Characteristics of drug-phospholipid coprecipitates. II: Bioavailability studies of griseofulvin in rats. 1988

S Venkataram, and J A Rogers
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.

The bioavailabilities of griseofulvin and dimyristoylphosphatidylcholine (DMPC) coprecipitates prepared from chloroform have been determined in rats. The dissolution rate of griseofulvin in pH 2.0 HCl:KCl buffer under sink conditions increased nonlinearly with an increase in DMPC in the coprecipitates. The initial dissolution rate, the amount dissolved after 60 min, Cmax, and AUC were all approximately twofold greater for coprecipitates than for griseofulvin over the range of 19:1 to 1.5:1 griseofulvin:DMPC weight ratio. In contrast, physical mixtures of griseofulvin:DMPC yielded results which were not significantly different from those of griseofulvin alone. The correlation between in vitro and in vivo parameters was at least 0.95. Thus, the reduction in particle size and solubilization of griseofulvin which is observed in vitro are believed to also occur in vivo and provide improved bioavailabilities.

UI MeSH Term Description Entries
D008297 Male Males
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D006118 Griseofulvin An antifungal agent used in the treatment of TINEA infections. Fulvicin-U-F,Grifulvin V,Gris-PEG,Grisactin,Grisefuline,Fulvicin U F,FulvicinUF,Gris PEG,GrisPEG
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities
D012995 Solubility The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Solubilities
D013535 Suspensions Colloids with liquid continuous phase and solid dispersed phase; the term is used loosely also for solid-in-gas (AEROSOLS) and other colloidal systems; water-insoluble drugs may be given as suspensions. Suspension
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

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