US 12,115,259 B2
Spherical beads for use in producing pharmaceutically active pellets
Tobias Heß, Niedernhausen (DE); André Huhn, Bischofsheim an der Rhön (DE); Christian Koch, Heidesheim (DE); Markos Papaioannou, Saulheim (DE); and Daniel Zakowiecki, Budenheim (DE)
Assigned to Chemische Fabrik Budenheim KG, Budenheim (DE)
Appl. No. 17/281,442
Filed by Chemische Fabrik Budenheim KG, Budenheim (DE)
PCT Filed Sep. 27, 2019, PCT No. PCT/EP2019/076135
§ 371(c)(1), (2) Date Mar. 30, 2021,
PCT Pub. No. WO2020/069987, PCT Pub. Date Apr. 9, 2020.
Claims priority of application No. 18198640 (EP), filed on Oct. 4, 2018.
Prior Publication US 2022/0000784 A1, Jan. 6, 2022
Int. Cl. A61K 9/16 (2006.01)
CPC A61K 9/1676 (2013.01) [A61K 9/1611 (2013.01); A61K 9/1682 (2013.01)] 12 Claims
 
1. Spherical beads for use in producing pharmaceutically active pellets prepared by depositing a pharmaceutically active agent on the surface of said spherical beads, wherein the spherical beads consist of a pharmaceutically acceptable carrier material, said carrier material consisting of a mixture of:
a) at least 60 wt. % of a phosphoric acid calcium salt, wherein the phosphoric acid calcium salt is dibasic calcium phosphate; and
b) at least 20 wt. % and up to 40 wt. % of an organic material, wherein the organic material is selected from the group consisting of microcrystalline cellulose, cellulose and its derivatives and mixtures thereof,
wherein ≥90 wt. % of the spherical beads have a particle size in the range of from 90 μm to 1200 μm, and wherein the spherical beads have:
a bulk density of at least 1000 g/l,
a specific surface area of at most 10 m2/g, and
a hardness of at least 600 g/mm2, and
wherein the spherical beads do not disintegrate when placed in water at a temperature of 25±1° C. for 24 hours.