Rapid transdermal delivery system of local anesthetics

A transdermal drug delivery system and a technology for local anesthetics, which can be used in drug devices, other medical devices, etc., to solve problems such as unsatisfactory anesthesia effect and long onset time.

Active Publication Date: 2013-03-20
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The purpose of the present invention is to overcome the technical problems of long onset time of local anesthetic transdermal administration and unsatisfactory anesthesia effect of trans...

Method used

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  • Rapid transdermal delivery system of local anesthetics
  • Rapid transdermal delivery system of local anesthetics
  • Rapid transdermal delivery system of local anesthetics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of biodegradable nanoparticle gel with lidocaine as an example

[0024] The preparation steps of the nano-controlled release preparation loaded with local anesthetic lidocaine:

[0025] a. take stannous octoate as a catalyst, adopt PEG 4000 (polyethylene glycol with a molecular weight of 4000) and ε-caprolactone (mass ratio is 1: 24), under nitrogen protection, 100 degrees Celsius polymerization reaction for 5 hours, then set In vacuum at 160 degrees Celsius for 20 minutes, cooled to room temperature under the protection of nitrogen to obtain PCEC polymer, the relative molecular weight of the triblock polymer is 1 × 10 4 ~5×10 4 .

[0026] b. dissolving the PCEC polymer prepared according to step a in dichloromethane, and re-extracting with cold petroleum ether to obtain a purified PCEC polymer.

[0027] c. Dissolve the purified PCEC copolymer and lidocaine base prepared according to step b in ethyl acetate at 4 degrees Celsius, add F127 aqueou...

Embodiment 2

[0030] Example 2: Rapid transdermal administration method and effect verification of biodegradable nanoparticle gel with lidocaine as an example

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Abstract

The invention belongs to the technical field of transdermal delivery, in particular to a rapid transdermal delivery system of local anesthetics, which directly uses a preparation that is loaded with the local anesthetic, characterized by nano-materials and can control the release for transdermal delivery, or adds the preparation into thermo-sensitive gel poloxamer F127 solution with the concentration of 5%-40%, prepares a gel or a cream by regulating the temperature and directly uses the gel or the cream for transdermal delivery, or realizes the rapid transdermal delivery through pretreatment or an ultrasonic transmission device and/or an iontophoresis device treating the skin simultaneously under the common action of ultrasonic introduction, iontophoresis introduction or the combination of the two methods. The rapid transdermal delivery system can lead the transdermal permeation amount, the anesthetic onset time and the anesthetic potency of the local anesthetics, such as lidocaine, tetracaine, prilocaine, bupivacaine, ropivacaine, dicaine and the like to be better than those of the ordinary surface anesthetic preparation, solve the defects of long onset time of the existing surface anesthetic and limited action effects, eliminate the obvious skin irritation and be used for symptomatic treatment of skin anesthesia and neuropathic pain with skin invasive operation.

Description

Technical field: [0001] The invention belongs to the technical field of transdermal administration, in particular to a rapid transdermal administration system for local anesthetics. Background technique: [0002] Transdermal drug delivery technology is a drug delivery method that actively or passively penetrates the drug from the outside of the intact skin to the subcutaneous tissue. Due to the barrier function of the skin, especially the stratum corneum of the skin, it takes a long time for the drug to enter the subcutaneous tissue, and the amount of entry is also relatively limited. Transdermal administration of local anesthetics is mainly used in invasive skin operations, such as catheter placement, skin surgery and other skin surface anesthesia, and the treatment of neuropathic pain, such as post-herpetic pain. At present, the onset time of related products is still long, and it is difficult to achieve a satisfactory anesthesia effect in a short period of time, so the c...

Claims

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Application Information

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IPC IPC(8): A61M37/00
Inventor 张文胜刘进黄华钱志勇魏于全吴兰尹芹芹苟马玲杨乐林李东
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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