S-Ornidazole phosphate amino acid salt, its preparation method and application

A technology of levo-ornidazole phosphate and amino acid, which is applied in the field of levo-ornidazole phosphate amino acid salt and its preparation, can solve the problems of unsafe, poor water solubility and low melting point of levo-ornidazole, and achieve good solubility and superior The effect of stability

Inactive Publication Date: 2012-06-27
HC SYNTHETIC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, levo-ornidazole has very poor water solubility and low melting point. It requires strong acidity when made into infusion preparations, and patients are prone to phlebitis when taking medication; and the toxic degradation product 2-methyl-5-nitroimidazole is relatively high during high-temperature sterilization of infusion solutions. , bringing great insecurity to clinical medication

Method used

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  • S-Ornidazole phosphate amino acid salt, its preparation method and application
  • S-Ornidazole phosphate amino acid salt, its preparation method and application
  • S-Ornidazole phosphate amino acid salt, its preparation method and application

Examples

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Effect test

Embodiment 1

[0029] Embodiment 1: Preparation of L-Ornidazole Phosphate Monoarginine Salt

[0030] Dissolve 100g of L-ornidazole phosphate in 500ml of methanol at 50°C, slowly add 58.2g of arginine under stirring, stir for 2 hours until the solids are completely dissolved, continue stirring for 1 hour, filter, evaporate to dryness under reduced pressure, add Dissolve the residue in 1800ml of 90% acetone solution at 60°C, decolorize with 0.5% activated carbon for 15min, filter, and place the filtrate for crystallization to obtain 113g of L-ornidazole phosphate monoarginine salt. (Purity 99.2%, calculated by normalization method).

Embodiment 2

[0031] Embodiment 2: Preparation of L-Ornidazole Phosphate Monolysine Salt

[0032] The preparation method is the same as in Example 1, except that arginine is replaced by lysine.

[0033] Embodiment 2: Preparation of L-Ornidazole Phosphate Monohistidine Salt

[0034] The preparation method is the same as in Example 1, except that arginine is replaced by histidine.

Embodiment 4

[0035] Example 4: Preparation of L-Ornidazole Phosphate Monoarginine Salt for Injection

[0036] Levonidazole Phosphate Monosperm 250g

[0037] Amino acid salt

[0038] Water for injection 2000ml

[0039] Makes 1000 bottles

[0040] Add 1900ml of water for injection in the liquid preparation container, add the prescribed amount of L-ornidazole phosphate monoarginine salt, stir to dissolve, add water to the full amount, then add 0.05% (W / V) medicinal charcoal, stir After 60 minutes, filter with a 0.22 μm filter membrane until the clarity is acceptable. After the content of intermediates is determined to be qualified, the fixed amount is divided into control vials, half stoppered, and the sample is pre-frozen at -50°C for 4 hours, and vacuumized. Keep the vacuum degree <20Pa, slowly raise the temperature to -20°C, keep it for 20 hours, then slowly raise the temperature to 20°C, keep it for 4 hours, the pressure recovery test is less than 30Pa / ...

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Abstract

The invention relates to an amino acid salt of S-Ornidazole phosphate, especially its monoamino acid salt. With a structural formula as shown in general formula I, the amino acid salt of S-Ornidazole phosphate is mainly used for treating anaerobic infections or protozoan infections.

Description

Technical field: [0001] The invention relates to a stable amino acid salt of levo-ornidazole phosphate and its preparation method and application. technical background: [0002] Ornidazole is a nitroimidazole derivative, which is a powerful drug against anaerobic infection and antiprotozoal infection. It is also developed after metronidazole with higher curative effect, shorter course of treatment, better tolerance and wider distribution in the body. The third generation of nitroimidazole derivatives. The antimicrobial effect of ornidazole is through the reduction of the nitro group in its molecule to an amino group in an oxygen-free environment or through the interaction with cell components in the form of free radicals, resulting in the death of microorganisms. [0003] Levo-ornidazole is the left-handed isomer of ornidazole. Chinese patents CN200510068478.9 and CN200510083517.2 describe that it is superior to ornidazole and dex-ornidazole in terms of neuroinhibition and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6506A61K31/675A61P31/04A61P33/02
Inventor 杨成强建华刘晓鹏
Owner HC SYNTHETIC PHARMA CO LTD
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