A kind of lidocaine microemulsion gel and preparation method thereof

Abstract

The invention discloses a lidocaine microemulsion-based gel. The lidocaine microemulsion-based gel comprises the components of, by mass, 2-6% of lidocaine, 0-0.8% of menthol, 3.75% of an oil phase, 8.75% of a surfactant, 82.1% of distilled water, 0.1% of a preservative and 0.4% of carbomer 980. A preparation method of the lidocaine microemulsion-based gel comprises the steps that the lidocaine andthe menthol are dissolved in the oil phase under 70 DEG C, and then the surfactant is added; then the distilled water is added drip by drip during stirring to form microemulsion; the preservative isadded; and after a mixture is subjected to still standing and cooled to the room temperature, the carbomer 980 is spread, and after full swelling, stirring, degassing and sterilization are conducted,the lidocaine microemulsion-based gel is obtained. The lidocaine microemulsion-based gel is a noninvasive local anesthetic, the toxic and side effects, caused by injection, for a whole body can be avoided, and the lidocaine microemulsion-based gel can be used for skin surgical operations, cosmetology, micro-plastic surgeries and the like.

Description

technical field

[0001] The invention relates to a local anesthetic, in particular to a lidocaine microemulsion gel for non-invasive transdermal administration and a preparation method thereof. Background technique

[0002] Skin surgery, as well as various cosmetic minimally invasive operations such as skin rejuvenation, anti-wrinkle, hair removal, eyebrow washing, tattoos and microplastic surgery, etc., will cause superficial traumatic and infiltrating pain on the human skin to varying degrees. Clinically, the method of injecting anesthetics is generally used for anesthesia and analgesia at the treatment site. However, there are many problems with injections, such as causing pain, difficult injections in some parts, beauty institutions cannot legally apply injection anesthesia, and more importantly, injections will cause systemic side effects. Therefore, it will be particularly necessary to develop a preparation that is non-injection, non-invasive, directly used on the skin...

Examples

Embodiment 1

[0020] Example 1 Dissolve 2g of lidocaine in a mixture of 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) at 70°C, and add 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to prepare 100 g of lidocaine microemulsion gel with a concentration of 2%.

Embodiment 2

[0021] Example 2 4g of lidocaine was dissolved in 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) mixed oil at 70°C, and 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to obtain 100 g of lidocaine microemulsion gel with a concentration of 4%.

Embodiment 3

[0022] Example 3 5g of lidocaine was dissolved in 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) mixed oil at 70°C, and 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to obtain 100 g of lidocaine microemulsion gel with a concentration of 5%.

technical field

[0001] The invention relates to a local anesthetic, in particular to a lidocaine microemulsion gel for non-invasive transdermal administration and a preparation method thereof. Background technique

[0002] Skin surgery, as well as various cosmetic minimally invasive operations such as skin rejuvenation, anti-wrinkle, hair removal, eyebrow washing, tattoos and microplastic surgery, etc., will cause superficial traumatic and infiltrating pain on the human skin to varying degrees. Clinically, the method of injecting anesthetics is generally used for anesthesia and analgesia at the treatment site. However, there are many problems with injections, such as causing pain, difficult injections in some parts, beauty institutions cannot legally apply injection anesthesia, and more importantly, injections will cause systemic side effects. Therefore, it will be particularly necessary to develop a preparation that is non-injection, non-invasive, directly used on the skin...

Examples

Embodiment 1

[0020] Example 1 Dissolve 2g of lidocaine in a mixture of 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) at 70°C, and add 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to prepare 100 g of lidocaine microemulsion gel with a concentration of 2%.

Embodiment 2

[0021] Example 2 4g of lidocaine was dissolved in 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) mixed oil at 70°C, and 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to obtain 100 g of lidocaine microemulsion gel with a concentration of 4%.

Embodiment 3

[0022] Example 3 5g of lidocaine was dissolved in 3.75g of olive oil and vitamin E succinate (mass ratio 6:1) mixed oil at 70°C, and 8.75g of surfactant (polyoxyethylene hydrogenated Castor oil and Span 80 are mixed at a mass ratio of 5:1), and then the required amount of distilled water is added drop by drop under stirring to form a microemulsion. After adding 0.1g of preservative (sodium methylparaben and sodium propylparaben mixed at a mass ratio of 1:1), let it stand to cool to room temperature, then sprinkle 0.4g of Carbomer 980, fully After swelling, stir, degas, and sterilize to obtain 100 g of lidocaine microemulsion gel with a concentration of 5%.

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