Formulation, Characterization and Optimization of Valsartan Self-Microemulsifying Drug Delivery System Using Statistical Design of Experiment

Title
Formulation, Characterization and Optimization of Valsartan Self-Microemulsifying Drug Delivery System Using Statistical Design of Experiment
Author(s)
김종오포우델비자이마라시니니르말트란탄힙용철순최한곤[최한곤]
Keywords
BOX-BEHNKEN DESIGN; BIOAVAILABILITY; EXTRACTION; VARIABLES
Issue Date
201211
Publisher
PHARMACEUTICAL SOC JAPAN
Citation
CHEMICAL & PHARMACEUTICAL BULLETIN, v.60, no.11, pp.1409 - 1418
Abstract
The aim of the present research was to systematically investigate the main, interaction and the quadratic effects of formulation variables on the performance of self-microemulsifying drug delivery system (SMEDDS) of valsartan using design of experiment. A 17-run Box-Behnken design (BBD) with 3-factors and 3-levels, including 5 replicates at the centre point, was used for fitting a 2nd-order response surface. After the preliminary screening, Labrafil M 2125 CS as oil, Tween 20 as surfactant and Capryol 90 as co-surfactant were taken as independent variables. The dependent factors (responses) were particle size, polydispersity index (PDI), dissolution after 15 min and equilibrium solubility. Coefficients were estimated by regression analysis and the model adequacy was checked by an F-test and the determination coefficient (R-2). All the responses were optimized simultaneously by using desirability function. Our results demonstrated marked main and interaction effects of independent factors on responses. The optimized formulation consisted of 26.8% (w/w) oil, 60.1% (w/w) surfactant and 13.1% (w/w) co-surfactant, and showed average micelle size of 90.7 nm and 0.246 PDI, 91.2% dissolution after 15 min and 226.7 mg/g equilibrium solubility. For the optimized formulation, predicted value and experimental value were in close agreement. After oral administration, the optimized formulation gave more than 2-fold higher area under curve (AUC) and about 6-fold higher C-max in rats than valsartan powder (p<0.05). The BBD facilitated in the better understanding of inherent relationship of formulation variables with the responses and in the optimization of valsartan SMEDDS in relatively time and labor effective manner.
URI
http://hdl.handle.net/YU.REPOSITORY/26997
ISSN
0009-2363
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