• Korean Journal of Veterinary Research
• /
• v.40 no.3
• /
• pp.471-478
• /
• 2000

The pharmacokinetic properties of KR-V compounds, recently developed as new anti-HIV agents, were studied after i.v. and p.o. administration in rats. The concentrations of the KR-V series were determined in rat plasma using an high-performance liquid chromatography (HPLC)-UV detection system. Of the 19 KR-V compounds investigated in the present study, only KR-V 3, 10, 14, 16 and 18-1 showed oral bioavailability. The plasma concentration-time data could be adequately described by an one-compartment open model. In the i.v. kinetic study (10mg/kg), the CLt of KR-V 3, 10, 14 and 16 (>4L/hr/kg) were significantly higher than that of KR-V 18-1 (1.1 L/hr/kg). The AUC of KR-V 18-1 was greater ($8.97{\mu}g{\cdot}hr/ml$) than that of the other compounds, but the Vd (0.58 L/kg) was lower. In the p.o. kinetic study (50mg/kg), although the t-1/2 of KR-V 18-1 was shorter than that of the other compounds, the AUC ($3.659{\mu}g{\cdot}hr/ml)$ and $C_{max}(1.891{\mu}g/ml$) were markedly higher. In a seperated in vitro experiment, only KR-V 18-1, of the 5 compounds with bioavailibility, exhibits potent activity against HIV-1 mutant strains. Therefore, KR-V 18-1 is expected to become a new potent anti-AIDS drug candidate/lead compound.

• Korean Journal of Veterinary Research
• /
• v.40 no.4
• /
• pp.741-746
• /
• 2000

We have developed a rapid, simple and precise high-performance liquid chromatographic (HPLC) method using an UV detection system for the determination of new anti-HIV candidates, nineteen KR-V compounds, in rat plasma. We used a analytical columnn of $C_{18}$ ($5{\mu}m$, $250{\times}2.0mm$ I.D.) and a mobile phase of water and ACN mixture (40/60, v/v). Under these conditions, all the KR-V compounds were readily separated from plasma with retention times of 4-12 min. The limits of quantitation for the 19 KR-V compounds were 15-30 ng/ml. The recoveries from the plasma were higher than 85% (C.V.<10%) with exception of KR-V 2, 7 and 15. The compounds KR-V 2, 7 and 15, containing ester moieties, were found to be unstable in plasma. This result suggests that esters, like KR -V 2, 7 and 15, should be excluded from future structure design studies of anti-HIV KR-V agents. In conclusion, the current HPLC method is a valuable analytical tool for investigating the pharmacokinetics of the KR-V series in rats.

• Journal of the Korean Institute of Illuminating and Electrical Installation Engineers
• /
• v.29 no.3
• /
• pp.81-87
• /
• 2015

In order to effectively protect electrical and electronic circuits which are extremely susceptible to lightning surges, multi-stage surge protection circuits are required. This paper presents the operational characteristics of the two-stage hybrid surge protection circuit in extra-low voltage DC power lines. The hybrid surge protective device consists of the gas discharge tube, transient voltage suppressor, and series inductor. The response characteristics of the proposed hybrid surge protective device to combination waves were investigated. As a result, the proposed two-stage surge protective device to combination wave provides the tight clamping level of less than 50V. The firing of the gas discharge tube to lightning surges depends on the de-coupling inductance and the rate-of-change of the current flowing through the transient voltage suppressor. The coordination between the upstream and downstream components of the hybrid surge protective device was satisfactorily achieved. The inductance of a de-coupler in surge protective circuits for low-voltage DC power lines, relative to a resistance, is sufficiently effective. The voltage drop and power loss due to the proposed surge protective device are ignored during normal operation of the systems.