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Application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy

A technology of trimethoxyphenol and diabetic nephropathy, which is applied in the field of application of 3,4,5-trimethoxyphenol in the preparation of drugs for the prevention and treatment of diabetic nephropathy, and can solve the problems that have not been reported yet, and the ideal therapeutic effect has not been achieved.

Active Publication Date: 2017-09-26
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

However, the current treatment of diabetic nephropathy is mainly through controlling the patient's blood sugar, blood pressure, and regulating lipid metabolism, but has never achieved the desired therapeutic effect. When the disease develops to the stage of renal failure, dialysis can only be used to maintain life
[0004] And 3,4,5-trimethoxyphenol (3,4,5-Trimethoxyphenol) is an important pharmaceutical intermediate, which is widely used in the synthesis of anti-inflammatory and anticancer drugs, and it is also the main flavonoid traditional Chinese medicine. Synthetic raw materials, but its application in diabetic nephropathy drugs has not been reported

Method used

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  • Application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy
  • Application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy
  • Application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy

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Experimental program
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Effect test

Embodiment 13

[0030] The preparation of embodiment 13,4,5-trimethoxyphenol

[0031] According to the conventional preparation method, 3,4,5-trimethoxyphenol was obtained by extracting, separating and purifying from Cortex Mori:

[0032] Weigh 10 kg of Cortex Mori, chop and grind it into a coarse powder, add 100 L of water to decoct and extract three times, each time for 1 hour, combine the extracts, concentrate under reduced pressure to an appropriate volume, add to D101 macroporous resin, and elute with water first, Then elute with 95% ethanol solution, collect 95% ethanol partial solution eluate, concentrate under reduced pressure to obtain 150g extract, get 130g extract and separate with silica gel chromatography column, elute with petroleum ether-ethyl acetate, after normal Repeated purification with silica gel and SephadexLH-20 yielded 50 mg of colorless flaky crystals, which were identified as 3,4,5-trimethoxyphenol, and its purity was >98% by HPLC.

[0033] The physicochemical and s...

Embodiment 2

[0036] Embodiment 2 prevents and treats the pharmaceutical composition granule of diabetic nephropathy

[0037] The present embodiment provides a pharmaceutical composition granule for preventing and treating diabetic nephropathy, and each pack of granule comprises the following mass numbers of components:

[0038] 3,4,5-Trimethoxyphenol 5.0mg

[0039] Starch 2497.5mg

[0040] Microcrystalline Cellulose 2497.5mg

[0041] The preparation method of described pharmaceutical composition granule comprises the following steps:

[0042] Pass 3,4,5-trimethoxyphenol through a 80-mesh sieve, mix evenly with starch and microcrystalline cellulose, make soft material with appropriate amount of water, granulate, dry, granulate, and pack separately.

Embodiment 3

[0043] Embodiment 3 prevents and treats the pharmaceutical composition tablet of diabetic nephropathy

[0044] The present embodiment provides a kind of pharmaceutical composition tablet of preventing and treating diabetic nephropathy, each tablet comprises the component of following mass number:

[0045]

[0046] The preparation method of described pharmaceutical composition tablet comprises the following steps:

[0047] Pass 3,4,5-trimethoxyphenol through a 80-mesh sieve, mix well with lactose and cornstarch, add appropriate amount of water and granulate the powder, after drying, sieve the granules and mix with the rest of the excipients, Tablets are available.

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Abstract

The invention relates to the application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy. 3,4,5-Trimethoxyphenol has a new medical application in the treatment of diabetic nephropathy, it can inhibit the apoptosis of endothelial cells induced by AGEs, reduce the oxygen stress level of mesangial cells induced by AGEs, and inhibit the chemotaxis of macrophages induced by AGEs Increase, and can improve urinary microalbumin, blood pressure, and blood sugar abnormalities in STZ-induced diabetic nephropathy model rats. 3,4,5-Trimethoxyphenol can be prepared into a pharmaceutical composition with a drug carrier, and then prepared into various oral dosage forms, such as granules, tablets, capsules, pills, etc., which are easy to use, safe and reliable.

Description

technical field [0001] The invention relates to the technical field of chemistry and medicine, in particular to the application of 3,4,5-trimethoxyphenol in the preparation of drugs for preventing and treating diabetic nephropathy. Background technique [0002] Diabetic nephropathy (diabetic nephropathy, DN) is one of the most important microvascular complications of diabetes, and is currently the leading cause of end-stage renal disease (ESRD). Clinically, diabetic nephropathy mainly manifests as proteinuria, hypertension, and progressive renal dysfunction, and its marker is the appearance of urinary microalbumin. Increased glomerular capillary oxidative stress and subsequent apoptosis, as well as repeated episodes of mild inflammation, are an important pathological change in the development of the disease. At the same time, more and more studies have shown that advanced glycation end products (AGEs) are involved in the entire pathogenesis of diabetes and its complications...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/09A61P3/10A61P13/12
Inventor 何宝郑兆广朱荃石兴华段婷婷王汝上杨琳琳陈丹扬胡琴高雪晖顾斐程慧荃高俊飞杨丹屈夏菁
Owner 广州康臣药业有限公司
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