Granular material for dosage forms
View Patent ↗A granular material which has a mean particle diameter of 150 to 800 micrometers; and an unsettled bulk density of 0.1 to 0.35 g/cm3 and/or a compactibility which results in a compact with a tensile strength of at least 1.7 MPa when the granular material is subjected to a compaction pressure of 266 MPa; and wherein the main component of the granular material is a cellulose derivative or an alkylene oxide homo- or copolymer or a blend thereof is useful for preparing dosage forms with a controlled release profile.
1. A granular material having a mean particle diameter of 250 to 350 micrometers and a compactibility resulting in a compact with a tensile strength of at least 1.7 MPa when the granular material is subjected to a compaction pressure of 266 MPa, at least 80 percent of the granular material being a water-soluble cellulose ether, water-soluble cellulose ester, an alkylene oxide homo- or copolymer or a blend thereof, wherein the granular material has been obtained by subjecting the water-soluble cellulose ether, water-soluble cellulose ester, alkylene oxide homo- or copolymer or blend thereof in powder form to a granulation step.
2. The granular material of claim 1 having an unsettled bulk density of 0.1 to 0.35 g/cm 3 .
3. The granular material of claim 1 having a particle size distribution span of 0.75 to 4.
4. The granular material of claim 3 having a particle size distribution span of 1 to 2.
5. The granular material of claim 1 having an average aspect ratio of 1 to 2.
6. The granular material of claim 1 having a compactibility which results in a compact with a tensile strength of 2 to 4 MPa when the granular material is subjected to a compaction pressure of 266 MPa.
7. The granular material of claim 1 having an unsettled bulk density of 0.15 to 0.25 g/cm 3 .
8. The granular material of claim 1 being an excipient for a dosage form.
9. The granular material of claim 8 being an excipient for a sustained-release dosage form.
10. The granular material of claim 1 wherein the water-soluble cellulose ether is a hydroxypropyl methyl cellulose having a hydroxypropoxyl substitution of 4 to 12 percent and a methoxyl substitution of 19 to 30 percent.
11. A direct compression process for preparing a dosage form comprising the step of
a.) blending an active ingredient, the granular material of claim 1 and one or more optional adjuvants in the absence of a substantial amount of added solvent or heat, and
b.) compressing the resulting composition to a dosage form.
12. A process for granulating a polymer powder comprising the step of granulating in a fluid bed granulator a water-soluble cellulose ether, water-soluble cellulose ester, an alkylene oxide homo- or copolymer or a blend thereof to produce the granular material of claim 1 .
13. A granular material having a mean particle diameter of 250 to 350 micrometers, a particle size distribution span of 1 to 2 and a compactibility resulting in a compact with a tensile strength of at least 1.7 MPa when the granular material is subjected to a compaction pressure of 266 MPa, at least 90 percent of the granular material being a hydroxypropyl methyl cellulose having a hydroxypropoxyl substitution of 4 to 12 percent and a methoxyl substitution of 19 to 30 percent, wherein the granular material has been obtained by subjecting the hydroxypropyl methyl cellulose in powder form to a granulation step.