• Proceedings of the PSK Conference
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• 2002.04a
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• pp.224.3-225
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• 2002

• YAKHAK HOEJI
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• v.44 no.2
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• pp.189-192
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• 2000

We examined a dermal pharmacokinetics for a new SYC-fentanyl patch in rabbits. Determination of fentanyl in the plasma was performed using a gas chromatography with nitrogen-phosphorus detection system and a capillary column. One patch per animal (fentanyl 2.5 mg) was applied to clipped back skin for 72 hours. The plasma fentanyl concentration profile of SYC-patch was similar to that of a conventional patch (Durogesi $c^{R}$, Janssen Co.). No significant difference was observed in the pharmacokinetic parameters, the area under the concentration-time curve (AU $C^{0-}$72hrs/) and the total area under the first moment-time curve (AUM $C^{0-}$7hrs/), between the two patch types. The AU $C^{0-}$7hrs/ and AUM $C^{0-}$72hrs/ of durogesi $c^{R}$ were 183.3$\pm$46.28 ng＊hr/ml and 6,450$\pm$1,939ng＊h$r^2$/ml, and those of SYC-fentany patch were 217.2$\pm$50.51$\pm$ng＊hr/ml and 8,022$\pm$2,245ng＊h$r^2$/ml, respectively (n=3). This result indicates that the new SYC patch has a similar bioavailability compared to durogesi $c^{R}$ patch. Therefore, the SYC-patch may be considered as a bioequivalent fentanyl patch.patch.tch.

• YAKHAK HOEJI
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• v.39 no.6
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• pp.577-584
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• 1995

On the combination of antacid, the pharmacokinetics and gastric adhesion of [$^{14}c$]aceglutamide aluminium complex([$^{14}C$]AGA) were examined in rats. Specially, this study was focused on the drug interaction that the co-administration of antacid may affect the oral absorption and gastric adhesion of aceglutamide aluminium complex(AGA). In the study of the oral co-administration of [$^{14}C$] AGA and antacid(aluminium hydroxide and magnesium hydroxide(AM)), the radioactivity of plasma and urinary recovery was lower than that of [$^{14}C$]AGA alone administered group. However, the cumulative recovery of radioactivity in feces was increased significantly. The comparative bioavailability of [$^{14}C$] AGA from the plasma concentration-time curve and urinary recovery was about 60%. In vitro, the effect of antacid on the gastric adhesion of AGA was not significatly different between AGA and AGA/antacid treatment. And it accorded well with the result of in vivo experiment. In conclusion, on the combination of antacid, the oral absorption of AGA was decreased by the gastric adhesion was not affected in respect of drug interaction.

• Mass Spectrometry Letters
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• v.2 no.4
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• pp.88-91
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• 2011

The pharmacokinetic properties of S-amlodipine were studied using racemic amlodipine and single S-enantiomer (SK310) administration to rats. Plasma levels of the drug were determined using chiral liquid chromatography coupled with tandem mass spectrometry following solid phase extraction. The stereospecific analysis of amlodipine was performed on an ${\alpha}$-acid glycoprotein (AGP) column using a mobile phase comprising 10 mM ammonium acetate (pH 4.0) and propanol at a flow rate of 0.2 mL/min. This method was used to perform a comparative study of the pharmacokinetics of amlodipine and SK310. The results revealed that the pharmacokinetic profile of S-amlodipine after the administration of SK310 was comparable to that following the administration of the racemic mixture.

• Bulletin of the Korean Chemical Society
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• v.34 no.5
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• pp.1559-1562
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• 2013

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.97-97
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• 1995

On the combination of antacid, the pharmacokinetics and gastric adhesion of $\^$14/C-aceglutamide aluminum complex($\^$14/C-AGA) were examined in rats. Specially, This study was focused on the drug interaction that the coadministration of antacid may affect the oral absorption and gastric adhesion of aceglutamide aluminum complex(AGA). After the oral administration of $\^$14/C-AGA and antacid to rats, the radioactivity of plasma and urinary recovery was lower than that of $\^$14/C-AGA administered group. Relatively, the cumulative recovery of radioactivity in feces was increased significantly. The comparative bioavailability of $\^$14/C-AGA from the plasma concentration-time curve and urinary recovery was about 60%. in vitro, the effect of antacid in the gastric adhesion of AGA was not significantly different between AGA and AGA/antacid treatment. And it accorded well with the result of in vivo experiment. In conclusion, on the combination of antacid, the oral absorption of AGA was decreased but the gastric adhesion was not affected in respect of drug interaction.

