Linezolid tablets in stable crystal form and preparation method thereof

Abstract

The invention discloses linezolid tablets in a stable crystal form and a preparation method thereof. The linezolid tablets contain low-melting-point wax materials such as polyethylene glycol, poloxamer, higher aliphatic alcohol and higher aliphatic acid; and the low melting point wax materials are melted and then mixed with the crystal form IV of linezolid to prepare the tablets, so that the crystal form IV in the linezolid tablets can be prevented from being transformed into the crystal form II. Experiments prove that the linezolid tablets are stable in crystal form and high in dissolution and do not crack, and the friability of the linezolid tablets meets the pharmacopoeia requirement.

Description

Technical field: [0001] The invention relates to a linezolid tablet with stable crystal form and a preparation method thereof. Background technique: [0002] Linezolid is a polymorphic compound, including crystal form I, crystal form II, crystal form III and crystal form IV. [0003] Two problems are prone to occur during the preparation of linezolid tablets containing crystal form IV: [0004] 1. Linezolid crystal form IV is easy to transform into linezolid crystal form II, especially when it comes into contact with solvents such as ethanol, isopropanol or water, resulting in unstable tablet crystal form. The different crystal forms of the drug will affect the bioavailability, safety or stability of the drug. [0005] 2. Linezolid crystal form IV has poor compressibility during the preparation of tablets, high rate of splitting, and friability difficult to meet the requirements of the Chinese Pharmacopoeia (2010 edition). This is due to the irregular flakes of this type of crystals...

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a formulation of linezolid tablets with stable crystal form, which solves the problem that the crystal form of linezolid is unstable, that is, the crystal form IV of linezolid is easily transformed into form II of linezolid, and at the same time solves the problem of linezolid crystal form IV Problems with the shards of Zolamide tablets

[0013] The inventors found that adding a low melting point waxy material to the formulation of linezolid tablets, and controlling the addition ratio and adding method of the low melting point waxy material can solve the problem of unstable crystal form and splitting of linezolid tablets

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