Mepivacaine xinafoate and long-acting sustained release preparation thereof

A technology of mepivacaine xinafoate and mepivacaine, which is applied to medical preparations containing active ingredients, anesthetics, anti-inflammatory agents, etc., can solve the problems of short duration of anesthesia, short biological half-life, and high medical and nursing costs , to achieve the effect of prolonging anesthesia time, prolonging half-life and high safety

Active Publication Date: 2019-10-15
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the in vivo biological half-life of mepivacaine hydrochloride injection is short, which makes the duration of local anesthesia short for one-time administration.
At present, in clinical local anesthesia, frequent administration of small doses is required to maintain an effective therapeutic concentration, and the cost of medical care is relatively high
When the dose is larger, the maintenance time of the effective therapeutic concentration is prolonged, but the maximum blood concentration C max Beyond the therapeutic window, leading to side effects

Method used

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  • Mepivacaine xinafoate and long-acting sustained release preparation thereof
  • Mepivacaine xinafoate and long-acting sustained release preparation thereof
  • Mepivacaine xinafoate and long-acting sustained release preparation thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] The preparation of embodiment 1 mepivacaine xinafoate

[0032] Mepivacaine base (12.3 g; 50 mmol) and xinafoic acid (9.41 g; 50 mmol) were added to absolute ethanol (300 mL), and stirred at 60° C. for 5 hours. Subsequently, 2L of water was added to the reaction solution, and a white solid was precipitated, which was filtered and vacuum-dried to obtain mepivacaine xinafoate salt. The powder X-ray diffraction pattern of gained xinafoate mepivacaine is as attached figure 1 , the DSC diagram is attached figure 2 .

Embodiment 2

[0033] The preparation of embodiment 2 mepivacaine xinafoate

[0034] Mepivacaine base (1.23 g; 5 mmol) and xinafoic acid (0.94 g; 5 mmol) were added to DMSO (20 mL), and stirred at 50° C. for 4 hours. Subsequently, the reaction solution was added dropwise to 300 mL of water, and a white solid was precipitated, which was filtered and vacuum-dried to obtain mepivacaine xinafoate salt.

Embodiment 3

[0035] Embodiment 3 prepares the xinafoate mepivacaine salt of micron size

[0036] A jet mill (model JM-50A, Shanghai Minwang Machinery Technology Co., Ltd.) was used for jet micronization of mepivacaine xinafoate salt. The particle size distribution of mepivacaine xinafoate after airflow micronization was measured by a dry method using a Mastersizer 3000 laser scattering particle size distribution analyzer (Malvern Instrument, UK). The micronized mepivacaine xinafoate was determined to have the following particle size distribution: 10% < 2.16 μm, 50% < 4.21 μm and 90% < 7.85 μm.

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Abstract

The invention discloses a mepivacaine xinafoate which is a salt generated after mepivacaine reacts with xinafoate. The invention further discloses a mepivacaine long-acting sustained release preparation, wherein the mepivacaine long-acting sustained release preparation comprises the mepivacaine xinafoate. The pharmacokinetic test results show that according to the mepivacaine xinafoate and the mepivacaine long-acting sustained release preparation, the measured maximal concentration of the mepivacaine can be reduced significantly, and the half-life period of the mepivacaine is prolonged. The pharmacodynamic test results show that according to the mepivacaine xinafoate and the mepivacaine long-acting sustained release preparation, the anesthesia time of animals can be prolonged significantly. In addition, the mepivacaine xinafoate and the mepivacaine long-acting sustained release preparation further have high safety.

Description

technical field [0001] The invention relates to a new mepivacaine salt, especially mepivacaine xinafoate salt, and also relates to a mepivacaine long-acting slow-release preparation, which belongs to the technical field of medicine. Background technique [0002] Mepivacaine, whose chemical name is N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide, has the following chemical structure: [0003] [0004] Mepivacaine is a new type of local anesthetic. At present, its hydrochloride preparation is often used clinically, that is, mepivacaine hydrochloride injection, which is mainly used for surgical anesthesia and postoperative pain treatment. However, the biological half-life of mepivacaine hydrochloride injection in vivo is short, which makes the duration of local anesthesia short for one-time administration. At present, in clinical local anesthesia, frequent administration of small doses is required to maintain an effective therapeutic concentration, and the cost of m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4458A61K9/10A61K31/192A61K31/46A61P23/02A61P29/00A61K31/167A61K31/245A61K31/445
CPCA61K31/4458A61K9/0019A61K9/10A61K31/46A61P23/02A61P29/00A61K31/192A61K31/167A61K31/245A61K31/445A61K2300/00
Inventor 李寒梅唐川鄂何恩唐琦
Owner CHENGDU UNIV
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