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Preparation method of chlorogenic acid lipid nanoparticle solid dispersion

A technology of solid dispersion and lipid nanoparticles, which can be used in medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc., and can solve the problems of low drug percentage and large carrier amount.

Active Publication Date: 2019-08-06
BENGBU COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the amount of carrier used in the preparation of conventional solid dispersions is large, and the percentage of drugs is not high, so it is only suitable for small doses of drugs

Method used

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  • Preparation method of chlorogenic acid lipid nanoparticle solid dispersion
  • Preparation method of chlorogenic acid lipid nanoparticle solid dispersion
  • Preparation method of chlorogenic acid lipid nanoparticle solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1 prepares chlorogenic acid lipid nanoparticle solid dispersion

[0022] S1: Preparation of chlorogenic acid solution: Weigh 2 g of chlorogenic acid with a purity ≥ 98.5%, add it to 40 ml of absolute ethanol at room temperature, control the solid-liquid ratio to 0.05 g / ml, stir magnetically until completely dissolved, and obtain chlorogenic acid acid solution;

[0023] S2: Preparation of lipid film: at room temperature, add 6g of hydrogenated soybean lecithin, 2g of dipalmitoylphosphatidylethanolamine and 2g of cholesterol to 12.5ml of chloroform, control the solid-liquid ratio to 0.8g / ml, magnetically stir until completely dissolved, turn Into a rotary evaporator, chloroform was removed at 60°C to form a transparent lipid film;

[0024] S3: Preparation of chlorogenic acid nanoliposomes: at room temperature, drop 6.4ml of anhydrous ether on the surface of the lipid film to dissolve, then drop into the chlorogenic acid solution, transfer to a rotary evaporato...

Embodiment 2

[0026] Embodiment 2 prepares chlorogenic acid lipid nanoparticle solid dispersion

[0027] S1: Preparation of chlorogenic acid solution: Weigh 2 g of chlorogenic acid with a purity ≥ 98.5%, add it to 20 ml of absolute ethanol at room temperature, control the solid-liquid ratio to 0.1 g / ml, stir magnetically until completely dissolved, and obtain chlorogenic acid acid solution;

[0028] S2: Preparation of lipid film: at room temperature, add 14g of hydrogenated soybean lecithin, 10g of dipalmitoylphosphatidylethanolamine and 5g of cholesterol to 14.5ml of chloroform, control the solid-liquid ratio to 2g / ml, magnetically stir until completely dissolved, transfer to In a rotary evaporator, remove chloroform at 70°C to form a transparent lipid film;

[0029] S3: Preparation of chlorogenic acid nanoliposomes: at room temperature, drop 17.4ml of anhydrous ether on the surface of the lipid film to dissolve, then drop into the chlorogenic acid solution, transfer to a rotary evaporato...

Embodiment 3

[0032] Measure the solubility of the chlorogenic acid lipid nanoparticles solid dispersion prepared by Example 1-2:

[0033] Weigh 1 mg of chlorogenic acid with a purity of ≥98.5% with an electronic balance, and weigh the corresponding amount of chlorogenic acid lipid nanoparticle solid dispersion prepared in Example 1-2 according to the standard that the content of chlorogenic acid in the medicine is 1 mg , with 10mL of artificial gastric juice as the dissolution medium, add 1mg of chlorogenic acid respectively, and the solid dispersion of chlorogenic acid lipid nanoparticles (containing 1 mg of chlorogenic acid) prepared in Example 1-2 is placed in a 37°C constant temperature water bath , 0.45μm microporous membrane filter, measure the absorbance and calculate the solubility of different samples at 37°C. Solubility calculation formula:

[0034]

[0035] With the chlorogenic acid bulk drug as the control group, the chlorogenic acid lipid nanoparticle solid dispersion prep...

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Abstract

The invention discloses a preparation method of a chlorogenic acid lipid nanoparticle solid dispersion. The method comprises the following steps: S1: anhydrous ethanol dissolves chlorogenic acid witha purity being greater than or equal to 98.5%, wherein the solid-liquid ratio is (0.05-0.1) g / ml; S2: adding hydrogenated soybean lecithin, dipalmitoylphosphatidylethanolamine and cholesterol to chloroform, wherein the solid-liquid ratio is (0.8-2) g / ml, and removing chloroform at 60 DEG C-70 DEG C; S3: dissolving a lipid membrane with diethyl ether, dropping a chlorogenic acid solution, removingan organic solvent at 60 DEG C-70 DEG C, adding a PBS buffer solution, hydrating the material for 1 h, drying and pulverizing the material through a 100-meshes sieve; S4: adding PVPK30, alpha-cyclodextrin, and sodium alginate to distilled water at 60 DEG, wherein the solid-liquid ratio is (0.6-1)g / ml, adjusting the pH to 5.0-5.5, and adding a catalyst and solid chlorogenic acid nanoliposomes, reacting the materials at 80 DEG-85 DEG C for 3-6 h, and performing sprayed drying. The method greatly improves the lipolysis and oral bioavailability of chlorogenic acid, prolongs the elimination half-life in vivo, and improves drug safety and stability, a prepared novel drug product has a solubility of up to 83 [mu]g / ml and a cumulative dissolution of up to 81% at 90 minutes.

Description

technical field [0001] The invention belongs to the field of solid dispersion pharmaceutical preparations, in particular to a preparation method of chlorogenic acid lipid nanoparticle solid dispersion. Background technique [0002] Chlorogenic acid and its derivatives have a stronger free radical scavenging effect than ascorbic acid, caffeic acid and tocopherol (vitamin E), can effectively remove DPPH free radicals, hydroxyl free radicals and superoxide anion free radicals, and can also inhibit low Oxidation of density lipoproteins. Chlorogenic acid plays an important role in effectively removing free radicals in the body, maintaining the normal structure and function of body cells, preventing and delaying the occurrence of tumor mutations and aging. Chlorogenic acid contains a special ingredient that can promote the synthesis and decomposition of collagen in the skin, bones, and muscles of the human body. It has the function of promoting metabolism and preventing decline. ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/216A61P39/06
CPCA61K9/5161A61K31/216A61P39/06
Inventor 李妍
Owner BENGBU COLLEGE
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