Open AccessIn vitro evaluation of the complexation of non‐steroidal anti‐inflammatory drugs with caffeine
Author(s) -
GERBER JAN J.,
VILLIERS MELGARDT M.,
TOONGSUWAN SIRIPORN,
LIEBENBERG WILNA
Publication year - 1997
Publication title -
international journal of pharmacy practice
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.42
H-Index - 37
eISSN - 2042-7174
pISSN - 0961-7671
DOI - 10.1111/j.2042-7174.1997.tb00884.x
Subject(s) - caffeine , ibuprofen , naproxen , ketoprofen , medicine , bioavailability , mefenamic acid , dissolution , differential scanning calorimetry , pharmacology , dissolution testing , chromatography , nuclear chemistry , chemistry , organic chemistry , physics , alternative medicine , biopharmaceutics classification system , pathology , thermodynamics
The complexation of five non‐steroidal anti‐inflammatory drugs (NSAIDs) with caffeine was evaluated. Mixtures were prepared by powder mixing, trituration in a mortar with a pestle and recrystallisation from a common solvent. The properties of the mixtures and the recrystallised materials, evaluated by differential scanning calorimetry (DSC) and dissolution rate measurements, differed significantly ( P <0.05). Disappearance of peaks in DSC thermograms, or lowering of melting points of the NSAIDs in NSAID‐caffeine co‐precipitates were ascribed to the complexation of caffeine with the NSAIDs. The dissolution rate of ketoprofen was not affected by the addition of caffeine but the dissolution rates of ibuprofen, mefenamic acid, naproxen and indomethacin were significantly enhanced ( P 0.05) after being co‐precipitated, or mixed in a mortar or V‐blender, with caffeine. Higher dissolution rates, because of the complexation of caffeine and the drugs in solution, could translate into changed bioavailability and different pharmacokinetic parameters. Less gastrointestinal irritation and quicker onset of required blood levels might improve the efficacy of NSAIDs, a factor that, if confirmed, should be considered when prescribing these drugs to patients.