CN100577168C - Cream for treating hair loss and preparation method thereof - Google Patents

Abstract

The invention discloses a cream for treating hair loss, which is composed of minoxidil, stearic acid, glyceryl monostearate, white petrolatum, liquid paraffin, glycerin, triethanolamine, sodium lauryl sulfate, hydroxyl Prepared from phenethyl ester, sodium thiosulfate, disodium edetate, propylene glycol, etc. The propylene glycol adopted in the present invention is not only a solvent but also a transdermal accelerator, which can promote the medicine to penetrate into the scalp. Since -N in the minoxidil structure is easily oxidized, according to the test, adding 0.25% sodium thiosulfate and 0.2% disodium ethylenediaminetetraacetic acid as an anti-oxidant by grinding at the same time has a better effect. The cream of the invention has the advantages of non-allergic, non-irritating, remarkable curative effect, short course of treatment, less times of administration, low price, safe and convenient to carry. It can be used to treat various alopecias.

Description

Cream for treating hair loss and preparation method thereof

technical field

The invention relates to a cream for treating alopecia and a preparation method thereof, belonging to the technical field of externally used medicines for treating alopecia.

Background technique

Alopecia is a kind of common disease, frequently-occurring disease, and there is constantly increasing tendency. In the prior art, there are also some medicines for treating hair loss, but there are problems such as poor hair growth effect, long course of treatment, and high price. Minoxidil (Minoxidil) is a kind of direct relaxation of smooth muscle, opening ATP-sensitive potassium channel and lowering blood pressure. It is the second or third-line drug for the treatment of hypertension. After taking it for more than one month, almost all patients will develop hirsutism side effect. This suggests that it can be used to treat alopecia. Based on this feature, we have repeatedly tested the drug from the preparation process to the clinical application, and it has been formulated into Minoxidil in the preparation room of our hospital since 1989. Er tincture, for local clinical use in our hospital, has achieved remarkable curative effect in the treatment of alopecia cases. But, find in clinical application process, because this medicine is with ethanol as solvent, stay time in treatment part is short, needs to increase administration frequency, has many patients to ethanol allergy, adds carrying inconvenient and unsafe (easy to catch fire) ), so that the use of this preparation is limited.

Contents of the invention

The purpose of the present invention is to provide a non-allergic, non-irritating, significant curative effect, short course of treatment, low price, safe and convenient to carry cream for treating hair loss and its preparation method. For the treatment of alopecia areata, male pattern baldness, seborrheic alopecia and other alopecia.

The cream for treating hair loss of the present invention is prepared from the following raw materials in parts by weight: 15.0-25.0 grams of minoxidil, 100.0-150.0 grams of stearic acid, 50.0-100.0 grams of glyceryl monostearate, white Vaseline 50.0-100.0 grams, liquid paraffin 150.0-200.0 grams, glycerin 150.0-200.0 grams, triethanolamine 2.0-4.0 ml, sodium lauryl sulfate 1.6-2.0 grams, ethylparaben 1.0-2.0 grams, sodium thiosulfate 2.5-3.5 grams, 2.0-3.0 grams of disodium edetate, 20.0-25.0 milliliters of propylene glycol.

In order to achieve a better effect, it can be prepared from the following raw materials in parts by weight: 20.0 grams of minoxidil, 125.0 grams of stearic acid, 75.0 grams of glyceryl monostearate, 75.0 grams of white petrolatum, and 175.0 grams of liquid paraffin , Glycerin 175.0g, Triethanolamine 3.0ml, Sodium Lauryl Sulfate 1.8g, Ethylparaben 1.5g, Sodium Thiosulfate 3.0g, Disodium EDTA 2.5g, Propylene Glycol 23.0ml.

Add 0.6-1.2 grams of essence to the above raw materials, and add 456-186 milliliters of distilled water. Or add 0.9 grams of essence to the above raw materials, and add 322.0 milliliters of distilled water.

The preparation method of the cream for treating hair loss of the present invention comprises weighing stearic acid, glyceryl monostearate, liquid paraffin, white petrolatum, heating and melting, and keeping warm at 80-90° C. to make the oil phase; Add triethanolamine, sodium lauryl sulfate, and glycerin after phenethyl ester, and then keep warm to 82-92°C to make the water phase; add the oil phase to the water phase, stir in the same direction until it solidifies, and obtain oil-in-water ( O/W) type emulsifiable cream base is standby; Minoxidil is dissolved in propylene glycol again, gets sodium thiosulfate, edetate disodium to dissolve in water and both grind into paste, then gradually ( Add the oil-in-water (O/W) cream base according to the equal-volume incremental method, stir while adding (in the same direction), then add the essence, stir and mix well, pack in sealed light-proof containers, and store below 25°C That's it.

