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A linezolid tablet and linezolid technology are applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, and pill delivery, etc. , poor compressibility, etc.
Active Publication Date: 2014-07-02
CHENGDU GUOHONG PHARMA
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[0008] In view of the poor compressibility of linezolid crystalline form III and the high dose of the main drug in a single tablet of linezolid, the amount of excipients that can be added to each linezolid tablet is extremely limited, and the prior art does not provide any extremely limited excipients. The added amount makes the tablet formulation of linez
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Embodiment 1
[0073] Prescription Prescription amount % by weight
[0074] Linezolid Form III 300.0mg 75.00%
[0075] Lactose 19.2mg 4.80%
[0076] Microcrystalline Cellulose 36.0mg 9.00%
[0077] Crospovidone 33.6mg 8.40%
[0078] Hypromellose 10.0mg 2.50%
[0079]Magnesium Stearate 1.2mg 0.30%
[0080] Total 400.0mg.
Embodiment 2
[0082] Prescription Prescription amount % by weight
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Abstract
The invention relates to a tablet containing a linezolid crystal form III. The tablet contains 67.0-75.0wt% of linezolid, 2.0-4.8wt% of lactose, 9.0-18.0wt% of microcrystalline cellulose as well as disintegrating agent, binding agent, lubricant and other medicinal excipients, wherein preferably, the tablet contains 67.0-75.0wt% of linezolid, 2.0-4.8wt% of lactose, 9.0-18.0wt% of microcrystalline cellulose, 2.0-10.0wt% of disintegrating agent, 1.2-4.0wt% of binding agent and 0.3-2.0wt% of lubricant. The tablet containing the linezolid crystal form III of the prescription, in an extremely limited additive adding range, guarantees characteristics of good compressibility, excellent formability and rapid dissolution.
Description
technical field [0001] The invention relates to pharmaceutical preparations, in particular to a tablet containing linezolid crystal form III. Background technique [0002] Linezolid (LINEZOLID, (S)-N-{[3-(3-fluoro4-(4-morpholinyl)benzene)2-oxo-5azoline]methyl}-acetamide) also known as Linezolid Ketone, morpholinozolidone, is a new synthetic oxazolidinone antibiotic that acts on the 50S ribosomal subunit of bacteria and is closest to the site of action. Unlike other drugs, linezolid does not affect the activity of peptidyl transferase, but only acts on the initial stage of the translation system, inhibits the connection between mRNA and ribosomes, prevents the formation of the 70S initiation complex, and thus inhibits bacterial protein synthesis. [0003] Linezolid was researched and developed by Pharmacia & Upjohn Company of the United States, and was approved by the FDA in 2000 for the treatment of Gram-positive (G + ) cocci, including suspected or confirmed hospital-acqu...
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