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In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. I. Exploration of alternative methodology: microcalorimetry

(1989) In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. I. Exploration of alternative methodology: microcalorimetry. International Journal of Pharmaceutics , 51 (3) pp. 245-251. 10.1016/0378-5173(89)90198-1.

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Abstract

The possibility of using a microcalorimeter as an analytical method to monitor dissolution in complex media (to simulate fed and fasted patients) has been explored. The dissolution of Phyllocontin continus tablets (controlled release aminophylline, 225 mg) has been studied by conventional USP methodology under the following conditions: (i) buffer at pH 2.5; (ii) buffer at pH 2.5 followed by pH 5.6; (iii) halved tablet at pH 5.6; (iv) halved tablet in Ensure/buffer mixture at pH 5.6. The results showed dissolution to be independent of pH and almost independent of tablet integrity. The use of Ensure to simulate a fed patient produced a change in the first stage of the tablet dissolution kinetics. A microcalorimeter was used to monitor tablet dissolution with studies being undertaken on placebo and active tablets. Dissolution in buffer, buffer/Ensure, and buffer/Intralipid mixtures was studied. Where it was possible to effect comparisons it was clear that changes observed in the USP method were similar to those seen by microcalorimetry, the microcalorimetric results showing that Ensure altered the first, but not the second stage of dissolution kinetics, and that Intralipid altered the second but not the first stage. A major media-induced difference observed by microcalorimetry, was the timing of the change between the two processes. A tentative explanation of these results has been proposed. Microcalorimetry seems to be a useful tool by which dissolution into complex media (which due to the presence of factors such as colour and suspended matter cannot be used with conventional analysis techniques without labour intensive separation/dialysis techniques) can be monitored. The results provide an indication of mechanism of release/interaction. This could be a useful aid to formulators and could provide a convenient in vitro initial indicator of the effects of food on drug release, without recourse to expensive animal experiments. © 1989.

Type: Article
Title: In vitro dissolution testing of oral controlled release preparations in the presence of artificial foodstuffs. I. Exploration of alternative methodology: microcalorimetry
DOI: 10.1016/0378-5173(89)90198-1
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/1512303
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