Interspecies differences in pharmacokinetics of the original neuroleptic drug dilept have been studied in experimental animals (rabbits and rats) and volunteers after single oral administration of tablets and tablet mass of the drug. Parent drug in the rabbit blood plasma was detected for 4 h, in the rat plasma for about 2 h, and in the human blood plasma for about 1 h after drug administration. The degrees of dilept biotransformation into metabolites (defined as metabolism intensity, AUCM/AUCP) in rats were 21.3 (for M-1) and 1645 (for M-2), in human volunteers - 5.8 and 658.5, and in rabbits - 1.6 and 125.8, respectively. Thus, the intensity of drug metabolism in experimental animals and volunteers was different and decreased in the series rats humans rabbits.
Download full-text PDF |
Source |
---|
Dokl Biochem Biophys
January 2025
Center for Strategic Planning and Management of Biomedical Health Risks, Federal Medical and Biological Agency, Moscow, Russia.
Unlabelled: The association of the pathogenesis of neurodegenerative diseases, depression, anxiety, and cognitive disorders with neurotrophin-3 deficiency determines the prospect of creating drugs with a similar mechanism of action. Since the use of full-length NT-3 is limited by unsatisfactory pharmacokinetic properties, the creation of low-molecular mimetics of neurotrophin-3 that are active when administered systemically is relevant. The Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies has created a dimeric dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-γ-oxybutyryl-L-glutamyl-L-asparagine) with the laboratory code GTS-302, which activates TrkC and TrkB receptors.
View Article and Find Full Text PDFEur J Drug Metab Pharmacokinet
January 2025
College of Basic Medicine and Forensic Medicine, Henan University of Science and Technology, Luoyang, 471023, China.
Background And Objective: Total glucosides of paeony (TGP) capsules, tripterygium glycoside tablets (TGT), and celecoxib are commonly used drugs in clinical practice for the treatment of Rheumatoid arthritis (RA). An UPLC-MS/MS method for the analysis of celecoxib in beagle dogs was developed, the herb-drug interactions (HDIs) between TGP and TGT with celecoxib were studied based on pharmacokinetics.
Methods: The method of acetonitrile precipitation was applied to process plasma samples.
J Vet Intern Med
January 2025
Boehringer Ingelheim Pharma GmbH & Co., Ingelheim, Germany.
Background: Myxomatous mitral valve disease (MMVD) is frequently diagnosed in small breed dogs. Pimobendan oral solution has been developed to improve dosing accuracy in small and toy breed dogs.
Hypothesis/objectives: Demonstrate bioequivalence of pimobendan oral solution with pimobendan chewable tablets using a pharmacokinetic and a pharmacodynamic study in healthy purpose bred dogs.
Clin Drug Investig
January 2025
Medical Science Department, Shionogi & Co., Ltd., Osaka, Japan.
Background: Anti-obesity medications are recommended for patients who do not achieve and maintain weight loss despite lifestyle interventions. S-309309 is a novel oral inhibitor of monoacylglycerol O-acyltransferase 2 being developed as a treatment for obesity.
Objective: The objective of the study was to investigate the safety, clinical pharmacology, pharmacokinetics and pharmacodynamic biomarker of S-309309.
Front Pharmacol
January 2025
Phase I Clinical Trial Site, Nanjing Gaoxin Hospital, Nanjing, Jiangsu, China.
Background: Fluticasone propionate is a synthetic trifluoro-substituted glucocorticoid, a highly selective glucocorticoid receptor agonist. Fluticasone propionate nebuliser suspensions is an inhaled corticosteroid with the low systemic bioavailability which provides a low risk (benefit outcome without the adverse effects that accompany systemically administered corticosteroids), referred as a first-line preventive agent for patients with persistent asthma. China has become one of the countries with the highest asthma mortality rate in the world in the past years.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!