| 摘要 |
Coated microparticle capsules comprise at least an active principle (AP) covered by at least two distinct film coatings and have an average diameter of lower than 2000 microns, preferably 100-600 microns. The film coatings, in combination, are able: to release AP by two different trigger mechanisms, one based on a variation of pH and the other allows the AP release at the end of a predetermined residential time in the stomach; and to induce an in vitro dissolution behavior. Coated microparticle capsules comprise at least an active principle (AP) covered by at least two distinct film coatings and have an average diameter of lower than 2000 microns, preferably 100-600 microns. The film coatings, in combination, are able: to release AP by two different trigger mechanisms, one based on a variation of pH and the other allows the AP release at the end of a predetermined residential time in the stomach; and to induce an in vitro dissolution behavior (determined as indicated in the dissolutest in European Pharmacopeia 5.2 or type II apparatus in the US Pharmacopeia 28-NF23 maintained at 37[deg]C and agitated at 100 rpm). The in vitro dissolution behavior of the microcapsules is such that, at a constant pH of 1.4, a latency phase =8 hours, preferably 1-5 hours is observed and the change from pH 1.4 to pH 7.1, results in a prolonged release phase of the AP that starts without a latency period such as the t1/2 i.e. duration necessary to release 50% of PA contained in the coated microparticles, being 0.25-20 hours, preferably 0.25-4 hours. Independent claims are included for: (1) microparticles coated with (A) and (T); and (2) a pharmaceutical, veterinary or dietetic formulation, comprising numerous coated microparticles, preferably 5000-500000 microparticles. |
