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PubMed · 10677806

Development of matrix-based theophylline sustained-release microtablets.

Abstract

Microtablets containing high theophylline content (from 60% to 80%) based on a Eudragit RS PO matrix were produced on a rotary tablet press. The influence of the compaction pressure, the plasticizer content used for the granulation of theophylline particles, and the amount of theophylline on the drug release were investigated. The effects of surface area and the addition of magnesium stearate as a hydrophobic agent on the drug release were studied. The storage stabilities of the release rate at room temperature and at 50 degrees C were also determined. Dissolution profiles expressed as percentage of theophylline dissolved were obtained over 8 hr in 900 ml of purified water at 37 degrees C and 75 rpm. It was observed that the compaction pressure (from 200 MPa to 250 MPa) had no effect on the theophylline release. The use of triethyl citrate (TEC) as a plasticizer in the granulation of theophylline enhanced the physical properties of the microtablets. Theophylline content in the range 60% to 80% did not affect the drug release. The theophylline release obtained was a function of the quotient surface area/tablet weight and therefore was dependent on the tablet diameter. To reduce the dissolution rates, magnesium stearate was added in a concentration up to 50% of the matrix material. Tablets of this hydrophobic formulation fulfilled the requirements of USP 23 for theophylline sustained-release preparations. Storage at room temperature for 3 months and at 50 degrees C for 2 months showed no significant influence on the theophylline release.

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BibTeXRIS

H Rey, K G Wagner, P Wehrlé, P C Schmidt. 2000. Development of matrix-based theophylline sustained-release microtablets.. https://doi.org/10.1081/ddc-100100323

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