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High concentration glycerol-type minoxidil tincture and preparation method thereof

A minoxidil tincture and high-concentration technology, which is applied in the direction of medical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve the problem of poor transdermal effect of alcohol, inability to reach concentration, volatilization Fast and other problems, to avoid discomfort and hair loss, the time used for dissolution is short, and the effect of increasing hair growth speed

Inactive Publication Date: 2012-02-15
刘国辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The problem with the existing products is that the formula contains high concentration of propylene glycol, which has three functions: 1. Dissolve minoxidil well. The solubility of minoxidil in alcohol and water is very low, and it cannot reach more than 2%. Concentration, propylene glycol is a good co-solvent, the molecule contains 2 hydrophilic hydroxyl groups and a hydrophobic methyl group, which can make minoxidil dissolve to a concentration of more than 5% or even 15%.
[0005] In addition, it is also possible to directly dissolve minoxidil in a solvent containing water, glycerin, and alcohol, but no matter how the ratio of the three is adjusted, the concentration of minoxidil cannot reach more than 2%, and the polarity of glycerin is too large to penetrate the skin. The effect is too poor, the alcohol transdermal effect is not good, and it evaporates quickly

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Take by weighing 100 grams of minoxidil solid with electronic balance. Mix 500ml of ethanol with minoxidil, stir for 10 minutes to disperse minoxidil in ethanol, let it stand for 20 minutes to fully precipitate insoluble minoxidil, pour out the supernatant and record it as solution A.

[0032] Weigh 9 grams of sodium hydroxide, 3 grams of arginine, and 2 grams of disodium edetate and dissolve them in 100 ml of water. This solution is designated as solution B.

[0033]Weigh 0.1 gram of cystine and mix it with minoxidil precipitation, add 0.5 mol or 30 g of glacial acetic acid, mix well, then add 60 ml of pure water (to ionize acetic acid), put the mixture in a boiling water bath, and stir rapidly at the same time , until the solid matter is basically completely dissolved, avoiding an increase in the oxidation rate of minoxidil caused by a long-term water bath, and this solution is recorded as solution C.

[0034] Add solution B to solution C, and while stirring solution...

Embodiment 2

[0038] Fully dissolve 7 grams of sodium hydroxide, 7 grams of arginine, and 3 grams of disodium edetate in 50 ml of pure water, and set aside.

[0039] Dissolve 100 grams (about 0.53 mol) of azelaic acid in 1200 ml of alcohol. After fully dissolving, 100 grams of minoxidil was mixed with it, and after stirring for 15 minutes, 500 ml of glycerin was mixed with it and stirred for 15 minutes.

[0040] Quickly mix the solutions prepared in the previous two steps, add 20ml of water-soluble azone and 1g of taurine, adjust the pH value of the solution to 5.8, and finally dilute to 2000ml with pure water, mix well, the mass percentage of minoxidil 5%. The minoxidil tincture obtained will be stored in an environment at room temperature of 20 degrees, and stored in an opaque volumetric flask in the dark.

Embodiment 3

[0042] Take by weighing 150 grams of minoxidil solid with electronic balance. Mix 500ml of ethanol with minoxidil, stir for 10 minutes to disperse minoxidil in ethanol, let it stand for 20 minutes to fully precipitate insoluble minoxidil, pour out the supernatant and record it as solution A.

[0043] Weigh 18 grams of arginine and 5 grams of disodium edetate and dissolve them in 40 ml of water. This solution is designated as solution B.

[0044] Take by weighing 0.5 gram of cystine and minoxidil precipitation mix, add 0.75mol namely 45g glacial acetic acid, mix well, then add 40ml pure water (make acetic acid ionization), this mixture is placed in boiling water water bath, stirs rapidly simultaneously, Until the solid matter is basically completely dissolved, and the long-term water bath is avoided to cause the oxidation rate of minoxidil to increase, this solution is recorded as solution C.

[0045] Add solution B to solution C, and while stirring solution C, slowly add solu...

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Abstract

The invention relates to a high concentration glycerol-type minoxidil tincture for treating alopecia and a preparation method thereof. The high concentration glycerol-type minoxidil tincture of the invention comprises components of minoxidil, alcohol, glycerol, water-soluble azone, acids, ethylene diamine tetraacetic acid, arginine, cystine and water. Traditional propylene glycol is substituted by glycerol and water-soluble azone, so as to realize a minoxidil concentration of 5-15%, solve allergic problem caused by propylene glycol and realize a high minoxidil dissolving concentration; amino acids are added in the components to increase hair growing speed; when necessary, the arginine and / or sodium hydroxide is added with a pH buffer solution to stabilize a scalp pH at an optimum pH andavoid discomfort and hair shedding caused by pH change along with application of the hair grower. The invention employs a minoxidil step-by-step dissolving method with a short dissolving time to solve a problem of minoxidil oxidation during dissolving in a traditional technology.

Description

technical field [0001] The invention relates to a minoxidil tincture, in particular to a high-concentration glycerol-type minoxidil tincture for treating hair loss and a preparation method thereof. Background technique [0002] Hair loss is a major problem faced by many people. There are many reasons for hair loss. Common hair loss diseases include androgenetic alopecia (seborrheic alopecia), male pattern baldness, hereditary alopecia, alopecia areata, etc., which can occur in both men and women. Minoxidil (Minoxidil, chemical name is 2,4-diamino-6-piperidinyl pyrimidine-3-oxide) is the only topical chemical drug that has obvious curative effect on hair loss in the world. Minoxidil can grow hair through a variety of ways, and a large number of clinical trials have proved that minoxidil has a good curative effect on the above diseases and is very safe. Oral minoxidil can cause systemic reactions, including hirsutism and cardiovascular reactions, and various solutions contain...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K47/22A61K47/08A61P17/14
Inventor 刘国辉
Owner 刘国辉
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