Reduced Food-Effect on Intestinal Absorption of Dronedarone by Self-microemulsifying Drug Delivery System (SMEDDS)
| Autor: | Byoung Moon Kim, Sang Won Jung, Sang Duk Han, Myung Joo Kang, Sun Woo Jang, Miwon Son |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Glycerol
Male Drug Castor Oil media_common.quotation_subject Cmax Administration Oral Amiodarone Polysorbates Pharmaceutical Science Absorption (skin) Pharmacology Intestinal absorption Glycerides Polyethylene Glycols Food-Drug Interactions Surface-Active Agents Dogs Drug Delivery Systems medicine Animals Self-microemulsifying drug delivery system Dronedarone media_common Meal Chemistry Kolliphor EL General Medicine Intestinal Absorption Drug delivery Emulsions Anti-Arrhythmia Agents medicine.drug |
| Zdroj: | Biological & Pharmaceutical Bulletin. 38:1026-1032 |
| ISSN: | 1347-5215 0918-6158 |
| DOI: | 10.1248/bpb.b15-00110 |
| Popis: | The oral absorption of dronedarone (DRN), a benzofuran derivative with anti-arrhythmic activity, is significantly affected by food intake. The absolute bioavailability of the marketed product (Multaq, Sanofi, U.S.) was about 4% without food, but increased to 15% when administered with a high fat meal. Therefore, to reduce the food-effect on the intestinal absorption of DRN, a novel self-microemulsifying drug delivery system (SMEDDS) was formulated and the comparative in vivo absorption studies with the marketed product were carried out using male beagle dogs either in the fasted or fed state. The SMEDDS consisted of the drug, Labrafil M 1944CS, and Kolliphor EL in a weight ratio of 1 : 1 : 2, rapidly formed a fine oil-in-water emulsion with a droplet size less than 50 nm. An in vivo absorption study revealed that the area-under-curve (AUC0-24 h) and maximal plasma concentration (Cmax) were 10.4-fold (p |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|