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Slow release type linezolid medicament for eyes and preparation method thereof

A technology of linezolid ophthalmic and linezolid, which is applied in the field of slow-release linezolid ophthalmic medicine and its preparation, can solve the problems of poor solubility and stability of linezolid, achieve simple and feasible preparation process, increase treatment The effect of high success rate and high yield

Inactive Publication Date: 2018-07-17
广州君博医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above-mentioned defects in the prior art, the purpose of the present invention is to provide a sustained-release linezolid eye ointment with good curative effect, few side effects, strong intraocular penetration, stable properties, and no drug resistance, which solves the problem of linezolid eye ointment. The problem of poor solubility and stability of azole amide in simple aqueous solution

Method used

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  • Slow release type linezolid medicament for eyes and preparation method thereof
  • Slow release type linezolid medicament for eyes and preparation method thereof
  • Slow release type linezolid medicament for eyes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0019] A sustained-release linezolid eye ointment, comprising components: linezolid, polycarbophil, polysorbate, safflower flavin, anhydrous lanolin, liquid paraffin and yellow petrolatum, and the mass fraction ratio of each component is Linezolid: polycarbophil: polysorbate: safflower flavin: anhydrous lanolin: liquid paraffin: yellow petrolatum = 1:0.5~2:0.05~0.2:0.01~0.5:8~15:2~ 10:75-95.

[0020] The above-mentioned ophthalmic drugs are prepared with linezolid as the main active ingredient, safflower flavin, polycarbophil and polysorbate as the mucoadhesive polymer drug delivery system, and prepared with excipients. release formulations.

[0021] Among them, the raw materials and proportions of the sustained-release linezolid ophthalmic drugs in each of Examples 1 to 3 are shown in Table 1:

[0022] Table 1 The raw materials and proportioning situation of the sustained-release linezolid eye ointment of Examples 1-3

[0023]

[0024]

[0025] The preparation method...

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Abstract

The invention relates to a slow release type linezolid medicament for eyes. The medicament comprises linezolid, polycarbophil, polysorbate, saffower yellower, an accessory, and injection water; the mass ratio of linezolid to polycarbophil to polysorbate to saffower yellower to an accessory is 1:0.5-2:0.05-0.2:0.01-0.5:0.102-1.5, and the mass fraction of linezolid is 0.1-1%. The product is externally applied to parts of eyes, and has obvious bacteria preventing or killing effects; the product is suitable for treating and preventing bacterial infection of conjunctivitis, keratitis and other parts. The product has good penetrability in eyes, higher bioavailability in eyes, good penetration, good targeting effects, and small toxic and side effects.

Description

technical field [0001] The invention relates to an ophthalmic pharmaceutical preparation for treating bacterial infection, in particular to a slow-release linezolid ophthalmic medicine and a preparation method thereof. Background technique [0002] Linezolid is a synthetic oxazolidinone antibiotic 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. Linezolid is a brand-new class of oxazolone antibacterial drugs, which comprehensively covers drug-resistant strains of Gram-positive bacteria - Staphylococcus aureus / Enterococcus / Streptococcus, etc. It is an inhibitor of bacterial protein synthesis and acts on bacterial 50S ribosomes subunit and is closest to the site of action. Unlike other drugs, l...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/22A61K47/32A61K47/26A61K31/5377A61P31/04A61P27/02
CPCA61K9/0048A61K9/06A61K31/5377A61K47/22A61K47/26A61K47/32
Inventor 谭上彬王志军陈宇明黄俊杰崔明
Owner 广州君博医药科技有限公司
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