ABSTRACT
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.
Subject(s)
Antiplatyhelmintic Agents/chemical synthesis , Antiplatyhelmintic Agents/pharmacology , Glycyrrhizic Acid/chemistry , Mechanical Phenomena , Opisthorchiasis/drug therapy , Praziquantel/chemical synthesis , Praziquantel/pharmacology , Animals , Antiplatyhelmintic Agents/pharmacokinetics , Antiplatyhelmintic Agents/therapeutic use , Biological Availability , Chemical Phenomena , Chemistry Techniques, Synthetic , Cricetinae , Praziquantel/pharmacokinetics , Praziquantel/therapeutic useSubject(s)
Galactans/chemistry , Larix , Nitrogen Oxides/pharmacokinetics , Animals , Capillary Permeability/drug effects , Electron Spin Resonance Spectroscopy , Free Radicals/pharmacokinetics , Galactans/pharmacokinetics , Gastrointestinal Absorption/drug effects , Male , Molecular Structure , Nitrogen Oxides/chemistry , Permeability , Rats, Wistar , Solubility , Solutions , Spin LabelsSubject(s)
Aspirin/administration & dosage , Drug Compounding/methods , Galactans/chemistry , Larix/chemistry , Platelet Aggregation/physiology , Ulcer/chemically induced , Animals , Aspirin/adverse effects , Aspirin/chemistry , Dose-Response Relationship, Drug , Galactans/adverse effects , Macromolecular Substances/adverse effects , Macromolecular Substances/chemical synthesis , Male , Platelet Aggregation/drug effects , Platelet Aggregation Inhibitors/administration & dosage , Platelet Aggregation Inhibitors/chemical synthesis , Rats , Rats, Wistar , Solubility , Stress, Mechanical , Ulcer/prevention & controlSubject(s)
Anti-Bacterial Agents/pharmacology , Nanostructures/chemistry , Silicon Dioxide/chemistry , Animals , Anti-Bacterial Agents/chemical synthesis , Chemistry, Pharmaceutical , Disease Models, Animal , Dose-Response Relationship, Drug , Drug Design , Escherichia coli/drug effects , Mice , Mice, Inbred C57BL , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/pathogenicity , Sepsis/drug therapy , Sepsis/microbiology , Sepsis/mortality , Staphylococcus aureus/drug effectsABSTRACT
This work was undertaken partly with financial support of the RBRF of the Ministry of Science of the Russian Government (N95-03-09682a) and partly with financial support of the Ministry of Education, Science, Sports and Culture (MONBUSHO) of the Government of Japan.Sols of hydrated aluminium oxide, hydrated zirconium oxide and their mixtures were investigated during the xerogel-amorphous-product-crystalline-product transition by SAXS using synchrotron radiation. In the different temperature regions certain changes in structure and morphology were observed. Some correlation between the characteristics of the initial sols and their mixtures (the size and shape of the pores) was observed. In the temperature region 298-1173 K the characteristics of the mixed sol are defined by the characteristics of the initial sols.