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Sustained-release praziquantel tablet: Pharmacokinetics and the treatment of clonorchiasis in beagle dogs

Title
Sustained-release praziquantel tablet: Pharmacokinetics and the treatment of clonorchiasis in beagle dogs
Authors
Hong S.-T.Lee S.H.Lee S.-J.Kho W.-G.Lee M.Li S.Chung B.-S.Seo M.Choi M.-H.
Ewha Authors
이승진
SCOPUS Author ID
이승진scopus
Issue Date
2003
Journal Title
Parasitology Research
ISSN
0932-0113JCR Link
Citation
vol. 91, no. 4, pp. 316 - 320
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Praziquantel is rapidly absorbed and secreted; and thus fractional doses are recommended for the treatment of cestode and trematode infections. In the present study, we developed a new praziquantel tablet formula allowing sustained-release (SRP). In vitro dissolution of SRP tablets showed that praziquantel at 300 mg/tablet combined with hydroxypropyl methylcellulose dissolved completely at a constant rate over 10 h, whereas the conventional praziquantel tablet (PZQ) was only 40% dissolved. Pharmacokinetic studies in dogs confirmed that SRP was absorbed more slowly than PZQ. The mean value of the area under the concentration/time curve from 0 h to the final observation time, the maximum concentration in serum, and the time of maximum concentration in serum for SRP were 3,471,500 ng/min for 0.25 ml, 10,300 ng for 0.25 ml, and 192 min, while the values for PZQ were 688,600 ng/min for 0.25 ml, 2,500 ng for 0.25 ml, and 135 min. The cure rate in dogs with a heavy infection (500 metacercariae) treated with a single dose of SRP (150 mg/tablet) at 50 mg/kg was 80%, while in dogs treated with a single dose of SRP (300 mg/tablet) at 30 mg/kg it was 60%, and the cure rate with PZQ was 20%. In each case, the egg reduction rate was similar (over 90%). No abnormal liver functions or hepatic or renal pathologies were observed in dogs administered with SRP at 30 mg/kg. The SRP tablet showed sustained release and slow absorption; and it had an improved anthelmintic efficacy against Clonorchis sinensis in experimental dogs, compared with conventional praziquantel.
DOI
10.1007/s00436-003-0958-7
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약학대학 > 약학과 > Journal papers
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