Acetazolamide medicine composition and medical application thereof

A technology of acetazolamide and its composition, which is applied in the field of acetazolamide pharmaceutical composition, can solve problems such as related reports on the prevention and treatment of Parkinson's disease with acetazolamide, and achieve outstanding substantive features, improved prevention and treatment effect, Significantly improved effect

Inactive Publication Date: 2016-08-17
SUZHOU BINUOJIA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there has been no report on the correlation between the pharmaceuti...

Method used

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  • Acetazolamide medicine composition and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0020] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0021] Separation method: (a) Grind the dried roots (2kg) of Polygonum cuspidatum, extract with 80% ethanol under heat reflux (15L×3 times), combine the extracts, concentrate until no alcohol smell (3L), and then use petroleum ether (3L× 3 times), ethyl acetate (3L×3 times) and water-saturated n-butanol (3L×3 times) to obtain petroleum ether extract, ethyl acetate extract and n-butanol extract respectively; (b) step (a) The ethyl acetate extract in (a) was removed with D101 macroporous resin. First, 8 column volumes were eluted with 10% ethanol, and then 10 column volumes were eluted with 70% ethanol. The 70% eluate wa...

Embodiment 2

[0024] Embodiment 2: Prevention and treatment of Parkinson's disease model

[0025] In this example, MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) was used to prepare a Parkinson's disease (PD) mouse model, and the drug was observed to improve the animal's limb coordination ability and regulate the brain Anti-PD effects in terms of neurotransmitter imbalance, restoration of DAergic neuron function, etc.

[0026] 1. Materials and methods

[0027] 1.1 Animals

[0028] 72 C57BL / 6 mice, ♂, 7-8 weeks old, weighing 18-22 g, were purchased from the Institute of Experimental Animals, Chinese Academy of Medical Sciences, certificate number: SCXK (Beijing) 2014-0001. The animals were kept in a ventilated and dry environment with a temperature of (22±1)°C, a relative humidity of 55%-65%, and a 12-h light cycle, and were fed with maintenance diet 1022 for rats and mice.

[0029] 1.2 Reagents and samples

[0030] Acetazolamide was purchased from Shanghai Jiwei Biotechnology Co., ...

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Abstract

The invention discloses a pharmaceutical composition of acetazolamide and its medical application. The pharmaceutical composition of acetazolamide provided by the invention contains acetazolamide and a natural acetazolamide with a novel structure isolated from the dried root of Polygonum cuspidatum. When the product compound (I), acetazolamide and the natural product compound (I) act alone, the prevention and treatment effect on Parkinson's disease is weak; when the two act together, the prevention and treatment effect on Parkinson's disease is significantly improved, and can be developed The medicine for preventing and treating Parkinson's disease has outstanding substantive features and remarkable progress compared with the prior art.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the prevention and treatment of Parkinson's disease, in particular to a pharmaceutical composition of acetazolamide and its medical application for preventing and treating Parkinson's disease. Background technique [0002] The chemical name of acetazolamide is N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide, which is currently commonly used in the prevention and treatment of glaucoma, cardiac edema, and cerebral edema. Petit mal seizures. [0003] Acetazolamide is a carbonic anhydrase inhibitor. Carbonic anhydrase is distributed in renal tubular epithelial cells, gastric mucosa, pancreatic cells, eye ciliary body epithelial cells, red blood cells and central nervous cells. The main function of this enzyme is to promote CO 2 and H 2 O binds to carbonic acid and dissociates carbonic acid to H + with HCO 3- . When the function of carbonic anhydrase is inhibited, any functional activiti...

Claims

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Application Information

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IPC IPC(8): C07D471/14A61K31/4375A61K31/433A61P25/16
CPCC07D471/14A61K31/433A61K31/4375
Inventor 徐珍
Owner SUZHOU BINUOJIA PHARMA CO LTD
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