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Bromhexine hydrochloride compound and pharmaceutical composition thereof

A technology of bromhexine hydrochloride and a compound, applied in the field of medicine, can solve the problems of high process requirements, instability of bromhexine hydrochloride, poor stability, etc., and achieves the advantages of simple prescription process, improved safety and effectiveness, and improved stability. Effect

Active Publication Date: 2013-06-12
湖北美林药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the new crystalline compound prepared by this application has good stability in the accelerated test, we found that its stability under light conditions is poor
[0007] In the existing technical solutions represented by the above-mentioned technical solutions, in order to overcome the unstable problem of bromhexine hydrochloride, relatively complicated preparation techniques are generally used or more excipients are added or new drug crystal forms are developed. The general process requirements are high, the addition increases the cost and unsafe factors or the quality improvement is not comprehensive, thus limiting the use of bromhexine hydrochloride preparations

Method used

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  • Bromhexine hydrochloride compound and pharmaceutical composition thereof
  • Bromhexine hydrochloride compound and pharmaceutical composition thereof
  • Bromhexine hydrochloride compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The preparation of embodiment 1 bromhexine hydrochloride compound

[0052] Put 100g of bromhexine hydrochloride crude product in a mixed solution of 1200g ethanol and methanol (volume ratio 15:1), heat up to 50°C at 0.5°C / min while stirring at a speed of 150 rpm, and stir until completely dissolved; Maintain 50°C, add 1.5g of activated carbon, stir at 200 rpm for 30 minutes, filter to remove carbon, and filter the filtrate through a 0.22μm filter membrane; at 45°C, at a stirring speed of 100 rpm, stir while stirring Add 4800g of a mixed solution of water and acetone with a volume ratio of 5:1 dropwise at a speed of 1 min; cool down to 8°C at 2°C / min, stop stirring; cool down to 2°C at 0.2°C / min and let stand to grow crystals for 12 hours, filter; filter the cake Wash twice with 2 times the weight of acetone, and dry in vacuum at 45° C. for 8 hours to obtain the bromhexine hydrochloride compound.

[0053] The melting point of this compound is 245-248°C. X-ray powder di...

Embodiment 2

[0054] Embodiment 2 The preparation of bromhexine hydrochloride compound

[0055] Put 100 g of bromhexine hydrochloride crude product in a mixed solution of 1200 g ethanol and methanol (volume ratio 15:1), heat up to 50 °C at 0.5 °C / min while stirring at a speed of 200 rpm, and stir until completely dissolved; Maintain 50°C, add 1.5g of activated carbon, stir at 250 rpm for 30 minutes, filter to remove carbon, and filter the filtrate through a 0.22μm filter membrane; Add 4800g of a mixed solution of water and acetone with a volume ratio of 5:1 dropwise at a speed of 1 min; cool down to 12°C at 2.5°C / min, stop stirring; cool down to 5°C at 0.5°C / min and let the crystal grow for 12 hours, filter; filter the cake Wash twice with 2 times the weight of acetone, and dry in vacuum at 50° C. for 10 hours to obtain the bromhexine hydrochloride compound. The melting point of this compound is 245-248°C. The X-ray powder diffraction pattern is consistent with Example 1.

[0056] The br...

Embodiment 3

[0057] The preparation of embodiment 3 bromhexine hydrochloride compound powder injection (specification: 4mg)

[0058] The bromhexine hydrochloride compound prepared by the present invention is aseptically sub-packed according to the bromhexine hydrochloride dose of 4 mg / bottle in a 100-grade aseptic environment, stoppered, and packed after passing the crimping inspection.

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Abstract

The invention relates to a bromhexine hydrochloride compound. The bromhexine hydrochloride compound is a crystal body and determined by using an X-ray powder diffraction method, and the characteristic peaks of the bromhexine hydrochloride compound are shown in a map in which 2theta plus or minus 0.2 degree is equal to 7.0 degrees, 10.9 degrees, 14.6 degrees, 15.8 degrees, 17.9 degrees, 21.1 degrees, 22.2 degrees, 23.4 degrees, 25.2 degrees, 29.3 degrees, 30.3 degrees, 33.4 degrees, 36.7 degrees and 39.6 degrees. The invention further provides a preparation and a pharmaceutical composition preparation which comprise the bromhexine hydrochloride compound, wherein the preparations can be prepared to form powder injection, freeze-dried powder injection, water injection and tablets. The formulation technology of the powder injection, freeze-dried powder injection, water injection and tablets of the bromhexine hydrochloride compound provided by the invention is simple in process, the stability of the bromhexine hydrochloride compound is obviously improved, and the safety and effectiveness of medication are improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a bromhexine hydrochloride compound and a pharmaceutical composition thereof. Background technique [0002] Bromhexine hydrochloride, its chemical name is: N-methyl-N-cyclohexyl-2-amino-3,5-dibromobenzylamine hydrochloride. Drug aliases: Hexyl ammonium bromide, benzyl cyclohexyl ammonium bromide, benzalkonium, bromhexine hydrochloride, will eliminate phlegm, benzalkonium bromide, benzyl cyclohexyl bromide. This product is white or off-white crystalline powder; odorless and tasteless. This product is slightly soluble in ethanol or chloroform, very slightly soluble in water. This product can directly act on bronchial glands, promote the release of lysosomes of mucus secreting cells, and make the sticky sugar fibers in sputum differentiate and crack; it can also inhibit the synthesis of acid glycoproteins in mucous glands and goblet cells, making them Secrete low-viscosity small m...

Claims

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Application Information

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IPC IPC(8): C07C211/52C07C209/84A61K31/137A61P11/12A61P11/10
Inventor 李美林马虹胡成忠
Owner 湖北美林药业有限公司
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