Polyethylene glycol-phosphatidyl ethanolamine polymer or medicinal acid addition salt and application thereof in pharmacy

A technology of phosphatidylethanolamine and polyethylene glycol, which is applied in the direction of medical preparations, antipyretics, antitumor drugs, etc. of non-active ingredients, can solve the problems of high price, limited use, long residence time, etc., and achieve product The effect of stable quality

Inactive Publication Date: 2007-08-15
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But its price in China is very expensive, about 6,000 RMB / piece, which greatly limits its use
At the same time, STEALTH  Liposomes stay in the body too long (half-life in the body is about 55 hours)

Method used

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  • Polyethylene glycol-phosphatidyl ethanolamine polymer or medicinal acid addition salt and application thereof in pharmacy
  • Polyethylene glycol-phosphatidyl ethanolamine polymer or medicinal acid addition salt and application thereof in pharmacy
  • Polyethylene glycol-phosphatidyl ethanolamine polymer or medicinal acid addition salt and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] General method for preparing polyethylene glycol-phosphatidylethanolamine polymer general formula (II)

[0080] In a 1000ml three-necked bottle, add MPEG-2000 (20g; 0.01mol), distearoylphosphatidylethanolamine (0.01mol) and 500ml of chloroform, then add paraformaldehyde (3g, 0.1mol), stir and heat to reflux , slowly drop into concentrated hydrochloric acid 10ml, continue the reaction, TLC monitors the reaction process, the developer is 2-butanone / acetic acid / water=40 / 25 / 5, v / v / v, iodine color development, distearoyl phospholipid The Rf value of acyl ethanolamine was 0.68, and after 10 hours, distearoylphosphatidylethanolamine had mostly reacted completely, and the reaction solution was evaporated to dryness, and the residue was dissolved in 10ml of dichloromethane, and the shaving column chromatography was carried out, and the eluent was Dichloromethane and Methanol. The product fractions were combined and concentrated to obtain 11 g of colorless waxy methoxypolyethyle...

Embodiment 2

[0082] General method for preparing polyethylene glycol-phosphatidylethanolamine polymer general formula (III)

[0083] In a 1000ml three-neck flask, add cephalin (0.01mol), p-hydroxybenzaldehyde (1.22g, 0.01mol) and 300ml of anhydrous toluene, reflux with water until the evaporated toluene is clear, monitor the reaction progress by TLC, and set aside.

[0084] In a 500ml three-necked flask, add MPEG-1900 (19g; 0.01mol) and 300ml of anhydrous chloroform, cool with an ice-salt bath, slowly add 10ml of triethylamine and 3ml of trifluoromethanesulfonic anhydride, protect with inert gas, and stir overnight . The next day, slowly drop the reaction solution into the above reaction solution, gradually increase the temperature and evaporate the chloroform, react at 110°C for 16 hours, evaporate the reaction solution to dryness, dissolve the residue with 10ml of dichloromethane, perform column chromatography, wash The dehydration is dichloromethane and methanol. The product fractions...

Embodiment 3

[0086] The preparation general method of polyethylene glycol-phosphatidylethanolamine polymer general formula (IV)

[0087] method one:

[0088] In a 500ml three-necked flask, add MPEG-1500 (15g; 0.01mol) and 300ml of anhydrous benzene, under stirring, slowly drop into oxalic anhydride (1.4g, 0.02mol), continue to reflux for 4 hours, cool to room temperature, Add 10ml of freshly steamed thionyl chloride, continue the reflux reaction for 4 hours, gradually increase the temperature and evaporate to dryness, add anhydrous benzoic acid 3 times, dissolve in 300ml of anhydrous benzene and set aside.

[0089] In a 1000ml three-neck bottle, add distearoylphosphatidylethanolamine or cephalin (0.01mol), 10ml of triethylamine and 300ml of anhydrous benzene, under stirring, slowly add the above solution dropwise in an ice-salt bath, and dropwise , continue the reflux reaction for 6 hours, evaporate the reaction solution to dryness, dissolve the residue with 10ml of dichloromethane, and p...

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Abstract

Polyethylene glycol-phospholipid choline polymeride or its medicinal acid salt and application in pharmacy belong to technology field of nanometer medicine preparation. Polyethylene glycol-phospholipid choline polymeride or its medicinal acid salt is indicated as the following general formula (I), namely methoxypolyethylene glycol and phospholipid choline is associative through link which is substituted methylene or ether substituted benzene methylene or oxalyl. The polymeride can be used as medicine carrier, especially in preparing antitumor liposome preparation, can thicken antitumor drug at tumour position. The invention provides the application of polymeride with general formula (I) or its medicinal acid salt in preparing medicine for treating tumour, cardio-cerebrovascular diseases, inflammation infection, and asthma.

Description

technical field [0001] The invention belongs to a polymer of polyethylene glycol (PEG) and phosphatidylethanolamine, a medicinal acid addition salt thereof, a preparation method thereof, and an application as a drug carrier in the preparation of medicines, and belongs to the technical field of nano-medicine preparation. Background technique [0002] Liposomes have targeting properties, longer blood residence time and higher organ distribution selectivity, which can improve the efficacy of drugs and reduce toxic and side effects. [0003] Liposomes are mainly used as carriers for intravenous drug delivery. However, reticuloendothelial tissue (RES) cells can quickly clear liposomes, which severely limits the scope of their use as a carrier for vascular drug delivery. Generally, after an intravenous injection, the RES system can remove 80%-95% of liposomes within one hour, which is much higher than the uptake rate of the predetermined target site. Therefore, the treatment of d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61P35/00A61P29/00A61P11/06A61P9/00A61K47/59A61K47/60
Inventor 吉民顾宁蔡进夏强吴晓晴张瑛余佳
Owner SOUTHEAST UNIV
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