• Journal of Veterinary Clinics
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• v.14 no.2
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• pp.195-200
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• 1997

In order to compare the pharmacokinetic profiles of enrofloxacin-HCL)ENFLX-HCL) and enrofloxacin-KOH (ENFLX-KOH) after oral administration in broiler chickens, the study was performed. The chickens used in this study weighed $1.82 {\pm}0.2 kg$ and clinically healthy. The dose of intravenous and lral administration was 5 mg per kg of body weight as enrofloxacin. After intravenous injection of enrofloxacin, it showed two-compartment model with the rapid distribution phase and the slow elimination phase. The mean apparent volume of distribution (Vd) was 2.70 l/kg. The mean half-life of elimination and distribution showed 8.26 h and 0.44 h, respectively. The mean area under curve (AUC) was calculated as $19.7 {\mu} g{\cdot} h/ml$. After oral administration of ENFLX-HCL and ENFLX-KOH with a rate of dose 5 mg of enrofloxacin/kg of body weight, Both of the products were showed one-compartment model unlike that of i.v. enrofloxacin standard solution showed the mean bioavailability of 79.64% for the ENFLX-KOG and 86.24% for the ENFLX-HCL. The mean total body clearance of the former was 0.24 l/kg/h and the latter 0.42 l/kg/h. Both enorfloxacin formulations seemed to have good tissue distribution and penetration as indicated by large volume of distribution : 2.72 l/kg for the -KOH and 4.44 l/kg for the -HCL. With the results obtained in this study, ENFLX-HCL could be used in place of its salt form in chickens.

• Archives of Pharmacal Research
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• v.8 no.3
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• pp.177-186
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• 1985

Effect of food on the absorption characteristics of oral rifampicin was studied in the fasted rats. Rifampicin dissolved in a new cosolvent was also injected to the rats intravenously, and the pharmacokinetic analysis was performed to explain the effect of food on the gastrointestinal absorption of rifampicin. Rifampicin was absorbed rapidly and completely in the fasting state. Food had a profound effect on the gastrointestinal absorption of rifampicin, i. e., bioavailability and the extent of absorption were decreased to less than one-third of the fasting state in the postprandial state. Food seemed to imhibit the absorption and reabsorption of rifampicin in the gastrointestinal tract, but not the absorption rate constant. Hepatobiliary excretion seemed to be the major route of elimination, since the renal clearance accounted for only 8 % of the systemic clearance. Nevertheless, first-pass effect was negligibly small and most of rifampicin absorbed could reach systemic circulation. Serum concentration change of oral rifampicin on multiple dosing differed markedly in the fasting and postprandial state, which suggested the need of careful adjustment of dosage regimen in both states.

• Korean Journal of Veterinary Research
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• v.44 no.2
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• pp.201-206
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• 2004

Norfloxacin (NFX) is a fluorquinolone antibacterial agent with a high antimicrobial activity and might have great potential for treating common infections in poultry. The objective of this study was to obtain comparative pharmacokinetic data after a single oral administration and medication with drinking water of norfloxacin-glycine acetate (NFX-GA) at the dose rate of 10 mg/kg bw in broilers. Fifty minutes following oral administration of NFX-GA, serum concentrations peaked at $1.32{\mu}g/mL$ (range $1.03-1.45{\mu}g/mL$). Serum concentration of NFX declined with a half-life of $7.21{\pm}1.81$ h. On the third day after administration of medicated drinking water, steady-state was reached, with mean concentrations of NFX of $0.70{\pm}0.35{\mu}g/mL$. The concentration of NFX after medication of NFX-GA with drinking for 3 days provides sufficient levels to obtain maximum therapeutic effects and maintains the serum persistence of concentration exceeding MIC.

• Korean Journal of Clinical Pharmacy
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• v.26 no.2
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• pp.150-162
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• 2016

Objective: First-in-human dose estimation is an essential approach for successful clinical trials for drug development. In this study, we systematically compared first-in-human dose and human pharmacokinetic parameter estimation approaches. Methods: First-in-human dose estimation approaches divided into similar drug comparison approaches, regulatory guidance based approaches, and pharmacokinetic based approaches. Human clearance, volume of distribution and bioavailability were classified for human pharmacokinetic parameter estimation approaches. Results: Similar drug comparison approaches is simple and appropriate me-too drug. Regulatory guidance based approaches is recommended from US Food and Drug Administration (FDA) and European Medicines Agency (EMA) regarding no-observed-adverse-effect level (NOAEL) or minimum anticipated biological effect level (MABEL). Pharmacokinetic based approaches are 8 approaches for human clearance estimation, 5 approaches for human volume of distribution, and 4 approaches for human bioavailability. Conclusion: This study introduced and compared all methods for first-in-human dose estimation. It would be useful practically to estimate first-in-human dose for drug development.