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Synthetic method for superfine sulfuric acid and salbutamol

A technology of albuterol sulfate and albuterol, which is applied in chemical instruments and methods, preparation of organic compounds, preparation of amino hydroxyl compounds, etc., and can solve the problems of unsuitability for industrial production, complicated operation process, and high cost

Inactive Publication Date: 2005-01-19
NANOMATERIALS TECH PTE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] Although these methods can better control the particle size, the operation process is complicated and the cost is high, so it is not suitable for industrial production.

Method used

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  • Synthetic method for superfine sulfuric acid and salbutamol
  • Synthetic method for superfine sulfuric acid and salbutamol
  • Synthetic method for superfine sulfuric acid and salbutamol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Dissolve 18 g of salbutamol purchased from the market (produced by Chongqing Dianjiang Yingte Chemical Co., Ltd., sold under the trade name salbutamol base 021112) in 500 ml of ethanol solvent, place in a constant temperature water bath, and heat to 50 ° C to make salbutamol in ethanol Reach near saturation; The ethanolic solution of gained salbutamol and the H of 2.5mol / l 2 SO 4 The solution was added into 1000ml reaction vessels with electric stirring through peristaltic pumps according to the flow ratio of 1:30, the reaction temperature was controlled at 50°C, the stirring speed was 500rpm, the reaction time was 10min, and the pH value was 5.5-6, and sulfuric acid was obtained. Crystal slurry of albuterol. Then carry out suction filtration and separation, wash the filter cake with ethanol three times and carry out vacuum drying at 50° C. for 12 hours to obtain superfine salbutamol sulfate powder. The particle size distribution of the product is uniform, the average...

Embodiment 2

[0058] Control other process parameters to be constant, change the reaction temperature of salbutamol and sulfuric acid to be 5 ℃, the appearance of obtained salbutamol sulfate powder is similar to that of Example 1, the average particle diameter of the product particles prepared thus is about 1 μm, wherein at least 80% of the particles have a particle size between 0.8 μm and 1.2 μm.

Embodiment 3

[0060] Control other technological parameters and be identical with embodiment 2 unchanged, and change stirring speed and be 900rpm, the appearance that obtains salbutamol sulfate powder is similar to that of embodiment 2, the product particle average particle diameter that prepares thus is about 600nm, wherein at least 80% of the particles have a particle size between 500nm-700nmm.

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Abstract

The invention relates to a synthetic method for superfine sulfuric acid and salbutamol through using salbutamol and sulfuric acid as reactants, dissolving salbutamol into inert organic solvent, controlling the process operation parameters of the reaction, separating out salbutamol sulfate crystallization, filtering, scouring and drying to obtain the end product.

Description

technical field [0001] The invention relates to a synthesis method of ultrafine medicine, in particular to a synthesis method of ultrafine albuterol sulfate (1-(4-hydroxyl-3-hydroxymethylphenyl)-2-(tert-butylamino)ethanol sulfate). Background technique [0002] Salbutamol Sulfate (Salbutamol Sulfate) has another name called albuterol, and its structural formula is: [0003] [0004] It is a potent selective beta 2 - Receptor agonists have been widely used clinically to treat respiratory diseases such as asthmatic bronchitis, bronchial asthma and emphysema patients' bronchospasm. It has the characteristics of strong action and fast curative effect, and is the first choice drug for clinical treatment of asthma. In recent years, salbutamol sulfate ranks before the 20th in the sales volume of the world pharmaceutical market. [0005] The current formulations of salbutamol sulfate mainly include: oral tablets and capsules; injections for injection and inhalation gas (powder...

Claims

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Application Information

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IPC IPC(8): C07C213/02C07C215/56
Inventor 陈建峰刘晓林续京吉米·云
Owner NANOMATERIALS TECH PTE
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