Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function

Title
Optimization of self-microemulsifying drug delivery system for telmisartan using Box-Behnken design and desirability function
Author(s)
김종오조혁준이동원마라시니니르말포우델비자이김정환티르거네쉬라마사미용철순유봉규[유봉규]최한곤[최한곤]
Keywords
II RECEPTOR ANTAGONISTS; SOLID DISPERSIONS; EXCIPIENTS; SMEDDS
Issue Date
201310
Publisher
WILEY-BLACKWELL
Citation
JOURNAL OF PHARMACY AND PHARMACOLOGY, v.65, no.10, pp.1440 - 1450
Abstract
Objectives To develop and optimize the novel self-microemulsifying drug delivery system (SMEDDS) formulation for enhanced water solubility and bioavailability of telmisartan (TMS) using the Box-Behnken design (BBD) and desirability function. Method TMS-SMEDDS formulation consisted of the mixture of oil (Peceol), surfactant (Labrasol), co-surfactant (Transcutol), TMS and triethanolamine. A three-level BBD was applied to explore the main effect, interaction effect and quadratic effect of three independent variables, including the amount of Peceol (X-1), Labrasol (X-2) and Transcutol (X-3). Determined conditions were 20 < X-1 < 40, 50 < X-2 < 80 and 5 < X-3 < 30. The response variables were droplet size (Y-1), polydispersity index (Y-2) and dissolution percentage of TMS after 15 min (Y-3). Key findings The optimized conditions were 28.93, 80 and 28.08 (mg) for X-1, X-2 and X-3, respectively, and the response variables were predicted to be 159.8 nm, 0.241 and 85.8% for Y-1, Y-2 and Y-3, respectively. The actual values from the optimized formulation showed good agreement with predicted values. The optimized TMS-SMEDDS formulation showed faster drug dissolution rate and higher bioavailability than TMS powder. Conclusions Our results suggest that response surface methodology using BBD and desirability function is a promising approach to understand the effect of SMEDDS variables and to optimize the formulation.
URI
http://hdl.handle.net/YU.REPOSITORY/28827http://dx.doi.org/10.1111/jphp.12115
ISSN
0022-3573
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약학대학 > 약학부 > Articles
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