Development and Evaluation of oral multiple-unit and single-unit hydrophilic controlled-release systems |
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Authors: | Manuel Efentakis Antonios Koutlis Marilena Vlachou |
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Institution: | (1) School of Pharmacy, Department of Pharmaceutical Technology, University of Athens, Panepistimiopolis, Zografou, 157 71 Athens, Greece |
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Abstract: | This study compared the release behavior of single-unit (tablets, capsules) and multiple-unit (minitablets in capsules) controlled-release
systems of furosemide. The swelling and erosion behaviors of these systems, which contained the swellable hydrophilic polymers
sodium alginate (high viscosity) and Carbopol 974P, were compared. Swelling and erosion experiments showed a high degree of
swelling and limited erosion for the Carbopol preparations, whereas less swelling but greater erosion was observed for the
sodium alginate preparations. The sodium alginate preparations were eroded in 6 hours, while Carbopol preparations exhibited
limited erosion within this period of time. These results appear to be attributed to the physicochemical characteristics of
the polymers used in this study. Polymer characteristics greatly influenced the release of furosemide (model drug) from the
formulations prepared and tested. Sodium alginate had a less pronounced sustained release effect compared with Carbopol (ie,
in 8 hours all 3 sodium alginate dosage forms displayed complete release of furosemide, while only 30% of the drug was released
from Carbopol dosage forms). Finally, all 3 Carbopol dosage forms (single- and multiple-unit) displayed similar release behavior
while sodium alginate dosage forms displayed a different and more distinctive behavior. Minitablets and tablets showed a greater
sustained release effect compared with capsules. Evaluation of the release data indicates that the release mechanism for sodium
alginate formulations may be attributed to erosion/dissolution, while for Carbopol it may be attributed mainly to polymer
relaxation and diffusion of the drug from the polymer surface. |
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Keywords: | Single-unit Multiple-unit Minitablets Controlled release Carbopol Sodium alginate Furosemide |
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