A kind of paeonol nano sustained-release preparation and preparation method thereof

A nano-sustained-release and paeonol technology, which is applied in pharmaceutical formulations, medical preparations of inactive ingredients, and capsule delivery, etc., can solve the problems of complex preparation conditions, production of toxic and harmful substances, complex preparation processes, etc. Simple process, increased medicinal effect and strong dispersibility

Active Publication Date: 2018-08-10
ANHUI AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large particle size of these preparations, they cannot be used for injection, the preparation process is complex, the preparation conditions are complicated, and the preparation process may produce toxic and harmful substances.

Method used

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  • A kind of paeonol nano sustained-release preparation and preparation method thereof
  • A kind of paeonol nano sustained-release preparation and preparation method thereof
  • A kind of paeonol nano sustained-release preparation and preparation method thereof

Examples

Experimental program
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Effect test

specific Embodiment 1

[0026] A kind of paeonol nano-sustained-release preparation described in the present embodiment, its raw material ratio is:

[0027] The proportion of oil phase raw materials is: 100 milliliters of acetone aqueous solution or acetone with a mass concentration greater than 20%, 0.04 grams of paeonol, 4.0 milliliters of ethyl acetate, and 0.26 milliliters of n-butyl α-cyanoacrylate;

[0028] The raw material ratio of the water phase is: 100 ml of ultrapure water, 0.8 g of poloxamer 188, and 0.8 g of dextran-70.

[0029] A kind of preparation method of paeonol nano-sustained-release preparation described in the present embodiment, comprises the following steps:

[0030] Step 1. Accurately weigh paeonol and acetone aqueous solution or acetone, place paeonol in acetone aqueous solution or acetone and sonicate for 5 minutes, fully dissolve to obtain solution 1, and set aside;

[0031] Step 2. Accurately measure n-butyl α-cyanoacrylate and ethyl acetate and mix thoroughly, and immed...

specific Embodiment 2

[0038] A kind of paeonol nano-sustained-release preparation described in the present embodiment, its raw material ratio is:

[0039] The proportion of oil phase raw materials is: 100 ml of acetone aqueous solution or acetone with a mass concentration greater than 20%, 0.05 g of paeonol, 5.0 ml of ethyl acetate, and 0.30 ml of n-butyl α-cyanoacrylate;

[0040] The raw material ratio of the aqueous phase is: 100 ml of ultrapure water, 0.5 g of poloxamer 188, and 1.0 g of dextran-70.

[0041] In the preparation method of a paeonol nano-sustained-release preparation described in this example, the pH value of the mixture during spontaneous interfacial polymerization is 3.0, and the remaining steps are the same as in Example 1. A kind of paeonol prepared in this example The transmission electron microscope (TEM) image, particle size visualization image and release percentage image of the skin phenol nano-sustained-release preparation are similar to those in Example 1.

specific Embodiment 3

[0042] A kind of paeonol nano-sustained-release preparation described in the present embodiment, its raw material ratio is:

[0043] The proportion of oil phase raw materials is: 100 ml of acetone aqueous solution or acetone with a mass concentration greater than 20%, 0.06 g of paeonol, 6.0 ml of ethyl acetate, and 0.35 ml of n-butyl α-cyanoacrylate;

[0044] The raw material ratio of the aqueous phase is: 100 ml of ultrapure water, 0.6 g of poloxamer 188, and 0.8 g of dextran-70.

[0045] In the preparation method of a paeonol nano-sustained-release preparation described in this example, the pH value of the mixture during spontaneous interfacial polymerization is 2.0, and the remaining steps are the same as in Example 1. A paeonol prepared in this example The transmission electron microscope (TEM) image, particle size visualization image and release percentage image of the skin phenol nano-sustained-release preparation are similar to those in Example 1.

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Abstract

The invention discloses a paeonol nanometer sustained release preparation.The preparation is prepared through the steps that paracyanogen n-butyl acrylate serves as a medicine carrier, under the room-temperature magnetic stirring condition, an oil phase containing paeonol, ethyl acetate, alpha-cyanogen n-butyl acrylate and acetonie is dropped into an acid water phase obtained by mixing a surfactant and ultra-pure water uniformly drop by drop, by means of spontaneous interfacial polymerization, then low-temperature rotating and evaporating are carried out to remove acetone, filtering is carried out, a pH value is adjusted to be neutral, milk white suspension is obtained by means of stirring complete polymerization, or freeze-dried powder is obtained by means of freeze drying.The paeonol nanometer sustained release preparation has the good slow release property and also has the advantages of being small in particle size, high in dispersity, good in stability and high in target ability, and releasing drugs slowly; meanwhile, solubility of paeonol is improved, stability is enhanced, drug action time is prolonged, the drug action is improved, and bioavailability is improved; moreover, the preparation technology of medicine nanometer capsules is simple, energy consumption is low, toxicity is small, and safety is high.

Description

technical field [0001] The invention relates to a paeonol nano sustained-release preparation and a preparation method thereof, belonging to the technical field of paeonol nano sustained-release preparations. Background technique [0002] Paeonol (paeonol) is the main active ingredient of commonly used traditional Chinese medicine Moutan Cortex and Xu Changqing, etc. It has significant analgesic, sedative, anti-infective, anti-oxidative and anti-tumor effects. It is clinically used to treat rheumatism, toothache, stomach pain, Skin diseases, high blood pressure, arrhythmia, etc. Paeonol has the disadvantages of being volatile, easily oxidized, poorly water-soluble, short biological half-life, and irritating to the gastrointestinal mucosa, which affect its stability in formulations and bioavailability in vivo. To improve these defects, many researchers are devoted to the study of paeonol preparations, such as paeonol emulsions, paeonol-β cyclodextrin inclusion complexes, paeo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K9/19A61K9/10A61K31/12A61K47/32
CPCA61K9/0002A61K9/0019A61K9/10A61K9/19A61K9/5138A61K31/12A61K47/32
Inventor 汪维云姚京京曾德成章扬新孙东东杨恩东刘海平
Owner ANHUI AGRICULTURAL UNIVERSITY
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