Stable high-drug-loading-ratio lidocaine transdermal patch and preparation method thereof

A technology of lidocaine and transdermal patches, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as crystal transformation or growth

Active Publication Date: 2019-02-12
DEMOTECH INC
View PDF4 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, due to the existence of crystals during storage and use of active ingredients, there is a risk of further transformation or growth of crystals

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
  • Stable high-drug-loading-ratio lidocaine transdermal patch and preparation method thereof
  • Stable high-drug-loading-ratio lidocaine transdermal patch and preparation method thereof
  • Stable high-drug-loading-ratio lidocaine transdermal patch and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] A lidocaine-containing transdermal patch comprises a polymer matrix layer; the polymer matrix layer contains active ingredient lidocaine and acrylic pressure-sensitive adhesive without functional groups. Further, the patch also includes a backing layer and a protective layer; the polymer matrix layer is located between the backing layer and the protective layer.

[0048] After mixing the lidocaine and the acrylic pressure-sensitive adhesive without functional groups, the temperature is raised to about 60-80° C., so that the two form a homogeneous blend dispersed with each other to form the polymer matrix layer.

[0049] In the present embodiment, the weight contents of lidocaine and acrylic pressure-sensitive adhesive without functional groups in the polymer matrix layer are 60% and 39.8% respectively; 0.2%) antioxidants (such as BHA).

[0050] In this embodiment, the lidocaine is lidocaine free base; the acrylic pressure-sensitive adhesive without functional groups is...

experiment example 1

[0059] Experimental example 1 Stability experiment

[0060] The patches of Example 1, Comparative Example 2, and Comparative Example 3 were placed under the same storage conditions (30 ± 2° C., 60% ± 10% RH), and were regularly observed by an electron microscope. The observation results are shown in figure 1 .

[0061] The results of continuous observation showed that the active ingredients of the patches prepared in Example 1 and Comparative Example 2 of the present invention did not change significantly during the observation period, and lidocaine was uniformly dispersed in the polymer matrix in the form of tiny particles, and different multiples of optical No lidocaine particles (crystals) exist under the microscope, and no crystallization phenomenon is observed, indicating that the patch of the present invention has good stability. In the lidocaine patch of comparative example 3, crystal particles of lidocaine can be clearly observed, especially under high magnification o...

experiment example 2

[0062] Experimental example 2 in vitro release test

[0063] In vitro release is an essential performance indicator of a patch, reflecting the interaction of the active ingredient with other components in the polymer matrix. The overall properties of the polymer matrix, the interactions between lidocaine and polymer PSA, and other components such as hydrogen bonds, ion pairs, van der Waals forces, etc., lead to different flow behaviors of lidocaine in the polymer matrix. In vitro release is the basis of transdermal absorption, and only appropriate release capacity can meet specific transdermal absorption requirements.

[0064] According to the dissolution and release determination method (Chinese Pharmacopoeia 2015 edition fourth general rule 0931 fourth method - paddle-disc method), with PBS as the dissolution medium, the medium temperature is 32 ℃, 25 rpm, operated according to law, after 20 In 20 minutes, take 5ml of the solution, filter, and get the continued filtrate to ...

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 discloses a stable high-drug-loading-ratio lidocaine transdermal patch and a preparation method thereof. The stable high-drug-loading-ratio lidocaine transdermal patch comprises a back lining layer, a protection layer and a high-molecular substrate layer, wherein the high-molecular substrate layer is positioned between the back lining layer and the protection layer; the high-molecular substrate layer is made of lidocaine as an active component and a pressure sensitive adhesive free from a functional group. In the patch, the lidocaine as the active component is uniformly dispersedin the high-molecular substrate in the form of fine microparticles, so that the recrystallization of the lidocaine is restrained, and the lidocaine can be stored stably for a long time. Moreover, higher medicine releasing speed and shorter onset time are achieved. The preparation method has the advantages of simple process and low production cost.

Description

technical field [0001] The invention belongs to the technical field of transdermal administration, and in particular relates to a stable high-loaded lidocaine transdermal patch and a preparation method thereof. Background technique [0002] It is a very common way of drug delivery to use a transdermal drug delivery system (patch) to introduce active ingredients into the body through the skin or mucous membranes to achieve local or systemic effects. Since the first scopolamine patch in 1979 Since the launch, people have made a lot of attempts to develop more transdermal drug delivery systems with therapeutic effects. At present, several patch products have been successfully commercialized. According to the combination of active ingredients and other excipients in the patch, the patch can be generally divided into reservoir systems and drug-in-adhesives. Among them, the glue mixed type is to dissolve or disperse active ingredients uniformly in a semi-solid composition compo...

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): A61K9/70A61K47/32A61K31/167A61P29/00
CPCA61K47/32A61P29/00A61K9/7023A61K31/167
Inventor 谢文委律嵩何双江程楠
Owner DEMOTECH INC
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