A preliminary in-vivo study was performed on a new modified release system which contained diltiazem hydrochloride. The system consisted of swellable minimatrices that were coated with an acrylic polymeric film. The film thickness, because of its pH-dependent solubility, might represent a critical variable with regard to in-vivo release. In order to evaluate the influence of such a variable on in-vivo behaviour, two minimatrices formulations with differing film thickness were tested versus a commercial tablet. The in-vivo study, which was based on a balanced incomplete block design, involved six volunteers in two sequences. The drug was quantified in plasma by an HPLC method. Computation and statistical analysis of pharmacokinetic parameters were performed by means of SIPHARR package (Simed, F). The results show that the approach of film coating, in order to modify the release rate from minimatrices, is feasible, but it must be improved; in particular the results point to the necessity of reducing the film susceptibility to pH changes.

Swelling-restricted minimatrices for controlled release of drugs. Preliminary in-vivo studies / C. Caramella, F. Ferrari, M. C. Bonferoni, A. Gazzaniga, M. E. Sangalli, U. Conte, M. De Bernardi di Valserra, F. Feletti. - In: BOLLETTINO CHIMICO FARMACEUTICO. - ISSN 0006-6648. - 128:10(1989 Oct), pp. 310-314.

Swelling-restricted minimatrices for controlled release of drugs. Preliminary in-vivo studies

A. Gazzaniga;M. E. Sangalli;
1989-10

Abstract

A preliminary in-vivo study was performed on a new modified release system which contained diltiazem hydrochloride. The system consisted of swellable minimatrices that were coated with an acrylic polymeric film. The film thickness, because of its pH-dependent solubility, might represent a critical variable with regard to in-vivo release. In order to evaluate the influence of such a variable on in-vivo behaviour, two minimatrices formulations with differing film thickness were tested versus a commercial tablet. The in-vivo study, which was based on a balanced incomplete block design, involved six volunteers in two sequences. The drug was quantified in plasma by an HPLC method. Computation and statistical analysis of pharmacokinetic parameters were performed by means of SIPHARR package (Simed, F). The results show that the approach of film coating, in order to modify the release rate from minimatrices, is feasible, but it must be improved; in particular the results point to the necessity of reducing the film susceptibility to pH changes.
Excipients; Chemistry, Pharmaceutical; Delayed-Action Preparations; Humans; Adult; Chromatography, High Pressure Liquid
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
BOLLETTINO CHIMICO FARMACEUTICO
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/181583
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