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Preparation method of novel medicinal transdermal penetration enhancer

A permeation enhancer, a new type of technology, applied in the field of preparation of new medicinal transdermal permeation enhancers, can solve the problems of limited penetration enhancement effect of macromolecular drugs and failure to achieve the penetration enhancement effect, and achieve long service life and low corrosion , high catalytic activity

Active Publication Date: 2015-01-14
XIAN IAMTECH POLYMER MATERIAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, so far, most penetration enhancers cannot achieve the ideal penetration enhancement effect and meet the purpose of drug treatment, and their penetration enhancement effect on macromolecular drugs is very limited.

Method used

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  • Preparation method of novel medicinal transdermal penetration enhancer

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Preparation of active catalyst: In a vacuum glove box, 1, 3-dimethylimidazole was mixed with TiCl 4 Mix the reaction under dichloromethane, and control the intensity of the reaction by stirring, wherein, satisfy n(1,3-dimethylimidazole): n(TiCl 3 ) = 1 : 2, the reaction temperature is controlled at 45°C, and the reaction time is 2 hours to obtain an active catalyst.

[0020] (2) Preparation of liquid polyolefin: firstly, the 2 L high-pressure reactor was dried, vacuumed, and nitrogen-filled to ensure that the inside of the reactor was inert gas to protect the environment. Next, add to the reactor = 480 HBPE and decene (C 10 ), the active catalyst system and methylene chloride, satisfying n(HBPE): n(C 10 ) = 1 : 0.35, V (HBPE + C 10 ): V (catalyst): V (organic solvent) = 5 : 0.5: 20, at 280 r min -1 Stir to make it fully contact, keep the pressure in the kettle at 0.6 MPa, the temperature at 55°C, and control the reaction time at 8 hours to obtain the primary p...

Embodiment 2

[0023] (1) Preparation of active catalyst: In a vacuum glove box, 1-methyl-3-ethylimidazole was mixed with AlCl 3 Mix the reaction under cyclohexane, and control the intensity of the reaction by stirring, wherein, satisfy n(1-methyl-3-ethylimidazole): n(AlCl 3 ) = 1 : 4, the reaction temperature was controlled at 30°C, and the reaction time was 4 hours to obtain an active catalyst.

[0024] (2) Preparation of liquid polyolefin: firstly, the 2 L high-pressure reactor was dried, vacuumed, and nitrogen-filled to ensure that the inside of the reactor was inert gas to protect the environment. Next, add to the reactor = 390 for HBPE and octene (C 8 ), active catalyst system and organic solvent, satisfying n(HBPE): n(C 8 ) = 1 : 0.45, V (HBPE + C 8 ): V (catalyst): V (cyclohexane) = 8 : 0.8: 44, at 260 r min -1Stir to make it fully contact, keep the pressure in the kettle at 1.5 MPa, the temperature at 35°C, and control the reaction time at 12 hours to obtain the primary produc...

Embodiment 3

[0027] (1) Preparation of active catalyst: In a vacuum glove box, 1-methyl-3-propylimidazole and ZnCl 2 The reaction was mixed under chloroform, and the intensity of the reaction was controlled by stirring, wherein, n(1-methyl-3-propylimidazole): n(ZnCl 2 ) = 1 : 2, the reaction temperature is controlled at 35°C, and the reaction time is 3.5 hours to obtain an active catalyst.

[0028] (2) Preparation of liquid polyolefin: firstly, a 10 L high-pressure reactor was dried, vacuumed, and nitrogen-gassed to ensure that the inside of the reactor was inert gas to protect the environment. Next, add to the reactor = 560 HBPE and octene (C 8 ), the active catalyst system and chloroform, satisfying n(HBPE): n(C 8 ) = 1 : 2.6, V (HBPE + C 8 ): V (catalyst): V (cyclohexane) = 6 : 0.5: 28, at 200 r min -1 Stir to make it fully contact, keep the pressure in the kettle at 2.0 MPa, the temperature at 45°C, and control the reaction time at 6 hours to obtain the primary product of liquid...

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Abstract

The invention discloses a preparation method of a novel medicinal transdermal penetration enhancer, and relates to a synthesis method of liquid hydrogenated polyolefin. The method includes the steps of catalyst preparation, olefin catalytic polymerization and polyolefin hydrogenation. Polyolefin obtained through the method is colorless, tasteless and nontoxic, has the characteristics of high chemical stability, chemical inertness and high permeability, has no irritation or discomfort to skins as a transdermal absorption enhancer, has good compatibility with the skins, has no pharmacological activity, is suitable for medicines of all transdermal absorption dosage forms, and is a novel transdermal absorption enhancer.

Description

technical field [0001] The invention relates to a preparation method of a novel medicinal percutaneous penetration enhancer, which belongs to the technical field of fine chemicals. Said invention includes the synthesis of catalysts, the catalytic polymerization of ethylene and the hydrogenation of polyolefins. The liquid polyolefin prepared by the method is suitable for medicines in various percutaneous absorption dosage forms, and is a novel skin penetration enhancer. Background technique [0002] The transdermal drug delivery system is a new way of drug delivery through the skin, which can make the drug continuously diffuse through the skin, enter the blood circulation after permeation and absorption, and keep the blood drug concentration stable for a long time. Its advantages are that it can avoid the first-pass effect of the liver, and the drug can directly enter the blood, which improves the predictability of the drug in the body; the drug administration can be interru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F255/02C08F4/14C08F4/10C08F4/16C08F8/04A61K47/32
Inventor 相鹏王静
Owner XIAN IAMTECH POLYMER MATERIAL
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