Physical chemical characterization of binary systems of prilocaine hydrochloride with triacetyl-β-cyclodextrin

摘要: Interaction products of prilocaine hydrochloride (PRL), a local anesthetic agent highly soluble in water, with triacetyl-β-cyclodextrin (TAβCD), hydrophobic CD derivative practically insoluble were prepared to estimate their suitability for the development prolonged-release dosage form drug. Equimolar PRL-TAβCD solid systems by different methods (physical mixing, kneading, co-grinding, sealed-heating, coevaporation, spray-drying), order investigate effectiveness and influence on physical chemical properties end products. Differential scanning calorimetry, X-ray powder diffractometry, FTIR spectroscopy environmental electron microscopy (ESEM) used solid-state characterization systems, whereas vitro dissolution determined according dispersed amount method. On basis overall studies results, ability bring about effective drug-TAβCD interactions varied order: spray-drying > co-grinding ≈ coevaporation sealed-heating kneading mixing. This rank was not observed studies, where coevaporated, kneaded sealed-heated exhibited very similar profiles, superimposable that pure drug mixture, all reaching 100% less than 10 min. Evidently, these techniques gave rise only weak surface interactions, rapidly destroyed solution. Some decrease rate co-ground system (100% dissolved after 40 min), probably due electrostatic aggregation phenomena associated high-energy mechanical treatment. A behaviour shown spray-dried system, which give an almost linear slow-dissolving profile, 420 min, suggesting this case formation actual inclusion compound. Thus, product obtained selected as best candidate future suitable oral PRL.