Cefuroxime axetil solid dispersion with polyglycolized glycerides for improved stability and bioavailability

Abstract

Improvement in physical stability of solid dispersions was attributed to hydrogen bonding, while improvement in bioavailability of SDCAGA compared to SDCAP, in spite of comparable solubility and dissolution profile, may be attributed to Gelucire, which utilizes intestinal esterase for lipolysis, protecting the prodrug from enzymatic degradation to its non-absorbable base form.

Bioavailability of indomethacin-saccharin cocrystals

“…The solubility and dissolution rate primarily depend on the solid‐state form of the active pharmaceutical ingredients (APIs). Whilst numerous formulation strategies have been considered for improving dissolution rate and bioavailability, solid‐form change has been the most important in product development [2,3] . The quest for solid forms of an API with optimal properties is thus a persistent activity within drug development groups [4] …”

Enhanced dissolution and stability of adefovir dipivoxil by cocrystal formation

“…The solid properties of an active pharmaceutical ingredient may be modulated by some pharmaceutical techniques, such as solid dispersion, [1] spray‐drying [2] and hot‐melt extrusion, [3] to enhance the physicochemical and pharmacokinetic performance. The solid properties are dominated not only by molecular structures but also by packing motif.…”

Novel cajaninstilbene acid derivatives as antibacterial agents

“…Carboxylic acid esters can be absorbed in vivo quickly and completely, and have been widely used to improve the bioavailability of drugs, such as cefuroxime ester [14]. Thus a series of cajaninstilbene acid ester derivatives were synthesized in this study, in which the carboxyl group of cajaninstilbene acid (CSA) on the A ring was esterified by methanol (4ae4k) to investigate whether the esterification of CSA will improve its activity or druggability.…”