Linezolid tablets in stable crystal form and preparation method thereof

A technology of linezolid tablets and linezolid, which is applied in the field of linezolid tablets and its preparation, can solve problems such as cracks, unstable crystal form of linezolid tablets, unstable crystal form of linezolid, etc., and achieve dissolution rate Good, good compressibility effect

Active Publication Date: 2013-01-23
CHONGQING HUAPONT PHARMA
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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 crysta

Method used

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  • Linezolid tablets in stable crystal form and preparation method thereof
  • Linezolid tablets in stable crystal form and preparation method thereof
  • Linezolid tablets in stable crystal form and preparation method thereof

Examples

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Example Embodiment

[0036] Example 1 Preparation of linezolid tablets (adding auxiliary materials after granulation)

[0037] Take 300g of linezolid crystal form IV, add 18g of the melted solution of polyoxy(40) stearate, mix uniformly to prepare granules, the prepared granules are added with 284g of microcrystalline cellulose, 174g of dextrin, 80g of low-substituted carboxylate Propyl cellulose and 4 g of magnesium stearate are mixed uniformly and compressed to obtain 1000 linezolid tablets.

[0038] The preparation methods of Examples 2 to 8 are the same as in Example 1, and the types and amounts of raw materials used are shown in Table 1. 1000 linezolid tablets were prepared respectively.

Example Embodiment

[0039] Example 9 Preparation of linezolid tablets (adding auxiliary materials before granulation)

[0040] Take 700g of linezolid crystalline form IV, mix it with 92g starch and 24g microcrystalline cellulose, add 72g polyethylene glycol 6000 melt, mix to make granules, the prepared granules add 18g talc powder and 4g stearic acid Magnesium was mixed well and compressed to obtain 1000 linezolid tablets.

Example Embodiment

[0041] Example 10 Preparation of linezolid tablets (adding auxiliary materials before granulation)

[0042] Take 340g of linezolid crystal form IV, mix it with 39g of talc, 4g of magnesium stearate, 155g of lactose, and 22g of sodium carboxymethyl starch, then add 240g of cetyl alcohol melt, mix to make granules, press to obtain 1000 linezolid tablets.

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/5377A61K47/10A61K47/12A61K47/14A61K47/32A61K47/34A61K47/36A61K47/38A61P31/04
Inventor 肖礼海曾丹
Owner CHONGQING HUAPONT PHARMA
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