Lidocaine cream as well as preparation method and application thereof

A lidocaine and cream technology, which is applied in the field of medicine, can solve the problems of damage to the nervous system, heart, poor skin penetration of lidocaine, increased toxicity of lidocaine, etc., and achieve the effect of avoiding side effects

Active Publication Date: 2021-04-27
BLOOMAGE BIOTECHNOLOGY CORP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Lidocaine has poor transdermal property. Therefore, in the process of use, it often causes physiological toxicity to the human body due to excessive concentration, causing allergic reactions, etc., supplemented by transdermal absorbents, and the instantaneous blood drug concentration is too high due to excessive absorption speed. Increase the toxicity of lidocaine, damage the nervous system, heart

Method used

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  • Lidocaine cream as well as preparation method and application thereof
  • Lidocaine cream as well as preparation method and application thereof
  • Lidocaine cream as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0182] (1) 3g polyethylene glycol-6 stearate, 4g cetostearyl alcohol, 0.3g hydrogenated lecithin, 0.8g tocopheryl acetate, 9g mineral oil, 2g polydimethylsiloxane, 0.3g of methylparaben and 0.1g of ethylparaben were stirred and heated to 80°C to completely melt to obtain solution A;

[0183] (2) 4g of 1,3-propanediol, 6g of glycerin, 0.4g of xanthan gum, 0.3g of the first sodium hyaluronate with a molecular weight of 200kDa, 0.3g of the second sodium hyaluronate with a molecular weight of 8kDa, and 0.2g of a molecular weight of 5kDa third sodium hyaluronate and 0.1g allantoin were mixed and added to the remaining 85°C deionized water and stirred to dissolve to completely dissolve to obtain solution B, which was maintained at 80°C, wherein the above-mentioned The sum of the mass of components and lidocaine and benzyl alcohol is 100g;

[0184] Add solution A to solution B, keep emulsification and homogeneity at 80°C for 10 minutes, stir and cool down to 55°C, add 4g lidocaine a...

Embodiment 2

[0186] (1) Mix 6g polyethylene glycol-6 stearate, 8g cetostearyl alcohol, 0.2g hydrogenated lecithin, 1g tocopheryl acetate, 6g mineral oil, 4g polydimethylsiloxane, 0.3 g methylparaben and 0.1g ethylparaben were stirred and heated to 80°C to completely melt to obtain solution A;

[0187] (2) 5g of 1,3-propanediol, 6g of glycerin, 0.1g of xanthan gum, 0.2g of the first sodium hyaluronate with a molecular weight of 400kDa, 0.5g of the second sodium hyaluronate with a molecular weight of 6kDa, 0.5g of a molecular weight of 2kDa The third sodium hyaluronate and 0.3g allantoin were mixed and added to the remaining 80°C deionized water, stirred and heated to 80°C to completely dissolve to obtain solution B, and solution B was maintained at 75°C, wherein the above-mentioned The sum of the quality of the components and lidocaine and benzyl alcohol is 100g;

[0188] (3) Add solution A to solution B, keep emulsified and homogenized at 80°C for 10 minutes, stir and cool down to 60°C, a...

Embodiment 3

[0190] (1) 6g polyethylene glycol-6 stearate, 8g cetostearyl alcohol, 0.1g hydrogenated lecithin, 1g tocopheryl acetate, 12g mineral oil, 3g polydimethylsiloxane, 0.3 g methylparaben and 0.1g ethylparaben were stirred and heated to 80°C to completely melt to obtain solution A;

[0191] (2) 4g of 1,3-propanediol, 6g of glycerin, 0.3g of xanthan gum, 0.1g of the first sodium hyaluronate with a molecular weight of 500kDa, 0.8g of the second sodium hyaluronate with a molecular weight of 9kDa, 0.1g of a molecular weight of Mix the third sodium hyaluronate of 5kDa and 0.1g allantoin, add the remaining amount of 80°C deionized water, stir and heat to 80°C to completely dissolve to obtain solution B, and keep solution B at 85°C, wherein, the above The sum of the quality of various components and lidocaine and benzyl alcohol is 100g;

[0192] (3) Add solution A to solution B and keep it emulsified and homogeneous at 85°C for 10 minutes. After stirring and cooling down to 60°C, add 3g ...

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Abstract

The invention discloses lidocaine cream as well as a preparation method and application thereof. The lidocaine cream comprises an active ingredient lidocaine, an oil-phase composition and a water-phase composition, the water-phase composition comprises first hyaluronic acid or a salt thereof, second hyaluronic acid or a salt thereof and third hyaluronic acid or a salt thereof, and the oil-phase composition comprises hydrogenated lecithin. According to the cream, the drug release speed is controlled while the active ingredient lidocaine quickly transdermally generates an analgesic effect, and the blood concentration is controlled at a relatively low level, so that the lidocaine plays a local analgesic role, and meanwhile, side effects caused by too high blood concentration are avoided.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a lidocaine cream, a preparation method and an application thereof. Background technique [0002] Molecular formula of Lidocaine: C 14 h 22 N 2 O, molecular weight 234.34, white crystalline powder, melting point 66–69°C, easily soluble in ethanol, chloroform and dichloromethane, insoluble in water, stable chemical properties, is a common amide local anesthetic and antiarrhythmia It can be used for local analgesia, usually in the form of hydrochloride monohydrate, which is a derivative of cocaine, but it is not addictive. Lidocaine has obvious excitatory and inhibitory biphasic effects on the central nervous system after being absorbed through the blood or after intravenous administration, and there may be no precursor excitement. When the blood concentration is low, analgesia, drowsiness, pain threshold Increase; as the dose increases, the effect or toxicity increases, and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/36A61K47/24A61K31/167A61P23/02A61P29/00
CPCA61K9/06A61K9/0014A61K47/36A61K47/24A61K31/167A61P23/02A61P29/00
Inventor 杨林红阚洪玲董建军陈柏秀李锋田昕刘晓云王太安
Owner BLOOMAGE BIOTECHNOLOGY CORP LTD
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