초록 ▼

The present invention is directed to an active agent dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of a liquid, active agent formulation to a fluid environment of use. The liquid, active agent formulation is sorbed into porous particles that are disp

The present invention is directed to an active agent dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of a liquid, active agent formulation to a fluid environment of use. The liquid, active agent formulation is sorbed into porous particles that are dispersed in a polymer matrix that swells upon contact with the fluids of the stomach. A portion of the polymer matrix may be surrounded by a band of insoluble material that prevents the covered portion of the polymer matrix from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.

대표청구항 ▼

1. A dosage form comprising: a bioerodible carrier formulated to facilitate retention of the dosage form within a stomach of a subject and erode over a prolonged period of time as the dosage form is retained in the stomach; and a plurality of porous particles having a liquid active agent formula

1. A dosage form comprising: a bioerodible carrier formulated to facilitate retention of the dosage form within a stomach of a subject and erode over a prolonged period of time as the dosage form is retained in the stomach; and a plurality of porous particles having a liquid active agent formulation absorbed therein, wherein said plurality of porous particles is dispersed within said bioerodible carrier, the porosity of said plurality porous particles is such that liquid active agent formulation comprises at least about 5% and up to about 70% of die weight of the plurality of porous particles said plurality of porous particles is adapted to resist compaction forces sufficient to form a compacted drug layer without significant exudation of the liquid active agent formulation, the dosage form is formulated such that porous particles included in said plurality of porous particles are released from the dosage form as said bioerodible carrier erodes in the stomach; and said liquid active agent formulation is formulated such that 70% or more of an active agent included in said liquid active agent formulation is released from said plurality of porous particles within about 20 minutes from introduction of said porous particles into a fluid environment of use. 2. The dosage form of claim 1, wherein the bioerodible carrier comprises a polymer matrix. 3. The dosage form of claim 1, wherein the plurality of porous particles comprises a calcium hydrogen phosphate represented by the formula CaHPO4.mH2O, wherein m satisfies the relationship 0≤m≤2.0. 4. The dosage form of claim 1, wherein the plurality of porous particles comprises a magnesium aluminonietasilicate represented by the formula AL2O3MgO.2SiO2.nH2O, wherein n satisfies the relationship 0≤n≤10. 5. The dosage form of claim 1, wherein said active agent comprises a compound that is absorbed more readily in a portion of the upper gastrointestinal tract of the subject than in any portion of the lower gastrointestinal tract of the subject. 6. The dosage form of claim 1,wherein the plurality porous particles comprises a substantially amorphous material. 7. The dosage form of claim 6, wherein the porosity of said plurality of porous particles is such that the liquid active agent formulation comprises from about 60% to about 70% of the weight of the plurality of porous particles. 8. The dosage form of claim 1, wherein the plurality of porous particles comprises a substantially crystalline material. 9. The dosage form of claim 8, wherein the porosity of said plurality of particles that the liquid active agent formulation comprises from about 30% to of the weight of the plurality of porous particles.