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Tranexamic acid skin externally applied nano-preparation, as well as preparation method and use thereof

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, skin irritation, unclear mechanism, etc., to improve local skin. Dullness, treatment of hyperpigmentation, increased efficacy

Inactive Publication Date: 2014-02-12
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 externally applied nano-preparation, as well as preparation method and use thereof
  • Tranexamic acid skin externally applied nano-preparation, as well as preparation method and use thereof
  • Tranexamic acid skin externally applied nano-preparation, as well as preparation method and use thereof

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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 use magnetic stirring (manufactured by IKA Company, model: RET Basic C) at 70±10°C. Stir at 300 rpm for about 10 minutes until the tranexamic acid is completely dissolved to obtain an 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, add the prescribed amount of polyoxyethylene castor oil (manufactured by BASF, Germany, trade name: Cremophor EL) and VE (manufactured by DSM Vitamin (Shanghai) Co., Ltd.) after ethylparaben is completely dissolved, and continue stirring Mix the solution evenly to obtain the oil phase.

[0046] ③Put ...

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 skin externally applied nano-preparation, as well as a preparation method and a use thereof. The nano-preparation is prepared from tranexamic acid, medicated oil, an emulsifier, pharmaceutical additives, a thickener and pure water. The tranexamic acid skin externally applied nano-preparation provided by the invention has good physiological skin compatibility and can effectively promote the percutaneous absorption of tranexamic acid, improve the effect of preventing or treating pigmentation of the tranexamic acid and avoid toxicity and side effects, which are caused by systemic administration of the tranexamic acid.

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 Applications(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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