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Mepivacaine xinafoate and its long-acting sustained-release preparation

A technology of mepivacaine xinafoate and mepivacaine xinafoate, which is applied in the field of medicine, can solve the problems of short duration of anesthesia, short biological half-life, high medical expenses, etc., to prolong anesthesia time, prolong half-life, and high safety sexual effect

Active Publication Date: 2022-07-26
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 its long-acting sustained-release preparation
  • Mepivacaine xinafoate and its long-acting sustained-release preparation
  • Mepivacaine xinafoate and its long-acting sustained-release preparation

Examples

Experimental program
Comparison scheme
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, 2 L of water was added to the reaction solution to precipitate a white solid, which was filtered and dried in vacuo to obtain mepivacaine xinafoate salt. The powder X-ray diffraction pattern of the obtained mepivacaine xinafoate 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 was added dropwise to 300 mL of water, and a white solid was precipitated, which was filtered and dried in vacuo to obtain mepivacaine xinafoate salt.

Embodiment 3

[0035] Example 3 Preparation of micron-sized mepivacaine xinafoate salt

[0036] The mepivacaine xinafoate salt was air-jet micronized using a jet mill (model JM-50A, Shanghai Minwang Machinery Technology Co., Ltd.). The particle size distribution of mepivacaine xinafoate after air flow micronization was determined by dry method using a Mastersizer 3000 laser scattering particle size distribution analyzer (Malvern Instrument, UK). 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 mepivacaine xinafoate, which is a salt formed by the reaction of mepivacaine and xinafoic acid, and also discloses a long-acting sustained-release preparation of mepivacaine, which contains Mepivacaine xinafoate as described. Pharmacokinetic test results show that the present invention can significantly reduce the peak concentration of mepivacaine and prolong its half-life. The drug effect test results show that the invention can significantly prolong the anesthesia time of animals. In addition, the present invention also has high security.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(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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