Preparation method of liposome based on drug-phospholipid-cholesterol ternary complex

A ternary compound and cholesterol technology, which is applied in the direction of liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of unsuitability for industrialization, low production efficiency, high production cost, etc., and achieve easy industrial scale-up , reduced usage, high production efficiency

Active Publication Date: 2020-03-13
CHINA PHARM UNIV
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Problems solved by technology

[0007] However, the inventors have found through further research that in the prior art represented by the above-mentioned patents, although phospholipids and drugs or phospholipids, cholesterol and drugs are reacted to form binary or ternary complexes, but in the preparation of liposomes In the process, the thin-film dispersion method is inevitably used, and the thin-film dispersion method has obvious disadvantages: the method uses a lot of organic solvents, the amount of single treatment is small, and the production equipment occupies a large area, so the production efficiency Low, high production cost, not suitable for industrialization

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  • Preparation method of liposome based on drug-phospholipid-cholesterol ternary complex
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  • Preparation method of liposome based on drug-phospholipid-cholesterol ternary complex

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preparation example Construction

[0032] The method for preparing liposomes based on the drug-phospholipid-cholesterol ternary complex specifically implemented in the present invention includes:

[0033] The first step is to divide the prescription amount of phospholipids into the first amount of phospholipids and the second amount of phospholipids, the first amount is less than the second amount; take the target drug, the first amount of phospholipids and cholesterol into a container, and add a reaction solvent to make the material Dissolve completely, keep stirring at 30℃-80℃ for 1-8h, and then evaporate to remove the reaction solvent. The resulting product is placed in a vacuum for 8-16h to obtain a powdery solid or sponge-like semi-solid Drug-phospholipid-cholesterol ternary complex; the mass of the first amount of phospholipid is at least 3 times the mass of the target drug, and the mass ratio of the target drug to cholesterol is 1: (0.1-10); the amount of reaction solvent used is enough to 1-1.5 times the m...

Embodiment 1

[0041] The mass volume concentration (g / ml) of each component in the prescription is:

[0042] Baicalein 0.8%

[0043] Egg yolk lecithin 16.08%

[0044] Cholesterol 1.36%

[0045] The balance is pure water.

[0046] Preparation process: According to the above prescription, weigh baicalein, cholesterol and 3 times the mass of baicalein's egg yolk lecithin (that is, the mass ratio of baicalein to the first amount of egg yolk lecithin is 1:3, and the mass ratio of baicalein to cholesterol is 1:1.7), placed in an eggplant-shaped bottle, using tetrahydrofuran as the reaction solvent to completely dissolve the three, and after stirring at 30°C for 1 hour, the solvent was removed by evaporation, and the resulting product was kept under vacuum for 12 hours to obtain baicalein-egg yolk lecithin- Cholesterol ternary complex, take out, protect from light, and store in a cool place. The essence of this step is to prepare a ternary complex of baicalein-egg yolk lecithin-cholesterol by the solvent...

Embodiment 2

[0050] The mass volume concentration (g / ml) of each component in the prescription is:

[0051] Quercetin 0.2%

[0052] Egg yolk lecithin 4.49%

[0053] Cholesterol 0.4%

[0054] The balance is pure water.

[0055] Preparation process: According to the above prescription, weigh quercetin, cholesterol and egg yolk lecithin with 3.2 times the mass of quercetin (that is, the mass ratio of quercetin to the first amount of egg yolk lecithin is 1:3.2, quercetin and cholesterol The mass ratio is 1:2), placed in an eggplant-shaped bottle, using tetrahydrofuran as the reaction solvent to completely dissolve the three, and after stirring at 55°C for 4 hours, the solvent is evaporated and the resulting product is kept under vacuum for 12 hours to obtain quercetin -Egg yolk lecithin-cholesterol ternary complex, take it out, avoid light, and store in a cool place.

[0056] Weigh the remaining egg yolk lecithin in the prescription (that is, the second amount of egg yolk lecithin, the mass of the seco...

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Abstract

The invention relates to a liposome preparation method based on a drug-phospholipid-cholesterol ternary complex. The method comprises the steps of dividing phospholipid in prescription dosage into phospholipid in first dosage and phospholipid in second dosage, preparing the drug-phospholipid-cholesterol ternary complex from a target drug, the phospholipid in the first dosage and cholesterol, preparing phospholipid aqueous dispersion liquid from the phospholipid in the second dosage, and putting the drug-phospholipid-cholesterol ternary complex obtained in the first step in the phospholipid aqueous dispersion liquid for treatment to form a drug liposome. According to the method, the consumption of an organic solvent can be reduced; the treatment capacity of a single time is high; the technology is simple; the production efficiency is high; industrial amplification is easy.

Description

Technical field [0001] The invention relates to a method for preparing liposomes based on a medicine-phospholipid-cholesterol ternary complex, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] According to reports, at least 40% of the drugs in the development of new drugs exhibit low water solubility, which may lead to unsatisfactory oral bioavailability or difficulty in developing into liquid formulations (such as injections, etc.), thus becoming a bottleneck restricting drug development . Traditional strategies to improve the solubility of poorly soluble drugs include the formation of soluble salts, pH adjustment, latent dissolution, and solubilization. However, for some drugs, even if the above methods are used, it is sometimes difficult to reach a concentration suitable for clinical use, or there is a potential safety risk due to excessive use of excipients. Therefore, researchers have been exploring more and safer methods for ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K31/352A61K31/405
CPCA61K9/127A61K31/352A61K31/405A61K47/24A61K47/28
Inventor 柯学王悦陈默钱康侯玉婷袁梦
Owner CHINA PHARM UNIV
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