RESUMO
The mechanochemical preparation of solid compositions of praziquantel with plant saponin (glycyrrhizic acid disodium salt) is described. The study of a number of physicochemical parameters showed that dissolving solid compositions in water is accompanied by the inclusion of praziquantel molecules into micelles, which are formed in the solution of the glycyrrhizic acid disodium salt. Using the opisthorchiasis model caused by Opisthorchis felineus, we found a 4- to 11-fold increase in the anthelmintic activity of praziquantel in the composition as compared to the official praziquantel. According to the pharmacokinetic data, the use of the composition increased the bioavailability of praziquantel 3 times.
Assuntos
Antiplatelmínticos/síntese química , Antiplatelmínticos/farmacologia , Ácido Glicirrízico/química , Fenômenos Mecânicos , Opistorquíase/tratamento farmacológico , Praziquantel/síntese química , Praziquantel/farmacologia , Animais , Antiplatelmínticos/farmacocinética , Antiplatelmínticos/uso terapêutico , Disponibilidade Biológica , Fenômenos Químicos , Técnicas de Química Sintética , Cricetinae , Praziquantel/farmacocinética , Praziquantel/uso terapêuticoRESUMO
A new water-soluble form of the calcium blocker nifedipine (NF) with glycyrrhizic acid (GA) (with molecular ratio 1:4) has been obtained by mechanochemical synthesis. Its pharmacological advantages in comparison with nifedipine were determined. An effective dose of nifedipine in complex reduced to 10 times as compared to its therapeutic dose while high antihypertensive activity preservation and pleiotropic antiarhythmic activity enhancement. This new antihypertensive and antiarhythmic agent (complex of NF:GA = 1:4) is chemically stable and safe for parenteral administration.