| 摘要 |
Microcapsules (I) of average diameter less than 1000 Microm, for modified release of orally administered, sparingly soluble active agent(s) (A) (other than hypoglycemic agents). Microcapsules (I) of average diameter less than 1000 (preferably 50-800, especially 100-600) Microm, for modified release of orally administered, sparingly soluble active agent(s) (A) (other than hypoglycemic agents), comprise a core (II) containing (A) and a release prolonging coating (III) containing film-forming polymer(s) (P1) insoluble in gastrointestinal liquids, water-soluble polymer(s) (P2), plasticizer(s) (PL) and, optionally, lubricating surfactant(s). Coating (III) forms at least 3% (preferably at least 5%) of (I); (III) contains 40-90 (preferably 50-80)% (P1); the (P2)/((P1) + (P2)) ratio is 15-60 (preferably 15-55)%; and the (PL)/((P1) + (PL)) ratio is 1-30 (preferably 5-25)% (all based on dry weight). Coating (III) is other than an enteric coating or a coating of the following specific composition (percentages being based on the overall dry weight of (III)): (1) 50-90% (P1) comprising ethyl cellulose and/or cellulose acetate; (2) 2-25% (P2) comprising polyacrylamide and/or polyvinyl pyrrolidone; (3) 2-20% (PL) selected from glycerol esters, phthalates, citrates, sebacates, cetyl alcohol esters, castor oil, salicylic acid and/or cutin; and (4) 2-20% (SA) selected from alkali(ne earth metal) salts of fatty acids, polyoxyethylene sorbitan esters, polyoxyethylene hydrogenated castor oil, and/or lubricants (such as stearates, stearylfumates or glycerol behenate) or their mixtures. An independent claim is also included for medicaments containing (I), specifically in solid form (especially as tablets, capsules or powder) or liquid form (especially as aqueous suspension). |
