ABSTRACT
Manufacturing process for anthelmintic embovin in a micronized form have been developed. Embovin in the micronized form exhibited the highest activity.
Subject(s)
Antinematodal Agents/chemical synthesis , Antinematodal Agents/therapeutic use , Pyrantel Pamoate/chemical synthesis , Pyrantel Pamoate/therapeutic use , Animals , Antinematodal Agents/chemistry , Antinematodal Agents/toxicity , Drug Evaluation, Preclinical , Mice , Nippostrongylus , Pyrantel Pamoate/chemistry , Pyrantel Pamoate/toxicity , Strongylida Infections/drug therapy , Technology, Pharmaceutical/methodsABSTRACT
The toxicity and anthelminthic activity of the earlier synthetized tricyclic analogues of praziquantel and 4-acylpiperazinones-2 have been studied. Tricyclic compounds have shown the acute toxicity similar to that of praziquantel and neurotoxic effect typical of praziquantel. 4-acylpiperazinones-2 toxicity correlated with their anthelminthic effect. The determination of anthelminthic activity of the above compounds in opisthorchiasis and hymenolepiasis has shown that they are less effective than praziquantel or have no anthelminthic activity. A biological activity-structure relationship has been traced in the compounds under study.
Subject(s)
Anthelmintics/toxicity , Piperazines/toxicity , Praziquantel/analogs & derivatives , Animals , Anthelmintics/therapeutic use , Cricetinae , Drug Evaluation, Preclinical , Female , Hymenolepiasis/drug therapy , Lethal Dose 50 , Male , Mesocricetus , Mice , Opisthorchiasis/drug therapy , Piperazines/therapeutic use , Praziquantel/therapeutic use , Praziquantel/toxicity , Structure-Activity RelationshipABSTRACT
The ways of searching for new anthelminthic agents among diverse chemical compounds are analysed. The most promising chemical groups are presented. It is recommended to test every drug using as many as possible experimental models. For drug screening it is advisable to apply a multi-stage investigation method as the most economic and perspective one. The drug selection technique, experimental study procedure and ways of increasing anthelminthic efficiency are outlined.
Subject(s)
Anthelmintics/therapeutic use , Animals , Anthelmintics/toxicity , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical/methods , Helminthiasis/drug therapy , Research DesignABSTRACT
New formulations have been designed to increase the efficacy and bioavailability of the oral drugs mebendazole and nocodazole and were tested in CBA mice. A considerable increase in efficacy was established for a solid disperse formulation of certain composition with a relatively lower toxicity than in aqueous suspensions of the drugs.
