Pharmaceutical composition for treating diabetic nephropathy and preparation method and application thereof

A technology for diabetic nephropathy and a composition is applied in the field of pharmaceutical compositions for the treatment of diabetic nephropathy and the field of preparation thereof to achieve the effects of clear active ingredients, prevention of glomerular damage, and reduction of urine volume and urine protein

Active Publication Date: 2010-07-21
广州康臣药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main active ingredients of Morus alba are flavonoids, alkaloids, polysaccharides and coumarins (umbelliferone, scopoletin), etc. Studies have proved that flavonoids, alkaloids and polysaccharides in Morus alba have certain hypoglycemic effects Among them, the effect of alkaloids is the strongest, and the coumarin component in Morus alba is mainly used as a diuretic, antitussive and asthma-relieving, there is no literature report on its use as a treatment for diabetic nephropathy, but according to domestic research reports in recent years It shows that coumarin has various biological activities such as anti-HIV, anti-cancer, antihypertensive, anti-arrhythmia, anti-osteoporosis, analgesia, anti-asthma and antibacterial. The new use of the element in the field of medicine

Method used

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  • Pharmaceutical composition for treating diabetic nephropathy and preparation method and application thereof
  • Pharmaceutical composition for treating diabetic nephropathy and preparation method and application thereof
  • Pharmaceutical composition for treating diabetic nephropathy and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of 7-hydroxycoumarin

[0032]Take 10kg of Cortex Mori (Cotex Mori), chop and grind it into powder, add 100L water to reflux and extract three times, each time for 2 hours, combine the extracts, concentrate under reduced pressure to a certain volume, put it into D101 macroporous resin, and wash with water first Then elute with 95% ethanol, collect the alcohol eluate, and concentrate under reduced pressure to obtain the extract. The extract was separated by silica gel chromatography, eluting with petroleum ether, petroleum ether-ethyl acetate 100:1, petroleum ether-ethyl acetate 50:1 and petroleum ether-ethyl acetate 20:1, petroleum ether-acetic acid Ethyl ester 20: 1 elution part has light yellow powder to precipitate, and acetone recrystallizes repeatedly to obtain pure product, and its structure is determined as 7-hydroxycoumarin (7-Hydroxycoumarin) by infrared, ultraviolet, nuclear magnetic resonance and mass spectrometry analysis. , tha...

Embodiment 2

[0034] Embodiment 2: the preparation of 7-hydroxy-6-methoxy coumarin

[0035] Take 10kg of Cortex Mori (Cotex Mori), chop and grind it into powder, add 100L water to reflux and extract three times, each time for 2 hours, combine the extracts, concentrate under reduced pressure to a certain volume, put it into D101 macroporous resin, and wash with water first Then elute with 95% ethanol, collect the alcohol eluate, and concentrate under reduced pressure to obtain the extract. Elute with petroleum ether, petroleum ether-ethyl acetate 100:1 and petroleum ether-ethyl acetate 50:1 respectively, and the elution part of petroleum ether-ethyl acetate 50:1 has a light yellow powder. The pure product was obtained by secondary recrystallization, and its structure was determined to be 7-hydroxy-6-methoxycoumarin (7-hydroxy-6-methoxycoumarin) through infrared, ultraviolet, nuclear magnetic resonance and mass spectrometry analysis, i.e. scopoletin ( scopoletin), molecular formula: C 10 h ...

Embodiment 3

[0037] Embodiment 3: the preparation of pharmaceutical composition capsule of the present invention (active ingredient is 7-hydroxy-6-methoxy coumarin)

[0038] Proceed as follows:

[0039] A. Take 4.2g of beeswax, add 125g of evening primrose oil, melt and mix in a water bath at 80°C, cool to room temperature (25°C), add an appropriate amount of tert-butyl-p-hydroxyanisole and citrate, and mix well;

[0040] B. Add 0.25g of 7-hydroxy-6-methoxycoumarin and 5g of lecithin through a 100-mesh sieve, add evening primrose oil to 250g, mix well, use as capsule heart fluid, and press into 1000 capsules.

[0041] The capsules obtained in this embodiment have good effects in treating hyperglycemia, diabetic nephropathy and the like.

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Abstract

The invention discloses a pharmaceutical composition for treating diabetic nephropathy, a preparation method thereof, and application in the preparation of a drug for treating diabetic complications. The pharmaceutical composition consists of one or two of 7-hydroxycoumarin or 7-hydroxy-6-methoxy coumarin as active ingredients and a conventional drug carrier, and the content of weight percentage of the active ingredients is 0.1-99.5%. The pharmaceutical composition is mainly used in the preparation of the drug for treating diabetic nephropathy. The pharmaceutical composition has rich source of raw materials, obvious preventive effect for diabetic nephropathy, and convenient use, and provides a novel drug candidate for treatment.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine pharmacy, in particular to a pharmaceutical composition for treating diabetic nephropathy, a preparation method and application thereof. Background technique [0002] Diabetes and its chronic complications have seriously affected human health and quality of life. In recent years, the incidence of diabetes has been on the rise. The incidence of diabetes in all age groups worldwide was about 2.8% in 2000 and is expected to be 4.4% by 2030. The number of people living with diabetes will increase from 171 million in 2000 to 333 million in 2030. The incidence of diabetes in China is rising every year, and the number of patients is second only to India, ranking second in the world. The prevention and treatment of diabetes and its chronic complications is an important issue facing today. Diabetic nephropathy (diabetic nephropathy, DN) is one of the important complications of diabetes, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/37A61P3/10A61P13/12
CPCA61K9/2054A61K31/353A61K9/2018A61K9/4875A61K9/2027A61K31/37A61K9/0056A61K9/2059A61K9/2031A61P3/10A61P13/12
Inventor 朱荃石兴华汤丹郑兆广何宝段婷婷顾斐程慧荃黄晓玲黄艳霞王汝上
Owner 广州康臣药业有限公司
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