Liposome preparation method based on drug-phospholipid-cholesterol ternary complex

A technology of ternary complex and cholesterol, which is applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of unsuitability for industrialization, low production efficiency and high production cost, and achieves easy industrialization and amplification , High production efficiency, the effect of reducing the amount of use

Active Publication Date: 2017-05-31
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 example Construction

[0032] The liposome preparation method based on the drug-phospholipid-cholesterol ternary complex embodied by the present invention comprises:

[0033] The first step, the phospholipid of prescription amount is divided into the phospholipid of the first dosage and the phospholipid of the second dosage, and the first dosage is less than the second dosage; Get target medicine, the phospholipid of the first dosage and cholesterol put container, add reaction solvent to make material Dissolve completely, keep stirring at 30°C-80°C for 1-8h, then evaporate to remove the reaction solvent, place the product in vacuum for 8-16h, and then get powdery solid or spongy semi-solid Drug-phospholipid-cholesterol ternary complex; the quality of the first amount of phospholipid is at least 3 times that of the target drug, and the mass ratio of the target drug to cholesterol is 1:(0.1-10); 1-1.5 times of the minimum amount for complete dissolution, and the reaction solvent is one of tetrahydrofu...

Embodiment 1

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

[0042] Baicalein 0.8%

[0043] Yolk Lecithin 16.08%

[0044] Cholesterol 1.36%

[0045] The balance is pure water.

[0046] Preparation process: according to the above prescription, take baicalein, cholesterol and egg yolk lecithin with 3 times the quality of baicalein (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 a reaction solvent to completely dissolve the three, and after stirring at 30°C for 1 hour, evaporated to remove the solvent, and kept the product under vacuum for 12 hours to obtain baicalein-egg yolk lecithin- Cholesterol ternary complex, take out, avoid light, and store in a sealed place in a cool place. The essence of this step is to prepare the baicalein-egg yolk lecithin-cholesterol ternary complex by solvent met...

Embodiment 2

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

[0051] Quercetin 0.2%

[0052] 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 quality 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 a reaction solvent to completely dissolve the three, and after stirring at 55°C for 4 hours, evaporated to remove the solvent, and kept the product under vacuum for 12 hours to obtain quercetin -Egg yolk lecithin-cholesterol ternary complex, take it out, keep it away from light, and keep it sealed in a cool place.

[0056] Weigh the remaining egg yolk lecithin in the prescription (i.e. the second dosage of egg yolk lecithin...

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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 liposome preparation method based on a drug-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 current new drug development show low water solubility, which may lead to unsatisfactory oral bioavailability, or it is difficult to develop into liquid preparations (such as injections, etc.), thus becoming a bottleneck restricting drug development . Traditional strategies to improve the solubility of poorly soluble drugs include forming soluble salts, adjusting pH, latent dissolution, and solubilization, etc. However, for some drugs, it is sometimes difficult to achieve a concentration suitable for clinical use even with the above methods, or there may be potential safety risks due to excessive use of excipients. Therefore, researchers have been exploring more and safer methods for improvi...

Claims

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Application Information

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Patent Type & Authority Applications(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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