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Novel chemical skin penetration enhancer containing cholic acid group

A technology of absorption enhancer and enhancer, applied in the field of medicine, can solve problems such as toxic and side effects reducing application value, and achieve the effects of increasing solubility, excellent penetration promoting effect, and enhancing fluidity

Inactive Publication Date: 2015-08-26
云南白药集团无锡药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Further studies have found that on the basis of the active structure of the original penetration enhancer, many new derivatives with penetration enhancer activity can be obtained through structural modification, such as lipid synthesis inhibitors and terpenes, etc., but their toxic side effects Seriously reduces the application value of these substances

Method used

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  • Novel chemical skin penetration enhancer containing cholic acid group
  • Novel chemical skin penetration enhancer containing cholic acid group
  • Novel chemical skin penetration enhancer containing cholic acid group

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Diethylene glycol cholate (CAPEG-2) is prepared through the following steps:

[0037] (1) In a 250mL round bottom flask, dissolve 2g (4.9mmol) cholic acid and 0.6g (6.0mmol) diethylene glycol in 50mL dichloromethane (DCM), and add 0.05g (0.4mmol) Catalyst 4-lutidine (DMAP);

[0038] (2) Dissolve 1.24g (6.0mmol) N,N-dicyclohexyldiimine (DCC) in a mixed solvent of 10mL dichloromethane and acetonitrile (dichloromethane / acetonitrile=1 / 1), and stir state, the solution was dropped into the system of step (1), and reacted at room temperature for 18h;

[0039] (3) After the reaction is over, add 60mL of water to the system, then transfer it to a separatory funnel, let it stand until the layers are separated, remove the water layer, and wash the organic solution layer three times with 20mL distilled water and three times with 20mL saturated sodium bicarbonate solution , washed three times with 20 mL of saturated brine, collected the final organic phase, and dried with anhydrou...

Embodiment 2

[0042] Triethylene glycol cholate (CAPEG-3) is prepared through the following steps:

[0043] (1) In a 250mL round bottom flask, dissolve 2g (4.9mmol) cholic acid and 0.9g (6.0mmol) triethylene glycol in 30mL dichloromethane (DCM), and add 0.05g (0.4mmol) Catalyst 4-lutidine (DMAP);

[0044] (2) Dissolve 1.24g (6.0mmol) N,N-dicyclohexyldiimine (DCC) in a mixed solvent of 10mL dichloromethane and acetonitrile (dichloromethane / acetonitrile=1 / 1), and stir state, the solution was dropped into the system of step (1), and reacted at room temperature for 18h;

[0045] (3) After the reaction is over, add 60mL of water to the system, then transfer it to a separatory funnel, let it stand until the layers are separated, remove the water layer, and wash the organic solution layer three times with 20mL distilled water and three times with 20mL saturated sodium bicarbonate solution , washed three times with 20 mL of saturated brine, collected the final organic phase, and dried with anhydr...

Embodiment 3

[0049] Triethylene glycol cholate (CAPEG-4) is prepared through the following steps:

[0050] (1) In a 250mL round bottom flask, dissolve 2g (4.9mmol) cholic acid and 1.16g (6.0mmol) tetraethylene glycol in 50mL dichloromethane (DCM), and add 0.05g (0.4mmol) Catalyst 4-lutidine (DMAP);

[0051] (2) Dissolve 1.24g (6.0mmol) N,N-dicyclohexyldiimine (DCC) in a mixed solvent of 10mL dichloromethane and acetonitrile (dichloromethane / acetonitrile=1 / 1), and stir state, the solution was dropped into the system of step (1), and reacted at room temperature for 18h;

[0052] (3) After the reaction is over, add 60mL of water to the system, then transfer it to a separatory funnel, let it stand until the layers are separated, remove the water layer, and wash the organic solution layer three times with 20mL distilled water and three times with 20mL saturated sodium bicarbonate solution , washed three times with 20 mL of saturated brine, collected the final organic phase, and dried with anh...

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Abstract

The invention discloses a novel chemical skin penetration enhancer containing a cholic acid group, which is prepared by reacting cholic acid with polyethylene glycol. A medicine composite can be prepared by mixing the enhancer with a medicine and a medicine carrier; and a patch, an ointment, gel or cream can be prepared. The enhancer is odorless, can be dissolved in most organic solvents or water, has no obvious toxicity to a cell, represents amphipathy, and has an obvious penetration enhancement effect on the medicine.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a novel chemical penetration enhancer prepared from cholic acid and polyethylene glycol as main raw materials and containing cholic acid groups. Background technique [0002] Oral administration is one of the main routes of administration of pharmaceutical preparations at present, but there are many disadvantages; first, drugs with short half-lives require frequent administration, and patients' compliance is poor; second, drugs are prone to "peaks and valleys" in plasma phenomenon, resulting in an increased possibility of side effects associated with peak concentrations; thirdly, the hepatic first-pass effect and gastrointestinal metabolism associated with oral administration will lead to low bioavailability of the drug. Therefore, overcoming the above disadvantages, developing an effective and sustained drug delivery system would be much superior to oral regimens. [0003] The...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/70A61K9/06A61K47/28A61K45/00A61P5/38A61P29/00A61P35/00A61P23/00A61P25/24A61P5/32A61P5/28A61P5/36A61P33/00A61P9/12A61P7/02A61P9/10A61P31/10A61P13/08A61P21/02A61P25/22A61P11/08A61P25/18A61P25/16
Inventor 邵瑜肖宇刘跃陆晔辉
Owner 云南白药集团无锡药业有限公司
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