New application of ethyl 4-hydroxybenzoate to pharmacy

Abstract

The invention relates to new application of ethyl 4-hydroxybenzoate to pharmacy, and belongs to the field of medicine. Ethyl 4-hydroxybenzoate has the control effect on diabetic nephropathy, can inhibit glomerular mesangial cell multiplication and endothelial cell apoptosis caused by AGEs (Advanced Glycation End Products), can reduce endothelial cell oxidative stress level caused by AGEs, and can improve rat urine protein, urine creatinine, serum creatinine and creatinine clearance rates and blood glucose and blood pressure abnormality, caused by STZ-CFA, of a diabetic nephropathy model. Medicine compositions can be prepared from ethyl 4-hydroxybenzoate and drug carriers, so that various oral dosage forms such as granule, tablet, capsule and pill can be prepared; the use is convenient, safe and reliable.

Description

technical field

[0001] The invention relates to the field of medicine, in particular to the new application of ethyl p-hydroxybenzoate in pharmacy. Background technique

[0002] Diabetes and its complications have seriously affected human health and quality of life. As of 2004, 3.4 million people had died from diabetes and its complications, and the World Health Organization predicts that this number will double between 2005 and 2030. Diabetic nephropathy is one of the most common and serious chronic microvascular complications of diabetes, and is the leading cause of death in diabetic patients. According to the data of the World Health Organization, if blood sugar is not controlled, about 30% of patients with type 1 diabetes and 25%-40% of patients with type 2 diabetes will develop diabetic nephropathy. Therefore, it is of great significance to actively seek effective measures to prevent and treat diabetic nephropathy. Clinically, diabetic nephropathy mainly manifests as...

Examples

Embodiment 1

[0031] The preparation of embodiment 1 ethyl p-hydroxybenzoate

[0032] References (Liu Jing, Wang Yunfang. Synthesis of ethyl p-hydroxybenzoate. Journal of Weinan Normal University 2005,20(5):5-7) synthesized ethyl p-hydroxybenzoate.

[0033] Add 0.05mol (6.9g) p-hydroxybenzoic acid, 0.2mol (11.65ml) ethanol and 0.017mol (1.66g) catalyst to a three-necked flask equipped with an electric stirrer, a thermometer, and a reflux device with a water separator Sulfamic acid was heated to reflux for 3 hours, the catalyst was filtered out while it was hot, and the raffinate was quickly poured into cold water, and the solid crude product was precipitated from the water. Filtration, the filter cake was washed with 5% Na 2 CO 3 Wash with aqueous solution and water, and dry to obtain crude product. In a round bottom flask equipped with a reflux condenser, add the crude product of ethyl p-hydroxybenzoate, ethanol, water and 0.1% activated carbon at a molar ratio of 1:4:0.5, heat to reflu...

Embodiment 2

[0034] The preparation of embodiment 2 ethyl p-hydroxybenzoate granules

[0035] Each packet of granules contains the following components:

[0036] Ethylparaben 5mg

[0037] Starch 2497.5mg

[0038] Microcrystalline cellulose 2497.5mg

[0039] The preparation method is as follows: pass ethyl p-hydroxybenzoate through 80-mesh sieve, mix evenly with starch and microcrystalline cellulose, use appropriate amount of water to make soft material, granulate, dry, granulate, and pack.

Embodiment 3

[0040] The preparation of embodiment 3 ethyl p-hydroxybenzoate tablet

[0041] Each tablet contains the following ingredients:

[0042]

[0043] The preparation method is as follows: pass ethyl p-hydroxybenzoate through a 80-mesh sieve, mix evenly with lactose and cornstarch, add appropriate amount of water and granulate the powder, after drying, sieve the granules and mix with magnesium stearate, Tablets are available.

technical field

[0001] The invention relates to the field of medicine, in particular to the new application of ethyl p-hydroxybenzoate in pharmacy. Background technique

[0002] Diabetes and its complications have seriously affected human health and quality of life. As of 2004, 3.4 million people had died from diabetes and its complications, and the World Health Organization predicts that this number will double between 2005 and 2030. Diabetic nephropathy is one of the most common and serious chronic microvascular complications of diabetes, and is the leading cause of death in diabetic patients. According to the data of the World Health Organization, if blood sugar is not controlled, about 30% of patients with type 1 diabetes and 25%-40% of patients with type 2 diabetes will develop diabetic nephropathy. Therefore, it is of great significance to actively seek effective measures to prevent and treat diabetic nephropathy. Clinically, diabetic nephropathy mainly manifests as...

Examples

Embodiment 1

[0031] The preparation of embodiment 1 ethyl p-hydroxybenzoate

[0032] References (Liu Jing, Wang Yunfang. Synthesis of ethyl p-hydroxybenzoate. Journal of Weinan Normal University 2005,20(5):5-7) synthesized ethyl p-hydroxybenzoate.

[0033] Add 0.05mol (6.9g) p-hydroxybenzoic acid, 0.2mol (11.65ml) ethanol and 0.017mol (1.66g) catalyst to a three-necked flask equipped with an electric stirrer, a thermometer, and a reflux device with a water separator Sulfamic acid was heated to reflux for 3 hours, the catalyst was filtered out while it was hot, and the raffinate was quickly poured into cold water, and the solid crude product was precipitated from the water. Filtration, the filter cake was washed with 5% Na 2 CO 3 Wash with aqueous solution and water, and dry to obtain crude product. In a round bottom flask equipped with a reflux condenser, add the crude product of ethyl p-hydroxybenzoate, ethanol, water and 0.1% activated carbon at a molar ratio of 1:4:0.5, heat to reflu...

Embodiment 2

[0034] The preparation of embodiment 2 ethyl p-hydroxybenzoate granules

[0035] Each packet of granules contains the following components:

[0036] Ethylparaben 5mg

[0037] Starch 2497.5mg

[0038] Microcrystalline cellulose 2497.5mg

[0039] The preparation method is as follows: pass ethyl p-hydroxybenzoate through 80-mesh sieve, mix evenly with starch and microcrystalline cellulose, use appropriate amount of water to make soft material, granulate, dry, granulate, and pack.

Embodiment 3

[0040] The preparation of embodiment 3 ethyl p-hydroxybenzoate tablet

[0041] Each tablet contains the following ingredients:

[0042]

[0043] The preparation method is as follows: pass ethyl p-hydroxybenzoate through a 80-mesh sieve, mix evenly with lactose and cornstarch, add appropriate amount of water and granulate the powder, after drying, sieve the granules and mix with magnesium stearate, Tablets are available.

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