Pharmacokinetic Profile of µSMIN Plus™, a new Micronized Diosmin Formulation, after Oral Administration in Rats
| Autor: | Michele Ciccone, Fabio Terruzzi, Rosario Russo, Claudio Pisano, Angelo Mancinelli, Lorella Severino |
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| Přispěvatelé: | Russo, Rosario, Mancinelli, Angelo, Ciccone, Michele, Terruzzi, Fabio, Pisano, Claudio, Severino, Lorella |
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Male
Chronic venous insufficiency Cmax Diosmin Plant Science Pharmacology Dosage form Rats Sprague-Dawley Pharmacokinetics Oral administration Drug Discovery Medicine Animals Dosage Forms Flavonoids business.industry General Medicine medicine.disease Diosmin Flavonoids Pharmacokinetic Bioavailability Rats Complementary and alternative medicine Tolerability Area Under Curve business medicine.drug Half-Life |
| Popis: | 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 (t1/2), 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. |
| Databáze: | OpenAIRE |
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