Ropivacaine mesylate compound, preparation process thereof and pharmaceutical composition thereof

A technology of ropivacaine mesylate and a compound, applied in the field of medicine, can solve the problems of slow dissolution rate, poor water solubility, low solubility and the like, and achieve the effects of high solubility, high solubility and easy compatibility

Inactive Publication Date: 2013-09-18
四川省惠达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Ropivacaine mesylate in the above-mentioned patents and the prior art is dissolved in an aqueous solution under acidic conditions with a pH value below 5, but its water solubility becomes significantly worse as the pH value increases, and it is insoluble in alkaline conditions In water, if the pH value is 7, the solubility is small and the dissolution rate is slow; when the pH value is 8, it is slightly soluble in water and precipitates when placed

Method used

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  • Ropivacaine mesylate compound, preparation process thereof and pharmaceutical composition thereof
  • Ropivacaine mesylate compound, preparation process thereof and pharmaceutical composition thereof
  • Ropivacaine mesylate compound, preparation process thereof and pharmaceutical composition thereof

Examples

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Effect test

Embodiment 1

[0043] The preparation of ropivacaine mesylate compound:

[0044] Get ropivacaine mesylate crude drug 50g, add the mixed solution of DMF / isopropanol, wherein the volume ratio of DMF and isopropanol is 2:1, the consumption of ropivacaine mesylate crude drug and mixed solution The ratio is 1g: 15ml, heated to 45°C, after the ropivacaine mesylate crude drug is dissolved, add activated carbon for decolorization, the amount of activated carbon added is 0.2% g / ml of the total volume of the liquid, stir and adsorb for 25min, filter Decarbonize and sterilize, move the filtrate to a reaction kettle, put it in an oven at 150°C and let it stand for 48 hours, then lower the temperature to 55°C, open the kettle, adjust the pH to 9, and slowly add acetone under stirring conditions, the volume of acetone and the mixed solution The ratio was 3:1, the temperature was lowered to 5°C, filtered, washed 3 times with a mixed solution of DMF / isopropanol, and dried under reduced pressure for 5 hours ...

Embodiment 2

[0047] The preparation of ropivacaine mesylate compound:

[0048] Get ropivacaine mesylate crude drug 50g, add the mixed solution of DMF / isopropanol, wherein the volume ratio of DMF and isopropanol is 4:1, the consumption of ropivacaine mesylate crude drug and mixed solution The ratio is 1g:10ml, heated to 40°C, after the ropivacaine mesylate crude drug is dissolved, add activated carbon for decolorization, the amount of activated carbon added is 0.3% g / ml of the total volume of the liquid, stir and adsorb for 30min, filter Decarbonize and sterilize, move the filtrate to a reaction kettle, put it in an oven at 120°C and let it stand for 24 hours, then lower the temperature to 45°C, open the kettle, adjust the pH to 7, and slowly add acetone under stirring conditions, the volume of acetone and the mixed solution The ratio was 6:1, cooled to 0°C, filtered, washed 3 times with a mixed solution of DMF / isopropanol, and dried under reduced pressure for 4 hours to obtain a white powd...

Embodiment 3

[0051] Preparation of Ropivacaine Mesylate Small Volume Injection

[0052]

[0053] Take 70% of the prepared total amount of fresh water for injection at 70°C in the treated batching tank, and pass nitrogen for 60 minutes. Drop into the ropivacaine mesylate and sodium chloride prepared by the embodiment 1 of the prescription amount, stir and dissolve under nitrogen protection, add water for injection to the full amount, stir and mix evenly, adjust the pH to 5.5. Lower the temperature of the liquid medicine to 30°C, and continue nitrogen protection. Add 0.05% (g / ml) medicinal charcoal to the medicinal liquid, stir and adsorb for 20 minutes under nitrogen protection, and decarbonize and filter. Fine filter with a microporous membrane with a pore size of 0.45 μm, take a sample for inspection of visible foreign matter, and transport it to potting after meeting the requirements. Nitrogen filling and sealing: according to the specifications, it is filled and sealed in ampoules...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a ropivacaine mesylate compound. The structural formula of the ropivacaine mesylate compound is shown in the description, and an X-ray powder diffraction spectrogram obtained by measuring the ropivacaine mesylate compound with Cu-K alpha rays is shown in figure 1. The invention also provides a preparation process of the ropivacaine mesylate compound, a pharmaceutical composition containing the ropivacaine mesylate compound and a preparation process of the pharmaceutical composition. Dosage forms of the ropivacaine mesylate pharmaceutical composition are powder injections, small volume injections and large volume injections. The ropivacaine mesylate compound is high in solubility and high in dissolution rate, and the pharmaceutical composition of the ropivacaine mesylate compound is good in dissolubility, easy to dissolve and composite and high in bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ropivacaine mesylate compound, a preparation method of the ropivacaine mesylate compound, a pharmaceutical composition containing the ropivacaine mesylate compound, and the medicine Method of preparation of the composition. Background technique [0002] Ropivacaine is a single enantiomer (S-shaped) long-acting amide local anesthetic. Its mechanism of action is the same as that of other local anesthetics. It blocks nerve excitation and conduction by inhibiting nerve cell sodium ion channels. The blocking effect on motor nerves is related to the drug concentration. The concentration of 0.2% is better for sensory nerve block, but almost no motor nerve block effect; 0.75% produces better motor nerve block effect. Ropivacaine is an amide local anesthetic, mainly used for surgical anesthesia: epidural anesthesia (including epidural anesthesia for cesarean section); loca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/60C07C309/04C07C303/32A61K31/445
Inventor 闫晓晔
Owner 四川省惠达药业有限公司
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