Tablet containing linezolid crystal form III

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...

AI Technical Summary

Problems solved by technology

[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 linezolid crystalline form III have good compressibility and rapid dissolution characteristics at the same time, so a tablet formulation suitable for linezolid crystalline form Ⅲ is developed, which makes it have good compressibility, Good formability, and the dissolution rate can reach more than 85% in 15 minutes, so it is very necessary to take effect quickly