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System for promoting permeation of active ingredients into skin

A technology that promotes activity and skin. It is applied in the direction of organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients. Improves therapeutic efficacy without irritation and adverse effects

Pending Publication Date: 2020-07-14
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to solve the technical problem that active ingredients (such as insoluble drugs and / or poorly permeable drugs) are difficult to cross the skin barrier based on the current situation of the prior art, and provide a system for promoting active ingredients to penetrate the skin and its effect on the skin. Application in the drug system; the system for promoting active ingredients to penetrate the skin can deliver drug molecules to the epidermis and dermis, and rarely penetrate the skin into the blood, which can significantly enhance the effect of drugs for treating skin diseases

Method used

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  • System for promoting permeation of active ingredients into skin
  • System for promoting permeation of active ingredients into skin
  • System for promoting permeation of active ingredients into skin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1 choline malate system promotes dextran to penetrate the skin

[0033] A choline malate system containing dextran (FD4) labeled with fluorescein isothiocyanate (FITC) was prepared for transdermal experiments, and the detailed component descriptions are shown in Table 1;

[0034] Table 1. The mass percentage of the detailed components of the dextran-choline malate system (moisture content=0)

[0035] DL-malic acid (Sinopharm Group) Choline bicarbonate (Sigma) FD4 (Sigma Corporation) 66.4％ 32.6％ 1％

[0036] Add malic acid and choline bicarbonate to methanol at a molar ratio of 5:2 to dissolve, stir at room temperature for 4 hours until the generation of carbon dioxide stops, remove methanol and water by rotary evaporation at 60°C, and vacuum dry for 48 hours to remove residual solvent to obtain Infiltration system, add 1% FD4 into the system, stir and dissolve;

[0037] In this example, FD4 was dissolved by choline malate, and its abi...

Embodiment 2

[0038] Example 2 Choline citrate system is used to promote hyaluronic acid skin penetration

[0039] A choline citrate system containing hyaluronic acid was prepared for transdermal experiments, and the detailed component descriptions are shown in Table 2;

[0040] Table 2. Mass percentages of detailed components of the hyaluronic acid-choline malate system (moisture content=0)

[0041] Citric Acid Monohydrate (Sinopharm Group) Choline bicarbonate (Sigma) Hyaluronic Acid (Sinopharm Group) 29.5％ 69.5％ 1％

[0042] Add citric acid and choline bicarbonate to methanol at a molar ratio of 1:3 to dissolve, stir at room temperature for 4 hours until the generation of carbon dioxide stops, remove methanol and water by rotary evaporation at 60°C, and vacuum dry for 48 hours to remove residual solvent to obtain the Osmotic system; add 1% hyaluronic acid into the system, stir to dissolve;

[0043] In this example, pigskin was used as an in vitro model, the hyalur...

Embodiment 3

[0044] Embodiment 3 glycine choline system is used to promote ketoconazole skin penetration

[0045] Glycine choline system containing ketoconazole was prepared for transdermal experiment, and the detailed components are shown in Table 3.

[0046] Table 3. The mass percentage of the detailed components of the ketoconazole-glycine choline system (moisture content=0)

[0047] Glycine (Sinopharm Group) Choline bicarbonate (Sigma) Glycerin (Sinopharm Group) Ketoconazole (Sinopharm Group) 50.1％ 27.9％ 20％ 2％

[0048] Glycine and choline bicarbonate were dissolved in methanol at a molar ratio of 4:1, stirred at room temperature for 4 hours until the generation of carbon dioxide ceased, methanol and water were removed by rotary evaporation at 60°C, and the remaining solvent was removed by vacuum drying for 48 hours to obtain permeation enhancement system; add 20% glycerin and 2% ketoconazole into the system, stir and dissolve;

[0049] Taking the abdominal...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a system for promoting permeation of active ingredients into skin. The system comprises an organic acid andan organic base and / or a salt thereof, the organic acid and the organic base or the salt thereof are mixed under certain conditions to form a liquid at room temperature, and the liquid can dissolve active ingredients including an insoluble drug and a biomacromolecular drug. The system provided by the invention can deliver drug molecules to epidermis and dermis, enables the drug molecules to rarelypenetrate through the skin to enter blood, and can obviously enhance the effect of the drugs in treating skin diseases.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and relates to a system for promoting the penetration of active ingredients into the skin. The system for promoting the penetration of active ingredients into the skin contains at least one organic acid, and at least one organic base and / or its salt, which can deliver drug molecules to the epidermis and dermis, and rarely penetrate the skin into the blood, which can significantly Enhance the effect of medicines to treat skin diseases. Background technique [0002] The prior art discloses that there are various biological barriers in the human body, so as to protect the stability of the internal environment of the body and avoid the invasion of toxic substances or microorganisms in the external environment, such as skin, nasal mucosa, gastrointestinal mucosa, vagina and rectum. Mucous membranes, etc. The prior art also discloses that the skin is the most extensive coverage in ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K45/00A61K47/12A61K47/18A61K47/28A61K31/716A61K31/728A61K31/496A61K38/13
CPCA61K9/0014A61K9/06A61K45/00A61K47/12A61K47/183A61K47/28A61K31/716A61K31/728A61K31/496A61K38/13
Inventor 戚建平武喜营吴伟卢懿
Owner FUDAN UNIV
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