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Preparation method and application of drug-loading and permeation-promoting integrated transdermal drug delivery system matrix

A delivery system and drug technology, applied in the field of transdermal drug delivery system, can solve problems such as toxic side effects, limit the development of transdermal drug delivery system, and achieve the effect of avoiding irritation

Pending Publication Date: 2022-05-06
JIHUA LAB +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional chemical penetration enhancement is limited to drugs with small doses, small molecular weight and appropriate water-solubility and fat-solubility at the same time. The use is limited, and it has certain toxic and side effects, which limits the further development of transdermal drug delivery systems.

Method used

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  • Preparation method and application of drug-loading and permeation-promoting integrated transdermal drug delivery system matrix
  • Preparation method and application of drug-loading and permeation-promoting integrated transdermal drug delivery system matrix
  • Preparation method and application of drug-loading and permeation-promoting integrated transdermal drug delivery system matrix

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preparation example Construction

[0036] The present invention proposes a method for preparing a drug-loaded permeation-promoting integrated transdermal drug delivery system matrix. The preparation method of the drug-loaded permeation-promoting integrated transdermal drug delivery system matrix includes the following steps:

[0037] S10, after mixing the hydrogen bond donor and the hydrogen bond acceptor, heating to form a deep eutectic solvent;

[0038] In this embodiment, the hydrogen bond acceptor includes any one of L-diethyl tartrate, L-tartaric acid, citric acid, malonic acid, cinnamic acid, triglyceride, and cinnamate. Donors include choline chloride. In the present invention, the hydrogen bond donors in the ratio of the deep eutectic solvent include but are not limited to choline chloride, betaine and other hydrogen bond donors and hydrochloric acid thereof Salt. In the present embodiment, the hydrogen bond donor is preferably choline chloride, the hydrogen bond acceptor is preferably L-diethyl tartra...

Embodiment 1

[0051] (1) Heating choline chloride and diethyl L-tartrate at a molar ratio of 1:2 at 70°C for 30 minutes to form a transparent and uniform deep eutectic solvent, named CL12;

[0052] (2) Diclofenac diethylamine (60 mg / mL) was added to CL12, heated and dissolved to obtain the drug-loaded permeation-promoting integrated transdermal drug delivery system matrix, which was named CL12D.

[0053] (3) Apply CL12D on the non-woven fabric.

Embodiment 2

[0055] (1) Heating choline chloride and diethyl L-tartrate at a molar ratio of 1:4 at 70°C for 30 minutes to form a transparent and uniform deep eutectic solvent, named CL14;

[0056] (2) Diclofenac diethylamine (60 mg / mL) was added to CL14, heated and dissolved to obtain the drug-loaded permeation-promoting integrated transdermal drug delivery system matrix, which was named CL14D.

[0057] (3) Apply CL14D on the non-woven fabric.

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Abstract

The invention discloses a preparation method and application of a drug-loading and permeation-enhancing integrated transdermal drug delivery system matrix, and the preparation method of the drug-loading and permeation-enhancing integrated transdermal drug delivery system matrix comprises the following steps: mixing a hydrogen bond donor and a hydrogen bond receptor, and heating to form a eutectic solvent; and dissolving a hydrophobic drug in the deep-eutectic solvent to obtain the drug-loading and permeation-promoting integrated transdermal drug delivery system matrix. The deep-eutectic solvent is constructed through hydrogen bond interaction of the L-diethyl tartrate and the choline chloride, then the hydrophobic drug is dissolved in the deep-eutectic solvent, and the hydrophobic drug integrally shows certain viscosity and can be used as a matrix material of a transdermal drug delivery system. Meanwhile, the system has a certain solubilizing effect and permeation enhancing performance on hydrophobic drugs, and irritation to the skin is avoided.

Description

technical field [0001] The invention relates to a drug delivery system for transdermal administration, in particular to a preparation method and application of a drug-loaded and permeation-promoting integrated transdermal drug delivery system matrix. Background technique [0002] With the development of the pharmaceutical industry, transdermal drug delivery is the third largest drug delivery system after oral administration and injection, because it has many advantages, such as avoiding the hepatic first-pass effect, maintaining a constant blood drug concentration and increasing patient compliance etc., have received widespread attention. According to the forecast of the World Health Organization, more than 30% of oral drugs will need to be converted to transdermal drug delivery in the future, and the total market will reach 81.4 billion US dollars in 2024. At present, gel plasters and rubber plasters are commonly used, especially for hydrophobic drugs, rubber plasters are ...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/12A61K47/14A61K47/18A61K31/167A61K31/196A61K31/352
CPCA61K9/7023A61K47/12A61K47/14A61K47/186A61K31/196A61K31/167A61K31/352
Inventor 吕建华雷凯君赵岩商磊何明丰欧小玉方雅茹吴秘李怀国郑芳昊
Owner JIHUA LAB
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