Liposome containing local anesthetic and preparation method thereof

A technology of local anesthetics and liposome composition, which is applied in the direction of medical preparations containing active ingredients, liposome delivery, anesthetics, etc., and can solve the problems of poor stability, easy oxidation and deterioration, etc.

Pending Publication Date: 2022-06-28
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the stability of the buffer system such as histidine is poor, and it is easy to oxidize and deteriorate, which makes the product have potential quality risks

Method used

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  • Liposome containing local anesthetic and preparation method thereof
  • Liposome containing local anesthetic and preparation method thereof
  • Liposome containing local anesthetic and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1: Preparation of ropivacaine liposomes

[0056]

[0057] Note: (1) and (2) are removed during preparation, (3) is only added during reconstitution.

[0058] DMPC, cholesterol, and ropivacaine free base in the prescribed amounts were weighed and dissolved in an 80% tert-butanol-water mixed solution. The sample was lyophilized in a lyophilizer to produce a solid composition. The ropivacaine liposome is obtained by redissolving with the reconstituting solution and mixing evenly. The content (calculated as ropivacaine free base) and encapsulation efficiency of each prescription liposome were obtained by detection, as shown in the following table.

[0059]

Embodiment 2

[0060] Example 2: In vitro release of ropivacaine liposomes

[0061] 1. Cleaning of the dialysis bag:

[0062] Weigh 10g of sodium bicarbonate and 0.168g of EDTA·2Na in 500ml of water and mix well. Cut the dialysis bag into 10cm pieces, boil it with lotion in a 1L beaker for 10min, then wash the dialysis bag with 200ml of purified water for 10 times; add 500ml of purified water and boil for 10min. The dialysis bags that have not been used for a long time can be stored in 10% ethanol and washed 10 times with 200ml of purified water each time before use.

[0063] 2. Configuration of release media:

[0064] Weigh 2.3g potassium dihydrogen phosphate, 7.6g dipotassium hydrogen phosphate trihydrate, 5.6g sodium chloride and 132mg ammonium sulfate in a 1000ml volumetric flask, add water to volume, and mix well.

[0065] 3. Stakeout and sampling measurement of release samples:

[0066] Use a pipette to accurately measure 1.0ml of the liposome solution to be tested and add it to a 10...

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Abstract

The invention relates to a liposome containing a local anesthetic and a preparation method thereof. Specifically, the present disclosure relates to liposomes comprising (1) a lipid comprising at least one phospholipid, and (2) a free base of a local anesthetic; and a hydrating fluid comprising a pharmaceutically acceptable salt, complex or chelate of a local anesthetic, the liposome having improved release properties.

Description

technical field [0001] The present disclosure belongs to the field of pharmacy, and relates to a liposome containing a local anesthetic and a preparation method thereof. Background technique [0002] Liposomes, also known as lipid vesicles, are fully enclosed lipid bilayer membranes that contain an internal volume containing an aqueous medium. Lipid bilayers are typically composed of phospholipids such as lecithin and related materials such as glycolipids. Lipid bilayer membranes generally function in a manner similar to cell membranes. They thus exhibit some biological properties, such as the ability to be readily accepted into the environment of living cells. Accordingly, in recent years there has been increasing interest in the use of liposomes as vehicles for the delivery of compounds with particular biological or pharmaceutical properties to patients. [0003] Liposomes can be divided into unilamellar liposomes and multilamellar liposomes according to the number of b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/445A61P23/02A61P29/00A61K9/08
CPCA61K9/1277A61K31/445A61K9/08A61P23/02A61P29/00
Inventor 仝新勇邹爱峰段子卿李东王萍萍邬程伟马中华
Owner JIANGSU HENGRUI MEDICINE CO LTD
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