Piroxicam ternary solid dispersion system for improvement of dissolution (%) and in vitro anti-inflammation effects
The improvement of drug solubility is a challenging task in the pharmaceutical industry; moreover, drug stability is also important. This study was designed to improve the dissolution (%) and in vitro anti-inflammation effects of piroxicam (PRX) and maintain its stability using a ternary solid dispersion (SD) system.
Highlights
• The PRX-solid dispersion with ternary system were prepared using a melting method.• The SD1 improved the dissolution (%) compared to that of Feldene® in different dissolution medium.
• In vitro anti-inflammation effects of SD1 showed improved compared to Feldene®.
• The SD1 has a good stability for 12 months (20 ± 5.0 °C, RH 50-60%).
The solubilizer (poloxamer 407 [P407®]) and carrier (Aerosil®200) were selected based on solubility test and pre-dissolution test, respectively. The SD1 formulation (PRX: Aerosil®200: P407® = 1:1:3 wt ratio) improved the dissolution (%) by over 1.11-/1.17-/1.21-fold and 1.77-/2.26-/1.39-fold compared with commercial products, Feldene® and pure PRX, respectively, in pH 1.2/distilled water/pH 6.8 buffer for 60 min, respectively. The anti-inflammation study of SD1 observed similar or improved compared to that of Feldene®. In conclusion, the SD1 was developed with significantly enhanced dissolution (%) and stability for 12 months. Thus, the SD1 is expected to improve bioavailability and be effective in anti-inflammatory treatment in animal study. Continue reading on Piroxicam ternary solid dispersion system
Keywords Piroxicam, Solid dispersion, Solubility, Pre-dissolution (%), Dissolution (%), StabilityI, n vitro anti-inflammatory, Kolliphor® (P188® and P407®), PEG6000, Kolliphor® HS-15, Kollicoat® IR (polyvinyl alcohol-polyethylene glycol graft-copolymer), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®), D-α-tocopheryl polyethylene glycol-1000-succinate (TPGS), and Kollidon® (12, 17, 30, 90) , Aerosil® 200, Mannitol (200SD), Lactose (Flowlac® 100) Microcrystalline cellulose (MCC, Avicel® PH-102)