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• W2023981646 abstract "The release control of theophylline from tablets was conducted by hybridizing its hydrophilic, hydrophobic and ionizable cyclodextrin (CyD) complexes, i.e. those with the parent β-CyD, heptakis(2,6-di-O-ethyl)-β-CyD (DE-β-CyD) and carboxymethyl-ethyl-β-CyD (CME-β-CyD), respectively. The rate of release of theophylline from tablets was accelerated by β-CyD, while that from the DE-β-CyD complex was decelerated, both showing pH-independent release. On the other hand, the CME-β-CyD complex showed pH-dependent release, i.e. the rate increased with increase in pH of the medium. The drug release from tablets could be arbitrarily modified by mixing two complexes: a mixture of the DE-β-CyD and CME-β-CyD complexes in a 1:3 molar ratio released the drug above 90% within ca. 8 h in an apparent zero-order fashion. Double-layer tablets consisting of the parent β-CyD complex as a fast-releasing fraction and the mixture of the DE-β-CyD and CME-β-CyD complexes as a slow-releasing fraction released the drug rapidly at the initial stage (within ca. 30 min), followed by slow release. Among various combinations, a double-layer tablet consisting of β-CyD-(DE-β-CyD: CME-β-CyD, 1 : 3) = 1 : 3 was the most suitable to offer a more balanced bioavailability. This formulation gave an initial rapid increase in plasma level of theophylline, followed by a longer maintenance of the relatively constant level, after oral administration to dogs. The mean residence time (MRT) in the systemic circulation increased about 1.5 times for the double-layer tablet compared with the plain tablet of drug alone. The Nimmerfall absolute retarding parameter (Ri,abs = 83.1%) for the double-layer tablet was higher than the lower limit (75%) for discrimination of a retarding effect. In addition, no appreciable decrease in bioavailability was observed for the double-layer tablet. The results suggest that the release of theophylline from tablets can be arbitrarily modified by hybridizing hydrophilic, hydrophobic and ionizable CyD derivatives in appropriate ratios." @default.
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• W2023981646 date "1991-04-01" @default.
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• W2023981646 title "Release control of theophylline by β-cyclodextrin derivatives: hybridizing effect of hydrophilic, hydrophobic and ionizable β-cyclodextrin complexes" @default.
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• W2023981646 doi "https://doi.org/10.1016/0168-3659(91)90075-o" @default.
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