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Compound external preparation for treating alopecia areata and preparation method thereof

An external preparation and compound technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of difficult to dissolve, lack of continuous effective or permanent reversal of alopecia areata hair loss treatment methods, difficult to prepare Solubility, storage stability, compound preparations for external use, etc.

Active Publication Date: 2022-01-21
CHANGSHA JINGYI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the main function of minoxidil is to improve the microcirculation disorder and accelerate the hair growth rate, which is a symptomatic treatment, so it is only effective for mild alopecia areata, and has little effect on the more harmful alopecia totalis and general alopecia
[0006] In addition, the inventors have found in their research that tofacitinib or its pharmaceutically acceptable salt and minoxidil or its pharmaceutically acceptable salt are difficult to dissolve in various solvents, or even if they are dissolved, the It is also easy to crystallize during the process, and it is difficult to prepare a compound preparation for external use with good solubility and good storage stability
[0007] To sum up, whether it is tofacitinib for cause treatment or minoxidil for symptomatic treatment, both have certain limitations when used alone in the treatment of alopecia areata, and there is currently a lack of sustained effective or permanent treatment for alopecia areata , there is an urgent need for an external compound preparation with good effect, simple preparation, good solubility and good storage stability

Method used

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  • Compound external preparation for treating alopecia areata and preparation method thereof
  • Compound external preparation for treating alopecia areata and preparation method thereof
  • Compound external preparation for treating alopecia areata and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Embodiment 1: water-alcohol type foaming agent

[0126] (1) Prescription

[0127] components Content (based on the total mass or total volume of the composition) Tofacitinib 1.5wt% Minoxidil 2% (w / v) Sodium dodecyl sulfate 2wt% Tween 80 1wt% glycerin 4wt% Polyvinylpyrrolidone 2wt% xanthan gum 1wt% cetyl alcohol 1wt% Propylene Glycol 8wt% PEG400 25wt% Tetrafluoroethane 10wt% purified water margin

[0128] (2) Preparation method

[0129] In the preparation container, add the prescribed amount of purified water, PEG 400 and propylene glycol, and stir evenly to form a mixed solvent. While stirring, slowly add the prescribed amount of Tween 80, sodium lauryl sulfate, tofacitinib, minoxidil, glycerin, polyvinylpyrrolidone, xanthan gum, cetyl alcohol, and then homogenize or ultrasonically dissolve , to obtain a pre-foamed mixture. The prepared pre-foaming mixture is filled in...

Embodiment 2

[0130] Embodiment 2: water-alcohol type foaming agent

[0131] (1) Prescription

[0132] components Content (based on the total mass or total volume of the composition) Tofacitinib 1.5wt% Minoxidil 2% (w / v) Sodium Fatty Alcohol Polyoxyethylene Ether Sulfate 2wt% Tween 80 1wt% glycerin 4wt% hypromellose 1.5wt% carbomer 1wt% stearyl alcohol 1wt% ethanol 10wt% PEG400 30wt% purified water margin

[0133] (2) Preparation method

[0134] In the preparation container, add the prescribed amount of purified water, PEG 400 and ethanol, and stir evenly to form a mixed solvent. While stirring, slowly add Tween 80, sodium fatty alcohol polyoxyethylene ether sulfate, tofacitinib, minoxidil, glycerin, hypromellose, carbomer, stearyl alcohol in the prescribed amount, and then Substance or ultrasonic dissolution to obtain a pre-foamed mixture. Put the prepared pre-foaming mixture into a hand-pressed...

Embodiment 3

[0135] Embodiment 3: Emulsion foam

[0136] (1) Prescription

[0137] components Content (based on the total mass or total volume of the composition) Tofacitinib 1.5wt% Minoxidil 2% (w / v) Soybean oil 4wt% coconut oil 3wt% Isopropyl myristate 3wt% cetyl alcohol 1wt% stearyl alcohol 2wt% xanthan gum 1wt% Polyvinylpyrrolidone 1wt% Sodium dodecyl sulfate 2wt% Tween 80 2wt% glycerin 4wt% PEG400 30wt% Tetrafluoroethane-heptafluoropropane 10wt% purified water margin

[0138] (2) Preparation method

[0139] Preparation of water phase mixture: Add the prescribed amount of xanthan gum, polyvinylpyrrolidone, sodium lauryl sulfate, Tween 80, glycerin, etc. into the mixed solvent of water and polyethylene glycol 400 while stirring, and heat to 50°C dissolve it;

[0140] Preparation of the oil phase mixture: heat soybean oil, coconut oil, and isopropyl myristate to 50°C...

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PUM

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Abstract

The invention discloses a compound external preparation for treating alopecia areata and a preparation method thereof, the compound external preparation comprises an active component A and an active component B, the active component A is one or more of a JAK (Janus kinase) inhibitor or pharmaceutically acceptable salts thereof, and the active component B is minoxidil or pharmaceutically acceptable salts thereof. The compound external preparation is good in drug effect, good in solubility and good in storage stability. The preparation method is simple to operate, and the solubility, the dissolution speed and the placement stability of the active ingredients are improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a compound external preparation for treating alopecia areata and a preparation method thereof. Background technique [0002] Alopecia areata is a common non-scarring hair loss disease caused by hair follicle inflammation. According to pathological features and severity, it can be divided into localized patchy alopecia areata, total alopecia and general alopecia. The global incidence rate is about 1% to 2%, and most of the patients are children and young adults. Alopecia areata affects the appearance and mental health of patients. Conventional treatment drugs (including glucocorticoids, compound glycyrrhizin, contact sensitizers, hair growth promoting agents, etc.) limitations, and therefore require the development of new therapeutic modalities. [0003] Alopecia areata is an inflammatory autoimmune disease, which is related to the destruction of hair follicl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/519A61K31/506A61K9/12A61K9/107A61K47/26A61K47/20A61P17/14
CPCA61K45/06A61K31/519A61K31/506A61K9/122A61K9/124A61K9/107A61K9/0014A61K47/26A61K47/20A61P17/14A61K2300/00A61K47/10A61K9/06
Inventor 张海龙
Owner CHANGSHA JINGYI PHARM TECH CO LTD
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