| Autor: |
Donald L. Heald, I.R. Wilding, Robert A. Sparrow, Stanley S. Davis, John Ziemniak |
| Rok vydání: |
1995 |
| Předmět: |
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| Zdroj: |
Journal of Controlled Release. 33:89-97 |
| ISSN: |
0168-3659 |
| DOI: |
10.1016/0168-3659(94)00066-4 |
| Popis: |
The gastrointestinal transit and in vivo release behaviour of a modified release (Geomatrix®) diltiazem formulation has been evaluated by the combined technique of gamma scintigraphy and pharmacokinetic assessment (pharmacoscintigraphy) in eight healthy male subjects under fasting and fed conditions. The dosage form consisted of four mini-tablets, composed of both hydrophilic (core) and hydrophobic (caps) polymers designed to release diltiazem as a function of swelling. Preparation of the tablets for the pharmacoscintigraphic evaluation was by neutron activation, which enabled routine manufacture of a complex delivery system. The tablet cores were labelled with samarium-153 and the caps with erbium-171. The individual tablets swelled in vivo and traversed the gastrointestinal tract as discrete and separate modified release units. In the fasted state, the tablets remained intact for an average of 17 h and the pharmacokinetic data demonstrated that diltiazem is readily absorbed from the colon. Administration of the formulation after a high fat breakfast slightly increased the overall extent of absorption but did not compromise the controlled release characteristics of the system. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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