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Huperzine-a lipid micro-sphere preparation

A technology of huperzine A lipid and huperzine A, which is applied in the field of medicine, can solve problems such as difficult dissolution of huperzine A water, achieve the goal of no toxic side effects, reduce irritation and side effects, and improve cognitive function Effect

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

[0006] The object of the present invention is to provide a kind of huperzine A lipid microsphere preparation and preparation method thereof, the present invention not only has good curative effect, and has overcome the shortcoming that huperzine A water is not easy to dissolve, has reduced irritation and side effect (dizziness, nausea, vomiting, sweating, etc.), improved drug stability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 : Huperzine A lipid microsphere preparation, including:

[0032]

[0033]

[0034] The preparation method of huperzine methyl lipid microsphere preparation:

[0035] (1) Preparation of the oil phase: Take 1g of hydrogenated egg yolk lecithin, add ethanol to dissolve it, add huperzine A and stir to dissolve it, evaporate the ethanol under reduced pressure, then add the remaining hydrogenated egg yolk lecithin and acetylated monoglyceride 1. Soybean oil, in a water bath at 70-80°C, stirring to make it dissolve, to obtain the oil phase;

[0036] (2) Preparation of the water phase: adding glycerin to water, stirring to dissolve it, and heating to 70-80°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 70-80°C, disperse through high-speed shearing, the shearing speed is 2000rpm, and the time is 120 minutes. get colostrum;

[0038] (4) The colostrum is rapid...

Embodiment 2

[0040] Example 2 : Huperzine A lipid microsphere preparation, including:

[0041]

[0042] The preparation method of huperzine methyl lipid microsphere preparation:

[0043] (1) Preparation of the oil phase: Take 0.5 g of soybean lecithin, add ethanol to dissolve it, add huperzine A and stir to dissolve it, evaporate the ethanol with nitrogen while stirring, then add the remaining soybean lecithin, soybean oil, acetyl Melt monoglyceride, bath in 70-80°C water, stir to dissolve, and obtain oil phase;

[0044] (2) Preparation of the water phase: adding trehalose into water, stirring to dissolve it, and heating to 70-80°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 70-80°C, disperse through high-speed shearing, the shearing speed is 10000rpm, and the time is 120 minutes. get colostrum;

[0046](4) The colostrum is rapidly cooled to 15-40°C, homogenized by a high-pressur...

Embodiment 3

[0048] Example 3 : Huperzine A lipid microsphere preparation, including:

[0049]

[0050] The preparation method of huperzine methyl lipid microsphere preparation:

[0051] (1) Preparation of the oil phase: take 10 g of hydrogenated egg yolk lecithin, add ethanol to dissolve it, add huperzine A and stir to dissolve it, evaporate the ethanol with nitrogen while stirring, then add soybean lecithin, corn oil, acetylated mono Glyceride, in a water bath at 70-80°C, stir to dissolve to obtain an oil phase;

[0052] (2) Preparation of the water phase: adding sorbitol into water, stirring to dissolve it, and heating to 70-80°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 70-80°C, disperse through high-speed shearing, the shearing speed is 5000rpm, and the time is 60 minutes. get colostrum;

[0054] (4) The colostrum is rapidly cooled to 15-40°C, homogenized by a high-pressur...

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Abstract

The invention discloses a huperzine-a lipid micro-sphere preparation. The huperzine-a lipid micro-sphere preparation is mainly made of huperzine-a, oil for injection, emulsifiers and isotonic agents. The huperzine-a lipid micro-sphere preparation has the advantages that perfect treatment effects can be realized, problems of insolubilization of huperzine-a in water and adverse reaction under high-dosage conditions can be solved, the stability of medicine can be improved, irritation and toxic reaction can be reduced, the quality of preparation products can be improved, and the huperzine-a lipid micro-sphere preparation is applicable to industrial large-scale production.

Description

technical field [0001] The invention relates to a lipid microsphere preparation, in particular to a huperzine A lipid microsphere preparation and a preparation method thereof, belonging to the technical field of medicine Background technique [0002] Huperzine A [Huperzine A, HupA] is a semiterpene alkaloid isolated from the fern Huperzine serrata, which is a highly efficient, highly selective and reversible acetylcholinesterase (AchE) inhibitor. Huperzine A is white or off-white to slightly yellow crystalline powder, with a melting point of 228-230°C, easily soluble in methanol and chloroform, soluble in ethanol, and insoluble in water. Animal experiments show that this product is rapidly and completely absorbed orally, and the distribution is also fast. The half-life of the distribution phase is 9.8 minutes, and the bioavailability is high. The half-life of the elimination phase is 247.5 minutes. Modern pharmacological studies have shown that huperzine A can be combined w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/4748A61K47/24A61K47/44A61K47/14A61P25/28A61P25/00A61P21/04
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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