Hydrophilic polyglycol supported ursolic acid medicines and their prepn process

A polyethylene glycol and polyethylene glycol grafting technology, which is applied in the direction of pharmaceutical formulations, antineoplastic drugs, drug combinations, etc., can solve problems such as unsatisfactory effects

Inactive Publication Date: 2007-08-22
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the effect is not very good

Method used

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  • Hydrophilic polyglycol supported ursolic acid medicines and their prepn process
  • Hydrophilic polyglycol supported ursolic acid medicines and their prepn process
  • Hydrophilic polyglycol supported ursolic acid medicines and their prepn process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Synthesis of polyethylene glycol-diacid 4 (PEG-DA)

[0021] Take 20g (10mmol) PEG-2000 and dissolve in 150mL anhydrous chloroform (CaH 2 In the presence of distilled), add 5g (50mmol) of succinic anhydride, 4mL of dry pyridine, stirred under reflux for 48h, the reaction mixture was evaporated to dryness under reduced pressure, the residue was dissolved in 150ml of saturated NaHCO 3 In aqueous solution, filter, cool the filtrate to 0°C-5°C, acidify with concentrated hydrochloric acid, extract three times with chloroform, wash the combined chloroform solution with water three times, anhydrous Na 2 SO 4 After drying, the filtrate was concentrated after removing the desiccant, and a large amount of anhydrous ether was added to precipitate the product. The product was recrystallized three times with ether, weighed after drying, and the product was 18.6g. Yield 92%.

[0022] IR (KBr, cm -1 ): 2890, 1732, 1469, 1343, 1107

[0023] In the same way, PEG-400-diacid, PEG-100...

Embodiment 2

[0033] Take 150g of PEG-6000-diacid-UA, add 20,000ml of purified water for injection, dissolve, filter, prepare 2ml / bottle, and sterilize to obtain 10,000 water injections. Each tube contains PEG-6000-dioic acid-UAl5mg.

Embodiment 3

[0035] Surface contact angle test: KRuSSDSA100 contact angle optical measuring instrument. Grinding tablet method for sample preparation, select a flat diaphragm, measure with deionized water, take the average value of three consecutive measurement errors within 0.5° as the test result.

[0036]Tab 1 Properties of UA Supported by Polyethylene Glycol

[0037] Sample No.

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Abstract

The present invention is serial hydrophilic polyglycol supported ursolic acid medicines obtained through organic synthesis and polymerization to grafting hydrophilic polyglycol onto cyclohydroxy group of ursolic acid A. The structure analysis and experiments show that activated polyglycol is grafted successfully onto ursolic acid said water insoluble ursolic acid becomes water soluble polyglycol-ursolic acid. Polyglycol-ursolic acid has excellent blood compatibility and high physiological activity, so that polyglycol supported ursolic acid medicines may be prepared into different forms, including injection, oral liquid, capsule, tablet, etc. The polyglycol has average molecular weight of 200-60,000.

Description

technical field [0001] The invention relates to the technical field of medicine, and directly grafts hydrophilic polyethylene glycol onto the carbon 3 hydroxyl group of the A ring of ursolic acid through methods such as organic synthesis and polymer polymerization to obtain a series of modified polyethylene glycols. Alcohol-supported ursolic acid new drug, using IR, 1 The structure of the product was characterized by H-NMR. At the same time, many tests such as water solubility and hemolysis were carried out. The results showed that the activated polyethylene glycol was successfully grafted onto ursolic acid, making the water-insoluble Ursolic acid became water soluble pegylated ursolic acid. And has good blood compatibility and physiological activity. Therefore, the ursolic acid series new drugs supported by polyethylene glycol can be made into oral liquids including injections, capsules, tablets and other clinically suitable dosage forms. technical background [0002] Ur...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K47/48A61K31/56A61P35/00A61K47/60
Inventor杨定菊尹述凡李颖郭彩红
OwnerSICHUAN UNIV