Solid pharmaceutical formulations for slow, zero order release via controlled surface erosion: expanded range

摘要

A new class of solid pharmaceutical formulations enables the attainment of slow, zero order in vivo release of a wide range of pharmaceutically active ingredients upon oral administration. A broad range of release rates can be preselected by suitable adjustments of tablet properties. The formulations are based upon control of active ingredient release from the surface of the tablet via a controlled surface erosion mechanism. These compositions comprise: (a) an effective amount in the range of 10-90 wt. % of a pharmacologically active compound having a water solubility (20 DEG C.) of 1/5-1/1000 (w/w); (b) 1-40 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20 DEG C.) of 1/1-1/40 (w/w); (c) 2-20 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20 DEG C.) of 1/1-1/10 (w/w); (d) an amount in the range of 0.05-1.0 wt. % of a disintegrating agent for pharmaceutical compositions, at which amount the compound is ineffective as a disintegrating agent; (e) 0.1-2.0 wt. % of a surfactant which is pharmaceutically acceptable in oral compositions; and, as necessary for tablet manufacturing purposes; (f) 1-20 wt. % of a binder which is pharmaceutically acceptable in oral compositions; or (g) 0.5-5.0 wt. % of a die wall lubricant which is pharmaceutically acceptable in oral compositions.