The use of micronized cellulose disintegrants as insoluble swellable matrices for sustained-release tablets.
Five cellulose disintegrants--low-substituted hydroxypropylcellulose (L-HPC), microcrystalline cellulose (MCC), carboxymethylcellulose (CMC), cross-linked NaCMC (C.L.NaCMC), and CaCMC-were evaluated as directly compressed matrices for sustained-release (SR) tablets in vitro, using procainamide hydrochloride as a model drug. Coarser particles (14-19 microns) of the jet mill ground disintegrants, as well as intact disintegrants, provided rapidly disintegrating tablets with fast drug release but finer particles (2.5-3.5 microns) provided matrix-type SR tablets. The SR tablets based on non-ionic polymers (L-HPC and MCC) did not disintegrate at any pH; those based on anionic polymers (C.L.NaCMC and CaCMC) did not disintegrate at pH 1.2, but they disintegrated gradually from the exterior in water and in a pH 6.8 medium. We conclude that the particle size and concentration of the cellulose disintegrants are determinant factors in the formulation of SR matrices.
Pharmaceutical Formulation Research Center, Daiichi Pharmaceutical Co. Ltd., Tokyo, Japan.
H
H
Nakagami
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M
Nada
D002130:Calcium Phosphates / Q000737:chemistry; D002482:Cellulose / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients; D006863:Hydrogen-Ion Concentration; D010316:Particle Size; D011342:Procainamide / Q000008:administration & dosage / Q000737:chemistry; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D014867:Water / Q000032:analysis
D002130:Calcium Phosphates; D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D014867:Water; D002482:Cellulose; D011342:Procainamide