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Purpose . 31 P CP/MAS NMR is used to characterize stability and changes in solid state properties of disodium clodronate tetrahydrate upon variable temperature and slow dehydration. Methods . Variable temperature 31 P CP/MAS NMR spectroscopy. Results . A fast rise in temperature leads to loss of...
Purpose . Utility values obtained with the standard gamble (SG) method using the probability equivalence approach (PE) have a reported bias due to the "certainty effect." This effect causes individuals to overvalue a positive outcome when it occurs under certainty. Researchers in the decision...
Purpose . Twelve synthetic spider toxin analogs were prepared in an effort to better understand the structure-activity relationships of the polyamine portion of argiotoxin-636 (Arg-636), a noncompetitive NMDA receptor (NMDAR) antagonist. Methods . The l,13-diamino-4,8-diazatridecane portion of...
Purpose . This study aims to assess the drug absorption kinetics of three drugs and compare their resulting first-order intestinal permeation rate constants to their Caco-2 monolayer permeabilities. Methods . In vitro dissolution — in vivo absorption analysis was conducted on four formulations...
Purpose . To apply cocktail approaches for protein binding (PB) and pharmacokinetics (PK) within a discovery program as a means of providing timely systemic exposure (AUC and C max ) data. Methods . For PB data, a procedure of cocktail ultrafiltration, mixed matrix sample preparation and single...
Purpose . Biliary organic anion excretion is mediated by an ATP-dependent primary active transporter, a so-called canalicular multispecific organic anion transporter (cMOAT). As there appear to be many canalicular organic anion transports, we examined the effects of various organic anions and...
Purpose . To investigate the effect of ultrasound on the histological integrity and permeability properties of whole rat skin in vitro . Methods . A defined, field-free source of ultrasound was used to irradiate excised rat skin prior to in vitro transport studies in Franz-type cells using...
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