Lucas, Dominic published the artcileDesigning highly porous amorphous celecoxib particles by spray freeze drying leads to accelerated drug absorption in-vivo, Application In Synthesis of 169590-42-5, the publication is European Journal of Pharmaceutics and Biopharmaceutics (2022), 20-28, database is CAplus and MEDLINE.
Poorly water-soluble drugs are still a major challenge to overcome in order to achieve sufficiently high oral bioavailability. Spray freeze drying (SFD) is proposed here as an alternative for the preparation of amorphous, free-flowing porous celecoxib spheres for enhanced drug dissolution Tert-Bu alc. solutions of celecoxib + excipient (povidone, hydroxypropyl methylcellulose acetate succinate (HPMC-AS) and Soluplus) at variable ratios were sprayed into a cooled spray tower, followed by vacuum freeze drying. Final porous particles were free-flowing, highly spherical (circularity ≥ 0.96) and mean diameters ranging from 210 to 800μm, depending on excipient and drug content. XRPD measurements showed that Celecoxib was amorphous in all formulations and remained stable during 6 mo storage. Kollidon 25 and HPMC-AS combinations resulted in the highest dissolution rates as well as dissolved drug amounts (30.4 ± 1.5μg/mL and 41.8 ± 1.7μg/mL) which in turn was 2-fold and 1.3-fold increase compared to film casted amorphous reference formulations, resp. This phenomenon also translated into a faster onset of the drug absorption in-vivo, with significantly lower tmax values, while AUC values were non-significantly lowered compared to amorphous references The high porosity of SFDs led to the advantageous accelerated dissolution which also translated into faster onset of absorption in-vivo.
European Journal of Pharmaceutics and Biopharmaceutics published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C17H14F3N3O2S, Application In Synthesis of 169590-42-5.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics