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Tranexamic acid skin topical nano-preparation and its preparation method and use

A tranexamic acid and nano-formulation technology, applied in skin diseases, peptide/protein components, emulsion delivery, etc., can solve the problems of poor skin penetration ability of aqueous solution, unclear mechanism, skin irritation, etc., and improve local skin. Dullness, increasing efficacy, treating hyperpigmentation effects

Inactive Publication Date: 2016-06-22
CENT HOSPITAL XUHUI DISTRICT SHANGHAI CITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, tranexamic acid has strong polarity and poor transdermal ability of aqueous solution. Directly making tranexamic acid into a simple skin external preparation seriously affects its curative effect.
[0006] At present, there is no self-developed external preparation of tranexamic acid for the skin, and it has been reported that a simple combination of tranexamic acid and other components (Chinese patent CN99800921.0, Chinese patent CN200580031837, Chinese patent CN201110122382.1), with To achieve whitening or prevent pigmentation, but this composition is complex, the mechanism is not clear, it has certain irritation and damage to the skin, and it mostly belongs to the field of cosmetics

Method used

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  • Tranexamic acid skin topical nano-preparation and its preparation method and use
  • Tranexamic acid skin topical nano-preparation and its preparation method and use
  • Tranexamic acid skin topical nano-preparation and its preparation method and use

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Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0041] Prescription 1:

[0042]

[0043] Preparation:

[0044] ① Dissolve the prescription amount of tranexamic acid and glycerin (manufactured by Shantou Ziguang Guhan Amino Acid Co., Ltd.) in purified water, and stir at 300rpm with magnetic stirring (manufactured by IKA, model: RETBasicC) at 70±10°C About 10 minutes, until the tranexamic acid is completely dissolved to obtain the aqueous phase.

[0045] ②Weigh the prescribed amount of ethylparaben (manufactured by Hunan Erkang Pharmaceutical Co., Ltd.), soybean oil (manufactured by Tieling Beiya Pharmaceutical Oil Co., Ltd.), preheat to 70±10°C, and stir at 300rpm with magnetic stirring After about 10 minutes, after ethylparaben is completely dissolved, add the prescribed amount of polyoxyethylene castor oil (manufactured by BASF, Germany, trade name: CremophorEL) and VE (manufactured by DSM Vitamins (Shanghai) Co., Ltd.), and continue stirring to The solution was mixed evenly to obtain an oil phase.

[0046] ③Put the ...

preparation Embodiment 2

[0051] Prescription 2:

[0052]

[0053] Preparation:

[0054] ①Weigh the prescribed amount of tranexamic acid, glycerin, and sodium D-ascorbate (manufactured by Sinopharm Group Chemical Co., Ltd.) and dissolve them in pure water. Stir at 300rpm for about 10min with magnetic stirring at 70±10°C until it reaches the concentration of ammonia. The cyclic acid is completely dissolved to obtain an aqueous phase.

[0055] ②Weigh the prescribed amount of propylparaben (manufactured by Hunan Erkang Pharmaceutical Co., Ltd.), caprylic capric triglyceride (manufactured by Tieling Beiya Pharmaceutical Oil Co., Ltd.), egg yolk lecithin (manufactured by Japan Kewbi Co., Ltd.), Preheat to 70±10°C, and stir at 300rpm for about 10min with a magnetic stirrer to dissolve each substance to obtain an oil phase.

[0056] ③Put the oil phase and water phase in a water bath at 70±10°C, and cut them with a high shear machine for 10 minutes to form colostrum.

[0057] ④ Pass the colostrum through...

preparation Embodiment 3

[0061] Prescription 3:

[0062]

[0063] Preparation:

[0064] ①Weigh the prescribed amount of tranexamic acid, glycerin, and benzalkonium bromide (manufactured by Taicang Pharmaceutical Factory) and dissolve them in purified water, and stir at 300 rpm for about 10 minutes with magnetic stirring at 70±10°C until the tranexamic acid is completely Dissolved in the aqueous phase.

[0065] ②Weigh the prescribed amount of butylhydroxytoluene (provided by Beijing Fengli Jingqiu Trading Co., Ltd.), castor oil (manufactured by Hunan Erkang Pharmaceutical Co., Ltd.), Tween 80 (manufactured by Shanghai Shenyu Pharmaceutical Chemical Co., Ltd.), pre- Heat to 70±10°C, and stir at 300rpm for about 10min with a magnetic stirrer to dissolve each substance to obtain an oil phase.

[0066] ③Put the oil phase and water phase in a water bath at 70±10°C, and cut them with a high shear machine for 10 minutes to form colostrum.

[0067] ④ Pass the colostrum through a high-pressure homogenizer...

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Abstract

The invention relates to a tranexamic acid nano preparation for skin external use, a preparation method and application thereof. The nano preparation is prepared from tranexamic acid, medicinal oil, emulsifier, medicinal additive, thickener and purified water. The tranexamic acid nano preparation has good skin physiological compatibility, can effectively promote the transdermal absorption of tranexamic acid, improve the effect of tranexamic acid on preventing or treating pigmentation, and avoid systemic administration of tranexamic acid resulting toxic side effects.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and more specifically relates to a nano-preparation of tranexamic acid for external use on the skin, a preparation method and application thereof. The nano-preparation of tranexamic acid for external use of the present invention has good skin physiological compatibility, can effectively promote the percutaneous absorption of tranexamic acid, improve the effect of tranexamic acid in preventing or treating pigmentation, and avoid the effects of tranexamic acid Toxic side effects caused by systemic medication. Background technique [0002] Tranexamic acid is also called tranexamic acid, tranexamic acid, the chemical name is trans-4-(aminomethyl)cyclohexanecarboxylic acid, molecular formula: C 8 h 15 NO 2 , molecular weight: 157.21, has the following chemical structure: [0003] [0004] Tranexamic acid is an antifibrinolytic hemostatic drug. Since tranexamic acid is similar in structure to t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/195A61P17/00
Inventor 郭仕艳李大宁甘勇李梅云张馨欣张裕坤刘进芬
Owner CENT HOSPITAL XUHUI DISTRICT SHANGHAI CITY
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