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A freeze-dried preparation containing lipid vesicles

A technology for lipid vesicles and freeze-dried preparations, applied in the field of freeze-dried preparations, can solve problems such as difficulty in lubricating joints, inability to provide suitable lubrication, and cardiovascular damage to the liver and kidneys.

Active Publication Date: 2022-04-05
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically used analgesics or anti-inflammatory drugs are mainly oral preparations, and patients are prone to gastrointestinal adverse reactions after taking them for a long time, and there are certain damages to the liver, kidneys and cardiovascular system
Hyaluronic acid is easily decomposed by enzymes in the joints in a short period of time, and it is difficult to effectively lubricate the joints
[0005] It is well known that liposomes are able to provide a lubricating film to mitigate the effects of inflammatory injury, but in order to be effective the liposomes must be highly hydrated, highly compressible and very stable, lacking any of these properties Vesicles will not be able to provide the proper lubrication to overcome the lack of natural lubrication in inflamed joints

Method used

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  • A freeze-dried preparation containing lipid vesicles
  • A freeze-dried preparation containing lipid vesicles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Mix the prescribed amount of 1% PEGylated phospholipids and 10% mannose in ethanol, use phosphate buffer to adjust the pH of the solution to 6-8, stir well, add the prescribed amount of 50% DMPC, 25% DPPC and 14% cholesterol , the above solution is hydrated to obtain a lipid vesicle suspension, filtered through a filter membrane, the filtrate is subjected to filter sterilization treatment, and the water is removed by freeze drying to obtain a lipid vesicle preparation.

Embodiment 2

[0028] Mix the prescribed amount of 2% PEGylated phospholipids with 16% mannose in ethanol, use phosphate buffer to adjust the pH of the solution to 6-8, stir well, add the prescribed amount of 20% DMPC, 40% DPPC and 22% cholesterol , the above solution is hydrated to obtain a lipid vesicle suspension, filtered through a filter membrane, the filtrate is subjected to filter sterilization treatment, and the water is removed by freeze drying to obtain a lipid vesicle preparation.

Embodiment 3

[0030] Mix the prescribed amount of 0.5% PEGylated phospholipids and 2% mannose in ethanol, use phosphate buffer to adjust the pH of the solution to 6-8, stir well, add the prescribed amount of 54.5% DMPC, 30.5% DPPC and 12.5% ​​cholesterol , the above solution is hydrated to obtain a lipid vesicle suspension, filtered through a filter membrane, the filtrate is subjected to filter sterilization treatment, and the water is removed by freeze drying to obtain a lipid vesicle preparation.

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Abstract

The invention provides a lyophilized preparation containing lipid vesicles, wherein the lipid vesicles are monolayer or multilayer lipid molecular layer vesicles, which contain PC phospholipids (phosphatidylcholine), PEGylated phospholipids (polyethylene glycol) Diol derivatized phospholipids), monosaccharides or polysaccharides capable of condensation with PEGylated phospholipids, and the monosaccharides or polysaccharides are condensed on the PEGylated phospholipids. The lipid vesicle preparation of the present invention has high compressibility, can stably exist in the joint cavity, plays a role of joint lubrication, and can effectively prevent and / or treat joint damage.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a freeze-dried preparation containing lipid vesicles. Background technique [0002] In a healthy joint, the bones are not connected directly but are held together by connective tissue that forms a capsule around the ends of the bones. The cartilage layer covers the ends of the bones in the joint and is composed of 1-2 mm thick collagen fibers, glycoproteins, and hyaluronic acid aggregates. The area between the bones in the capsule is filled with synovial fluid. The surface of the cartilage layer at the end is covered with a layer of phospholipids, which are anchored in the cartilage structure and act like a cushion when hydrated, absorbing and distributing the weight-bearing and mechanical forces experienced, allowing the joint to move freely without pain or discomfort. [0003] When joints are damaged, such as those caused by osteoarthritis, overuse, overweight, etc....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/12A61K9/19A61K47/24A61K47/28A61K47/26A61K47/36A61P19/02A61P29/00A61P19/06
CPCA61K9/1273A61K9/19A61K47/24A61K47/28A61K47/26A61K47/36A61P19/02A61P29/00A61P19/06
Inventor 周丽莹刘亚男陆潇筠佟淑文
Owner BEIJING TIDE PHARMA