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A kind of sulfuric acid or berberine hydrochloride multivesicular liposome and preparation method thereof

A technology of berberine hydrochloride and multivesicular liposomes, which is applied in the field of liposomes, hydrochloric acid or sulfated liposomes, can solve the problem of high solubility of berberine sulfate or berberine hydrochloride, the inability to obtain stable final products, and the difficulty of multivesicular systems Damaged and other problems, to achieve the effect of good appearance, uniform size and large number of vesicles

Active Publication Date: 2019-12-13
SOUTHWEST UNIVERSITY FOR NATIONALITIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Different from the above-mentioned products, berberine sulfate or berberine hydrochloride has high solubility in water, and the encapsulation efficiency is low when using common multivesicular liposome preparation methods, the multivesicular system is easily destroyed, and complex coagulation problems are prone to occur during the preparation process, so it is impossible to obtain stable end product

Method used

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  • A kind of sulfuric acid or berberine hydrochloride multivesicular liposome and preparation method thereof
  • A kind of sulfuric acid or berberine hydrochloride multivesicular liposome and preparation method thereof
  • A kind of sulfuric acid or berberine hydrochloride multivesicular liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] (1) Dissolve 0.2g of lecithin, 0.1g of cholesterol, 0.1mL of oleic acid, and 0.5mL of triolein in 7.5mL of a mixed solvent of 1:1 by volume of ethyl ether and chloroform. In the oil phase;

[0050] (2) Dissolve berberine sulfate with a mass of 0.0375g in 7.5mL of a 5wt% sucrose solution to form an internal aqueous phase;

[0051] (3) Take the internal water phase with a volume ratio of 1:1 to the oil phase and slowly inject it into the oil phase, and pass it through a high-speed homogenizer at 12000r.min -1 Homogenize for 9 minutes at a rate of, to obtain colostrum;

[0052] (4) Measure 4mL of colostrum and quickly pour it into the mixed solution to form the outer water phase, and pass it through a high-speed homogenizer at 9500r.min -1 Homogenize for 1 min at a rate of 1 to obtain a double emulsion. The concentration of L-lysine in the mixed solution is 40 mmol.L -1 , The concentration of sodium alginate is 0.5wt%, and the concentration of glucose is 5wt%;

[0053] (5) Continu...

Embodiment 2

[0057] (1) Dissolve 0.2g of lecithin, 0.2g of cholesterol, 0.5mL of oleic acid, and 0.3mL of triolein in 7.5mL of a mixed solvent of ethyl ether and chloroform with a volume ratio of 0.5:1 to obtain oil phase;

[0058] (2) Dissolve 0.1 g of berberine sulfate in 3.75 mL of sucrose solution with a concentration of 7 wt% to form an internal aqueous phase;

[0059] (3) Take the internal water phase with a volume ratio of 0.5:1 to the oil phase and slowly inject it into the oil phase, and pass it through a high-speed homogenizer at 10000r.min -1 Homogenize for 15 min at a rate of, to obtain colostrum;

[0060] (4) Measure 5mL of colostrum and quickly pour it into the mixed solution to form the outer water phase, and pass it through a high-speed homogenizer at 9000r.min -1 Homogenize for 3 minutes at a rate of 3 to obtain a double emulsion. The concentration of L-lysine in the mixed solution is 30 mmol.L -1 , The concentration of sodium alginate is 0.3wt%, and the concentration of glucose ...

Embodiment 3

[0064] (1) Dissolve 0.2g of lecithin, 0.04g of cholesterol, 0.3mL of oleic acid, 0.4mL of triolein in 7.5mL of a mixed solvent of ethyl ether and chloroform with a volume ratio of 1.5:1 to obtain the oil phase ;

[0065] (2) Dissolve 0.05 g of berberine sulfate in 11.25 mL of sucrose solution with a concentration of 6 wt% to form an internal aqueous phase;

[0066] (3) Take the internal water phase with a volume ratio of 1.5:1 to the oil phase and slowly inject it into the oil phase, and pass it through a high-speed homogenizer at 11000r.min -1 Homogenize for 10 min at a rate of 100 to obtain colostrum;

[0067] (4) Measure 6mL of colostrum and quickly pour it into the mixed solution to form the outer water phase, and pass it through a high-speed homogenizer at 10000r.min -1 Homogenize for 1 min at a rate of 1 to obtain a double emulsion. The concentration of L-lysine in the mixed solution is 50 mmol.L -1 , The concentration of sodium alginate is 0.4wt%, and the concentration of gluc...

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Abstract

The invention discloses a berberine sulfate or hydrochloride multi-vesicular liposome and a preparation method thereof. The preparation method comprises the following steps: dissolving lecithin, cholesterol, oleic acid and triolein into a mixed solvent to form an oil phase; dissolving berberine sulfate or hydrochloride into a cane sugar solution to form an inner water phase; preparing primary emulsion through the inner water phase and the oil phase; adding the primary emulsion into a specific mixed solution so as to obtain compounded emulsion; and finally performing preparation, thereby obtaining the berberine sulfate or hydrochloride multi-vesicular liposome which is high in berberine sulfate or hydrochloride encapsulation efficiency, large in drug loading capacity, remarkable in slow-release effect, stable in drug release concentration, high in vesicle content and uniform in appearance.

Description

Technical field [0001] The present invention relates to the technical field of liposomes, in particular to the technical field of hydrochloric acid or sulfate liposomes. Background technique [0002] Berberine, also known as berberine, is the active ingredient of the traditional Chinese medicine Coptis, an isoquinoline alkaloid, and has been used in China and India for more than 3,000 years. It can treat diarrhea caused by various causes. Berberine sulfate is the sulfate of berberine, especially suitable for veterinary use. It is used in livestock and poultry, piglet red diarrhea, yellow diarrhea, white diarrhea, enteritis, edema, paratyphoid fever, etc. caused by sensitive bacteria and treponema infection. Berberine hydrochloride is the hydrochloride of berberine, which is more suitable for human use. It has a broad antibacterial spectrum and can be used to treat gastroenteritis, bacillary dysentery, conjunctivitis, suppurative otitis media and other diseases. It also has block...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/12A61K47/24A61K47/14A61K47/28A61K31/4375A61P1/12A61P1/00A61P27/02A61P27/16
CPCA61K9/0002A61K9/127A61K31/4375A61K47/12A61K47/14A61K47/24A61K47/28
Inventor 何黎黎张玉燕
Owner SOUTHWEST UNIVERSITY FOR NATIONALITIES
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