title: Pharmacokinetic Profile of µSMIN Plus™, a new Micronized Diosmin Formulation, after Oral Administration in Rats.
abstract: Diosmin is a naturally occurring flavonoid present in citrus fruits and other plants belonging to the Rutaceae family. It is used for the treatment of chronic venous insufficiency (CVI) for its pheblotonic and vaso-active properties, safety and tolerability as well. The aim of the current in vivo study was to investigate the pharmacokinetic profile of a branded micronized diosmin (µSMIN Plus™) compared with plain micronized diosmin in male Sprague-Dawley rats. After oral administration by gastric gavage, blood samples were collected via jugular vein catheters at regular time intervals from baseline up to 24 hours. Plasma concentrations were assessed by LC/MS. For each animal, the following pharmacokinetic parameters were calculated using a non-compartmental analysis: maximum plasma drug concentration (Cmax), time to reach Cmax (Tmax), area under the plasma concentration-time curve (AUC0-last), elimination half-life (t½), and relative oral bioavailability (%F). The results of the current study clearly showed an improvement in the pharmacokinetic parameters in animals treated with µSMIN Plus™ compared with animals treated with micronized diosmin. In particular, µSMIN Plus™ showed a 4-fold increased bioavailability compared with micronized diosmin. In conclusion, the results from the current study provided a preliminary pharmacokinetic profile for µSMIN Plus™, which may represent a new tool for CVI management.
authors.forename: Rosario
authors.initials: R
authors.lastname: Russo
authors.forename: Angelo
authors.initials: A
authors.lastname: Mancinelli
authors.forename: Michele
authors.initials: M
authors.lastname: Ciccone
authors.forename: Fabio
authors.initials: F
authors.lastname: Terruzzi
authors.forename: Claudio
authors.initials: C
authors.lastname: Pisano
authors.forename: Lorella
authors.initials: L
authors.lastname: Severino
mesh_terms: D000818:Animals; D019540:Area Under Curve; D004145:Diosmin / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D004304:Dosage Forms; D005419:Flavonoids / Q000097:blood / Q000493:pharmacokinetics; D006207:Half-Life; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D004304:Dosage Forms; D005419:Flavonoids; D004145:Diosmin; C039602:diosmetin