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Process for producing salbutamol sulfate fine powder

A technology of albuterol sulfate and fine powder, which is applied in the fields of pharmaceutical formulation, drug delivery, respiratory diseases, etc., can solve the problems of reduced curative effect, reduced solute solubility, large grain size distribution range, etc., and achieves low preparation cost and high particle size. The effect of narrow distribution and strong practicality

Inactive Publication Date: 2009-05-13
CHINA NAT ACAD NANOTECH & ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] According to the physiological structure of the respiratory tract, in order to effectively distribute or deposit the drug on the treatment site, the particle size of the drug is usually required to be below 7 μm, and the particle size is too large (greater than 10 μm) or too small (less than 0.5 μm) may make the drug cannot be effectively deposited. reduce the curative effect
In order to obtain drug particles, the traditional physical method is to physically sieve the raw materials through crushing, grinding, and ball milling. The property is not ideal; the traditional chemical method uses evaporation, heating, cooling or adding another component in the solution to reduce the solubility of the solute, so that the solute is deposited from a saturated solution to form a crystalline or amorphous powder. The diameter distribution range is still large, and it is easy to produce different crystal forms

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 0.4g of salbutamol sulfate raw material and dissolve it in 5ml of water, then add 80ml of dimethyl sulfoxide, mix with ultrasonic, and filter to obtain a clear solution; set the system parameters of supercritical recrystallization equipment: temperature 45°C, pressure 150bar, CO 2 The flow rate is 20g / min, the CO 2 After pumping into the heater, enter the crystallization tank until the system is balanced; pump the above-mentioned salbutamol sulfate solution into the crystallization tank at a flow rate of 1ml / min; stop the input of the salbutamol sulfate solution, keep the system state, and continue to feed CO 2 For 30-40 minutes, it is used to dry the crystallization of salbutamol sulfate and remove the residual solvent in the crystallization tank to obtain fine powder of salbutamol sulfate. The obtained above-mentioned fine powder was observed by SEM, and the results showed that the particle size of albuterol sulfate micropowder was round and uniform, with an av...

Embodiment 2

[0021] The pressure, temperature and flow in the preparation method and process parameters are all the same as in Example 1, and only the preparation method of salbutamol sulfate solution is changed, that is, 0.4 g of salbutamol sulfate is directly dissolved in 120 ml of dimethyl sulfoxide. The obtained fine powder was observed by SEM, and the results showed that the appearance of the obtained product was similar to that of Example 1, but the average particle size of the crystals was about 5 μm; as measured by a particle size distribution analyzer, 90% of the particles had a particle size within 8 μm. .

Embodiment 3

[0023] The pressure, flow rate and solution concentration in the preparation method and process parameters are the same as in Example 1, only the temperature in the crystallization tank is changed to 55°C. The obtained above-mentioned fine powder is observed by SEM, and the result shows that: the appearance of the obtained product is similar to that of Example 1, but the crystal is rod-shaped, and the average particle diameter of the long diameter is about 7 μm; measured by a particle size distribution analyzer, 90% of the particles are The diameter is within 13 μm.

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Abstract

The invention relates to a method for preparing fine powder of salbutamol sulfate. The method is carried out by using a supercritical recrystallization device, and comprises the following steps: inputting CO2 into a heater through a pump, and after heating, transforming the CO2 into supercritical CO2 which then entering a crystallization kettle; pumping salbutamol sulfate solution into the crystallization kettle; blending the supercritical CO2 with the salbutamol sulfate solution in a nozzle and spraying out via the nozzle, and separating out salbutamol sulfate crystal; after stopping adding the solution, continuing washing and drying the crystal through the supercritical CO2, and finally obtaining the fine powder of salbutamol sulfate. The method has the advantages that the prepared fine powder crystal has uniform grain size and good smoothness, the grain size is in narrow distribution, the obtained granules have smooth surface and are basically spherical; the technique is simple and easy to control, the practicability is strong, the preparation cost is low, the used organic reagent is recoverable, and CO2 can not cause pollution after being discharged to the air; the fine powder of salbutamol sulfate can be used as the main component of dry powder inhalation or aerosol, and pharmaceutical preparation can be prepared by blending the fine powder of salbutamol sulfate with other auxiliary materials.

Description

(1) Technical field [0001] The invention relates to a preparation technology of fine powder medicine, in particular to a preparation method of albuterol sulfate fine powder. (2) Background technology [0002] Salbutamol sulfate [1-(4-hydroxy-3-hydroxymethylphenyl)-2-(tert-butylamino)ethanol sulfate] is a potent and fast-acting selective β 2 Receptor agonists have a good therapeutic effect on respiratory diseases such as bronchospasm in patients with asthmatic bronchitis, bronchial asthma and emphysema. At present, albuterol sulfate is on the market, usually in the form of aerosols, capsules, sustained-release dispersible tablets, and sustained-release pellets. However, the Society of Allergy and Immunology of the American Medical Association recommends that inhalation should be the first choice for the use of salbutamol for asthma. way. [0003] According to the physiological structure of the respiratory tract, in order to effectively distribute or deposit the drug on the ...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K31/137A61P11/06
Inventor 郑洪浩
Owner CHINA NAT ACAD NANOTECH & ENG
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