BIOAVAILABILITY OF THEOPHYLLINE FROM GLUTARALDEHYDE CROSS-LINKED CASEIN MICROSPHERES IN RABBITS FOLLOWING ORAL-ADMINISTRATION
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Date
1995
Journal Title
Journal ISSN
Volume Title
Publisher
JOURNAL OF CONTROLLED RELEASE
Abstract
Theophylline loaded bovine casein microspheres were prepared by the glutaraldehyde cross linking of an aqueous alkaline dispersion of the protein containing the drug in a non-aqueous dispersion medium. The cross-linking of the protein droplets was carried out via the organic phase by the addition of varying quantities of glutaraldehyde- saturated toluene. In vitro release of the drug was examined in simulated gastric fluid at 37 degrees C from spheres having three different cross-linking densities. The bioavailability of theophylline released from the microspheres of different cross-linking densities was studied in rabbits following single oral administration. Microspheres with higher cross-linking densities were found to sustain theophylline release even up to 24 h. The peak serum concentrations of such preparations were well within therapeutic limits. Determinations of in vitro/in vivo correlation based on the data showed that a fairly good relationship exists between in vitro and in vivo release. The study demonstrated the potential of cross-linked milk protein as a matrix for sustained release oral preparations.
Description
Keywords
Chemistry; Pharmacology & Pharmacy
Citation
34 ,1;1-7