Betahistine hydrochloride liposome and preparation method thereof

A technology of betahistine and liposome preparation, which is applied in the field of betahistine hydrochloride liposome and its preparation, can solve skin itching and other problems, achieve the goal of enhancing drug efficacy, reducing adverse drug reactions, and improving therapeutic effect Effect

Active Publication Date: 2012-08-15
黑龙江亿达鸿药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, there are some adverse reactions of betahistine hydrochloride in the common dosage form, such as occasional dry mouth, stomach discomfort, palpitations, skin itching, etc. In some cases, nausea, dizziness, dizziness, sweating, etc.

Method used

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  • Betahistine hydrochloride liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation method of the present invention:

[0026] (1) Weigh lecithin and phytosterol according to the mass ratio of 3:1, and then dissolve them with 20mL of dichloromethane. After completely dissolving, evaporate under reduced pressure until a film is formed;

[0027] (2) Pour 40mL of ether into the lipid film, so that the film is completely dissolved in ether;

[0028] (3) Prepare a phosphate buffer solution containing 5 mg / mL of betahistine hydrochloride, the pH of which is 5.7;

[0029] (4) Mix the solution described in step (2) (3) evenly, and sonicate for 15 minutes;

[0030] (5) The mixed solution after ultrasonication is evaporated under reduced pressure on a rotary evaporator until all organic reagents evaporate;

[0031] (6) Pass the suspension prepared above through a high-pressure homogenizer with a pressure of 500 bar, and then pass through a liposome extruder (filter membrane pore size is 0.4 μm) to obtain betahistine hydrochloride liposomes (experime...

Embodiment 2

[0040] Preparation method of the present invention:

[0041] (1) Weigh lecithin and phytosterol according to the mass ratio of 4:1, and then dissolve the two in 25mL of dichloromethane. After completely dissolving, evaporate under reduced pressure until a film is formed;

[0042] (2) Pour 60mL of ether into the lipid film, so that the film is completely dissolved in ether;

[0043] (3) Prepare a phosphate buffer solution containing 10 mg / mL of betahistine hydrochloride, the pH of which is 6.5;

[0044] (4) Mix the solution described in step (2) (3) evenly, and sonicate for 20 minutes;

[0045] (5) The mixed solution after ultrasonication is evaporated under reduced pressure on a rotary evaporator until all organic reagents evaporate;

[0046] (6) Pass the above-prepared suspension through a high-pressure homogenizer with a pressure of 800 bar, and then pass it through a liposome extruder (with a filter membrane pore size between 0.3 μm) to obtain betahistine hydrochloride li...

Embodiment 3

[0056] Preparation method of the present invention:

[0057] (1) Weigh lecithin and phytosterol according to the mass ratio of 5:1, and then dissolve the two in 25mL of dichloromethane. After completely dissolving, evaporate under reduced pressure until a film is formed;

[0058] (2) Pour 60mL of ether into the lipid film, so that the film is completely dissolved in ether;

[0059] (3) Prepare a phosphate buffer solution containing 20 mg / mL of betahistine hydrochloride, the pH of which is 6.8;

[0060] (4) Mix the solution described in (2) (3) evenly, and sonicate for 20 minutes;

[0061] (5) The mixed solution after ultrasonication is evaporated under reduced pressure on a rotary evaporator until all organic reagents evaporate;

[0062] (6) Pass the above-prepared suspension through a high-pressure homogenizer with a pressure of 900 bar, and then pass it through a liposome extruder (the filter membrane pore size is between 0.5 μm) to obtain betahistine hydrochloride liposom...

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Abstract

The invention relates to a betahistine hydrochloride liposome and a preparation method of the betahistine hydrochloride liposome. The preparation method comprises the steps of: firstly dissolving lipide ingredients in methylene dichloride, and carrying out reduced-pressure evaporation in water bath until a film is formed; dissolving the film in diethyl ether, and then adding phosphate buffer containing betahistine into the solution; carrying out ultrasonic treatment on the mixed suspension liquid, placing the treated liquid on a rotary evaporator, and carrying out reduced-pressure vaporization until all the organic reagent is evaporated; and finally, obtaining the betahistine hydrochloride liposome. The betahistine hydrochloride is made into liposome, so that the medicine effect is obviously improved, the permeability of blood capillary can be improved, and the dosage of the medicine reaching blood vessels of the brain can be increased; the betahistine hydrochloride liposome is used for improving the treatment effect of Meniere syndrome, reduces the gastrointestinal irritation and the adverse drug reaction, and is beneficial to reducing the side effects such as stomach upset, nausea, dizziness and the like.

Description

technical field [0001] The invention relates to a betahistine hydrochloride liposome and a preparation method thereof, belonging to the technical field of pharmaceutical preparations and preparation methods thereof. Background technique [0002] Betahistine hydrochloride has a more obvious expansion effect on cerebrovascular and cardiovascular, especially on the vertebral artery system, can increase blood flow in the heart, brain and peripheral circulation, improve blood circulation, and lower systemic blood pressure. In addition, it can increase cochlear and Anterior blood flow, thereby eliminating inner ear vertigo, tinnitus and ear closure, can also increase capillary permeability, promote the absorption of extracellular fluid, and eliminate lymphatic edema; it can resist the vasoconstriction effect of catecholamines and reduce arterial pressure. And it can inhibit plasma coagulation and platelet aggregation induced by ADP, can prolong the time of thrombosis in vitro in ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4402A61K47/28A61P9/08A61P9/10A61P7/10A61P9/12A61P7/02A61P27/16A61P1/08
Inventor 滕利荣王立英张瑶刘明石孟凡欣杨东生赵明智吴丽艳金元宝王艳珍孟庆繁
Owner 黑龙江亿达鸿药业有限公司
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