The applicant has overcome the shortcoming of minoxidil tincture by preparing the cream preparation with O/W type cream as the base, and through clinical application, this preparation has no allergies, no stimulation, safe and convenient to carry, and can be used in the treatment of The advantages of long retention time at the site and less frequency of administration. The applicant has done a lot of tests to verify the cream of the present invention. When selecting the raw materials of the cream, it is found that minoxidil is insoluble in water. After dissolving it in propylene glycol, it is mixed with the prepared cream base , to achieve the purpose of full mixing and uniformity. Propylene glycol is both a solvent and a skin penetration enhancer, which can promote the penetration of drugs into the scalp. The -N in the minoxidil structure is easily oxidized. According to the test, adding 0.25% sodium thiosulfate and 0.2% disodium ethylenediaminetetraacetic acid as an anti-oxidant by grinding at the same time has a better effect. The results confirmed that after the preparation was placed at room temperature for 9 months, its appearance color and pH value changed little, and there was no oil-water separation and flatulence phenomenon, and the content of the main ingredient was determined to be within the qualified range.

The cream of the present invention is used for skin irritation test: select healthy adult rabbits with similar numbers of males and females, and remove hair on both sides of the spine of the rabbit's back before administration to keep the skin intact. During the test, Shengfaling cream was applied to the right depilatory area, and the cream base was applied to the left depilatory area as a blank control, twice a day for a total of 7 days. No redness, swelling or erosion was observed at the application site. , indicating that the preparation is non-irritating.

The emulsifiable paste of the present invention is done skin allergy test: choose healthy adult white guinea pig, male and female half and half, before the test 24h, guinea pig back both sides are depilated, guinea pig is divided into 2 groups at random, and the 1st group is coated with emulsifiable cream matrix control, The second group applied Shengfaling cream twice a day for 7 days. The application site was observed, and no erythema or edema was seen in both groups, indicating that the preparation has no skin allergies.

Cream of the present invention is used for alopecia patients, and the treatment results are as follows:

Case selection 228 cases of hair loss patients are outpatient cases, excluding patients with hypertension, diabetes and liver and kidney diseases. 228 cases were randomly divided into two groups, 193 cases in the treatment group, 113 males and 80 females, aged 18-54 years, with an average age of 35 years, including 102 cases of alopecia areata (>3 bald spots) and 51 cases of total alopecia , 40 cases of alopecia universalis; course of disease 1 to 4 years (average 1.6 years). The control group consisted of 35 cases, including 21 males and 14 females, aged 19 to 56 years, with an average age of 37 years, and a course of 1 to 4 years (average 1.7 years). The degree of alopecia was similar to that of the treatment group. The two groups of patients were comparable.

Administration method: The treatment group is rubbed with the emulsifiable paste of the present invention on the alopecia, 1-2 times a day, and the course of treatment is 3-6 weeks. The control group applied cream base on the hair loss area, 1-2 times a day, and the course of treatment was the same as above. The two groups also tapped the hair loss area with plum blossom needles to flush the skin, and then applied fresh ginger juice. During the treatment period, the two groups did not use other drugs.

Efficacy evaluation criteria: recovery: new hair growth, dense distribution, hair thickness, and color are the same as normal hair; marked effect: new hair growth > 70%, hair thickness, and color close to normal; effective: new hair growth 10% to 70%, including vellus hair Growth, black or white in color; invalid: observation for 5 months, new hair growth <10% or continued hair loss.

The curative effect of the treatment results is shown in the attached table.

The comparison of curative effect of the two groups in the attached table for the treatment of alopecia cases

Adverse reactions During the application of the emulsifiable paste of the present invention, no adverse reactions occurred in the patient.

Detailed ways

Embodiments of the present invention: 20 grams of minoxidil, 100 grams of stearic acid, 50 grams of glyceryl monostearate, 50 grams of white petrolatum, 150 grams of liquid paraffin, 150 grams of glycerin, 2 ml of triethanolamine, lauryl 1.6 grams of sodium sulfate, 1 gram of ethylparaben, 2.5 grams of sodium thiosulfate, 2.1 grams of disodium edetate, 20 milliliters of propylene glycol, 0.9 grams of essence, distilled water was added to the rest, and the total amount was added to 1000 grams.

