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Freeze-drying flash release tablet for local skin anaesthesia, as well as preparation method and application thereof

A freeze-dried flash-release, topical skin technology, applied in the field of medical anesthesia, can solve the problems of increasing the anxiety of surgical patients, easily producing bacteria on the skin surface, and waiting too long, achieving good sterilization effect, maintaining temperature, and improving permeability. Effect

Inactive Publication Date: 2018-06-15
AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In clinical practice, in order to shorten the waiting time for anesthesia to take effect, after applying anesthesia ointment on the skin, the area is further sealed with plastic wrap to promote the absorption of the anesthetic. However, this method of wrapping with plastic wrap is not only troublesome, but also effective The waiting time is still too long, generally about an hour. While waiting for the anesthetic to take effect for a long time, it will virtually increase the anxiety of the surgical patient, and bacteria are likely to be produced on the surface of the skin during the long waiting process.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] The preparation method of this freeze-dried flash-release tablet is as follows:

[0030]Take compound anesthetic, nano-photocatalyst, freeze-drying protective agent, soybean lecithin, hydroxypropyl methylcellulose, and polyethylene glycol and add them to the emulsification pot, then add ultra-pure water, and put them at a temperature of 65-75°C and a pressure of 600- Homogeneously emulsify for 20 to 30 minutes at 800 bar and 1500 to 2000 rpm to obtain an emulsion, fill the emulsion into a cavity formed by double aluminum diaphragms, place it on the plate of the freeze dryer, and quickly cool down to -160 to Perform deep-condensation drying at -120°C for 1.5 to 2.0 hours, then gradually increase the temperature to 25°C, take it out and seal it, and obtain freeze-dried flash-release tablets. The gradient temperature rise is divided into five stages: Stage 1, gradually increase the temperature to -100°C within 10 hours; stage 2, gradually increase the temperature to -70°C ...

Embodiment 1

[0034] Preparation of compound anesthetic: Add 1g of toadstool, 1.5g of Aconitum aconitum extract, 1.5g of Aconitum aconitum extract, 2g of Zanthoxylum bungeanum extract, and 4g of peppermint extract into 150mL of 5wt% ethanol solution, stir until completely dissolved, and then add 30g of After phosphatidylcholine was stirred for 10 minutes, it was ultrasonically oscillated at 50-60°C for 20 minutes, and vacuum-dried to obtain complex liposomes; 24.3g trehalose and 2.4g hyaluronic acid were dissolved in phosphate buffer solution with pH=6.5 to obtain Protective solution, adding complex liposomes into the protective solution and stirring for 10 minutes, followed by ultrasonication in an ice bath at 50-60° C. for 20 minutes, and freeze-drying to obtain a compound anesthetic.

[0035] Preparation of nanophotocatalyst: 5g of anatase-type titanium dioxide with a spongy porous structure was dispersed in 120mL of absolute ethanol, then 2.5g of γ-methacryloxypropyltrimethoxysilane (MPS...

Embodiment 2

[0038] Preparation of compound anesthetic: Add 0.5g of toad venom, 2.0g of Aconitum aconitum extract, 1.0g of Aconitum aconitum extract, 2g of Zanthoxylum bungeanum extract, and 4g of peppermint extract into 150mL of 5wt% ethanol solution, stir until completely dissolved, and then add After stirring 30g of phosphatidylcholine for 10min, ultrasonically oscillate at 50-60°C for 20min, and vacuum-dry to obtain complex liposomes; take 21.7g of trehalose and 2.17g of hyaluronic acid and dissolve them in a phosphate buffer solution with a pH of 6.5. The protective solution was obtained, the complex liposome was added into the protective solution and stirred for 10 minutes, then ultrasonicated in an ice bath at 50-60° C. for 20 minutes, and freeze-dried to obtain a compound anesthetic.

[0039] The preparation of the nano photocatalyst is the same as that of the nano photocatalyst in Example 1.

[0040] Preparation of lyophilized flash-release tablets: Take 15g of compound anesthetic...

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PUM

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Abstract

The invention relates to the technical field of medical anesthesia, in particular to a freeze-drying flash release tablet for local skin anaesthesia, as well as a preparation method and application thereof. The freeze-drying flash release tablet is packaged in a double-aluminum-film cavity in a sealed way, and comprises the following raw materials in parts by weight: 10 to 25 parts of compound anesthetic, 10 to 20 parts of a nanometer photocatalyzer, 15 to 25 parts of a freezing and drying protecting agent, 3 to 8 parts of granulesten, 2 to 5 parts of hydroxypropyl methyl cellulose, and 10 to15 parts of polyethylene glycol, wherein the compound anesthetic adopts liposome taking anesthetic as a core and coated by a lipid layer and a hydrophilic protective layer from the inner part to the outer part. In addition, the invention further discloses a preparation method and application of the freeze-drying flash release tablet. The freeze-drying flash release tablet has the advantages that the lipid layer is taken as an anesthetic carrier, the hydrophilic protective layer is taken as an anesthetic protective layer, then the freeze-drying flash release tablet is formed, the permeability of anesthetic can be enhanced, the anesthetic effects of rapidness, effectiveness, safety and no stimulation are achieved, antibiosis disinfection is performed through the nanometer photocatalyzer, andanesthesia and sterilization and disinfection are performed at the same time.

Description

technical field [0001] The invention relates to the technical field of medical anesthesia, in particular to a freeze-dried flash-release tablet for local skin anesthesia and a preparation method thereof. Background technique [0002] Anesthesia is the use of drugs or other methods to temporarily deprive the patient of sensation in whole or in part, so as to achieve painless surgical treatment. Regarding anesthesia technology, the earliest written record in the world is Mabo Decoction, which appeared in the Han Dynasty in my country, and was invented by Hua Tuo, a famous ancient Chinese surgeon and Chinese medicine scientist. Mabo Decoction is a traditional Chinese medicine decoction equivalent to the current oral general anesthesia. After oral administration, the patient loses skin sensation and facilitates the operation. Later, Western medicine invented various anesthetics, such as lidocaine, bupivacaine, procaine, etc., which are popular now. [0003] Epidermal anesthesi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/758A61K9/20A61K47/24A61K47/36A61K47/26A61P23/02A61P31/02A61K35/65A61K33/24A61K9/50
CPCA61K9/0014A61K9/2018A61K9/2027A61K9/2095A61K9/5015A61K9/5036A61K9/5073A61K33/24A61K35/65A61K36/534A61K36/714A61K36/758A61K47/24A61K47/26A61K47/36A61K2300/00
Inventor 陈堃
Owner AFFILIATED YONGCHUAN HOSPITAL OF CHONGQING MEDICAL UNIV
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