Buprenorphine transdermal solution as well as preparation method and application thereof

A solution and transdermal technology, applied in the field of medicine, can solve the problems of short duration of drug effect, low bioavailability of buprenorphine, frequent administration, etc., achieve prolonged analgesic effect, avoid peak and valley phenomena, and reduce individual difference effect

Active Publication Date: 2022-07-01
JINAN GUANGSHENGYUAN BIOTECH
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Based on the above-mentioned problems existing in the prior art, the object of the present invention is to solve the problems of low bioavailability of buprenorphine, short duration of drug effect and frequent administration, and provide a buprenorphine transdermal solution and its Preparation method and application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Buprenorphine transdermal solution as well as preparation method and application thereof
  • Buprenorphine transdermal solution as well as preparation method and application thereof
  • Buprenorphine transdermal solution as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0053] Experimental Example 1 Preparation of buprenorphine transdermal solution

[0054] (1) Take DSPE-mPEG, disperse it in a non-polar solvent, ultrasonicate for 300w, 5min, and prepare a series of non-polar solvent solutions containing different concentrations of DSPE-mPEG;

[0055] (2) In the above solution, add buprenorphine (fixed dose of 2%, w / w) and preservatives (fixed dose of 0.05%, w / w), dissolve by ultrasonic until the solution is clear and transparent, and the ultrasonic condition is 400w, 5min.

[0056] The components and mass ratios in each recipe are set as shown in Table 1:

[0057]

Embodiment 2

[0058] Example 2 Study on the physicochemical properties of buprenorphine transdermal solution

[0059] After diluting the buprenorphine transdermal solution prepared by the recipe in Example 1 by an appropriate multiple, analyze it with a particle size analyzer to obtain the particle diameter and zeta potential of the reverse micelle (three samples are measured in parallel for each recipe, and the average value is obtained. ); the prepared buprenorphine transdermal solution was moderately diluted, then added dropwise to a copper mesh covered with carbon film, and the morphology of reverse micelle particles was observed under a transmission electron microscope after treatment. The particle size analysis results of different formulations are shown in Table 2.

[0060]

[0061] In Table 2, the PDI (Polymer dispersity index) is the polymer dispersity index, which is used to describe the molecular weight distribution of the polymer.

[0062] As can be seen from Table 2, compar...

Embodiment 3

[0065] Example 3 In vitro transdermal properties of buprenorphine transdermal solution

[0066] Preparation of buprenorphine solution-IPM solution: Dissolve the prescribed amount of buprenorphine and isooctyl salicylate in IPM to prepare a clear and transparent solution as a control solution.

[0067] In vitro transdermal properties studies of buprenorphine transdermal solutions using a modified Franz diffusion cell. The skin used was the dehaired back skin of healthy adult male guinea pigs, and normal saline was used as the receiving fluid. The treated skin was placed between the sample chamber and the receiving chamber, and 2 mL of the buprenorphine-IPM solution and prescription 2, 6, 7, and 10 transdermal solutions were accurately measured and injected into the sample chamber, and then the diffusion cell was placed in the sample chamber. It was placed in a constant temperature bath (37±0.5°C) and magnetically stirred at 100r / min. Samples were taken at 0.5h, 1h, 2h, 4h, 8h...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention provides a buprenorphine transdermal solution as well as a preparation method and application thereof, the solution takes buprenorphine as an active ingredient, contains phospholipid-polyethylene glycol, a transdermal enhancer and a non-polar solvent, solves the problems of frequent administration and skin irritation of mammal buprenorphine, and provides a new scheme for continuous pain control. The buprenorphine transdermal solution disclosed by the invention has the effects of rapid absorption, slow release, high safety and long-acting analgesia, and can be used for postoperative analgesia of mammals.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a buprenorphine transdermal solution and a preparation method and application thereof. Background technique [0002] The information disclosed in this Background section is only for enhancement of understanding of the general background of the invention and should not necessarily be taken as an acknowledgement or any form of suggestion that this information forms the prior art already known to a person of ordinary skill in the art. [0003] Pain management has become a routine procedure after surgery in veterinary medicine. For the drug treatment of pain, the WHO gives a "stepped" drug recommendation: it means that analgesic drugs of different intensities should be selected according to the degree of pain of the patient. ① Mild pain: Non-steroidal anti-inflammatory drugs (NSAIDs) can be used. ② Moderate pain: Weak opioids can be used, and non-steroidal anti-inflammatory drugs ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/485A61K9/08A61K47/24A61K47/14A61P25/00A61P29/00
CPCA61K31/485A61K9/08A61K47/24A61K47/14A61K9/0017A61P25/00A61P29/00
Inventor 杨志昆李斌张琦林洪军邹宇云董菊红
Owner JINAN GUANGSHENGYUAN BIOTECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap