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Flexible tranexamic acid liposome with effects of whitening and removing freckles as well as preparation method and application of flexible tranexamic acid liposome

A flexible liposome, whitening and freckle-removing technology, which is applied in liposome delivery, peptide/protein components, skin care preparations, etc., can solve the problems of low bioavailability of tranexamic acid, inconvenient use, poor compliance, etc. Achieve the effect of preventing melanin aggregation, increasing suppleness, and good skin affinity

Active Publication Date: 2019-03-19
广州市晨茜化工有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The conventional administration methods of tranexamic acid are mainly oral administration and injection, which often cause problems such as gastrointestinal irritation and inconvenient use and poor compliance; transdermal administration is a more direct and convenient way to treat skin pigmentation diseases, and patients are also easy to accept
However, the current conventional tranexamic acid topical cream is difficult to break through the stratum corneum barrier, resulting in low bioavailability of tranexamic acid, which is limited in application

Method used

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  • Flexible tranexamic acid liposome with effects of whitening and removing freckles as well as preparation method and application of flexible tranexamic acid liposome
  • Flexible tranexamic acid liposome with effects of whitening and removing freckles as well as preparation method and application of flexible tranexamic acid liposome
  • Flexible tranexamic acid liposome with effects of whitening and removing freckles as well as preparation method and application of flexible tranexamic acid liposome

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preparation example Construction

[0029] The present invention provides the preparation method of above-mentioned tranexamic acid flexible liposome, comprises the following steps:

[0030] (1) Prepare the oil phase: melt the phospholipid, cholesterol, membrane softener, ceramide, and emollient at a water bath temperature of 65 to 80°C, and set aside;

[0031] (2) Prepare the water phase: add tranexamic acid and polyols into the purified water of the formula, stir and heat at 65-80°C to dissolve the tranexamic acid and polyols, then add antioxidants and mix evenly, and set aside;

[0032] (3) Preparation of colostrum: Add the oil phase prepared in step (1) dropwise to the water phase prepared in step (2) and keep stirring, then 8000-15000r / min, high-speed shear emulsification for 5-15min, that is, get colostrum;

[0033] (4) Preparation of liposomes: heat the colostrum prepared in step (3) at 70° C., and then process it through high-pressure homogenization or high-pressure micro-jet treatment with a pressure o...

Embodiment 1

[0037] (1) Preparation of oil phase: 1.0% soybean lecithin, 0.5% cholesterol, 0.05% sodium cholate, 0.05% ceramide, 0.5% shea oil, 1.0% rosehip oil, 0.5% jojoba oil at 65-80°C Melt at the temperature of the water bath, mix evenly, and set aside;

[0038] (2) Prepare the water phase: add 0.1% tranexamic acid, 5.0% 1,3-butanediol, 0.5% vitamin C magnesium phosphate, and 0.5% vitamin C ethyl ether to 90.3% purified water, stir and heat Dissolve at 65-80°C and set aside;

[0039](3) Preparation of colostrum: drop the oil phase prepared in step (1) into the water phase prepared in step (2) and keep stirring, then emulsify at a high speed of 8000r / min for 5min to obtain colostrum;

[0040] (4) Preparation of liposomes: heat the colostrum prepared in step (3) at 70° C., and then process it through high-pressure homogenization equipment with a pressure of 500 bar and 3 cycles, and then cool down to 20-30° C. The flexible liposome of tranexamic acid was obtained. The particle size o...

Embodiment 2

[0042] (1) Prepare the oil phase: melt 2.0% egg yolk lecithin, 0.5% cholesterol, 0.2% sodium deoxycholate, 0.1% ceramide, 1.0% rosehip oil, and 1.0% olive oil at a temperature of 65-80°C in a water bath, Mix well and set aside;

[0043] (2) Prepare the water phase: add 0.5% tranexamic acid, 7.0% glycerin, and 0.5% vitamin C ethyl ether into 87.2% purified water, stir and heat at 65-80°C to dissolve, and set aside;

[0044] (3) Preparation of colostrum: add the oil phase prepared in step (1) dropwise to the water phase prepared in step (2) and keep stirring, then 10000r / min, high-speed shear emulsification for 5min, to obtain colostrum;

[0045] (4) Preparation of liposomes: heat the colostrum prepared in step (3) at 70°C, and then process it through high-pressure homogenization equipment with a pressure of 800 bar and a cycle of 3 times, then cool down to 20-30°C, The flexible liposome of tranexamic acid was obtained. The particle diameter of the tranexamic acid flexible lip...

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Abstract

The invention relates to a flexible tranexamic acid liposome with effects of whitening and removing freckles as well as a preparation method and application of the flexible tranexamic acid liposome. The flexible tranexamic acid liposome with effects of whitening and removing freckles is composed of the following components in percentage by mass: 0.1-6.0% of tranexamic acid, 1.0-12.0% of phospholipid, 0.5-5.0% of cholesterol, 0.05-1% of a membrane softener, 0.05-1.0% of ceramide, 0.5-3.0% of an emollient, 5.0-15.0% of polyhydric alcohols, 0.5-2.0% of an antioxidant and the balance of purified water. According to the flexible tranexamic acid liposome prepared in the invention, the various active ingredients realize functional complementation and can achieve synergistic effects; the drug loading capacity is high, the active ingredients with different effects, such as the tranexamic acid and the like, can be delivered to deep positions of the skin, and a long-term sustained release effectis achieved; and the accumulated transmission amount and retention volume of tranexamic acid cream are increased, the defect that an adverse reaction to the gastrointestinal tract is caused by oral medication is overcome, the compliance is improved, and the liposome is easily accepted by patients.

Description

technical field [0001] The invention belongs to the technical field of cosmeceuticals, and in particular relates to a flexible tranexamic acid liposome for whitening and removing freckles, a preparation method and application thereof. Background technique [0002] Chloasma is a kind of hyperpigmented skin disease caused by common pigmentation disorders, manifested as yellowish brown, dark brown or dark brown patches, usually symmetrically located on the cheeks, forehead, nose, lips and other parts, the surface is smooth without scales , often asymptomatic, more common in women of childbearing age. The pathogenesis of chloasma is still not very clear. Most scholars believe that it may be related to ultraviolet radiation, endocrine disorders, pregnancy, oral contraceptives, accumulation of oxygen free radicals, abnormal trace element content, visceral diseases and local microecological imbalance. [0003] Tranexamic acid, also known as: tranexamic acid, is another whitening a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K8/14A61K8/44A61K8/63A61K8/92A61K8/67A61Q19/02A61K9/127A61K31/195A61K36/54A61K36/185A61K36/32A61K36/738A61K31/375A61K47/28A61P17/00
CPCA61K47/28A61P17/00A61Q19/02A61K8/14A61K8/44A61K8/63A61K8/676A61K8/922A61K9/1271A61K9/1277A61K31/195A61K31/375A61K36/185A61K36/32A61K36/54A61K36/738A61K2800/782A61K2800/56A61K2800/592A61K2300/00
Inventor 胡克
Owner 广州市晨茜化工有限公司
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