Bioavailability of theophylline from glutaraldehyde cross-linked casein microspheres in rabbits following oral administration

Latha, M. S. ; Rathinam, K. ; Mohanan, P. V. ; Jayakrishnan, A. (1995) Bioavailability of theophylline from glutaraldehyde cross-linked casein microspheres in rabbits following oral administration Journal of Controlled Release, 34 (1). pp. 1-7. ISSN 0168-3659

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Official URL: http://linkinghub.elsevier.com/retrieve/pii/016836...

Related URL: http://dx.doi.org/10.1016/0168-3659(94)00088-C

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°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.

Item Type:Article
Source:Copyright of this article belongs to Controlled Release Society.
Keywords:Theophylline; Controlled Release; Microspheres; Casein; Cross-linking; Bioavailability
ID Code:13741
Deposited On:12 Nov 2010 15:01
Last Modified:03 Jun 2011 09:52

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