51. Flurbiprofen-Loaded Solid SNEDDS Preconcentrate for the Enhanced Solubility, In-Vitro Dissolution and Bioavailability in Rats
- Author
-
Han-Joo Maeng, Dong-Jin Jang, Kwan Hyung Cho, Jin-Ha Yoon, Rae Man Kim, Kyoung Ah Min, and Yu Chul Kim
- Subjects
Flurbiprofen ,lcsh:RS1-441 ,Pharmaceutical Science ,dissolution ,02 engineering and technology ,Polyethylene glycol ,030226 pharmacology & pharmacy ,Article ,lcsh:Pharmacy and materia medica ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Differential scanning calorimetry ,solid self-nanoemulsifying drug delivery system ,medicine ,Dissolution testing ,Solubility ,Dissolution ,Chromatography ,Chemistry ,food and beverages ,021001 nanoscience & nanotechnology ,Bioavailability ,flurbiprofen ,lipids (amino acids, peptides, and proteins) ,Particle size ,0210 nano-technology ,bioavailability ,medicine.drug - Abstract
The aim of this work was to prepare and optimize a solid self-nanoemulsifying drug delivery system pre-concentrate (SSP) containing water-insoluble flurbiprofen (FL) using a novel pseudo-ternary phase diagram. The pseudo-ternary phase diagram, composed of FL as the drug and dispersion core, Kollisolv MCT 70 as the oil phase, and TPGS (tocopherol polyethylene glycol 1000 succinate) as the surfactant, was constructed for the determination of the SSP region. SSP was investigated in terms of particle size, physical state by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), in vitro dissolution and oral pharmacokinetics in rats. The determined SSP (FL/Kollisolv MCT 70/TPGS = 10/10/80, weight %) in the pseudo-ternary phase diagram had the melting point of 32.37 °, C and uniform mean particle size of below 30 nm without any precipitation of FL in the dispersion. In the dissolution test, the SSP exhibited 95.70 ±, 3.40% of release at 15 min, whereas the raw FL showed poor dissolution (i.e., 6.75 ±, 1.30%) at that time point. In addition, the SSP showed the enhanced oral absorption (i.e., 1.93-fold increase in AUCinfinite) as compared to the suspension group of raw FL. Therefore, the developed SSP would be a promising drug delivery system with excellent solubilization, dissolution, and bioavailability for FL.
- Published
- 2018
- Full Text
- View/download PDF