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KMID : 0617320030120010181
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Journal of Pharmacetical Sceiences Ewha Womans University
2003 Volume.12 No. 1 p.181 ~ p.185
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Sustained-release praziquantel tablet
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Hong, Sung-Tae
Lee, Sang Hyup/Lee, Seung-Jin/Kho, Weon-Gyu/Lee, Mejeong/Li, Shunyu/Chung, Byung-Suk
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Abstract
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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 ㎎/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 ㎖, 10,300 ng for 0.25 ㎖, and 192 min. while the values for PZQ were 688,600 ng/min for 0.25㎖, 2,500 ng for 0.25㎖, and 135 min. The cure rate in dogs with a heavy infection (500 metacercariae) treated with a single dose of SRP (150 ㎎/tablet) at 50 ㎎/㎏ was 80%, while in dogs treated with a single dose of SRP (300 ㎎/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 ㎎/㎏. 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.
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