A kind of tranexamic acid flexible liposome for whitening and removing freckles and its preparation method and application

Abstract

The present invention relates to a tranexamic acid flexible liposome for whitening and removing freckles and its preparation method and application. ~12.0% phospholipids, 0.5%~5.0% cholesterol, 0.05%~1% membrane softener, 0.05%~1.0% ceramide, 0.5%~3.0% emollient, 5.0%~15.0% polyol, 0.5%~2.0 % antioxidants and the balance of purified water. The active ingredients in the tranexamic acid flexible liposome prepared by the present invention have complementary functions and can play a synergistic effect; the drug loading capacity is large, and active ingredients with different functions such as tranexamic acid can be transported to the deep layer of the skin to play a long-term effect. It improves the cumulative penetration and retention of tranexamic acid cream, improves the defects of oral administration of gastrointestinal adverse reactions, improves compliance, and is easy for patients to accept.

Description

technical field

[0001] The invention belongs to the technical field of cosmeceuticals, and in particular relates to a whitening and freckle-removing flexible liposome of tranexamic acid and a preparation method and application thereof. Background technique

[0002] Chloasma is a pigmented skin disease caused by a common pigment metabolism disorder. It is characterized by yellow-brown, dark-brown or dark coffee-colored patches, often symmetrically on the cheeks, forehead, nose, lips and other parts, with a smooth surface without scales , often asymptomatic, more common in women of childbearing age. The pathogenesis of melasma is not very clear at present, but most scholars believe that it may be related to ultraviolet radiation, endocrine disorders, pregnancy, oral contraceptives, accumulation of oxygen free radicals, abnormal content of trace elements, visceral diseases and local microecological imbalance.

[0003] Tranexamic acid, also known as tranexamic acid, is another ...

Examples

preparation example Construction

[0029] The present invention provides a method for preparing the above-mentioned tranexamic acid flexible liposome, comprising the following steps:

[0030] (1) prepare oil phase: phospholipid, cholesterol, membrane softener, ceramide, emollient are melted at 65~80 ℃ of water bath temperature, for subsequent use;

[0031] (2) Preparation of water phase: add tranexamic acid and polyol to the purified water in the formula amount, stir and heat at 65-80° C. to dissolve tranexamic acid and polyol, add antioxidant and mix evenly, for later use;

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

[0033] (4) Preparation of liposomes: the colostrum prepared in step (3) is kept at 70° C., and then processed by high-pressure homogenization or high-pressure micro-jet, the pressure is 500-120...

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 butter, 1.0% rosehip oil, 0.5% jojoba oil at 65~80℃ The temperature of the water bath is melted, mixed evenly, and ready for use;

[0038] (2) Preparation of water phase: add 0.1% tranexamic acid, 5.0% 1,3-butanediol, 0.5% vitamin C phosphate magnesium, 0.5% vitamin C ethyl ether to 90.3% purified water, stir and heat 65 ~ 80 ℃ to dissolve, for use;

[0039](3) Preparation of colostrum: the oil phase prepared in step (1) is added dropwise to the water phase prepared in step (2) and continuously stirred, and then 8000 r / min, high-speed shearing and emulsification for 5 min, to obtain colostrum;

[0040] (4) Preparation of liposomes: the colostrum prepared in step (3) is incubated at 70°C, and then processed by high-pressure homogenization equipment, the pressure is 500bar, the number of cycles is 3, and the temperature is lowered to 20~30°C, That is, t...

Embodiment 2

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

[0043] (2) Preparation of water phase: add 0.5% tranexamic acid, 7.0% glycerol, 0.5% vitamin C ethyl ether to 87.2% purified water, stir and heat at 65-80°C to dissolve, for later use;

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

[0045] (4) Preparation of liposomes: the colostrum prepared in step (3) was incubated at 70°C, then processed by high-pressure homogenization equipment, the pressure was 800bar, the number of cycles was 3, and the temperature was lowered to 20-30°C, That is, tranexamic acid flexible liposomes are obtained. The tranexam...

technical field

[0001] The invention belongs to the technical field of cosmeceuticals, and in particular relates to a whitening and freckle-removing flexible liposome of tranexamic acid and a preparation method and application thereof. Background technique

[0002] Chloasma is a pigmented skin disease caused by a common pigment metabolism disorder. It is characterized by yellow-brown, dark-brown or dark coffee-colored patches, often symmetrically on the cheeks, forehead, nose, lips and other parts, with a smooth surface without scales , often asymptomatic, more common in women of childbearing age. The pathogenesis of melasma is not very clear at present, but most scholars believe that it may be related to ultraviolet radiation, endocrine disorders, pregnancy, oral contraceptives, accumulation of oxygen free radicals, abnormal content of trace elements, visceral diseases and local microecological imbalance.

[0003] Tranexamic acid, also known as tranexamic acid, is another ...

Examples

preparation example Construction

[0029] The present invention provides a method for preparing the above-mentioned tranexamic acid flexible liposome, comprising the following steps:

[0030] (1) prepare oil phase: phospholipid, cholesterol, membrane softener, ceramide, emollient are melted at 65~80 ℃ of water bath temperature, for subsequent use;

[0031] (2) Preparation of water phase: add tranexamic acid and polyol to the purified water in the formula amount, stir and heat at 65-80° C. to dissolve tranexamic acid and polyol, add antioxidant and mix evenly, for later use;

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

[0033] (4) Preparation of liposomes: the colostrum prepared in step (3) is kept at 70° C., and then processed by high-pressure homogenization or high-pressure micro-jet, the pressure is 500-120...

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 butter, 1.0% rosehip oil, 0.5% jojoba oil at 65~80℃ The temperature of the water bath is melted, mixed evenly, and ready for use;

[0038] (2) Preparation of water phase: add 0.1% tranexamic acid, 5.0% 1,3-butanediol, 0.5% vitamin C phosphate magnesium, 0.5% vitamin C ethyl ether to 90.3% purified water, stir and heat 65 ~ 80 ℃ to dissolve, for use;

[0039](3) Preparation of colostrum: the oil phase prepared in step (1) is added dropwise to the water phase prepared in step (2) and continuously stirred, and then 8000 r / min, high-speed shearing and emulsification for 5 min, to obtain colostrum;

[0040] (4) Preparation of liposomes: the colostrum prepared in step (3) is incubated at 70°C, and then processed by high-pressure homogenization equipment, the pressure is 500bar, the number of cycles is 3, and the temperature is lowered to 20~30°C, That is, t...

Embodiment 2

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

[0043] (2) Preparation of water phase: add 0.5% tranexamic acid, 7.0% glycerol, 0.5% vitamin C ethyl ether to 87.2% purified water, stir and heat at 65-80°C to dissolve, for later use;

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

[0045] (4) Preparation of liposomes: the colostrum prepared in step (3) was incubated at 70°C, then processed by high-pressure homogenization equipment, the pressure was 800bar, the number of cycles was 3, and the temperature was lowered to 20-30°C, That is, tranexamic acid flexible liposomes are obtained. The tranexam...

Images