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Minoxidil-salicylate crystal form for treating alopecia and preparation method of minoxidil-salicylate crystal form

A technology of salicylate and salicylic acid, which is applied in the field of drug crystal forms, can solve the problems of slow and accelerated onset of effect, and achieve excellent therapeutic effect

Inactive Publication Date: 2021-10-15
SHANDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that external use of minoxidil can stimulate the proliferation and differentiation of hair follicle epithelial cells, and then promote hair growth. It can be used to treat hair loss, alopecia areata and other diseases, but it has the disadvantage of slow onset of action and many side effects, such as allergies , skin flushing, lower extremity edema, rapid heartbeat, etc.

Method used

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  • Minoxidil-salicylate crystal form for treating alopecia and preparation method of minoxidil-salicylate crystal form
  • Minoxidil-salicylate crystal form for treating alopecia and preparation method of minoxidil-salicylate crystal form
  • Minoxidil-salicylate crystal form for treating alopecia and preparation method of minoxidil-salicylate crystal form

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] (1) Weigh 200.0 mg of minoxidil and 132.6 mg of salicylic acid into a 50 mL round bottom flask, add 10 mL of distilled water, 2 mL of acetonitrile and 10 mL of ethanol.

[0021] (2) The reaction was stirred in a water bath at 70 °C for 1 hour, and the solid was completely dissolved.

[0022] (3) Filter the reaction solution with medium-speed filter paper, place the filtrate in a 50 mL beaker, cover the mouth of the beaker with plastic wrap, pierce 5 small holes with a 10 mL syringe, and let it stand for crystallization. A colorless needle-like solid precipitated after about 24 hours, which was minoxidil-salicylate crystal form.

Embodiment 2

[0024] (1) Weigh 100.0 mg of minoxidil and 66.4 mg of salicylic acid into a 50 mL round bottom flask, add 10 mL of methanol, 5 mL of distilled water and 1 mL of acetonitrile.

[0025] (2) Stir the reaction in a water bath at 70 °C for 1 hour, and the solids are completely dissolved.

[0026] (3) Filter the reaction solution with medium-speed filter paper, put the filtrate in a 50 mL beaker, cover the mouth of the beaker with plastic wrap, pierce 5 small holes with a 10 mL syringe, and let it stand for crystallization. A colorless needle-like solid precipitated after about 12 hours, which was minoxidil-salicylate crystal form.

Embodiment 3

[0028] (1) Weigh 422.1 mg of minoxidil and 279.2 mg of salicylic acid into a 50 mL round bottom flask, add 20 mL of ethanol, 2 mL of dichloromethane and 2 mL of acetonitrile.

[0029] (2) The reaction was stirred in a water bath at 40 °C for 3 hours, and the solids were completely dissolved.

[0030] (3) Filter the reaction solution with medium-speed filter paper, place the filtrate in a 50 mL beaker, cover the mouth of the beaker with plastic wrap, pierce 5 small holes with a 10 mL syringe, and let it stand for crystallization. A colorless needle-like solid precipitated after about 72 hours, which was minoxidil-salicylate crystal form.

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Abstract

The invention relates to a minoxidil-salicylate crystal form for treating alopecia and a preparation method of the minoxidil-salicylate crystal form. The minoxidil-salicylate crystal form is formed by combining three minoxidil cations, two minoxidil molecules, two salicylic acid anions, one salicylic acid molecule and five water molecules through interaction of ionic bonds and hydrogen bonds. The crystal structure belongs to a triclinic system, the space group is P-1, the axial length a is equal to 14.175 to 15.175 angstroms, the axial length b is equal to 14.643 to 15.643 angstroms, the axial length c is equal to 18.854 to 19.854 angstroms, the axial angle alpha is equal to 111.630 to 112.630 degrees, the axial angle beta is equal to 94.736 to 95.736 degrees, and the axial angle gamma is equal to 98.293 to 99.293 degrees. An animal model proves that the treatment effect of the minoxidil crystal form prepared by the method is superior to that of an original medicine.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical crystal forms, and in particular relates to a minoxidil-salicylate crystal form for treating hair loss and a preparation method thereof. Background technique [0002] In recent years, the field of drug research and development has developed rapidly and has broad prospects, but drug research and development has the characteristics of high investment and high risk. At the same time, the realization of the "Healthy China" strategy urgently requires targeted new medical solutions. It is a new "shortcut" for drug research and development to modify the crystal form of active ingredients of drugs by means of crystal engineering to obtain advantageous crystal forms that are more suitable for production, have better physical and chemical properties, and have better biological activity. Drug salt formation is one of the ways to modify the crystal form of drugs. Compared with the transformation metho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/50C07C65/10C07C51/43
CPCC07D239/50C07C65/10C07B2200/13
Inventor 任冬菊孙玉培冯梦娇张琪孙治夏张遨米佳钰刘宝明王琪彭元昌谢秀燕刘豪李丹萍叶凯姜柳郑康
Owner SHANDONG UNIV OF TECH
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