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Application of ultrafine powder and nanocrystallization technology in preparation of calcium hydroxybenzosulfonate as raw material

A calcium dobesilate, nano-technology, applied in the preparation of sulfonate, organic chemistry, anhydride/acid/halide active ingredients, etc., can solve the problems of dosage limitation, large dosage, etc., and achieve high bioavailability , the use of reduced dosage, the effect of oral convenience

Inactive Publication Date: 2010-12-01
姚春霞
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And calcium dobesilate preparation has its unique curative effect aspect prevention and treatment above-mentioned complication, and there is no alternative drug at present in the advantage of promoting microcirculation, it was listed in Europe in the seventies of the twentieth century, and in the nineties of the twentieth century At the beginning of the 1990s, it was imported to China by the Austrian Ibiva Pharmaceutical Factory. After nearly ten years of research in my country, the three major domestic pharmaceutical companies have successfully imitated it and put it on the market. In the past year, many manufacturers have imitated it and made it into raw materials and tablets. After nearly 40 years of application at home and abroad, the drug has a positive curative effect and less side effects, and is more and more accepted by doctors and patients. However, the drug is taken three times a day, 0.5 grams each time. It can be said that the dosage is relatively Big and expensive at the same time, so the amount used in the market is still relatively limited

Method used

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  • Application of ultrafine powder and nanocrystallization technology in preparation of calcium hydroxybenzosulfonate as raw material
  • Application of ultrafine powder and nanocrystallization technology in preparation of calcium hydroxybenzosulfonate as raw material
  • Application of ultrafine powder and nanocrystallization technology in preparation of calcium hydroxybenzosulfonate as raw material

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] The technical scheme provided by the invention is: hydroquinone is heated and refluxed with concentrated sulfuric acid for about 1 hour under the protection of nitrogen to form solid 2.5-dihydroxybenzenesulfonic acid, add water to the solid, stir, dissolve, add calcium carbonate in stages to neutralize, Make the pH between 4.6-6.0, leave to form calcium sulfate precipitate, filter, wash the calcium sulfate with water three times, combine the filtrate, concentrate under reduced pressure until the solid precipitates, add alcohol to stand, and crystallize, to obtain the crude product, then add the crude product to water, Adjust the pH to 6.0-7.0, place it to make the calcium sulfate completely precipitate, wash the calcium sulfate with water, add activated carbon to the combined filtrate for decolorization, filter, concentrate under reduced pressure, leave to precipitate crystals, filter, dry, and then enter the nano-sized pulverizer for pulverization Get this product and o...

Embodiment 2

[0017] The technical scheme provided by the invention is: hydroquinone is heated and refluxed with concentrated sulfuric acid for about 1 hour under the protection of nitrogen to form solid 2.5-dihydroxybenzenesulfonic acid, add water to the solid, stir, dissolve, add calcium carbonate in stages to neutralize, Make the pH between 4.6-6.0, leave to form calcium sulfate precipitate, filter, wash the calcium sulfate with water three times, combine the filtrate, concentrate under reduced pressure until the solid precipitates, add alcohol to stand, and crystallize, to obtain the crude product, then add the crude product to water, Adjust the pH to 6.0-7.0, place it to make the calcium sulfate completely precipitate, wash the calcium sulfate with water, add activated carbon to the combined filtrate to decolorize, filter, concentrate under reduced pressure, leave to precipitate crystals, filter, dry, and pulverize in the micronizer Get this product and other steps to prepare

[0018] ...

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Abstract

The invention relates to application of an ultrafine powder and nanocrystallization technology in the preparation of calcium hydroxybenzosulfonate as a raw material. A product is prepared through the following steps of: carrying out heating reflux of hydroquinone and concentrated sulfuric acid for about 1 hour under nitrogen protection to form 2,5-dihydroxybenzenesulfonic acid as a solid, adding water into the solid for stirring, dissolving, adding calcium carbonate for neutralization in several times to enable the pH to be 4.6-6.0, placing to generate calcium sulfate precipitates, filtering, washing calcium sulfate with water in three times, merging filtrates, carrying out decompression concentration until the solid is precipitated, adding alcohol for placing, precipitating crystals to obtain a crude product, then adding the crude product into the water, regulating the pH to be 6.0-7.0, placing to enable the calcium sulfate to be completely precipitated, washing the calcium sulfate with the water, merging the filtrates, adding activated carbon for decoloring, filtering, carrying out decompression distillation and concentration, placing to precipitate the crystals, filtering, drying, and then entering a nanocrystallization pulverizer for pulverization to obtain the product. The product is quite easy to absorb and has high bioavailability, the used dosage and the adverse reaction are reduced, the production cost can be lowered, great advantages are brought to patients, and the usage of medicine raw materials supplies a direction for the future development of preparations.

Description

technical field [0001] The invention relates to a preparation method and application of a raw material containing nano medicine, which belongs to the field of medicine. Background technique [0002] Diabetes is a common and frequently-occurring disease. With the improvement of people's living standards, its incidence is on the rise. With the prolongation of the course of diabetes, its complications are inevitable. Diabetic retinopathy and varicose veins caused by diabetes In terms of diabetes, gangrene, etc., the incidence rate of complications after five years is more than 30%, and the incidence rate after ten years is more than 95%. Therefore, while controlling diabetes blood sugar, prevent and treat complications caused by diabetes is a necessity. The calcium dobesilate preparation has its unique curative effect in the prevention and treatment of the above-mentioned complications, and there is no substitute drug at present for its advantages in promoting microcirculation...

Claims

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Application Information

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IPC IPC(8): C07C309/42C07C303/32A61K31/185A61P3/10B02C19/00
Inventor 姚春霞
Owner 姚春霞