Investigation of preparation parameters to improve the dissolution of poorly water-soluble meloxicam.
The rate of dissolution of drugs remains one of the most challenging aspects in formulation development of poorly water-soluble drugs. The meloxicam, a low molecular analgetic for oral administration, exhibits a slow dissolution. To improve the dissolution rate, the drug was formulated in a nanosuspension by using an emulsion-diffusion method, high-pressure homogenization or sonication. Optimization of the technological parameters (organic solvents, stabilizers, homogenization procedure and recovery of particles) allowed the formation of nanosuspensions with a particle size of 200-900 nm. SEM imaging confirmed the nanosized drug particles. Use of an SMCR method on the XRPD patterns of the nanosuspensions revealed the crystalline form of the drug and the strong interaction between meloxicam and the stabilizer. The rate of dissolution of the dried meloxicam nanosuspension was enhanced (90% in 5 min), relative to that of raw meloxicam (15% in 5 min), mainly due to the formation of nanosized particles. These results indicate the suitability of formulation procedure for preparation of nanosized poorly water-soluble drug with significantly improved in vitro dissolution rate, and thus possibly enhance fast onset of therapeutic drug effect.
Ambrus
R
R
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SI-1000 Ljubljana, Slovenia. revesz@pharm.u-szeged.hu
Kocbek
P
P
Kristl
J
J
Sibanc
R
R
Rajkó
R
R
Szabó-Révész
P
P
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004339:Drug Compounding / Q000379:methods*; D004655:Emulsions; D005079:Excipients; D005612:Freeze Drying; D007526:Isoelectric Point; D000077239:Meloxicam; D008855:Microscopy, Electron, Scanning; D015233:Models, Statistical; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D033362:Powder Diffraction; D011208:Powders / Q000737:chemistry; D012995:Solubility; D012997:Solvents; D013010:Sonication; D013535:Suspensions; D013843:Thiazines / Q000032:analysis / Q000737:chemistry*; D013844:Thiazoles / Q000032:analysis / Q000737:chemistry*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004655:Emulsions; D005079:Excipients; D011208:Powders; D012997:Solvents; D013535:Suspensions; D013843:Thiazines; D013844:Thiazoles; D000077239:Meloxicam