Composition containing levamlodipine besylate hydrate and its preparation method
AssigneesShihuida Pharmaceuticals Group (Jilin) Ltd, Beijing Wuwei Erchuang Technology Co., Ltd.
InventorsHuan Li, Fuqing Yao, Xitian Zhang
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Abstract
The present invention relates to a composition comprising levamlodipine besylate hydrate and its production, pharmaceutical preparations and use, especially the composition of (S)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylic acid-3-ethyl ester, 5-methyl ester benzenesulfonic acid hydrate and its production method and use. The composition of levamlodipine besylate crystallized in pure water and dried is easy for industrial production, has no organic solvent residue, good thermal stability and good dissolution amount in solid-form preparations.
Claims7
A fast-sustained-release tablet formulation comprising a sustained-release layer and a fast-release layer, each of which comprises levamlodipine besylate hydrate compounds having different crystalline water content, wherein the levamlodipine besylate hydrate has a molecular formula of C20H25CIN2O5·C6H6O3S·nH2O, wherein 1<n<2, and has the following structural formula:
- wherein the levamlodipine besylate hydrate comprises 4.5%-5.8% of crystalline water,
- wherein the sustained-release layer comprises levamlodipine, polyvinylpyrrolidone, hydroxypropyl cellulose, microcrystalline cellulose, and magnesium stearate in a mass ratio of 4-5:30-40:55-65:17-30:0.1-1, and
- wherein the fast-release layer comprises levamlodipine, microcrystalline cellulose, pregelatinized starch, cross-linked polyvinylpyrrolidone, polyvinylpyrrolidone, and magnesium stearate in a mass ratio of 1-2:40-45:35-45:1-8:5-15:0.1-1.
A fast-sustained-release combination tablet comprising a sustained-release combination layer and a fast-release combination layer, each of which comprises levamlodipine besylate hydrate compounds having different crystalline water content, wherein the levamlodipine besylate hydrate has a molecular formula of C20H25CIN2O5·C6H6O3S·nH2O, wherein 1<n<2, and has the following structural formula:
- wherein the levamlodipine besylate hydrate comprises 4.5%-5.8% of crystalline water,
- wherein the sustained-release combination layer comprises levamlodipine, polyvinylpyrrolidone, hydroxypropyl cellulose, microcrystalline cellulose, and magnesium stearate in a mass ratio of 4-5:30-40:55-65:17-30:0.1-1, and
- wherein the fast-release combination layer comprises levamlodipine, folic acid, microcrystalline cellulose, pregelatinized starch, cross-linked polyvinylpyrrolidone, polyvinylpyrrolidone, and magnesium stearate in a mass ratio of 1-2:0.1-1:40-45:35-45:1-8:5-15:0.1-1.
A composition comprising levamlodipine besylate hydrate compounds having different crystalline water content,
- wherein the levamlodipine besylate hydrate has a molecular formula of C20H25CIN2O5·C6H6O3S·nH2O, wherein n is within the range of 1.83 to 1.94, and has the following structural formula:
- and wherein the levamlodipine besylate hydrate comprises 4.5%-5.8% of crystalline water.
Dependencies are inferred from the claim text.