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Nicergoline lipid microspheres agent

A technology of nicergoline lipid and lipid microspheres, applied in the field of medicine, can solve problems such as the insoluble stability of Nicergoline water, and achieve the effects of no toxic and side effects, improving curative effect, and improving solubility and stability

Inactive Publication Date: 2015-10-07
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of Nicergoline lipid microsphere preparation and preparation method thereof, the present invention not only has good curative effect, and overcomes the shortcoming that Nicergoline is not easily soluble in water and poor stability, in addition, the present invention also has good drug loading and encapsulation efficiency

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  • Nicergoline lipid microspheres agent
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Nicergoline lipid microsphere formulations, including:

[0033]

[0034] The preparation method of nicergoline lipid microsphere preparation:

[0035] (1) Preparation of oil phase: get phosphatidylglycerol 0.5g, add ethanol and make it dissolve, add Nicergoline and vitamin C and stir to make it dissolve, evaporate ethanol under reduced pressure, then add remaining phosphatidylglycerol and ethyl oleate Esters and propylene glycol diesters were dissolved in a water bath at 40°C and stirred to obtain an oil phase;

[0036] (2) Preparation of the water phase: adding glycerin to water, stirring to dissolve it, and heating to 40°C to obtain the water phase;

[0037] (3) Preparation of colostrum: Add the oil phase in step (1) to the water phase in step (2) at a temperature of 40° C., and disperse through high-speed shearing at a shear rate of 5000 rpm for 30 minutes to obtain the initial colostrum milk;

[0038] (4) Rapidly cool the colostrum to 15°C, maintai...

Embodiment 2

[0040] Example 2: Nicergoline lipid microsphere formulations, including:

[0041]

[0042] The preparation method of nicergoline lipid microsphere preparation:

[0043] (1) Preparation of oil phase: get phosphatidylglycerol 6g, add methanol to dissolve it, add nicergoline and oleic acid and stir to make it dissolve, evaporate methanol to dryness under reduced pressure, then add remaining phosphatidylglycerol and ethyl oleate 1. Propylene glycol diester, in a water bath at 60°C, stir to dissolve it, and obtain the oil phase;

[0044] (2) Preparation of the water phase: adding mannitol into water, stirring to dissolve it, and heating to 60° C. to obtain the water phase;

[0045] (3) Preparation of colostrum: Add the oil phase in step (1) to the water phase in step (2) at a temperature of 60° C., and disperse through high-speed shearing at a shear rate of 10,000 rpm for 120 minutes to obtain the initial milk;

[0046] (4) Rapidly cool the colostrum to 30°C, maintain this ...

Embodiment 3

[0048] Example 3: Nicergoline lipid microsphere formulations, including:

[0049]

[0050] The preparation method of nicergoline lipid microsphere preparation:

[0051] (1) Preparation of oil phase: get phosphatidylglycerol 3g, add chloroform and make it dissolve, add Nicergoline and cholesterol and stir to make it dissolve, evaporate chloroform under reduced pressure, then add remaining phosphatidylglycerol and ethyl oleate, Propylene glycol diester, in a water bath at 50°C, stirred to dissolve to obtain an oil phase;

[0052] (2) Preparation of the water phase: adding mannitol into water, stirring to dissolve it, and heating to 50° C. to obtain the water phase;

[0053] (3) Preparation of colostrum: Add the oil phase in step (1) to the water phase in step (2) at a temperature of 50°C, disperse through high-speed shearing, the shearing speed is 8000rpm, and the time is 60 minutes to obtain the initial colostrum milk;

[0054] (4) Rapidly cool the colostrum to 20°C, main...

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Abstract

A nicergoline lipid microspheres agent is mainly prepared by nicergoline, oil for injection, an emulsifying agent and an isotonic agent. The nicergoline lipid microspheres agent has a perfect curative effect, the problems that the nicergoline cannot be dissolved in water and unwelcome reactions can be produced when the dosage of the nicergoline is large are solved, the medicine stability is improved, irritation and toxic reaction are reduced, the quality of the nicergoline lipid microspheres agent is improved, and the nicergoline lipid microspheres agent is suitable to be industrially produced widely.

Description

technical field [0001] The invention relates to a lipid microsphere preparation, in particular to a nicergoline lipid microsphere preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] In the current market, Nicergoline is a semi-synthetic ergot alkaloid derivative, which has α-receptor blockade and vasodilator effect, can strengthen the metabolism of brain cell energy, increase the utilization of oxygen and glucose; promote the production of neurotransmitter dopamine Convert to increase nerve conduction; strengthen brain protein synthesis and improve brain function. Clinically, it is mainly used to improve cerebral arteriosclerosis and cerebral arteriosclerosis and cerebral apoplexy sequela caused by low desire and emotional disorders, such as slow response, inattention, memory loss, lack of ideas, depression, restlessness, etc.; acute and chronic peripheral circulation disorders; also applicable For vascul...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/48A61K47/14A61K47/24A61P9/10A61P25/00A61P25/28A61P13/00
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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