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Ropivacaine freeze-drying agent capable of forming micelle

A technology of freeze-dried preparations and ropivacaine, which is applied in the field of medicine, can solve problems such as the inability to achieve sustained release, and achieve the effect of preventing organic acid salts and hydrolysis

Active Publication Date: 2016-03-30
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The lactic acid formed after the decomposition of the copolymer will form a salt with ropivacaine, and the obtained lactic acid ropivacaine has good solubility in water. When the lyophilized preparation is reconstituted, it will dissolve in water and cannot achieve the purpose of sustained release.

Method used

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  • Ropivacaine freeze-drying agent capable of forming micelle
  • Ropivacaine freeze-drying agent capable of forming micelle
  • Ropivacaine freeze-drying agent capable of forming micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Preparation of polyethylene glycol monomethyl ether-polylactic acid block copolymer

[0020] Weigh polyethylene glycol monomethyl ether 2000 and lactide with a mass ratio of 50:50 and place them in a three-neck flask, stir under nitrogen protection, and heat the reaction temperature to 130°C to make polyethylene glycol monomethyl ether In 2000, the lactide was melted, and after stirring and mixing, 0.2% of the total mass of stannous octoate was added, heated to 140°C under nitrogen protection, and stirred for 6 hours to obtain a colorless, clear and transparent viscous liquid; add dichloromethane to dissolve, and Precipitate with ice-cold anhydrous ether, filter the precipitate, and dry it under vacuum at room temperature for 24 hours. A polyethylene glycol monomethyl ether-polylactic acid block copolymer with an average relative molecular weight of 4000 was obtained, and the block ratio was 50:50.

[0021] According to the above method, weigh 90:10, 60:4...

Embodiment 2

[0022] Embodiment 2: the preparation of ropivacaine freeze-dried preparation

[0023] Dissolve 200 mg of polyethylene glycol monomethyl ether-polylactic acid block copolymer (block ratio 50:50) in 2-tert-butanol, add 20 mg of ropivacaine to obtain a clear solution, filter it and add it to a vial , freeze-dried in a lyophilizer after half-capping, and the finished product is obtained by capping and capping.

Embodiment 3

[0024] Embodiment 3: the preparation of ropivacaine freeze-dried preparation

[0025] Dissolve 200 mg of polyethylene glycol monomethyl ether-polylactic acid block copolymer (block ratio 40:60) in 2 mL of tert-butanol and 0.05 mL of water, add 20 mg of ropivacaine to obtain a clear solution, filter and add In the vials, freeze-dry in a freeze dryer after half-capping, and obtain the finished product by capping and rolling the cap.

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Abstract

The invention discloses a ropivacaine freeze-drying agent. Ropivacaine is a widely used pain-relief drug, and the ropivacaine freeze-drying agent is provided for extending the action period. The ropivacaine freezing agent comprises a segmented copolymer of methoxy poly(ethylene glycol)-poly(lactic acid), and has the advantage that after redissolving, a micelle can be formed, so the action period of the drug is extended, and the release effect is realized.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a freeze-dried preparation of ropivacaine. Background technique [0002] Ropivacaine hydrochloride and ropivacaine mesylate are clinically used for local anesthesia and analgesia. [0003] On January 22, 2013, Lapute Pharmaceutical Co., Ltd. disclosed a non-addictive anesthesia and analgesia sustained-release drug delivery system in Chinese patent application CN103142458A, which is a uniform oily composition, wherein the analgesic The agent is ropivacaine free base, the solvent is selected from benzyl alcohol, ethanol, benzyl benzoate, and the sustained release agent is selected from soybean oil and castor oil. [0004] On February 25, 2009, West China Medical College of Sichuan University disclosed a thermosensitive gel transdermal drug delivery system in Chinese patent application CN101810908A, in which ropivacaine can be selected as the local anesthetic. For topical anest...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/107A61K31/445A61K47/34A61P23/02
CPCA61K9/107A61K9/19A61K31/445A61K47/34
Inventor 涂家生孙如宁
Owner CHINA PHARM UNIV
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