| Autor: |
Phan, Nghia Thi, Tran, Yen Thi Hai, Nguyen, Linh Tran, Hoang, Yen Kieu, Bui, Cuong Khac, Nguyen, Hoa Dang, Vu, Giang Thi Thu |
| Zdroj: |
Current Drug Delivery; 2023, Vol. 21 Issue: 5 p734-743, 10p |
| Abstrakt: |
Background: Rosuvastatin, most commonly used in the form of calcium salt, belongs to the statin groups of synthetic antihyperlipidemic agents. Rosuvastatin possesses high permeability, however, its aqueous solubility is poor, causing a slow dissolution rate in water. Consequently, this dissolution rate has a decisive role in the release and absorption of rosuvastatin in the gastrointestinal tube.Objective: The aims of this study were to evaluate the absorption of the drug from the self-nano emulsifying drug delivery system of rosuvastatin (Ros SNEDDS) compared to rosuvastatin substance and to develop a level-A in vitro-in vivocorrelation (IVIVC) for Ros SNEDDS.Methods: An in-house developed LC-MS/MS method was used to determine the concentrations of rosuvastatin in dog plasma. Six beagle dogs received an intravenous dose, Ros SNEDDS, rosuvastatin substance. In vitrodissolution of the Ros SNEDDS was carried out with different conditions. Correlation models were developed from the dissolution and absorption results of Ros SNEDDS.Results: The results showed a 1.7-fold enhanced oral bioavailability and 2.1-time increase of rosuvastatin Cmaxin Ros SNEDDS form, compared to the rosuvastatin substance. A 900 ml dissolution medium of pH of 6.6 has demonstrated its suitability, the in vitrodissolution model was studied and supported by the Weibull equation with a weighting factor of 1/y2as it presented the lowest values of AIC.Conclusion: Ros SNEDDS demonstrated higher bioavailability of rosuvastatin in comparison to rosuvastatin substance and established a level A IVIVC used in future bioequivalence trials. |
| Databáze: |
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