• Title/Summary/Keyword: Pharmacokinetics of praziquantel

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Correlation between Pharmacokinetics of Praziquantel and Extermination of Microcotyle sebastis (Monogenea) in Cultured Rockfish Sebastes schlegeli

  • Kim Chun Soo;Kim Ki Hong
    • Fisheries and Aquatic Sciences
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    • v.4 no.4
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    • pp.197-200
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    • 2001
  • To investigate the re-treatment time of Microcotyle sebastis by oral administration of praziquantel, the residue levels of praziquantel in plasma of rockfish Sebastes schlegeli administered orally at a dose of 200 mg/kg B.W. were analyzed by reversed-phase HPLC, and the concentrations of praziquantel in the plasma were correlated with the extermination of M. sebastis. The absorption and depletion of praziquantel in the blood of rockfish were fast and the residual concentrations of praziquantel declined below $4\mu g/mL$ within 24 hr post treatment. Most of worms were exterminated within 3 hr after oral administration of praziquantel, however, a small number of M. sebastis were not killed by the treatment until end of the experiment. Considering fast drop of praziquantel in blood and extermination pattern of M. sebastis in the present results, retreatment at an interval of 9-12 hr would be effective for eradication of M. sebastis.

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Pharmacokinetics of Praziquantel in Rabbits (가토에서의 Praziquantel의 체내 동태)

  • Lee, Mi-Jeong;Shim, Chang-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • YAKHAK HOEJI
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    • v.34 no.1
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    • pp.40-46
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    • 1990
  • Pharmacokinetic studies on praziquantel in rabbits were performed in this paper. The pharmacologically active parent drug was separated from the pharmacologically inactive metabolites by HPLC method. The pharmacokinetic parameters of parent drug were obtained. In vitro partition to blood cells of praziquantel was measured. The mean value (n = 3) of partition to blood cells was 44% at concentrations between $1\;{\mu}g/ml$ and $40\;{\mu}g/ml$. Therefore, the relatively high partition to blood cells should be considered in further pharmacokinetic studies on praziquantel.

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Therapeutic evaluation of sustained-releasing praziquantel (SRP) for clonorchiasis: Phase 1 and 2 clinical studies

  • Choi, Min-Ho;Chang, Byung-Chan;Lee, Seung-Jin;Jang, In-Jin;Shin, Sang-Goo;Kho, Weon-Gyu;Chun, Jin-Ho;Hong, Sung-Tae
    • Parasites, Hosts and Diseases
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    • v.44 no.4 s.140
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    • pp.361-366
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    • 2006
  • Sustained-releasing praziquantel (SRP) tablet was designed for single dose treatment regimen of clonorchiasis. A previous pre-clinical study confirmed its sustained-releasing characteristics and a better cure rate than conventional praziquantel (PZQ). In this clinical study, the pharmacokinetics of this SRP tablet were investigated in human volunteers (phase 1; 12 volunteers), and its curative efficacy was examined in clonorchiasis patients (phase 2; 20 volunteers). In the phase 1 clinical study, blood concentrations of both tablets showed wide individual variation. The $AUC_{last}$ of SRP was $497.9{\pm}519.0ng{\cdot}hr/ml\;(mean{\pm}SD)$ and PZQ of $628.6{\pm}695.5\;ng{\cdot}hr/ml$, and the $AUC_{inf}$ of SRP was $776.0{\pm}538.5\;ng{\cdot}hr/ml$ and of PZQ $658.6{\pm}709.9\;ng{\cdot}hr/ml$. $C_{max}$ values of SRP and PZQ were $90.7{\pm}82.2ng/ml\;and\;214.9{\pm}251.9\;ng/ml$, and $T_{max}$ values were $3.42{\pm}1.43\;hr\;and\;1.96{\pm}1.23\;hr$, respectively. SRP tablets showed similar AUC values, but lower $C_{max}$ and longer $T_{max}$ values than PZQ. In the phase 2 study, SRP at 30 mg/kg (single dose) achieved a 60% cure rate and a 95.5% egg reduction rate. The cure rate of a single dose SRP was unsatisfactory compared with that of the conventional PZQ dose, but much better than that achieved by a single dose PZQ.