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Percutaneous absorption agent containing Ailamode, preparation method and medical uses thereof

A technology of transdermal absorbent and transdermal accelerator, which is applied in the field of transdermal absorbents containing iguratimod, which can solve problems such as difficulty in taking medicine, no report of topical transdermal absorption of iguratimod, and damage to the body

Inactive Publication Date: 2009-04-08
杨喜鸿
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] When iguratimod is administered in oral preparations, not only will there be a first-pass effect, but patients often have gastrointestinal reactions that make it difficult to take the medicine; Troublesome to use and damage to the body
Based on all the retrieved literature, there is no report on the research on the topical transdermal absorption of iguratimod and the development of dosage forms

Method used

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  • Percutaneous absorption agent containing Ailamode, preparation method and medical uses thereof
  • Percutaneous absorption agent containing Ailamode, preparation method and medical uses thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0157] Embodiment 1. Iguratimod gel and preparation thereof

[0158] Prescription: Iguratimod 0.5g, Carbomer 1g, Triethanolamine 2g, Propylene Glycol 10g, Laurocaprazine 2g, Glycerin 5g, Ethanol 5ml, Purified water to 100g.

[0159] Preparation: Take carbomer and add 35ml of purified water to make it fully swell, stir evenly to obtain a carbomer solution, adjust the pH value of the solution to 6.0-9.5 with triethanolamine, and stir well to obtain a blank gel; Dissolve Derong powder in ethanol, stir well, add propylene glycol, laurocapram, glycerin, stir evenly, then slowly add the liquid medicine into the carbomer matrix, stir evenly while adding, and finally add purified water to 100g, Get the iguratimod gel, packed in an aluminum tube, every 20g, to get final product.

Embodiment 2

[0160] Embodiment 2. Iguratimod gel and its preparation

[0161] Prescription: Iguratimod 1g, chitosan 1.5g, triethanolamine 1g, glycerin 8g, laurocapram 2g, ethanol 35ml, distilled water to 100g.

[0162] Preparation: Take iguratimod and glycerin, add 35ml of ethanol, stir evenly, add 50ml of distilled water to dissolve and dilute, sprinkle chitosan on the surface of the liquid, make it fully swell, stir well, add laurocaprolactone, stir well, and then Add triethanolamine, stir well, add distilled water to 100g, stir evenly to obtain Airamod gel, pack it.

Embodiment 3

[0163] Embodiment 3. Iguratimod gel and its preparation

[0164] Prescription: Ilamod 2g, Carbomer 9403g, Menthol 2.5g, Propylene Glycol 20g, Isopropanol 12g, Ethylparaben 0.2g, Triethanolamine amount, Purified water up to 100g.

[0165] Preparation: Sprinkle Carbomer 940 evenly in an appropriate amount of purified water to make it fully swell, add purified water to 50ml, and stir evenly to obtain a Carbomer solution. Use triethanolamine to adjust the pH value of the solution to 6.0-8, and stir well. Obtain a blank gel; add iguratimod, menthol, ethyl paraben, add isopropanol and propylene glycol to dissolve, add slowly while stirring the blank gel, stir evenly, add water to 100g, stir well, and get Aguratimod gel, ready to pack.

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PUM

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Abstract

The invention relates to a transdermal absorbent containing Iguratimod, which comprises gellies, ointment, and cream, wherein the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.1 and 10 percent, and preferably the mass percentage content of the Iguratimod in the transdermal absorbent is between 0.4 and 3 percent; and the invention also discloses requirements of the transdermal absorbent on the selections of matrix and a transdermal enhancer. Furthermore, the invention also provides a method for preparing the transdermal absorbent containing the Iguratimod and pharmaceutical application thereof.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and relates to a transdermal absorbent containing iguratimod, a preparation method thereof and its application in medicine. Background technique [0002] Iguratimod (Iguratimod, T-614, CAS RN: 123663-49-0), the chemical name is N-[3-(formamide)-4-oxo-6-phenoxy-4H-1-benzo Pyran-7-yl]-methanesulfonamide, English name: N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methanesulfonamide, the molecular structure is as follows: [0003] Molecular formula C 17 h 14 N 2 o 6 S, molecular weight 374.4. [0004] Iguratimod is a new non-steroidal anti-inflammatory drug that selectively inhibits cyclooxygenase-2. It has antipyretic and analgesic effects, anti-arthritis effects, and immune regulation effects. Sexual arthritis, osteoarthritis and ankylosing spondylitis have excellent curative effect, and can also relieve pain and joint pain caused by muscle and soft tissue damage. It can not on...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/352A61P29/00
Inventor 杨喜鸿
Owner 杨喜鸿
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