Method of preparing of hydroxypropyl methacrylate (HPMA) - dexamethasone polymer

A polymer and solution technology, which can be used in drug combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., can solve problems such as constraints, achieve good biocompatibility, and reduce systemic side effects.

Inactive Publication Date: 2013-04-24
卢来春
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to its strong anti-inflammatory and anti-rheumatic effects, dexamethasone has become a classic drug for the treatment of RA, but it is restricted by many clinical adverse reactions, such as liver and kidney damage, cardiovascular complications, immune system effects, drug withdrawal reactions, etc. usage of

Method used

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  • Method of preparing of hydroxypropyl methacrylate (HPMA) - dexamethasone polymer
  • Method of preparing of hydroxypropyl methacrylate (HPMA) - dexamethasone polymer
  • Method of preparing of hydroxypropyl methacrylate (HPMA) - dexamethasone polymer

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1 prepares HPMA

[0043] Dissolve 16ml (0.2mol) of 1-amino-2-propanol in 20ml of acetonitrile, stir at room temperature (20-25°C) for 10min, slowly drop methacryloyl chloride into the acetonitrile solution, and stir at room temperature for 1h. The reaction solution was kept at -35°C for 12 h until the white crystals were completely precipitated. Filter and wash the crystals with cold acetone. Dry under reduced pressure and recrystallize with a small amount of acetone. Yield: 63%. MS(ESI) m / z144(M+1).1H NMR(400MHz, CDCl 3):δ1.20and1.22(d,J=6.4Hz,3H),1.97(s,3H),3.18-3.21(m,1H),3.48-3.51(m,1H),3.95-3.96(m,1H ), 5.36(s,1H), 5.74(s,1H).

Embodiment 2

[0044] Embodiment 2 synthetic NAGGONP

[0045] Take 10ml of 0.5M NaOH (50.7mmol) aqueous solution to dissolve 5g of diglyglyceride (38mmol), then place it at 0°C and stir for 30min. Then slowly drop the mixture of 3.8m methacryloyl chloride (38mmol) and 10ml, 5M NaOH (50.7mmol) into the diglycyl peptide solution and keep stirring at 0°C for 30min. After completion, take out the solution, stir at room temperature for 2 hours, add HCl dropwise until the solution is neutral, stir slowly until a white solid precipitates, collect the solid and filter, wash with cold water, dry under reduced pressure, and recrystallize with a small amount of 50% ethanol solution . Yield: 30%. 1H NMR: (400MHz, DMSO-d6) δppm: 1.876(s, 3H), 3.766(d, 4H), 5.561(d, 2H), 8.132(t, 1H), 8.190(t, 1H), 12.594(s ,1H).Mp=175-205℃.

Embodiment 3

[0046] Embodiment 3 prepares HPMA polymer-NAGGONP conjugate

[0047] With 2,2-azobisisobutylcyanide (AIBN) as the initiator, 2.24g (15.6mmol) of HPMA monomer and 0.09g (0.55mmol) of AIBN were dissolved in 20ml of acetone, and 0.2g of NAGGONP (0.6mmol) was dissolved In 2mlDMSO, then the two solutions were mixed and miscible, and N was introduced into the solution 2 After 30 minutes, the system was sealed and heated and stirred in a water bath at 60°C for 18 hours. Stand still, filter after the precipitation is complete, wash the solid with cold acetone, dry under reduced pressure, dissolve in dichloromethane: methanol = 9:1, add cold acetone for recrystallization. Yield: 60%.

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Abstract

The invention relates to chemical synthesis high molecular material, namely hydroxypropyl methacrylate (HPMA). A chemical name of the HPMA is a {poly [N-(2-hydroxypropyl) methacrylamide-group-N-(3-amino propyl) methacrylamide]} polymer. The invention further discloses a method of combining of materials and dexamethasone. 1-amino-2-propyl alcohol, gly-gly and methacryloyl chloride are taken as starting raw materials and combine an HPMA-dexamethasone (DEX) polymer through steps, such as replacing, polymerization and condensation, and the HPMA-DEX polymer is used for improving effect environment of the dexamethasone, and reduces side effect to achieve the best curative effect.

Description

【Technical field】 [0001] The invention relates to a carrier material HPMA polymer and a production method of the compound intermediate, in particular to a method for preparing HPMA-dexamethasone polymer. 【Background technique】 [0002] Dexamethasone, adrenocortical hormone drug, English name: dexamethasone, synonym: Dexamethasone, etc., CAS number: 50-02-2, molecular formula: C 22 h 29 FO 5 , molecular weight: 392.5. The pharmacological effects are mainly anti-inflammatory, anti-toxic, anti-allergic, anti-rheumatic, and are widely used clinically. It is easily absorbed from the digestive tract, its plasma T1 / 2 is 190 minutes, and its tissue T1 / 2 is 3 days. Due to its strong anti-inflammatory and anti-rheumatic effects, dexamethasone has become a classic drug for the treatment of RA, but it is restricted by many clinical adverse reactions, such as liver and kidney damage, cardiovascular complications, immune system effects, drug withdrawal reactions, etc. usage of. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F220/58C08F220/60C08F8/18C08F8/30A61K31/785A61K47/32A61P29/00A61P19/02
Inventor 卢来春傅若秋李卓恒宋羿于彩平管海燕李沉纹
Owner 卢来春
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