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Novel drug encapsulation product and preparation method and application thereof

A wrapping and product technology, applied in the field of antibacterial drug wrapping products, can solve the problem of not using LAE and its derivatives, etc., and achieve the effects of being easily catabolized by biology, simple in production process and low in cost

Active Publication Date: 2019-10-01
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] At present, there is no report on the use of LAE and its derivatives for the preparation of drug-coated products

Method used

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  • Novel drug encapsulation product and preparation method and application thereof
  • Novel drug encapsulation product and preparation method and application thereof
  • Novel drug encapsulation product and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Example 1: Preparation method of synthetic ion-pair compound of lauroyl arginine ethyl ester hydrochloride and nicotinic acid

[0066] Dissolve 2.0 g of sodium nicotinic acid (purchased from Tixiai (Shanghai) Chemical Industry Development Co., Ltd.) in 50 mL of water to prepare a sodium nicotinic acid salt aqueous solution (A); 6.8 g of lauroyl arginine ethyl ester hydrochloride Dissolve in 40mL of water, heat to 90℃, until all the lauroyl arginine ethyl ester hydrochloride is dissolved to make the aqueous solution of lauroyl arginine ethyl ester hydrochloride (B); The saline solution (A) is slowly added to the lauroyl arginine ethyl ester hydrochloride solution (B), stirring constantly, reacting for 2 hours, cooling to room temperature, filtering, fully washing the precipitate with purified water, and drying the precipitate in vacuum at 60°C. 7.6 g of niacin ion pair compound is obtained.

Embodiment 2

[0067] Example 2: Analysis of the molecular formula and molecular weight of the compound of the nicotinic acid ion of ethyl lauroyl arginine

[0068] By mass spectrometry, 1 H-NMR, 13 The molecular formula of the compound obtained by C-NMR spectrum analysis is:

[0069] 1. Mass spectrometry (ESI) analysis

[0070] Cation B + The m / z of the molecular ion peak = 385.3, see figure 1 ;

[0071] Anion A - The m / z of the molecular ion peak = 122.1, see figure 2 .

[0072] The theoretical calculated value of the cation of the niacin ion pair compound is 507.4, and the measured value is consistent with the theoretical value.

[0073] 2.NMR analysis

[0074] Lauroyl arginine ethyl ester hydrochloride (see image 3 ), niacin 1 H-NMR (see Figure 4 ) And LAE niacin ion pair compound 1 H-NMR (see Figure 5 )Compared. Since the LAE ion-pair compound is in the process of salt formation, the peak shape and chemical shift of the ion-pair compound of lauroyl arginine ethyl ester change little, but all h...

Embodiment 3

[0075] Example 3: Preparation method of synthetic ion-pair compound of lauroyl arginine ethyl ester hydrochloride and tartaric acid

[0076] Dissolve 2.0 g of tartaric acid (purchased from Tixiai (Shanghai) Chemical Industry Development Co., Ltd.) in 50 mL of methanol, add equivalent NaOH, stir at room temperature until a white solid precipitates, filter with suction and wash with 30 mL of methanol three times to obtain sodium tartrate . Sodium tartrate is dissolved in 50mL of water to prepare a sodium tartrate solution (A); 5.6 g of lauroyl arginine ethyl ester hydrochloride is dissolved in 40 mL of water and heated to 90°C until the lauroyl arginine ethyl ester salt The acid salt is completely dissolved to prepare an aqueous solution of lauroyl arginine ethyl ester hydrochloride (B); the sodium tartrate aqueous solution (A) is slowly added to the aqueous solution of lauroyl arginine ethyl ester hydrochloride ( In B), continue to stir, react for 2 hours, cool to room temperatur...

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Abstract

The invention provides a novel drug encapsulation product. The product includes ethyl lauroyl arginate (LAE) and its ion pair derivatives. The invention further provides a method for preparing the drug encapsulation product containing the ethyl lauroyl arginate (LAE) and its ion pair derivatives. The drug encapsulation product has the advantages of being natural, free of toxics, capable of efficiently inhibiting bacteria and easy to degrade by animals and giving play to drug synergistic effects.

Description

Technical field [0001] The present invention relates to antibacterial drug packaging products (capsules and coatings), in particular to drug packaging products containing lauroyl arginine ethyl ester salt and its derivatives (ion-pair compounds). The lauroyl arginine ethyl ester ion It has an antibacterial effect, which can help the drug package product not only to contain and deliver the contents, but also to maintain stability and exert antibacterial and other synergistic effects. Background technique [0002] Capsules or capsule shells refer to capsules made of special film-forming materials (such as gelatin, cellulose, polysaccharides, etc.), and the contents (such as powder, liquid, various drugs, etc.) or dosed into them are convenient swallow. [0003] Capsules (shells) are usually divided into hard capsules and soft capsules. Hard capsules, also known as hollow capsules, are composed of two parts of the cap body; soft capsules are processed into products with film-forming...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K47/52A61K47/54A61K31/223A61P31/04
CPCA61K9/4816A61K47/52A61K47/542A61K47/545A61K31/223A61P31/04
Inventor 易正芳邵婷仇文卫王李婷刘明耀
Owner EAST CHINA NORMAL UNIV
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