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Application of catalpol as non-enzymatic glycosylation end product inhibitor

A kind of technology of catalpol and pharmaceutical dosage form, applied in the application field of catalpol as a non-enzymatic glycosylation end-product inhibitor, can solve the problems such as difficulty, poor chemical stability, and high polarity of catalpol, and achieves elimination of pathological effects , the effect of preventing or alleviating organ damage

Inactive Publication Date: 2016-12-07
北京九龙制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Due to the high polarity and poor chemical stability of catalpol, it is difficult to prepare a large amount of monomer components with a purity of more than 90%.

Method used

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  • Application of catalpol as non-enzymatic glycosylation end product inhibitor
  • Application of catalpol as non-enzymatic glycosylation end product inhibitor
  • Application of catalpol as non-enzymatic glycosylation end product inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Example 1: Preparation and structure identification of catalpol

[0087] 1.1 Preparation of catalpol:

[0088] Take fresh Rehmannia glutinosa, extract three times with water ultrasonic, add 6 times the amount of water each time, ultrasonic for 1 hour. The extracts were combined and concentrated under reduced pressure. Concentrate to a density of about 1.10 (60°C), use D101 macroporous adsorption resin column for chromatographic separation, elution with a water-ethanol gradient, discard the water eluent, collect the 20% ethanol eluent, and concentrate under reduced pressure to obtain The crude product is obtained by recrystallization from ethanol.

[0089] 1.2 Structure identification:

[0090] This self-made product is white powder (EtOH), easily soluble in solvents such as methanol, ethanol, and water. Melting point: 207-209°C (decomposition point). The melting point of the mixture with catalpol reference substance does not decrease, and the compound can be preliminarily j...

Embodiment 2

[0107] Example 2 Preparation of Catalpol Dropping Pills

[0108] Take 0.5 g of catalpol from Example 1 and 10.5 g of polyethylene glycol-6000, mix them uniformly, heat and melt, transfer to drip irrigation after dissolving, and drop the medicine into liquid paraffin at 6-8°C to remove oil. Get 400 drip pills.

Embodiment 3

[0109] Example 3 Preparation of Catalpol Tablets

[0110] Take 0.5 g of catalpol of Example 1, add 10 g of starch, 4.5 g of sucrose, and mix evenly, then granulate and press tablets to obtain.

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PUM

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Abstract

The invention relates to application of catalpol as a non-enzymatic glycosylation end product inhibitor. The catalpol is an iridoid glucoside compound and mainly exists in plants such as radix rehmanniae. The catalpol can prevent NO activation, can be used for preventing and treating related diseases such as diabetic complication caused by AGE disorder, Alzheimer's disease and atherosclerosis and has certain blood sugar reducing and blood lipid reducing effects.

Description

Invention field [0001] The present invention relates to catalpol effectively preventing the generation of non-enzymatic glycation end products AGE (advanced glycationendproducts AGE) or inhibiting the activity of AGE, and can also prevent NO activation, and can be used to prevent and treat diabetic complications caused by AGE imbalance. Murder disease, atherosclerosis and other related diseases. Background technique [0002] Advanced glycationend products (AGE) are the products of the combination of excess sugar and protein. There are two sources in the body. One is the synthesis of AGE in the body by excess sugar and protein, and the other is the combination of excess sugar and protein in the body. The existing AGE is taken into the body. The harmful effects of AGE on the human body: First, it can cause the glycosylation of proteins in the body, change the proteins on the blood vessels, and reduce the toughness of the blood vessel walls, which is easy to be damaged. Second, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P3/10A61P9/10A61P13/12A61P25/28A23L33/10A23L33/105
CPCA23V2002/00A61K31/7048A23V2200/328A23V2200/326A23V2200/30A23V2250/21
Inventor 卢兖伟杨喜峰
Owner 北京九龙制药有限公司
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