[Pharmaceutical and biologic availability of chlorpromazine from macromolecule-containing tablets].
The use of sufficiently high concentrations of polyvinylpyrrolidone (PVP), hydroxyethyl cellulose (HEC) and methyl cellulose (MC) in tablet formulations leads to depot preparations of the prolonged- or sustained-release type. Having swollen up with the dissolution medium, the tablets form a hydrated matrix from which the active agent diffuses for a considerable time at constant speed. The verification of the bioavailability of chlorpromazine from PVP-, MC- and HEC-containing tablets and of a macromoleculefree standard preparation on rabbits showed considerable differences among the plasma curves. With reference to the standard preparation, the cellulose-containing preparations have a relative bioavailability of 38.8 and 45.7%, respectively. The constancy of the plasma level values for almost 8 h is remarkable. The plasma level profile of these formulations corresponds to that of a depot form of the sustained-release type.
D000818:Animals; D001702:Biopharmaceutics; D001711:Biotransformation; D002482:Cellulose / Q000031:analogs & derivatives; D002746:Chlorpromazine / Q000008:administration & dosage* / Q000378:metabolism; D007700:Kinetics; D046911:Macromolecular Substances; D008747:Methylcellulose; D011205:Povidone; D011817:Rabbits
D046911:Macromolecular Substances; D002482:Cellulose; C002283:hydroxyethylcellulose; D008747:Methylcellulose; D011205:Povidone; D002746:Chlorpromazine
Zur pharmazeutischen und biologischen Verfügbarkeit von Chlorpromazin aus makromolekülhaltigen Tabletten.