different by bacterial strains. The difference could be depend on physiochemical properties of each strain. Phenanthrene was employed as an aged chemical. Seven bacteria were isolated from activated sludge and petroleum disposed soil. These strains were able to degrade phenanthrene and to grow using phenanthrene as a sole carbon source. According to the result of materialization and chemical extraction experiment, the bioavailable amount of aged phenanthrene which has been aged in Lima loam is different by each bacteria. Several physiochemical properties of each strain were tested to certify correlation with their different amount of bioavailability.

• 한국지하수토양환경학회:학술대회논문집
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• 한국지하수토양환경학회 2002년도 추계학술발표회
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• pp.92-95
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• 2002

Bioavailability study was conducted to elucidate the relationship between sorption/desorption and biodegradation of sorbed phenanthrene in seven different soils. Mineralization kinetics was determined for phenanthrene-sorbed soil slurries inoculated with Pseudomonas putida (ATCC strain 17484). Two biodegradation models were used to fit mineralization kinetics; (i) a first-order degradation model and (ii) a coupled degradation-desorption model. The biodegradation rates were in order of vermicompost >Bion peat > 50% organoclay > Pahokee > blank (no soil, medium only) > montmorillonite > Ohio shale. The mineralization rate constants increased as desorption-resistance of phenanthrene increased. Among the tested sorbents, active biodegradation of phenanthrene was observed in vermicompost and Bion peat. Biodegradation in these two sorbents exhibited little lag time and a high maximum mineralized capacity. The role of sorption/desorption in bioavailability of phenanthrene sorbed in soils was discussed.

• 한국임상약학회지
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• 제6권2호
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• pp.14-18
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• 1996

This study was attempted to investigate the dissolution rate and the bioavailability after oral administration of commercially available norfloxacin tablets in rabbits. The dissolution test was conducted in artificial gastric juice using basket method with for norfloxacin preparations (A, B, C and D) which were chemically equivalent. The results were as follows ; The dissolution rate was increased in the order of four different brand A>D>B>C. Area under the plasma concentration curve and peak plasma concentration were increased in the order of brand A>D>B>C. Absorption rate constant and peak time were increased in the order of brand B>A>C>D, and there was a little difference in elimination rate constant and biological half-life. The correlation of the dissolution rate and relative bioavailability showed significant linear relationship. From the results of this experiment, the bioavailability of norfloxacin tablets in rabbits may be predicted from the results of dissolution rate studies.

• Journal of Pharmaceutical Investigation
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• 제22권1호
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• pp.55-62
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• 1992

In order to measure the bioavailability of Coptidis Rhizoma preparations, berberine was extracted by the mixture (1:1 v/v) of methanol and water from Coptidis Rhizoma and formulated into pills with some excipients. Disintegration time, dissolution rate, intestinal absorption rate, antibacterial effect, and serum concentration were measured. All pills were disintegrated about 60 minutes in gastric and intestinal juices and disintegration time did not change upon storage at $40^{\circ}C$ for 30 days. The pills manufactured using the extract which was extracted with the solvent containing dilute sulfuric acid showed faster dissolution and absorption from the small intestine than the other samples. It also showed not only the largest area under the serum concentration time curve and relative bioavailability, but also more potent antibacterial effect against gram-positive and gram-negative bacterias than the other samples. The correlation of the dissolution rate with absorption rate constant or $t_{max}$ showed a significant linear relationship.

• 약학회지
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• 제44권5호
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• pp.424-431
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• 2000

A biopharmaceutics drug classification system for correlation between in vitro dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and extent of drug absorption. The objective of this study was to assess whether in vitro dissolution profiles of immediate-release beta-blocker tablets can be correlated with intestinal membrane permeability and/or in vivo bioavailability In vitro dissolution of the beta-blocker tablets was examined using KP VII Apparatus II methods at various pH. Intestinal membrane permeability was determined in vitro using the diffusion chamber method. Bioavailablity parameters were cited from literatures. The dissolution profiles did not accurately represent the in vivo bioavailablity However there were good correlations between intestinal membrane permeability and log P (noctanol/buffer). The correlations obtained in this study indicated that in vitro diffusion chamber method could be used to predict intestinal absorption in vivo.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.225.2-226
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• 2003

The prolonged mechanical grinding process may enhance the bioavailability of the drugs due to the change of solid state such as micronization and decrease of crystallinity. A series of attempts to enhance the bioavailability of insoluble drugs have been made by the fine grinding technique using a planetary mill. The objective of the present study is to investigate the possibility of improving the dissolution properties of poorly water- soluble drugs such as diphenyl hydrantoin (phenytoin) and diphenyl dimethyl dicarboxylate (DDB) based on the molecular interaction between drug and additives during pharmaceutical processing to be related with the bioavailability behavior. (omitted)

• Asian-Australasian Journal of Animal Sciences
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• 제2권3호
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• pp.181-182
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• 1989

• Biomolecules & Therapeutics
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• 제23권3호
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• pp.296-300
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• 2015

${\beta}$-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of ${\beta}$-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of ${\beta}$-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of ${\beta}$-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of ${\beta}$-lapachone was 15.5%. The considerable degradation of ${\beta}$-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of ${\beta}$-lapachone may be resulted from the first-pass metabolic degradation of ${\beta}$-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.

• Journal of Pharmaceutical Investigation
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• 제41권5호
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• pp.301-307
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• 2011

The aim of this study was to investigate the effects of kaempferol on the pharmacokinetics of nimodipine in rats. Nimodipine and kaempferol interact with cytochrome P450 (CYP) enzymes and P-glycoprotein (P-gp), and the increase in the use of health supplements may result in kaempferol being taken concomitantly with nimodipine as a combination therapy to treat orprevent cardiovascular disease. The effect of kaempferol on P-gp and CYP3A4 activity was evaluated and Pharmacokinetic parameters of nimodipine were determined in rats after an oral (12 mg/kg) and intravenous (3 mg/kg) administration of nimodipine to rats in the presence and absence of kaempferol (0.5, 2.5, and 10 mg/kg). Kaempferol inhibited CYP3A4 enzyme activity in a concentration-dependent manner with 50% inhibition concentration ($IC_{50}$) of $17.1{\mu}M$. In addition, kaempferol significantly enhanced the cellular accumulation of rhodamine-123 in MCF-7/ADR cells overexpressing P-gp. Compared to the oral control group, the area under the plasma concentration-time curve ($AUC_{0-\infty}$) and the peak plasma concentration ($C_{max}$) of nimodipine significantly increased, respectively. Consequently, the absolute bioavailability of nimodipine in the presence of kaempferol (2.5 and 10 mg/kg) was 29.1-33.3%, which was significantly enhanced compared to the oral control group (22.3%). Moreover, the relative bioavailability of nimodipine was 1.30- to 1.49-fold greater than that of the control group. The pharmacokinetics of intravenous nimodipine was not affected by kaempferol in contrast to those of oral nimodipine. Kaempferol significantly enhanced the oral bioavailability of nimodipine, which might be mainly due to inhibition of the CYP3A4-mediated metabolism of nimodipine in the small intestine and /or in the liver and to inhibition of the P-gp efflux transporter in the small intestine by kaempferol. The increase in oral bioavailability of nimodipine in the presence of kaempferol should be taken into consideration of potential drug interactions between nimodipine and kaempferol.