Preparation method of local anesthetic liposome

A technology of local anesthetics and liposomes, which is applied in the fields of anesthetics, liposome delivery, pharmaceutical formulations, etc., can solve the problems of low encapsulation efficiency of liposome products, low particle size uniformity, and complicated preparation methods, and achieve improved The effects of entrapment efficiency, prolonged residence time, and simple and easy preparation process

Active Publication Date: 2021-06-29
NANJING LUYE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the above problems, the application provides a method for preparing liposomes for local anesthetics, establishes a method for active drug loading-freeze-drying and reconstitution, and solves the problem of complex preparation methods for liposomes for amide local anesthetics, cumbersome processes, and liposome products. Low encapsulation efficiency and other issues, through the implementation of this method, local anesthetic liposome products with lower particle size and higher uniformity, and higher encapsulation efficiency can be prepared, and the operation is simple and easy to realize industrial production

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Examples

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Embodiment 1

[0033] A method of preparation of ropivacin liposomes, the specific steps are as follows:

[0034] A. Preparation of white liposomes: 20 ml of 0.02 mol / L phosphate buffer, slowly added with a syringe to DEPC (diel phosphatidylcholine) 240 mg and chooseol 160 mg of trichloromethane solution (V organic phase: V water phase = 1: 1), high speed stirred emulsifue until a stable W / O type emulsion is formed, and the resulting emulsion is reduced to remove trichloromethane in a rotary evaporator (35 ° C) to form a uniform film, and then add appropriate amount of phosphate buffer. The phospholipin film was continued to evaporate, i.e., the uniform liposome mixing solution was obtained, and then the polycarbonate film was used to obtain a blank liposome.

[0035] B. Blank liposome ultrafiltration concentration: Overhaplify the blank liposomes in step A, wherein the film material is a polyether sulfone, and the elongated molecular weight is 300 kDa. The ultrafiltration membrane assembly ...

Embodiment 2

[0038] A method of preparation of ropivacin liposomes, the specific steps are as follows:

[0039] A. Preparation of white liposomes: 20 ml of 0.02 mol / L phosphate buffer, slowly added with a syringe to DEPC (diel phosphatidylcholine) 240 mg and chooseol 160 mg of trichloromethane solution (V organic phase: V water phase = 1: 1), high speed stirred emulsifue until a stable W / O type emulsion is formed, and the resulting emulsion is reduced to remove trichloromethane in a rotary evaporator (35 ° C) to form a uniform film, and then add appropriate amount of phosphate buffer. The phospholipin film was continued to evaporate, i.e., the uniform liposome mixing solution was obtained, and then the polycarbonate film was used to obtain a blank liposome.

[0040] B. Blank liposome ultrafiltration concentration: Ultrafiltrate the blank liposomes in step A. The film material is a polyether sulfone, and the molecular weight is 100 kDa. The ultrafiltration membrane assembly film is 0.5 μm. ...

Embodiment 3

[0044] A method of preparation of ropivacin liposomes, the specific steps are as follows:

[0045] A. Preparation of white liposomes: 20 ml of 0.02 mol / L phosphate buffer, slowly added with a syringe to DEPC (diel phosphatidylcholine) 240 mg and chooseol 160 mg of trichloromethane solution (V organic phase: V water phase = 1: 1), high speed stirred emulsifue until a stable W / O type emulsion is formed, and the resulting emulsion is reduced to remove trichloromethane in a rotary evaporator (35 ° C) to form a uniform film, and then add appropriate amount of phosphate buffer. The phospholipin film was continued to evaporate, i.e., the uniform liposome mixing solution was obtained, and then the polycarbonate film was used to obtain a blank liposome.

[0046] B. Blank liposome ultrafiltration concentration: Ultrafiltrate the blank liposomes in step A. The membrane material is a polyether sulfone, and the medium is 100 kDa, the ultrafiltration membrane assembly film is 0.5 μm, the out...

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Abstract

The invention discloses a preparation method of a local anesthetic liposome, and belongs to the technical field of preparations. The preparation method of the local anesthetic liposome includes the steps of preparing a blank liposome; carrying out ultrafiltration concentration on the blank liposome; co-incubating drug to be encapsulated and the blank liposome, and performing sterilizing and filtering to obtain a drug-loaded liposome; and mixing the drug-loaded liposome with a poloxamer aqueous solution, performing subpackaging, performing freezing after subpackaging, and performing freeze-drying after subpackaging to prepare a liquid preparation, a frozen preparation or a freeze-dried preparation. According to the preparation method of the local anesthetic liposome, a local anesthetic liposome product with lower particle size, higher uniformity and higher entrapment rate can be prepared, the operation is simple, and industrial production is easy to realize.

Description

Technical field [0001] The present invention belongs to the art of the pharmaceutical preparation process, and more particularly to a local anesthetic liposome preparation method. Background technique [0002] Clinically used opioid drugs were treated with postoperative pain, but they had adverse respiratory respiratory inhibition and addiction. Local anesthetics are also the most important analgesic drugs, but the effective operation time of ordinary dosage forms is relatively short, so that the clinical use of the incision continuous analgesic device is carried out in the wound to maintain a certain treatment concentration. However, this device has certain defects, such as: the storage bag needs to carry it with you, inconvenient to the patient; the osmotic tube is placed in the body to increase local irritation, and there is a certain complications and osmotic catheter should not take problems, so development Long-acting bureau anesthetic new formulation has become a hot spot ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/10A61K45/00A61K31/445A61P23/02
CPCA61K9/127A61K47/10A61K45/00A61K31/445A61P23/02
Inventor 李锦王洋张国喜
Owner NANJING LUYE PHARMA
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