Ropivacaine mesylate freeze-dried powder injection for injection and preparation method thereof

A technology of ropivacaine mesylate and freeze-dried powder injection, which is applied in the field of preparation of ropivacaine mesylate freeze-dried powder injection for injection, and can solve the problem of unsuitability for large-scale industrial production, high cost input and complicated operation and other problems, to achieve the effect of good resolubility and clarity, high yield and good resolubility

Inactive Publication Date: 2016-10-26
SHANXI PUDE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation method adopts the aseptic low-temperature vacuum spray drying method, but using this method to prepare ropivacaine mesylate powder injection, the operation is complicated, the cost input is very high, and it is not suitable for industrialized large-scale production
[0006] In short, in order to ensure a good freeze-dried appearance, the prior art of preparing ropivacaine freeze-dried powder injections has added a large amount of excipients, such as mannitol, so as to solve the problems of poor product appearance and low yield
However, the addition of a large amount of excipients such as mannitol may bring safety risks during lumbar epidural injection (clinical safety of mannitol, Xia Xiaoping, Journal of Adverse Drug Reactions, 2003, No. 4) Therefore, for the anesthetic ropivacaine administered as an epidural injection, if any excipients can be reduced during the preparation of the powder injection, the clinical safety of the drug will be greatly increased

Method used

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  • Ropivacaine mesylate freeze-dried powder injection for injection and preparation method thereof
  • Ropivacaine mesylate freeze-dried powder injection for injection and preparation method thereof
  • Ropivacaine mesylate freeze-dried powder injection for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] A ropivacaine mesylate freeze-dried powder for injection, comprising the following components:

[0044] Ropivacaine mesylate 89.4g;

[0045] Mannitol 50g;

[0046] Add 5% ethanol aqueous solution to 1000mL;

[0047] Its preparation method is as follows:

[0048](1) Accurately weigh the ropivacaine mesylate of the prescription amount, add mass percentage concentration and be 5% ethanol solution, stir and dissolve; add the mannitol of recipe amount again, continue to stir and dissolve; Obtain mixed solution, wherein stir and dissolve When, the speed of stirring is 80 rpm;

[0049] (2) Regulate the pH value of the mixed solution obtained in step (1) to 4.0-6.0 with 0.1mol / L NaOH solution, and add an aqueous ethanol solution with a mass percentage concentration of 5% to the prescription amount;

[0050] (3) Add activated carbon for needles to the mixed solution obtained in step (2), the dosage of activated carbon for needles is 0.1% g / mL; after stirring and absorbing fo...

Embodiment 2

[0053] A ropivacaine mesylate freeze-dried powder for injection is characterized in that the freeze-dried powder includes the following components:

[0054] Ropivacaine mesylate 119.2g;

[0055] Mannitol 40g;

[0056] Add 10% ethanol aqueous solution to 1000mL;

[0057] Its preparation method is as follows:

[0058] (1) Accurately weigh the ropivacaine mesylate of the prescription amount, add the mass percent concentration and be 10% ethanol solution, stir and dissolve; add the mannitol of the recipe amount again, continue to stir and dissolve; obtain the mixed solution, the speed of stirring 120 rpm;

[0059] (2)) Use 0.1mol / L NaOH solution to adjust the pH value of the mixed solution obtained in step (1) to 4.0-6.0, and add an aqueous ethanol solution with a mass percentage concentration of 10% to the prescription amount;

[0060] (3) Add activated carbon for needles to the mixed solution obtained in step (2), the dosage of activated carbon for needles is 0.1% g / mL; afte...

Embodiment 3

[0063] The sample obtained in Example 1 of the present application is detected, and the obtained results are as follows:

[0064]

[0065] As can be seen from the above table, the ropivacaine mesylate freeze-dried powder injection prepared by the present application fully complies with the relevant regulations of the Pharmacopoeia.

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PUM

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Abstract

The invention discloses a ropivacaine mesylate freeze-dried powder injection for injection. The freeze-dried powder injection is prepared from 89.4 g of ropivacaine mesylate and 50 g of mannitol by adding ethanol water with mass percentage concentration of 5-10% till 1000 mL. The freeze-dried powder injection is good in product appearance, high in yield, good in redissolvability and high in clarity.

Description

technical field [0001] The application relates to a preparation method of ropivacaine mesylate freeze-dried powder for injection, which belongs to the technical field of medicines. Background technique [0002] Ropivacaine mesylate: chemical name is (S)-N-(2,6-dimethylphenyl)-1-propyl-2-piperidinecarboxamide mesylate, molecular formula C 18 h 30 N 2 o 4 S, molecular weight: 370.51, CAS No. 854056-07-8, is a white crystalline powder. [0003] Ropivacaine mesylate is a new domestic amide local anesthetic after changing the hydrochloride root of ropivacaine hydrochloride to mesylate root. It has low cardiotoxicity, more obvious separation of sensory block and motor block, and vasoconstriction. effect, so there is no need to add epinephrine when using it. Because it only blocks pain nerves when used, does not affect motor nerves, and hardly passes through the placenta at the same time, it has the following advantages: (1) it can provide effective analgesia for puerpera; (2)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/445A61K47/10A61P23/02A61P29/00
CPCA61K9/0019A61K9/19A61K31/445A61K47/10
Inventor 李立忠王勇苏志强何海忠武晋荣航
Owner SHANXI PUDE PHARMA CO LTD
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