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Preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving

A linezolid tablet, high drug loading technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of not being able to achieve rapid disintegration, and achieve high loading The effect of the dose

Active Publication Date: 2013-05-15
CHENGDU XINJIE HIGH TECH DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after verification by the applicant, if the 600mg linezolid tablet is in accordance with the declared specification, the prescription provided in the application cannot achieve rapid disintegration at all; the reason is that the raw materials of the IV crystal form have very strong hydrophobicity, and the ingredients of the provided formula cannot achieve According to the FDA dissolution method with the brand preparation (Pfizer), the similarity of dissolution curves in 4 solvents is in the range of 50-100

Method used

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  • Preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving
  • Preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Weigh the raw and auxiliary materials according to prescription 1 and implement according to the following production process:

[0063] 1. Pass linezolid through a 80-mesh sieve; corn starch, hydroxypropyl cellulose (low substitution), carboxymethyl starch sodium, microcrystalline cellulose, and povidone K30 pass through a 100-mesh sieve, and set aside.

[0064] 2. Weigh linezolid, corn starch, hydroxypropyl cellulose (low substitution), sodium carboxymethyl starch, microcrystalline cellulose, povidone K according to the prescription instructions 30 , silicon dioxide, magnesium stearate materials, spare.

[0065] 3. Put linezolid, corn starch, hydroxypropyl cellulose (low substitution), sodium starch glycolate, microcrystalline cellulose, povidone K30, and silicon dioxide in a multi-directional motion mixer, mix for 20 minutes, and collect materials.

[0066] 4. Put the mixed material in the tank mixer, start stirring, and add an appropriate amount of isopropanol sol...

Embodiment 2

[0077] Example 2 Dissolution Determination

[0078] method :

[0079] Take this product, according to the dissolution test method (Chinese Pharmacopoeia 2010 edition two appendix Ⅹ C second method), with pH6.8 phosphate buffer (take 129.6g of potassium dihydrogen phosphate and 147.6g of dipotassium hydrogen phosphate, add water to dissolve And dilute to 2000ml, as the stock solution. Take 50ml of the stock solution and dilute to 900ml with water) as the solvent, the speed is 50 rpm, and the operation is according to the law. At 30 minutes, take 10ml of the solution, filter it, add pH 6.8 phosphate buffer to dilute to a solution containing about 10μg of linezolid per 1ml, and use it as the test solution; Determined, use pH 6.8 phosphate buffer to make a solution containing about 10 μg of linezolid per 1 ml, as a reference solution. Take the above two solutions, according to the visible-ultraviolet spectrophotometric method (Chinese Pharmacopoeia 2010 Edition, Appendix IV A)...

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Abstract

The invention discloses a preparation method of IV crystal linezolid tablets having high drug loading capacity and capable of quickly dissolving. The preparation method comprises the following steps of preprocessing, premixing, mixing, granulating, drying, arranging granulates, centrally controlling, tabletting and coating. According to the preparation method, corn starch and silica are matched with each other, therefore, the tablets with hardness more than 30kg can be quickly cracked, and the in-vitro dissolution similarity ranging from 50 to 100 with respect to a referred product, as well as high drug loading capacity, can be realized.

Description

technical field [0001] The invention relates to a preparation method of linezolid IV crystal form tablets with high drug loading and fast dissolution in vitro, belonging to the field of pharmaceutical preparations. Background technique [0002] Linezolid, a synthetic oxazolidinone antibiotic, was approved by the US FDA in 2000 for the treatment of infections caused by Gram-positive (G+) cocci, including suspected or confirmed hospital-acquired pneumonia (HAP) caused by MRSA, Community-acquired pneumonia (CAP), complicated skin or skin and soft tissue infection (SSTI), and vancomycin-resistant enterococci (VRE) infection. [0003] Linezolid is a bacterial protein synthesis inhibitor that acts on the bacterial 50S ribosomal subunit 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/30A61K47/36A61K47/04A61K31/5377A61P31/04
Inventor 蒲洪林树李长生欧世荣张西彪
Owner CHENGDU XINJIE HIGH TECH DEV CO LTD
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