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Fat-reducing drug resveratrol-loading controlled release nano carrier for oral administration and preparation method thereof

A nano-carrier, resveratrol technology, applied in the direction of drug combination, pharmaceutical formula, non-active ingredient medical preparations, etc., can solve the problems of low bioavailability, short half-life, poor water solubility of resveratrol, etc. Improves solubility, prevents accumulation of triglycerides, improves solubility and bioavailability

Inactive Publication Date: 2018-11-27
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Due to the poor water solubility and short half-life of t-Res resveratrol, its bioavailability is low

Method used

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  • Fat-reducing drug resveratrol-loading controlled release nano carrier for oral administration and preparation method thereof
  • Fat-reducing drug resveratrol-loading controlled release nano carrier for oral administration and preparation method thereof
  • Fat-reducing drug resveratrol-loading controlled release nano carrier for oral administration and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Preparation of nanocarriers

[0035] 1. Dissolve 50 mg of PLGA in 5 ml of a mixed solvent of dichloromethane and acetone (volume ratio dichloromethane: acetone = 1:3) to form a uniform PLGA solution.

[0036] 2. Add 10 mg of free t-Res to the PLGA solution obtained in step 1, with an ultrasonic power of 100w and an ultrasonic time of 2min, and perform ice bath ultrasonication to obtain the s / o primary emulsion, which is the oil phase.

[0037] 3. Dissolve BSA in an appropriate amount of deionized water to obtain a uniform BSA solution with a concentration of 1%. This is the water phase. Add the oil phase obtained in step 2 dropwise to the water phase, and then perform ice bath ultrasound. The ultrasound power is 200w, ultrasonic time is 5min, to produce the final s / o / w emulsion.

[0038] 4. In order to disperse the final s / o / w emulsion, add 30ml of deionized water and stir with a magnetic force for 5h to remove the residual organic solvents to obtain a nanocarrier solution. ...

Embodiment 2

[0060] 1. Dissolve 100mg PLGA in 10ml of a mixed solvent of dichloromethane and acetone (volume ratio dichloromethane: acetone = 2:3) to form a uniform PLGA solution.

[0061] 2. Add 18 mg of free t-Res to the PLGA solution obtained in step 1, with an ultrasonic power of 200w and an ultrasonic time of 4min, and perform ice bath ultrasonication to obtain the s / o primary emulsion, which is the oil phase.

[0062] 3. Dissolve BSA in an appropriate amount of deionized water to obtain a uniform BSA solution with a concentration of 1%. This is the water phase. Add the oil phase obtained in step 2 dropwise to the water phase, and then perform ice bath ultrasound. The ultrasound power is 400w, ultrasonic time is 5min, to produce the final s / o / w emulsion.

[0063] 4. In order to disperse the final s / o / w emulsion, add 30ml of deionized water and stir with a magnetic force for 8h to remove the residual organic solvents to obtain a nanocarrier solution.

[0064] 5. Centrifuge the solution obtaine...

Embodiment 3

[0066] 1. Dissolve 80mg PLGA in 8ml of mixed solvent of dichloromethane and acetone (volume dichloromethane: acetone = 1:1) to form a uniform PLGA solution.

[0067] 2. Add 15mg of free t-Res to the PLGA solution obtained in step 1, with an ultrasonic power of 200w and an ultrasonic time of 3min, and perform ice bath ultrasonication to obtain the s / o primary emulsion, which is the oil phase.

[0068] 3. Dissolve BSA in an appropriate amount of deionized water to obtain a uniform BSA solution with a concentration of 1%. This is the water phase. Add the oil phase obtained in step 2 dropwise to the water phase, and then perform ice bath ultrasound. The ultrasound power is 400w, ultrasonic time is 5min, to produce the final s / o / w emulsion.

[0069] 4. In order to disperse the final s / o / w emulsion, add 30ml of deionized water and stir with a magnetic force for 6h to remove the residual organic solvents to obtain a nanocarrier solution.

[0070] 5. Centrifuge the solution obtained in step 4...

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Abstract

The invention belongs to the technical field of chemical drugs and in particular discloses a preparation method of a fat-reducing drug resveratrol-loading controlled release nano carrier for oral administration. The preparation method is a method of preparing drug-loading high molecules from a fat-reducing drug t-Res and a degradable functional macromolecular compound good in biocompatibility which are taken as raw materials. The fat-reducing drug t-Res is entrapped by means of self assembly of PLGA by adopting an emulsified solvent evaporation method. The carrier can effectively overcome thedefects of the liver first pass effect caused by oral administration, short half life of drugs, low biocompatibility, damaged drug activity and the like. By coating the active drug molecules with thebiodegradable PLGA with good biocompatibility as a shell, the degrading action and the liver first pass effect and the like of a gastrointestinal fluid to drug molecules can be alleviated, so that thebiocompatibility and the in vivo half life of the drug molecules are improved, and oral administration is facilitated.

Description

Technical field [0001] The invention belongs to the technical field of chemical drugs, and relates to a controlled-release nano-carrier of the oral fat-reducing drug resveratrol and a preparation method thereof. technical background [0002] With the progress of society and the improvement of people's living standards, more and more people are obese, and obesity has become an increasingly serious global epidemic. The World Health Organization defines obesity as a disease of excessive accumulation or abnormal distribution of fat in the body that endangers human health. Obesity is a chronic and persistent state, characterized by excessive body fat. Use body mass index (BMI) (weight (kg) / height (m 2 )] To define, BMI≥30 means obesity, and BMI=25~29.9 means overweight. Obesity is a risk factor for many chronic diseases in modern humans, including type 2 diabetes, biliary tract disease, dyslipidemia, anti-insulin effect, sleep apnea, dyspnea, endless anxiety, coronary heart disease,...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K31/05A61K47/34A61P3/06
CPCA61K9/5153A61K31/05A61P3/06
Inventor 魏坤万淑倩
Owner SOUTH CHINA UNIV OF TECH
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