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

  • Choi, Min-Ho (Department of Parasitology and Tropical Medicine and Institute of Endemic Diseases, Seoul National University College of Medicine) ;
  • Chang, Byung-Chan (Department of Parasitology and Tropical Medicine and Institute of Endemic Diseases, Seoul National University College of Medicine) ;
  • Lee, Seung-Jin (Department of Pharmacology, Ewha Womans University College of Pharmacy) ;
  • Jang, In-Jin (Department of pharmacology and Clinical Trial Center, Seoul National University College of Medicine) ;
  • Shin, Sang-Goo (Department of pharmacology and Clinical Trial Center, Seoul National University College of Medicine) ;
  • Kho, Weon-Gyu (Departments of Parasitology,Inje University College of Medicine) ;
  • Chun, Jin-Ho (Preventive Medicine, Inje University College of Medicine) ;
  • Hong, Sung-Tae (Department of Parasitology and Tropical Medicine and Institute of Endemic Diseases, Seoul National University College of Medicine)
  • Published : 2006.12.10

Abstract

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.

Keywords

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