US 12,226,530 B2
Lenalidomide gastro-retentive sustained-release tablet and preparation method thereof
Feng Liu, Guangdong (CN); Huafeng Luo, Guangdong (CN); Jingyu He, Guangdong (CN); Xiaofeng Tan, Guangdong (CN); and Shuting Lai, Guangdong (CN)
Assigned to DIQI PHARMACEUTICALS CO., LTD., Guangdong (CN)
Appl. No. 17/041,635
Filed by DiQi Pharmaceuticals Co., Ltd., Guangdong (CN)
PCT Filed Sep. 29, 2018, PCT No. PCT/CN2018/108771
§ 371(c)(1), (2) Date Sep. 25, 2020,
PCT Pub. No. WO2019/218576, PCT Pub. Date Nov. 21, 2019.
Claims priority of application No. 201810471714.9 (CN), filed on May 17, 2018.
Prior Publication US 2021/0128476 A1, May 6, 2021
Int. Cl. A61K 9/20 (2006.01); A61K 9/00 (2006.01); A61K 31/454 (2006.01)
CPC A61K 9/2054 (2013.01) [A61K 9/0065 (2013.01); A61K 9/2095 (2013.01); A61K 31/454 (2013.01)] 10 Claims
 
1. A lenalidomide gastro-retentive sustained-release tablet, wherein the sustained-release tablet consists of 3 wt % to 14 wt % of crystalline lenalidomide, 14 wt % to 68 wt % of release enhancer with low bulk density, 23 wt % to 70 wt % of sustained-release material with low bulk density, and the balance of other pharmaceutically acceptable excipients, wherein the bulk density of the release enhancer ranges from 0.24 g/cm3 to 0.52 g/cm3; and the bulk density of the sustained release material ranges from 0.29 g/cm3 to 0.51 g/cm3,
wherein the release enhancer is one or more selected from the group consisting of crospovidone, microcrystalline cellulose and croscarmellose sodium,
wherein the sustained-release material is one or more selected from the group consisting of hydroxypropyl methylcellulose, polyethylene oxide, hydroxypropyl cellulose, hydroxyethyl cellulose and sodium carboxymethylcellulose,
wherein the other pharmaceutically acceptable excipients comprise a lubricant and a glidant, the lubricant including one or more selected from the group consisting of magnesium stearate, sodium stearyl fumarate and talcum, and the glidant including one or more selected from the group consisting of silicon dioxide and talcum,
wherein the hardness of the lenalidomide gastro-retentive sustained-release tablet ranges from 3 kg/cm2 to 10 kg/cm2,
wherein a density of the lenalidomide gastro-retentive sustained-release tablet ranges from 0.755 g/cm3 to 0.991 g/cm3, and
wherein the lenalidomide gastro-retentive sustained-release tablet does not contain floating assistants and alkaline foaming agents, the floating assistants being octadecanol, stearic acid, glyceryl monostearate, glyceryl behenate, carnauba wax, white wax and hydrogenated vegetable oil, the alkaline foaming agents being alkaline carbonate and bicarbonate.