Berberine-sodium caprate solid dispersion and application of same in treating diabetes and complications thereof

A solid dispersion, Huanggui technology, applied in the fields of pharmacokinetics and pharmacodynamics, pharmaceutical preparations, chemical pharmaceuticals, can solve the problems of low intestinal mucosal permeability, poor water solubility of berberine, etc., to improve solubility and intestinal tract. The effect of mucosal permeability, improved bioavailability, and easy operation

Inactive Publication Date: 2014-10-01
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The object of the present invention is to solve the problems of poor water solubility of berberine and low permeability of intestinal mucosa, to provide a solid dispersion of Huang Gui conta

Method used

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  • Berberine-sodium caprate solid dispersion and application of same in treating diabetes and complications thereof
  • Berberine-sodium caprate solid dispersion and application of same in treating diabetes and complications thereof
  • Berberine-sodium caprate solid dispersion and application of same in treating diabetes and complications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Take 0.5g of berberine and place it in a round bottom flask, add 125ml of absolute ethanol and dissolve it by ultrasonic, then add 0.25g of sodium caprate and 0.5g of PVP K30, and dissolve by ultrasonic. Then, the solvent was removed by rotary evaporation under reduced pressure at 40°C, placed in a constant temperature dryer, dried at 50°C overnight, taken out the next day, and crushed through a 200-mesh sieve to obtain a solid dispersion of yellow decei.

Embodiment 2

[0047] Grind 1g of berberine, 0.5g of sodium caprate, and PEG60003g to mix evenly, place them in an autoclave, adjust the temperature of the reactor to 50°C, and introduce supercritical CO 2 , Adjust the pressure of the reaction kettle to 20KPa, and after standing for 24 hours, depressurize to obtain the solid dispersion of Huanggui.

Embodiment 3

[0049] Dissolve 1 g of berberine, 1886 g of POLOXAMER, and 0.5 g of sodium caprate in absolute ethanol, then spray-dry the solution with a spray dryer to obtain a yellow decane solid dispersion, and finally dry the solid dispersion at 50° C. for 2 hours.

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Abstract

The invention relates to the fields of chemical pharmacy, medicinal preparations, pharmacokinetics and pharmacodynamics, specifically to a berberine-sodium caprate multi-component solid dispersion and a preparation method and pharmacological activity thereof. The berberine-sodium caprate multi-component solid dispersion is characterized in that berberine, the absorption promoting agent sodium caprate and a solid dispersion carrier are employed to prepare the berberine-sodium caprate solid dispersion, wherein berberine is dispersed in the solid dispersion in an amorphous form. The berberine-sodium caprate solid dispersion provided by the invention has the following advantages: the preparation method is simple and is easy to operate, and solubility and intestinal permeability of berberine are substantially improved, thereby improving bioavailability. The berberine-sodium caprate solid dispersion has substantial treatment effects on diabetes, diabetic complications like diabetic cardiomyopathy, diabetic great vascular complications, diabetic encephalopathy and diabetic eye diseases (retinopathy) and diseases related to diabetes. The berberine-sodium caprate solid dispersion has widely available raw materials, is convenient to use and provides a novel candidate drug for treating diabetes and complications thereof.

Description

Technical field [0001] The invention relates to the fields of chemical pharmacy, pharmaceutical preparations, pharmacokinetics and pharmacodynamics, and in particular to a yellow kuei solid dispersion and its application in the treatment of diabetes and complications. technical background [0002] Berberine (English name: Berberine), commonly used berberine hydrochloride is also called berberine hydrochloride, molecular formula C 20 H 18 ClNO 4 ﹒ H 2 O, molecular weight 389.83, has the following chemical structure, [0003] [0004] Berberine is an important alkaloid and a traditional Chinese medicine that has been used for a long time in my country. It can be extracted from plants such as Coptis, Phellodendron chinense, Sankezhen. It has a significant antibacterial effect. In recent years, it has been discovered that berberine has a significant effect on lowering blood sugar, with definite curative effect and longer duration, and has the characteristics of sulfonylurea and bigu...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/4375A61K47/12A61P3/10
Inventor 陈立张明李晶孟昭杰
Owner JILIN UNIV
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