Pharmaceutical formulations of acid labile substances for oral use
AssigneeAktiebolaget Hassle
InventorsKurt I. Lovgren, Ake G. Pilbrant, Mitsuru Yasumura, Satoshi Morigaki, Minoru Oda, Naohiro Ohishi
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Abstract
Pharmaceutical preparation containing an acid labile compound together with an alkaline reacting compound or an alkaline salt of an acid labile compound optionally together with an alkaline compound as the core material, one or more subcoating layers comprising inert reacting compounds which are soluble or rapidly disintegrating in water, or polymeric, water soluble filmforming compounds, optionally containing pH-buffering alkaline compounds and an enteric coating as well as a process for the preparation thereof and the use in the treatment of gastrointestinal diseases.
Claims15
A pharmaceutical preparation comprising:
- (a) an alkaline reacting core comprising an acid-labile pharmaceutically active substance and an alkaline reacting compound different from said active substance, an alkaline salt of an acid labile pharmaceutically active substance, or an alkaline salt of an acid labile pharmaceutically active substance and an alkaline reacting compound different from said active substance;
- (b) an inert subcoating which rapidly dissolves or disintegrates in water disposed on said core region, said subcoating comprising one or more layers comprising materials selected from the group consisting of tablet excipients, film-forming compounds and alkaline compounds;
- and
- (c) an enteric coating layer surrounding said subcoating layer, wherein the subcoating layer isolates the alkaline reacting core from the enteric coating layer such that the stability of the preparation is enhanced.
A preparation according to dlaim 1 wherein the subcoating layer comprises one or more of magnesium oxide, magnesium hydroxide or composite substance [Al.sub.2 O.sub.3.6MgO.CO.sub.2.12H.sub.2 O or MgO.Al.sub.2 O.sub.3.2SiO.sub.2.nH.sub.2 O], wherein n is not an integer and less than two.
Process for the preparation of an oral pharmaceutical formulation containing an acid labile compound in which cores containing the acid labile compound mixed with an alkaline reacting compound or compounds or an alkaline salt of the acid labile compound optionally mixed with an alkaline reacting compound or compounds are coated with one or more inert reacting subcoating layers whereafter the subcoated cores are further coated with an enteric coating layer.
Dependencies are inferred from the claim text.