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Preparation method of ropivacaine methanesulfonate and its compound and preparation

A technology of ropivacaine mesylate compound and ropivacaine mesylate, which is applied in the fields of active ingredients of heterocyclic compounds, organic chemistry, drug combination, etc., which can solve the problem of difficult control of drying temperature and stable hygroscopicity Poor performance, high price and other problems, to achieve the effect of good salt stability and water solubility, good stability and stable product quality

Inactive Publication Date: 2004-08-04
ZHEJIANG XIANJU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In December 1998, Ropivacaine Hydrochloride Injection was approved to enter the Chinese market. Its product name is Nai Lepin. According to the clinical dosage requirements, there are three injections of 2, 7.5, and 10 mg / ml respectively. Unit clinical trials, the curative effect is better, but its price is high, each is 50-70 yuan, most domestic patients can not afford economically, in order to meet the clinical medication, reduce the pain and economic burden of patients, develop a kind of medicine that can allow the majority of patients Local anesthetics that can be used have become a concern of the pharmaceutical industry
In view of the fact that the methanesulfonate of ropivacaine is a crystal water and the hydrochloride of ropivacaine is a crystal water, its hygroscopicity is too strong and the stability is poor because of the ropivacaine hydrochloride. Salt is a crystalline water substance. It is difficult to control the temperature of the drying material, and it also brings certain technical difficulties to industrialized mass production.

Method used

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  • Preparation method of ropivacaine methanesulfonate and its compound and preparation
  • Preparation method of ropivacaine methanesulfonate and its compound and preparation
  • Preparation method of ropivacaine methanesulfonate and its compound and preparation

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Embodiment 1

[0023] The preparation method of the ropivacaine mesylate of the present invention comprises the following steps: material preparation—dissolution—adding methanesulfonic acid and a ketone solvent—adding a ketone solvent—filtering and drying—recrystallization. The specific content of described processing step is as follows

[0024] Preparation:

[0025] a.(-)-(S)-N-(2,6-dimethylphenyl)-1-propylpiperidine-2-carboxamide.: 200g;

[0026] b. Absolute ethanol: 1000ml;

[0027] c. Methanesulfonic acid: 80ml;

[0028] d. Acetone: 2000ml;

[0029] Dissolution: put ropivacaine single isomer (S) form and absolute ethanol into a container, stir and heat at 20-100°C to reflux, so that ropivacaine is completely dissolved in absolute ethanol;

[0030] Add methanesulfonic acid and ketone solvent: add methanesulfonic acid dropwise to the solution of ropivacaine and absolute ethanol, stir for 20 minutes after the dropwise addition, then add 800ml of acetone, and filter after the solution dr...

Embodiment 2

[0038] Using the ropivacaine mesylate compound of the present invention as a raw material for the preparation of injections comprises the following steps:

[0039] (1) Pretreatment according to the requirements of conventional injections;

[0040] (2) Dissolve 5 g of ropivacaine mesylate compound and 800 mg of sodium chloride in 500 ml of water for injection, add water for injection to 1000 ml after adding activated carbon for decolorization, and adjust the pH to 3.5-6.5 with HCL or NaOH, Finely filter through a 0.45um microporous membrane or ultrafiltration rod, and then treat it according to the conventional method for injection.

Embodiment 3

[0042] The prescription process of ropivacaine mesylate compound boutique configuration 10ml: 23.8mg injection is:

[0043] (1) The ampoule is treated according to the conventional treatment method, and is set aside;

[0044] (2) Dosing: Take 2.38g and 6-10g of sodium chloride, add it to the batching bucket, add injection water to 500ml, stir the solution, add 0.1% g / ml activated carbon for targeting and stir for 30 minutes;

[0045] (3) Filtration: first filter for decarburization, then add water for injection to 1000ml, stir evenly, adjust the pH to 3.9 with HCl or NaOH, and fine filter with a 0.45 micron microporous membrane or ultrafiltration rod;

[0046] (4) Filling: measure the pH value: 3.5-5.5; content: 90-110%, fill according to the requirements of 10ml: 23.8mg injection;

[0047] (5) Fusion sealing: use a wire drawing sealing machine to seal;

[0048](6) Sterilization: 0.07Mpa115°C, heat and then sterilize for 30 minutes;

[0049] (7) Picking up leaks: carry out ...

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Abstract

A ropivacaine methanesulfonate as anesthetic or analgetic has a chemical formula: (-)-(S)-N-(2,6-dimethylphenyl)-1-propyl piperidine-2-formamide methanesulfonate, and is prepared through preparing raw materials, dissolving, adding, methane sulfonic acid, adding ketone solvent, filtering, baking and recrystallizing. Its advantages are high stability and output rate and low cost.

Description

technical field [0001] The invention belongs to the technical field of anesthesia and analgesic drugs, in particular to a preparation method of ropivacaine mesylate and its compound and preparation. The chemical name of ropivacaine mesylate is: (-)- (S)-N-(2,6-Dimethylphenyl)-1-propylpiperidine-2-carboxamide methanesulfonate. Background technique [0002] During the late 1970s to the late 1980s, local anesthetics such as bupivacaine, mepivacaine, and prilocaine were developed, which contained an asymmetric carbon atom and thus could split Significant differences in intranerve blockade effects between enantiomers of these compounds have not been found, while stereoselectivity in other important pharmacological effects such as local anesthetic effects has been reported, such as absorption and metabolism. Since the discovery that long-acting local anesthetics may be associated with sudden cardiac arrest, people have been seeking safer low-fat-soluble a...

Claims

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Application Information

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IPC IPC(8): A61K31/445A61P25/04C07D211/60
Inventor 马群立黄庆云
Owner ZHEJIANG XIANJU PHARMA
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