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Stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application

A technology of levo-ornidazole phosphate ester and compound, which is applied to medical preparations, pharmaceutical formulations, chemical instruments and methods containing active ingredients, etc., can solve the problems of poor water-solubility, unsafety, low melting point and the like of levo-ornidazole, To achieve the effect of superior stability and good solubility

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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  • Stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application
  • Stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application
  • Stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application

Examples

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Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of L-ornidazole hydrochloride phosphate

[0026] Dissolve 100g of L-ornidazole phosphate in 500ml of acetone at 50°C, cool down to room temperature, add concentrated hydrochloric acid dropwise with stirring until almost no solid is produced, stir for 1 hour, filter, and dry the solid in vacuum at 40°C to dryness to obtain hydrochloric acid Levo-ornidazole phosphate 75g.

[0027] After 10 g of levo-ornidazole hydrochloride phosphate was heated and dissolved with 150 ml of 85% acetone, 0.01 g of activated carbon was added for decolorization, filtered, and the filtrate was cooled and crystallized, filtered, and dried to obtain 63 g of hydrate of levo-ornidazole hydrochloride phosphate. (purity 99.98% determination method: HPLC normalization method)

[0028] Substituting hydrochloric acid for hydrobromic acid can prepare levo-ornidazole hydrobromide phosphate according to the above method.

[0029] Substituting hydrochloric acid for hydroiodi...

Embodiment 2

[0030] Dissolve 100g of levo-ornidazole phosphate in 500ml of acetone at 50°C, cool down to room temperature, add sulfuric acid dropwise under stirring until almost no solid is produced, filter after stirring for 1 hour, and dry the solid in vacuum at 40°C to dryness to obtain levorotatory sulfuric acid Ornidazole phosphate 71g.

Embodiment 3

[0031] Embodiment 3: Preparation of Levonidazole Hydrochloride Phosphate for Injection

[0032] Levonidazole Phosphate Hydrochloride 250g

[0033] Cum water 2000ml

[0034] Makes 1000 bottles

[0035] Add 1900ml of water for injection in the liquid preparation container, add the prescribed amount of L-ornidazole hydrochloride phosphate, stir to dissolve, slowly add arginine to a pH of 4.8, add water to the full amount, and then add 0.05% (W / V) Stir for 60 minutes, filter with a 0.22 μm filter membrane until the clarity is qualified, after the content of the intermediate is determined to be qualified, the fixed amount is divided into control vials, half stoppered, and the sample is pre-frozen at -50°C 4 hours, vacuum, keep the vacuum degree <20Pa, slowly raise the temperature to -20°C, keep for 20 hours, then slowly raise the temperature to 20°C, keep for 4 hours, pressure recovery test <30Pa / min, press the plug, roll the cap to get it.

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Abstract

The invention relates to a stable pharmaceutical salt of L-aonitrate phosphate ester, its preparation method and application. The related strong acid salt of the L-aonitrate phosphate ester is shown by the formula I and is mainly used in treating anaerobic infection or protozoan infection.

Description

Technical field: [0001] The invention relates to a stable medicinal salt of levo-ornidazole phosphate, a preparation method and application thereof. 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 an...

Claims

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Application Information

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IPC IPC(8): C07F9/6506A61K31/675A61P31/04A61P33/02
Inventor 杨成施维刘晓鹏陆华龙
Owner HC SYNTHETIC PHARMA CO LTD
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