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Nimodipine micelle injection and preparation method thereof

A technology of nimodipine glue and micelle injection, 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 delivery. drug, improve water solubility and stability, low cost effect

Active Publication Date: 2014-06-18
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

[0055] It is called 50mg of egg yolk lecithin, sodium glycate acid of 50mg, and 1.25mg of Nimo -Hi -placed in a 50ml round bottle, add 10ml ethanol, dissolved, and uniform ultrasonic dispersion.Rotate the ethanol at 40 ° C at 40 ° C until the smell of no mellow, form a transparent film, and then disperse with a 2.5ml injection of water to obtain a dispersed solution with a mixed rubber beam.After adding 0.05%injection -level activated carbon and stirring for 15min, 12000rpm / min is separated for 5 minutes, and then filtered with 0.22 μm micropores filter, filtering, packaged, and sterilized at 121 ° C for 15 minutes.Bid injection.

[0056] According to the following examples, the solution efficiency is 96%, the concentration of Nimo Horizon is 0.48mg / ml, and the load is 1.2%.

Embodiment 2

[0058] It is called 50mg of egg yolk lecithin, 50mg of sodium glyceamate, and 1mg of Nimo -ground placed in a 50ml round bottle, add 10ml ethanol, dissolved, and uniform ultrasonic dispersion.Remove the ethanol again, the temperature of the water bath is 35 ° C, rotate until the mellow smell, forms a layer of transparent film, and then disperse with a 2.5ml injection of water to obtain a dispersed body solution with a mixed adhesive beam.After adding 0.05%injection -level activated carbon and stirring for 15min, 12000rpm / min is separated for 5 minutes, and then filtered with 0.22 μm micropores filter, filtering, packaged, and sterilized at 121 ° C for 15 minutes.Bid injection.

[0059] According to the following examples, the solution efficiency is 93%, the concentration of Nimo Horizon is 0.37mg / ml, and the loading capacity is 0.9%.

Embodiment 3

[0061] It is called 45mg of polymiel phospholipids, 40mg of sodium deoxate, and 1mg nimoen flat placed in a 50ml round bottle, adding 10ml ether, dissolved, and uniform ultrasonic dispersion.Under the temperature of the water bath, the rotation is steamed to remove the ether to form a layer of transparent film, and then disperse with a 2.5ml injection of water to obtain a dispersed body solution with a hybrid beam.After adding 0.05%injection -level activated carbon and stirring for 15min, 12000rpm / min is separated for 5 minutes, and then filtered with 0.22 μm micropores filter, filtering, packaged, and sterilized at 121 ° C for 15 minutes.Bid injection.

[0062] According to the following examples, the solution efficiency is 90%, the concentration of Nimo Horizon is 0.36mg / ml, and the loading capacity is 1.0%.

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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 present invention provides a Nimo Heping injection, which is specifically for Nimo Horizon's rubber injection, which belongs to the field of pharmaceutical technology. Background technique [0002] Nimo Ping is the second-generation 1,4-dihydrine pyridine calcium ion channel blocking agent. It is currently a commonly used medicine for cardiovascular and cerebrovascular. The main function is to prevent myocardialization by blocking the influx of calcium ions.Nemo Ping selectively suppress CA 2+ The calcium channels on the cell membrane enters the cells, which have the effects of dilating blood vessels and negative muscles, relaxing the smooth muscle of the blood vessels, reducing the peripheral vascular resistance, thereby reducing blood pressure.It acts on the smooth muscle of the cerebral blood vessels, expands the cerebral blood vessels, increases cerebral blood flow, and significantly reduces the ischemic brain damage caused by vascular spasm.In addi...

Claims

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Application Information

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Patent Type & Authority Patents(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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