Nimodipine micelle injection and preparation method thereof

A technology of nimodipine glue and micelle injection, which is applied in the field of medicine, can solve the problems of increasing the pain of patients and the mental burden of medical workers, not fundamentally solving the problems of serious side effects of organic solvents, increasing treatment costs, etc., and achieving convenient clinical administration. Drug, improve water solubility and stability, low cost effect

Active Publication Date: 2012-07-04
SICHUAN BAILI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the above method can reduce the incidence of phlebitis and reduce the degree of phlebitis, it does not fundamentally solve the serious side effects caused by organic solvents, which not only greatly increases the pain and mental burden of patients and the workload of medical workers, but also Greatly increase the cost of treatment and limit its clinical application

Method used

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  • Nimodipine micelle injection and preparation method thereof
  • Nimodipine micelle injection and preparation method thereof
  • Nimodipine micelle injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Weigh 50 mg of egg yolk lecithin, 50 mg of sodium glycocholate, and 1.25 mg of nimodipine into a 50 ml round bottom flask, add 10 ml of ethanol to dissolve, and disperse evenly by ultrasonication. The ethanol was removed by rotary evaporation at a water bath temperature of 40° C. until there was no alcohol smell and a layer of transparent film was formed, and then dispersed with 2.5 ml of water for injection to obtain a dispersion solution of drug-containing mixed micelles. After adding 0.05% activated carbon for injection and stirring for 15 minutes, centrifuge at 12000rpm / min for 5 minutes, then filter with a 0.22μm microporous membrane, take the filtrate, subpackage, and sterilize by autoclaving at 121°C for 15 minutes to obtain nimodipine mixed gel Bundle of injections.

[0060] The solubilization efficiency measured according to Example 5 below was 96%, the concentration of nimodipine was 0.48 mg / ml, and the drug loading was 1.2%.

[0061]

Embodiment 2

[0063] Weigh 50 mg of egg yolk lecithin, 50 mg of sodium glycocholate, and 1 mg of nimodipine into a 50 ml round bottom flask, add 10 ml of ethanol to dissolve, and disperse evenly by ultrasonication. Then spin evaporate to remove ethanol, the water bath temperature is 35 ℃, spin to no alcohol smell, form a layer of transparent film, then disperse with 2.5ml of water for injection, obtain the dispersion solution containing drug mixed micelles. After adding 0.05% activated carbon for injection and stirring for 15 minutes, centrifuge at 12000rpm / min for 5 minutes, then filter with a 0.22μm microporous membrane, take the filtrate, subpackage, and sterilize by autoclaving at 121°C for 15 minutes to obtain nimodipine mixed gel Bundle of injections.

[0064] The solubilization efficiency measured according to Example 5 below was 93%, the concentration of nimodipine was 0.37 mg / ml, and the drug loading was 0.9%.

[0065]

Embodiment 3

[0067] Weigh 45mg of polyene phosphatidylcholine, 40mg of sodium deoxycholate, and 1mg of nimodipine into a 50ml round bottom flask, add 10ml of ether, dissolve, and disperse evenly by ultrasonication. At a water bath temperature of 35° C., diethyl ether was removed by rotary evaporation to form a transparent film, which was then dispersed with 2.5 ml of water for injection to obtain a dispersion solution containing drug-mixed micelles. After adding 0.05% activated carbon for injection and stirring for 15 minutes, centrifuge at 12000rpm / min for 5 minutes, then filter with a 0.22μm microporous membrane, take the filtrate, subpackage, and sterilize by autoclaving at 121°C for 15 minutes to obtain nimodipine mixed gel Bundle of injections.

[0068] According to Example 5 below, the solubilization efficiency was 90%, the concentration of nimodipine was 0.36 mg / ml, and the drug loading was 1.0%.

[0069]

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Abstract

The invention discloses a nimodipine micelle injection and a preparation method thereof. The nimodipine micelle injection is prepared by using active ingredients, i.e. nimodipine and phospholipid/bile salt. According to the nimodipine micelle injection disclosed by the invention, the solubility of the nimodipine is greatly increased, and no crystal precipitation exists when the nimodipine micelle injection is diluted; the biocompatibility of the phospholipid/bile salt is good, and organic solvents with great toxic side effects, such as ethyl alcohol, propylene glycol and the like, are not needed to for solubilizing so that the toxicity of the nimodipine micelle injection is lowered, the vascular stimulation is little, and the adverse reaction of the nimodipine micelle injection is reduced; and the nimodipine micelle injection can be directly used for intravenous injection and can also be used for instilling after the nimodipine micelle injection is diluted to various degrees, and thus, the clinical administration is greatly facilitated.

Description

technical field [0001] The invention provides a nimodipine injection, specifically a nimodipine micellar injection, which belongs to the technical field of medicine. Background technique [0002] Nimodipine is a second-generation 1,4-dihydropyridine calcium ion channel blocker. It is currently a commonly used cardiovascular and cerebrovascular drug. Its main function is to cause myocardial cell depolarization by blocking the influx of calcium ions. Nimodipine selectively inhibits Ca 2+ Entering the cell through the calcium channel on the cell membrane, it has the effect of dilating blood vessels and negative muscle strength, relaxing vascular smooth muscle, reducing peripheral vascular resistance, thereby lowering blood pressure, but the blood flow of the brain, coronary arteries and kidneys does not decrease; it can selectively It acts on smooth muscle of cerebral vessels, expands cerebral vessels, increases cerebral blood flow, and significantly reduces ischemic brain inj...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4422A61P1/04A61P9/10A61P9/12A61P11/00A61P19/08A61P21/00A61P25/02A61P25/06A61P25/28A61P27/16A61P31/12
Inventor 龚涛孙逊
Owner SICHUAN BAILI PHARM CO LTD
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