Low-substituted hydroxypropylcellulose as a sustained-drug release matrix base or disintegrant depending on its particle size and loading in formulation.
Tablets of acetaminophen as a model drug were prepared with low-substituted hydroxypropylcellulose (L-HPC) of various particle sizes at various loadings in the formulation. Drug release into an aqueous dissolution medium (pH 1.2) was remarkably sustained from tablets prepared with fine L-HPC (LH41) at loadings of more than 20%. Tablets prepared with less than 20% LH41 or with coarse L-HPCs (LH11, LH21, and LH31) disintegrated in the medium, resulting in rapid release of the drug. The difference in behavior could not be explained in terms of differences in tablet strength, but in swelling and water uptake abilities of the tablet's polymer. Swelling work (swelling force), water penetration speed, and water uptake of LH41 (4.4-microns average particle size) were much smaller than those of coarse L-HPCs. The formation of a continuous gel-like layer on the surface of tablets containing more than 20% LH41 was another factor to sustain the drug release rate.
Kawashima
Y
Y
Gifu Pharmaceutical University, Japan.
Takeuchi
H
H
Hino
T
T
Niwa
T
T
Lin
T L
TL
Sekigawa
F
F
Kawahara
K
K
D000082:Acetaminophen / Q000008:administration & dosage; D002482:Cellulose / Q000031:analogs & derivatives*; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D005079:Excipients; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D012995:Solubility; D013607:Tablets; D013718:Tensile Strength
D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D000082:Acetaminophen; D002482:Cellulose; C008079:hydroxypropylcellulose