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In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. II. Probing drug/food interactions using microcalorimetry

Buckton, G; Beezer, AE; Chatham, SM; Patel, KK; (1989) In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. II. Probing drug/food interactions using microcalorimetry. International Journal of Pharmaceutics , 56 (2) pp. 151-157. 10.1016/0378-5173(89)90008-2.

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Abstract

The dissolution of tetracycline hydrochloride from a commercial sustained release product (Organon-Tetrabid) and from a dispersion of the drug in a semi-solid matrix was studied. Two techniques were used to follow dissolution, these were the USP paddle method (with UV analysis) and microcalorimetry. The influence of calcium on the dissolution rate was studied using the USP method, and was found to have no effect. Dissolution experiments were undertaken in the calorimeter using hydrochloric acid alone or with the addition of: (i) calcium; (ii) milk; (iii) Ensure; and (iv) Intralipid. It was possible to observe the known interaction between tetracycline and calcium, milk and Ensure during the dissolution process in the microcalorimeter. The calorimetric output during dissolution (a composite response for dissolution of the drug and base, and any measurable interaction that occurs) of the products in acid and the non-interacting Intralipid, being distinctly different to the output obtained during the dissolution in interacting fluids. This was equally true for both products. The kinetics describing the release from the semi-solid matrix show that an apparent zero-order process occurs for about 150 min followed by an apparent first-order process. The data obtained from the microcalorimeter showed considerable differences in the first-order release process, depending upon the nature of the dissolution fluid; those with the highest content of lipid giving different results to the more aqueous fluids. With careful selection of experiments microcalorimetry is a useful technique for the in vitro study of drug/food interactions and the influence of food on drug release profiles. © 1989.

Type: Article
Title: In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. II. Probing drug/food interactions using microcalorimetry
DOI: 10.1016/0378-5173(89)90008-2
UCL classification: UCL > Provost and Vice Provost Offices
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy > Pharmaceutics
URI: http://discovery.ucl.ac.uk/id/eprint/1390349
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