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Doxycycline hyclate liposome and production thereof

A technology of doxycycline hydrochloride and liposomes, which is applied in the directions of liposome delivery, tetracycline active ingredients, pharmaceutical formulations, etc., can solve problems such as increasing drug loading, and achieve prolonged action time, good stability, and good viscosity. additive effect

Inactive Publication Date: 2006-11-01
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the local action time and effect of specific drugs are related to the preparation method of liposomes and the components of liposomes; and for different drug active ingredients, especially for doxycycline hydrochloride water-soluble drugs, the lipid The encapsulation efficiency of the body, increasing the drug loading is also a problem

Method used

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  • Doxycycline hyclate liposome and production thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Co-dissolve 500mg soybean lecithin, 100mg cholesterol and 11mg vitamin C palmitate in ethanol, and form a film by rotary evaporation in a water bath at 50°C; dissolve 300mg poloxamer in 10ml of PBS buffer at pH 6.0 , and then 100 mg of doxycycline hydrochloride was dissolved in the solution; the prepared solution was added to the above-mentioned film, vortexed and dispersed to obtain a liposome suspension; finally, 0.1% by weight was added to the liposome sodium bisulfite.

[0035] The particle size of the obtained doxycycline hydrochloride liposome is measured between 200-300nm by a Nicomp 380ZLS (ParticleSizing Systems, USA) particle size analyzer; the encapsulation efficiency of the product is determined to be 60% by an ultrafiltration centrifugation method.

Embodiment 2

[0037] Co-dissolve 900mg egg yolk lecithin, 90mg cholesterol and 6.3mg vitamin E in ethanol, and form a film by rotary evaporation in a water bath at 30°C; dissolve 100mg poloxamer in 5ml of pH7.3 phosphate buffer 180 mg of doxycycline hydrochloride was dissolved in the buffer solution; then the prepared solution was added to the above-mentioned membrane, vortex mixed and then magnetically stirred and homogenized for 1 hour to obtain a liposome suspension; in the liposome Add 0.1% sodium sulfite by weight.

[0038] The particle size of the obtained doxycycline hydrochloride liposome is between 80-200nm; the encapsulation efficiency of the product is determined to be 70% by an ultrafiltration centrifugation method.

Embodiment 3

[0040] A total of 5 mg of soybean lecithin and synthetic phosphatidylserine (weight ratio 20:1), 0.5 mg of cholesterol, and 2.1 mg of vitamin E were dissolved in chloroform, and a film was formed by rotary evaporation in a water bath at 40 ° C; Wen 80 was dissolved in 2ml of phosphate buffer solution with pH 6.5, and then 1mg of doxycycline hydrochloride was dissolved in the above solution; the prepared solution was added to the above film, oscillated to disperse and then stirred and homogenized for 1 hour to obtain lipid Plastid suspension; adding 0.1% sodium thiosulfate in the liposome by weight.

[0041] The particle size of the obtained doxycycline hydrochloride liposome is between 100-300nm; the encapsulation efficiency of the product is measured to be 80% by an ultrafiltration centrifugation method.

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Abstract

A doxycycline hydrochloride liposome with high optical and thermal stability, high power to pass through skin and mucosa, and high antibacterial effect is prepared from phosphatide, cholesterol, doxycycline hydrochloride and emulsifier by film dispersing method, injection method, or reverse evaporation method.

Description

technical field [0001] The invention relates to a doxycycline hydrochloride liposome and a preparation method thereof. Background technique [0002] Doxycycline hydrochloride (doxycycline hydrochloride, doxycycline hydrochloride) is a tetracycline antibiotic. It can be widely used in respiratory, urinary, reproductive system and biliary tract infections, and has certain curative effects on skin and soft tissue infections, sepsis, acne, brucellosis, trachoma, gonorrhea, etc., and can effectively control subgingival plaque in periodontal pockets, Inhibit periodontal disease pathogenic bacteria. But the current doxycycline hydrochloride crude drug is unstable to light and heat, and is not easy to store. And doxycycline hydrochloride preparation mainly contains tablet and capsule at present, because the water solubility of doxycycline hydrochloride is better prepared into topical preparation, then the permeability to skin, mucous membrane is poor, local drug action time and an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/65A61K9/127A61K47/22A61K47/24A61P31/04
Inventor 芦洁金鸿莱胡纯贞奉建芳肖忠革
Owner SHANGHAI INST OF PHARMA IND CO LTD
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