High-activity slow-release pain-relieving patch and preparation process thereof

A high-activity, pain-relieving patch technology, applied in the direction of non-central analgesics, organic active ingredients, medical preparations of non-active ingredients, etc., can solve problems such as limiting the development of transdermal drug delivery preparations, skin allergies, and skin damage , to achieve the effects of improving production safety and drug safety, reducing allergic reactions, and reducing production costs

Pending Publication Date: 2021-10-08
ZHEJIANG DINGTAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, traditional analgesic transdermal preparations, such as black plasters and rubber plasters, have strong irritation and sensitization, and the drug loading is small, which greatly limits the further development of transdermal preparations.
[0003] At present, the traditional production method of the domestic transdermal plaster is the solvent method, for example, the patent document with the publication number CN107375891A discloses a preparation method of an external plaster for expelling rheumatism; because the solvent method uses gasoline as a sol...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The preparation process of the highly active sustained-release analgesic patch of the present embodiment comprises the following steps:

[0031] (1) Add 30wt% of the skeleton material natural rubber, 16wt% of thermoplastic rubber SIS, and 2wt% of PB2400 polyisobutylene into the mixing and dispersing machine to fully mix and disperse, then add 2wt% of lanolin, 1wt% of vaseline, 2wt% of liquid paraffin, and rosin glyceride 10wt% and 7wt% zinc oxide were kneaded and dispersed uniformly to obtain a matrix;

[0032] (2) 10wt% of methyl salicylate, 6.5wt% of menthol, 3.5wt% of camphor, and 10wt% of cyclodextrin are stirred evenly and added to the above-mentioned matrix for kneading, and then the slurry is filtered and refined by a filter to make each The ingredients are fully mixed and discharged;

[0033] (3) The paste is heated to 80 degrees by the coating machine and coated on the backing layer, and the cover isolation layer is cooled to 5 degrees by the cooling tunnel, a...

Embodiment 2

[0036] The preparation process of the highly active sustained-release analgesic patch of the present embodiment comprises the following steps:

[0037] (1) Add 15wt% of natural rubber, 10wt% of synthetic rubber, 15wt% of thermoplastic rubber SIS, and 2wt% of PB2400 polyisobutylene into the mixing and dispersing machine to fully mix and disperse, then add 2wt% of lanolin, 1wt% of vaseline, and 5wt of liquid paraffin %, rosin glyceride 10wt%, lithopone 3wt%, zinc oxide 6wt% kneading and dispersing evenly to obtain a matrix;

[0038] (2) Stir 10wt% of methyl salicylate, 6.5wt% of menthol, 3.5wt% of camphor, and 11wt% of kaolin evenly and add them to the above-mentioned matrix for mixing, and then filter and refine the paste through a filter to make each component fully Mix and discharge;

[0039] (3) The paste is heated to 80 degrees by the coating machine and coated on the backing layer, and the cover isolation layer is cooled to 5 degrees by the cooling tunnel, and then rolled...

Embodiment 3

[0042] The preparation process of the highly active sustained-release analgesic patch of the present embodiment comprises the following steps:

[0043] (1) Add 15wt% of natural rubber, 10wt% of synthetic rubber, 15wt% of thermoplastic rubber SIS, and 5wt% of polyisobutylene B50 into the mixing and dispersing machine to fully mix and disperse, then add 2wt% of lanolin, 1wt% of vaseline, and 5wt of liquid paraffin %, sodium carboxymethyl cellulose 10wt%, aluminum silicate 1wt%, zinc oxide 6wt% kneading and dispersing evenly to obtain a matrix;

[0044] (2) Stir 10wt% methyl salicylate, 6.5wt% menthol, 3.5wt% camphor, and 10wt% Eudragit (ethyl acrylate, methyl methacrylate copolymer) and add to the above matrix for kneading , and then filter and refine the slurry through a filter to fully mix and discharge the ingredients;

[0045] (3) The paste is heated to 80 degrees by the coating machine, and then coated on the backing layer, and the cover isolation layer is cooled to 5 degr...

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PUM

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Abstract

The invention relates to a high-activity slow-release pain-relieving patch and a preparation process thereof. The high-activity slow-release pain-relieving patch comprises a backing layer, a main body layer and an isolation layer which are sequentially stacked, wherein the main body layer comprises the following components: a matrix, active ingredients and an active ingredient slow-release inclusion material, wherein the matrix comprises 30-50wt% of a framework material and 12-28wt% of an auxiliary agent; the active ingredients comprise 6-12wt% of methyl salicylate, 5-8wt% of menthol and 1-4wt% of camphor; and the active ingredient slow-release inclusion material accounts for 6-18wt%. According to the high-activity slow-release pain-relieving patch, medicines with high activity and high volatility, namely methyl salicylate, menthol and camphor, are selected as the main body of the high-activity slow-release pain-relieving patch, and the active ingredients in the main body are included by adopting the slow-release inclusion material, so that the content of each active ingredient is kept to the maximum extent and is continuously and stably released, and the effectiveness of the medicines is ensured; and the matrix material with low sensitization and hydrophilicity is selected, and the preparation process adopts an innovative solvent-free production process technology, so that the transdermal patch is not easily allergic to a human body when being used for the human body, and the safety of the medicines is ensured.

Description

technical field [0001] The invention belongs to the technical field of drug transdermal patch preparation technology, and in particular relates to a highly active sustained-release pain-relieving patch and a preparation process thereof. Background technique [0002] Transdermal patches are effective in treating diseases, especially rheumatic joint pain, muscle pain, sprains, cervical spine, waist and leg pain, etc., and occupy a large proportion in clinical use. Transdermal administration is the third largest route of administration besides oral administration and injection. However, traditional analgesic transdermal preparations, such as black plasters and rubber plasters, are highly irritating and sensitizing, and the drug loading is small, which greatly limits the further development of transdermal preparations. [0003] At present, the traditional production method of the domestic transdermal plaster is the solvent method, for example, the patent document with the publi...

Claims

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Application Information

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IPC IPC(8): A61K31/618A61K9/70A61K47/69A61P29/00A61P19/02A61P21/00A61K31/045A61K31/125
CPCA61K31/618A61K31/045A61K31/125A61K9/7023A61K47/6951A61K47/6949A61P29/00A61P19/02A61P21/00A61K2300/00
Inventor 徐建峰施利群左伟平倪斌斌张利华付茂琦朗古特徐忠贤姜成炜
Owner ZHEJIANG DINGTAI PHARMA
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