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Sustained-release pro-drug with ibuprofen loaded by polylactic acid bonds, method for preparing sustained-release pro-drug by means of direct melt co-polymerization and application of sustained-release pro-drug

A polylactic acid, melt polycondensation technology, applied in pharmaceutical formulations, antipyretics, medical science and other directions, to achieve the effect of simple preparation technology and strong inhibitory activity

Active Publication Date: 2017-06-09
SOUTH CHINA NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In view of this, the present invention uses lactic acid and ibuprofen as raw materials, and has prepared a polylactic acid bond-loaded ibuprofen sustained-release prodrug through a simple and easy direct melt copolymerization method, which has expected biological activity, and these results have not been reported

Method used

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  • Sustained-release pro-drug with ibuprofen loaded by polylactic acid bonds, method for preparing sustained-release pro-drug by means of direct melt co-polymerization and application of sustained-release pro-drug
  • Sustained-release pro-drug with ibuprofen loaded by polylactic acid bonds, method for preparing sustained-release pro-drug by means of direct melt co-polymerization and application of sustained-release pro-drug
  • Sustained-release pro-drug with ibuprofen loaded by polylactic acid bonds, method for preparing sustained-release pro-drug by means of direct melt co-polymerization and application of sustained-release pro-drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Synthesis of Sustained-release Prodrug of Ibuprofen Supported by Polylactic Acid

[0038] (1) Use D, L-LA and ibuprofen as raw materials, mix evenly according to the ratio of substances n(D, L-LA):n(ibuprofen)=120:1, after 140°C, 4000Pa, 8h The intermediate is obtained after the pre-polymerization and water removal treatment;

[0039] (2) Add catalyst SnO (mass percentage is 0.3% of the intermediate), melt and polycondense at a temperature of 160°C and a pressure of 70Pa for 6h; Lactic acid bond loaded ibuprofen sustained-release prodrug;

[0040] The structure of the product was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography, and the measured intrinsic viscosity [η] = 1.113dL / g. The product structure data are characterized as follows:

[0041] Infrared spectrum related data: 3525.87, O-H stretching vibration absorption peak; 3180.65, C-H stretching vibra...

Embodiment 2

[0044] Synthesis of Sustained-release Prodrug of Ibuprofen Supported by Polylactic Acid

[0045] (1) Use D, L-LA and ibuprofen as raw materials, mix evenly according to the ratio of substances n(D, L-LA):n(ibuprofen)=120:1, after 140°C, 4000Pa, 8h The intermediate is obtained after the pre-polymerization and water removal treatment;

[0046] (2) Add catalyst ZnCl 2 (mass percentage is 0.3% of the intermediate), melting and polycondensation at a temperature of 160° C. and a pressure of 70 Pa for 6 hours; after the reaction, the product was dissolved in chloroform at room temperature, purified by methanol precipitation, and vacuum-dried to obtain a white powder polylactic acid bond-loaded ibuprofen Extended-release prodrugs.

[0047] In the same way as in Example 1, the structure of the product was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography, and the measured intr...

Embodiment 3

[0049] Synthesis of Sustained-release Prodrug of Ibuprofen Supported by Polylactic Acid

[0050] (1) Use D, L-LA and ibuprofen as raw materials, mix evenly according to the ratio of substances n(D, L-LA):n(ibuprofen)=120:1, after 140°C, 4000Pa, 8h The intermediate is obtained after the pre-polymerization and water removal treatment;

[0051] (2) Add catalyst SnO (mass percentage is 0.9% of the intermediate), melt and polycondense at a temperature of 160°C and a pressure of 70Pa for 6h; Lactic acid bond loaded ibuprofen sustained release prodrug.

[0052] In the same way as in Example 1, the structure of the product was confirmed by polymer characterization methods such as infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, and gel permeation chromatography, and the measured intrinsic viscosity [η]=0.375dL / g.

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Abstract

The invention discloses a sustained-release pro-drug with ibuprofen loaded by polylactic acid bonds, a method for preparing the sustained-release pro-drug by means of direct melt co-polymerization and application of the sustained-release pro-drug. The method includes steps of (1), mixing lactic acid and the ibuprofen with each other and carrying out pre-polymerization and dehydration treatment to obtain intermediates; (2), carrying out melt condensation polymerization on the obtained intermediates under the effects of catalysts, dissolving and precipitating reaction products and drying the reaction products under vacuum conditions to obtain the sustained-release pro-drug with the ibuprofen loaded by the polylactic acid bonds. The sustained-release pro-drug, the method and the application have the advantages that the sustained-release pro-drug with the ibuprofen loaded by the polylactic acid bonds is good in biological activity and is particularly excellent in antibacterial performance for Escherichia coli, staphylococcus aureus, candida albicans and the like; the method includes simple processes and is economical and practical; the sustained-release pro-drug with the ibuprofen loaded by the polylactic acid bonds can be used for preparing antibacterial drugs, anti-inflammatory drugs or anti-inflammatory dressing.

Description

technical field [0001] The invention relates to the field of sustained-release prodrug preparation, in particular to a polylactic acid-bonded ibuprofen sustained-release prodrug and its preparation method and application. Background technique [0002] Ibuprofen is a very important class of non-steroidal drugs clinically. It has anti-inflammatory, analgesic, and antipyretic effects, and can be used to treat rheumatoid arthritis, ankylosing spondylitis, and neuritis. However, due to the existence of disadvantages such as poor solubility and short half-life, it is urgent to develop ibuprofen sustained-release system to improve drug efficacy. [0003] Polymer-bonded drugs can achieve sustained release of drugs by breaking chemical bonds, which can improve the above shortcomings, improve the stability and effective utilization of drugs, and fully realize the targeted delivery of drugs to reduce the pain of patients. Therefore, polymer-bonded drugs have recently become a research...

Claims

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Application Information

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IPC IPC(8): A61K47/59A61K31/192C08G63/78C08G63/08A61P29/00A61P31/04A61P31/10A61L15/26A61L15/44
CPCA61L15/26A61L15/44A61K9/0002A61K31/192C08G63/08C08G63/78A61L2300/404A61L2300/41A61L2300/602A61L2300/21C08L67/04Y02A50/30
Inventor 汪朝阳罗时荷王群芳
Owner SOUTH CHINA NORMAL UNIVERSITY
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