Weigh stearic acid, glyceryl monostearate, liquid paraffin, white vaseline according to the above parts by weight, heat and melt, and keep warm at about 82°C to make the oil phase.

Dissolve the ethylparaben with an appropriate amount of hot water, add triethanolamine, sodium lauryl sulfate, and glycerin, and keep warm to about 80°C. Slowly add the oil phase into the water phase and stir until it solidifies, and then the O/W cream base is obtained for later use. Then dissolve minoxidil in propylene glycol, dissolve sodium thiosulfate and disodium edetate in a small amount of water, grind the two into a paste, add them to the cream base and stir while adding (in the same direction) Add essence, stir and mix well, pack in airtight light-proof containers, and store below 25°C.

When using, apply the cream to the hair loss area, 1-2 times a day, and the course of treatment is 3-6 weeks.

Claims (6)

1. ointment for the treatment of alopecia, it is characterized in that: it is that feedstock production by following weight parts obtains: minoxidil 15.0～25.0 grams, stearic acid 100.0～150.0 grams, glyceryl monostearate 50.0～100.0 grams, white vaseline 50.0～100.0 grams, liquid paraffin 150.0～200.0 grams, glycerol 150.0～200.0 grams, 2.0～4.0 milliliters of triethanolamine, sodium lauryl sulphate 1.6～2.0 grams, ethyl hydroxybenzoate 1.0～2.0 grams, sodium thiosulfate 2.5～3.5 grams, disodiumedetate 2.0～3.0 grams, 20.0～25.0 milliliters of propylene glycol.

2. the ointment of treatment alopecia according to claim 1 is characterized in that: it is that feedstock production by following weight parts obtains: minoxidil 20.0 grams, stearic acid 125.0 grams, glyceryl monostearate 75.0 grams, white vaseline 75.0 grams, liquid paraffin 175.0 grams, glycerol 175.0 grams, 3.0 milliliters of triethanolamine, sodium lauryl sulphate 1.8 grams, ethyl hydroxybenzoate 1.5 grams, sodium thiosulfate 3.0 grams, disodiumedetate 2.5 grams, 23.0 milliliters of propylene glycol.

3. the ointment of treatment alopecia according to claim 1 is characterized in that: add essence 0.6～1.2 gram in above-mentioned raw materials, add 456～186 milliliters of distilled water.

4. the ointment of treatment alopecia according to claim 3 is characterized in that: adding essence in above-mentioned raw materials is 0.9 gram, and adding distilled water is 330 milliliters.

5. as the preparation method of claim 1 or the described treatment alopecia of 2 arbitrary claim ointment, it is characterized in that: take by weighing stearic acid, glyceryl monostearate, liquid Paraffin, white vaseline, heating and melting by above-mentioned weight portion, be incubated 80～90 ℃ and make oil phase; With adding triethanolamine, sodium lauryl sulphate, glycerol behind hot water dissolving's ethyl hydroxybenzoate, be incubated again to 82～92 ℃ and make water; Oil phase is added aqueous phase, and same direction limit edged stirs to solidifying, and it is standby to obtain the oil-in-water type emulsifiable paste matrix; Again minoxidil is dissolved in propylene glycol, get sodium thiosulfate, disodiumedetate and in water, dissolve and both are ground into pasty state, add the oil-in-water type emulsifiable paste matrix by amount then, the limit edged stirs, stirring and evenly mixing is sub-packed in the sealing light resistant container, preserves below 25 ℃ to get final product.

6. as the preparation method of claim 3 or the described treatment alopecia of 4 arbitrary claim ointment, it is characterized in that: take by weighing stearic acid, glyceryl monostearate, liquid Paraffin, white vaseline, heating and melting by above-mentioned weight portion, be incubated 80～90 ℃ and make oil phase; With adding triethanolamine, sodium lauryl sulphate, glycerol behind hot water dissolving's ethyl hydroxybenzoate, be incubated again to 82～92 ℃ and make water; Oil phase is added aqueous phase, and same direction limit edged stirs to solidifying, and it is standby to obtain the oil-in-water type emulsifiable paste matrix; Again minoxidil is dissolved in propylene glycol, getting sodium thiosulfate, disodiumedetate dissolves in water and both is ground into pasty state, add the oil-in-water type emulsifiable paste matrix by amount then, the limit edged stirs, add essence again, stirring and evenly mixing is sub-packed in the sealing light resistant container, preserves below 25 ℃ to get final product.