Ozagrel ornithine and its injection form

A technology of ornithine and ornithine, applied in drug delivery, cardiovascular system diseases, respiratory system diseases, etc., can solve problems such as not being found

Inactive Publication Date: 2012-02-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the method of suppressing the production of insoluble foreign matter during preservation of Ozagrel injection has not yet been found.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Add 0.01mol ozagrel, 0.01mol ornithine and 30ml water into a 100ml glass bottle, stir at room temperature for 10 minutes, the raw materials dissolve rapidly, the resulting solution is colorless and transparent, and the pH of the solution measured with a pH meter is 6. Concentrate the obtained saline solution under reduced pressure, then transfer it to a petri dish and place it in a desiccator to evaporate the water and turn it into a transparent glassy solid, then continue to stand to let the water evaporate completely, and gradually turn it into a white solid. This product is the ozagrel ornithine salt of the present invention. Add 30ml of water to the solid and stir with a glass rod. Within 10 seconds, the solid is completely dissolved. Elemental analysis results: C60.29%, H6.57%, N15.61%, 017.65%; theoretical values: C60.155%, H6.731%, N15.589%, 017.807%

Embodiment 2

[0014] Ozagrel Ornithine Injection

[0015] Prescription: ozagrel ornithine (calculated as ozagrel) 20g

[0016] Ornithine or hydrochloric acid to adjust pH 6-9

[0017] Water for injection 1000ml

[0018] Preparation method: Dissolve ozagrel ornithine salt in water for injection, add ornithine or hydrochloric acid to adjust the pH value to 6-9, add carbon for injection, stir at room temperature for 10 minutes, filter to remove carbon, dilute with water for injection to the predetermined Concentration, pass through a 0.2μm microporous membrane to sterilize, put it into an ampoule and seal it under aseptic conditions, 1ml / bottle, and obtain the aqueous injection.

Embodiment 3

[0020] Ozagrel Ornithine For Injection

[0021] Prescription: ozagrel ornithine (calculated as ozagrel) 40g

[0022] Ornithine or hydrochloric acid to adjust pH 6-9

[0023] Mannitol 5g

[0024] Water for injection 1000ml

[0025] Preparation method: Take ozagrel ornithine, dissolve mannitol in water for injection, add ornithine or hydrochloric acid to adjust the pH value to 6-9, add needle with carbon and stir at room temperature for 10 minutes, filter to remove carbon, and inject with predetermined concentration Dilute with water, pass through a 0.2μm microporous membrane to sterilize, put it into a control bottle under sterile conditions, 1ml / bottle, half-tighten the stopper, pre-freeze at -40°C for 3 hours, and then press 3-5°C / h Raise the temperature to 35°C, keep it warm for 2 hours, press the stopper, and take out the aluminum cap to obtain the powder injection of the present invention. It can be used by adding it to the infusion before use.

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PUM

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Abstract

The invention discloses an ozagrel ornithine salt, which is used for preparing and treating cerebral vasospasm and accompanying cerebral insufficiency after subarachnoid hemorrhage, and movement disorders caused by acute cerebral thrombosis and thrombosis A drug for bronchial asthma. It is obtained by the reaction of water-insoluble ozagrel with ornithine in water, concentrated and dried or crystallized or freeze-dried with insoluble organic solvent. It is made of ozagrel ornithine for intravenous administration. The infusion agent of the medicine and the injection that can be added to the 5% glucose injection or the 0.9% sodium chloride injection, the solvent crystallization sub-packaging powder injection and the freeze-dried powder injection. The ornithine salt formed by the invention has higher solubility in water than the sodium salt and improves the stability of ozagrel. When the formed ornithine salt is made into an injection, the pH value is closer to that of the human body.

Description

Technical field: [0001] The invention relates to an ozagrel ornithine salt and an injection form made from it. Background technique: [0002] Ozagrel (chemical name: (E)-3-[p-(1H-imidazole-1-methyl)phenyl]-2-propenoate), an imidazole derivative, was researched and developed as a COX synthase inhibitor Medicament for the improvement of cerebral vasospasm after subarachnoid hemorrhage and its accompanying cerebral ischemic symptoms and cerebral thrombosis (acute phase) accompanied by movement disorders. At present, the ozagrel injection is prepared by adding sodium hydroxide to dissolve the ozagrel during the preparation of the injection. However, the aqueous solution of ozagrel sodium salt, whose pH is adjusted to be alkaline, usually cannot be stored for a long time due to the formation of insoluble foreign matter during long-term storage in glass containers. At the same time, ozagrel sodium salt has low solubility in acidic aqueous solution, and is prone to decomposition ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/60A61K9/08A61K31/4174A61P9/10A61P11/06
Inventor 王东凯
Owner SHENYANG PHARMA UNIVERSITY
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