Novel alkalized solid-liquid two-state skin quick-anaesthesia nano-emulsion and preparation method thereof

A nanoemulsion and epidermis technology, applied in anesthetics, liquid delivery, pharmaceutical formulations, etc., can solve the problems of epidermal cell damage caused by skin stratum corneum dissolution, limited anesthesia intensity and anesthesia maintenance time, thermodynamic instability, etc., to achieve anesthesia and Enhanced analgesic effect, strong skin penetration and absorption, and strong local anesthetic effect

Active Publication Date: 2009-01-07
董萍 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, clinically, various puncture examinations, skin venereal diseases (such as biopsy, electrocautery, curettage, laser, liquid nitrogen freezing and chemical peeling, etc.), plastic surgery and laser cosmetology and other invasive medical methods are caused. Superficial traumatic pain of the skin, which has been given sufficient attention but technically incapable of action
In order to reduce the pain caused by plastic surgery or medical aesthetic treatment, superficial skin surgery and puncture, subcutaneous local injection of anesthesia drug infiltration anesthesia is still generally used, but the pain and psychological fear caused by injection often lead to poor patient compliance. In particular, the fear and anxiety of children and women are becoming more and more obvious and prominent, and the injection of some treatment parts is difficult and not very convenient, especially the skin anesthetics currently used for external application, including some new ones. The developed anesthesia sprays, tinctures, emulsions, creams, ointments, gels, etc. seem to have solved the tediousness and pain of injection anesthesia, and are indeed simple and convenient to use. The onset time of anesthesia is usually more than 1 hour, and the anesthesia intensity and anesthesia maintenance time are very limited. Even if some sealing measures can improve some anesthesia effects, the effect is not very obvious, which seriously affects people's confidence and patience in use
[0006] As mentioned earlier, currently the most widely used skin topical anesthetic in the world is Enna cream (EMLA) developed and produced by AstraZeneca, Sweden, which is compound lidocaine cream, but the shortcoming of this preparation is the onset time It is relatively slow, and it is a topical anesthetic, which can only be used for minor surgical anesthesia, and it cannot achieve pain relief for such as dermabrasion and plastic surgery.
Moreover, prilocaine in Enna cream can increase blood methaemoglobin at high doses, which may affect tissue oxygenation a

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0085] Example 1: Preparation of alkalized blank nanoemulsion for external use on skin (taking preparation 100g as an example):

[0086] ①Accurately weigh 0.1g of sodium bicarbonate (AR) with an analytical balance and place it in a washed 100mL conical flask, then add 39.9g of distilled water, after fully dissolving, adjust its pH to 7.8±2.0 , clearly marked as water phase (A) 40g with a color marker.

[0087] ②Accurately weigh 15g of isopropyl myristate with a balance, put it in a washed 100mL conical flask, and use a color marker to clearly mark it as oil phase (B) 15g.

[0088] 3.According to the ratio of caprylic acid capric acid macrogol glyceride: polyglycerol fatty acid ester=3: 1, accurately weigh 36g caprylic acid caprylic acid macrogol glyceride and 12g polyglycerol fatty acid ester, respectively, and weigh the two. Place in a washed 100mL conical flask; quickly place it on the liquid rapid mixer, turn on the liquid rapid mixer, and mix thoroughly to form an emulsif...

Example Embodiment

[0092] Example 2: Preparation of Alkaliized Liquid Epidermal Anesthesia Nanoemulsion for Skin External Use (taking 100g as an example):

[0093] ①Accurately weigh 0.1g of sodium bicarbonate with an analytical balance and place it in a washed 100mL conical flask, then add 39.9g of distilled water, and after fully dissolving, adjust its pH to 7.8±2.0, and use A color marker is clearly marked as water phase (A) 40 g.

[0094] ②Accurately weigh 9.0 g of isopropyl myristate with a balance, and place it in a washed 100 mL conical flask; then use an analytical balance to weigh 2.0 g of chloroprocaine and 1.0 g of tetracaine respectively , lidocaine 2.0g, menthol 1.0g, respectively, were added to the 100mL conical flask containing 9.0g isopropyl myristate, mixed thoroughly to make it completely dissolved; if the part that could not be dissolved, use 10mL Anhydrous ethanol of analytical alcohol (AR grade) was slowly added dropwise with a pipette to promote complete dissolution and cle...

Example Embodiment

[0099] Example 3: Preparation of Alkalinized Solid State Epidermis Anesthesia Nanoemulsion for Skin External Use (taking 130g as an example):

[0100] ①Accurately weigh 0.1g of sodium bicarbonate (AR) with an analytical balance and place it in a washed 100mL conical flask, then add 39.9g of distilled water, after fully dissolving, adjust its pH to 7.8±2.0 , clearly marked as water phase (A) 40g with a color marker.

[0101] ②Accurately weigh 9.0 g of isopropyl myristate with a balance and place it in a washed 100 mL conical flask; then use an analytical balance to weigh 2.0 g of chloroprocaine and 1.0 g of tetracaine Lidocaine 2.0g and menthol 1.0g were added to the 100mL Erlenmeyer flask containing 9.0g isopropyl myristate respectively, and mixed thoroughly to dissolve them completely; if the part could not be dissolved, use a 10mL pipette Anhydrous ethanol for analytical alcohol (AR grade) was slowly added dropwise to facilitate complete dissolution and clearly marked as oi...

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Abstract

The invention relates to a novel alkalized liquid-state and solid-state rapid skin anesthesia nanometer emulsion for skin external application and a preparation method thereof. The inventive nanometer emulsion mainly comprises three systems: the first system is a skin anesthesia effective ingredient system, the second system is a nanometer emulsion composition system, and the third system is a nanometer emulsion excipient protective system. The three systems can be used for preparing a liquid-state and solid-state rapid anesthesia nanometer emulsion for skin external anesthesia. The inventive nanometer emulsion compounds three anesthetics with respective characteristics and contains menthol, so that the formula is more reasonable and the effect is more distinct, wherein tetracaine has strong transdermal capacity, rapid action and strong local anesthetic action, the anesthetic action of chloroprocaine is 4-6 times stronger than procaine and 2-3 times stronger than lidocaine, and the chloroprocaine has low toxicity, high penetration capacity, quick action and long-lasting anesthetic action.

Description

technical field [0001] The invention relates to a novel alkalized liquid and solid epidermal rapid anesthesia nanoemulsion for external use and a preparation method thereof, and the technical field belongs to pharmaceutical preparations and medical cosmetic products and technologies. Ornamentation (including eyebrow, lip, eyeliner, tattoo), freckles, black hemorrhoid removal, grinding, epidermal anesthesia and analgesia before eyebrow washing, can also be directly used in plastic surgery, dermatology and medical cosmetology Epidermal anesthesia and analgesia for surgery. Background technique [0002] Background technology of local anesthetics: Local anesthesia methods and routes of administration at home and abroad are mostly performed by subcutaneous injection of anesthesia injections, skin smearing of anesthesia external preparations, and surface spraying of anesthesia sprays. The most commonly used local anesthetics are: ① Procaine: the earliest synthetic ester local ane...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/245A61K31/167A61K47/34A61K47/14A61P23/02
Inventor 杨永鹏朱晓亮董萍丁宇丁克祥
Owner 董萍
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