In this work, we used a preparation of diminazene, which belongs to the group of aromatic diamidines. This compound acts on the causative agents of blood protozoan diseases produced by both flagellated protozoa (Trypanosoma) and members of the class Piroplasmida (Babesia, Theileria, and Cytauxzoon) in various domestic and wild animals, and it is widely used in veterinary medicine. We examined the behavior of water-disperse diminazene (immobilized in Tween 80 micelles) at the cellular and organismal levels. We assessed the interaction of an aqueous and a water-disperse preparation with cells of the reticuloendothelial system. We compared the kinetic parameters of aqueous and water-disperse diminazene in sheep erythrocytes and plasma. The therapeutic properties of these two preparations were also compared. We found that the surface-active substances improved intracellular penetration of the active substance through interaction with the cell membrane. In sheep blood erythrocytes, micellar diminazene accumulated more than its aqueous analog. This form was also more effective therapeutically than the aqueous analog. Our findings demonstrate that use of micellar diminazene allows the injection dose to be reduced by 30%.
Animals ; Babesiosis/drug therapy/veterinary ; Diminazene/metabolism/*pharmacokinetics ; Dose-Response Relationship, Drug ; Female ; Macrophages, Peritoneal/cytology/metabolism ; Male ; Micelles ; Polysorbates ; Rats ; Sheep/*blood ; Sheep Diseases/drug therapy ; Trypanocidal Agents/*pharmacokinetics

OBJECTIVETo investigate the effects of refining temperatures and amounts of sheep's oil used in processing Epimedii Folium on Kedney-yang deficiency rats.

METHODThe corticosterone was subcutaneous injected to establish the kidney yang deficiency rat model. With the temperatures and amounts of sheep's oil were 250 degrees C/30%, 120 degrees C/30% and 120 degrees C/20% respectively, the crude drug and three kinds of pressed Epimedii Folium were extracted by water and used as examined samples while total flavonoid of Epimedii Folium was used as positive control. After examined samples and control samples were intragastirc administrated, the pharmacologic action was analyzed.

RESULTAs compared to crude drug, all of the aqueous extracts of processed Epimedii Folium have stronger effect of warming kidney and enhancing yang, especially the Epimedii Folium processed by sheep's oil with refining temperatures 120 degrees C and amounts of sheep's oil 30%. Its mechanism might be related to improving the insufficiency of hypothalamic-pituitary-adrenal-thymus (HPAT) axis suppression.

CONCLUSIONThe refining temperature of sheep's oil can affect the quality of excipients and processed drugs. The results may be useful in explaining the mechanism of Epimedii Folium processing and establishment of pharmaceutical standard of sheep's oil used as processing excipients.

Animals ; Drugs, Chinese Herbal ; administration & dosage ; Hypothalamo-Hypophyseal System ; drug effects ; Kidney Diseases ; drug therapy ; physiopathology ; Male ; Oils ; administration & dosage ; Pituitary-Adrenal System ; drug effects ; Rats ; Rats, Sprague-Dawley ; Sheep ; Technology, Pharmaceutical ; Yang Deficiency ; drug therapy ; physiopathology