Polyasparagine-L-arginine and preparation method and medical application thereof

A technology of polyaspartic acid and arginine is applied in the application of polyaspartic acid-L-arginine as an antithrombotic agent, in the field of polyaspartic acid-L-arginine, which can solve the Amino acid blends don't have issues like exact doses

Inactive Publication Date: 2011-07-27
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In other words, a mixture of polyasparagine conta

Method used

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  • Polyasparagine-L-arginine and preparation method and medical application thereof
  • Polyasparagine-L-arginine and preparation method and medical application thereof
  • Polyasparagine-L-arginine and preparation method and medical application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1 Heating and decompression method prepares the polysuccinimide that chain length is 59

[0031] 5 g of finely ground DL-aspartic acid, 2 ml of phosphoric acid (85%) and 2 ml of distilled water were mixed thoroughly in a 250 ml round bottom flask. The reaction mixture was reacted under reduced pressure in an air bath at 180°C for 2.5 hours, and then 20ml of DMF was added to it while it was still hot. After the solution became clear, it was dropped into 100ml of distilled water. The precipitate was collected, washed neutral with distilled water, and dried to yield 3.4 g (93.4%) of the title compound. Elemental analysis (C 4 h 3 NO 2 ) n : C, 46.76; H, 3.35; N, 13.64.

Embodiment 2

[0032] Embodiment 2 Azeotropic water removal method prepares polysuccinimide with a chain length of 59

[0033] A suspension of 50 g of finely ground DL-aspartic acid and 500 ml of tetralin (chemical alcohol) was refluxed for 100 hours, and the generated water was removed through a water separator. After the reaction mixture was cooled to room temperature, it was filtered, and the filter residue was washed with ether first, and then washed with saturated NaHCO 3 Wash with aqueous solution (3 x 100ml). The filter cake was washed repeatedly with water and dilute hydrochloric acid (1%), and finally washed repeatedly with distilled water until AgNO 3 Cl cannot be detected - . The filter cake was dried to yield 16 g (44%) of the title compound. Elemental analysis (C 4 h 3 NO 2 ) n : C, 45.24; H, 3.85; N, 13.30.

Embodiment 3

[0034] Embodiment 3 melting method prepares the polysuccinimide that chain length is 59

[0035] 30g of finely ground DL-aspartic acid was evenly spread on the bottom of a vessel with a diameter of 30cm, heated at 200°C for 3 hours, and the reaction product was orange-red. After the reactant was cooled, the saturated NaHCO 3After triturating with aqueous solution (3×100ml), the obtained solid was repeatedly washed with distilled water, centrifuged, and the precipitate was dried to obtain 5 g (17%) of the title compound. Elemental analysis: (C 4 h 3 NO 2 ) n : C, 46.63; H, 3.33; N, 13.63.

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Abstract

The invention discloses polyasparagine-L-arginine and a preparation method and medical application thereof. In the invention, arginine serves as a pharmacophore, polyaspartic acid serves as a medicine loading system, and the arginine and the polyaspartic acid are bonded to form the polyasparagine-L-arginine with the chain length of 59. An in-vivo/in-vitro antithrombotic model experiment shows that: the polyasparagine-L-arginine compound has accurate antithrombotic activity.

Description

technical field [0001] The present invention relates to polyasparagyl-L-arginine with a chain length of 59, and the present invention also relates to a preparation method of the polyasparagine-L-arginine and the polyasparagine-L-arginine The application as an antithrombotic agent belongs to the field of polyamino acid compounds. Background technique [0002] Polyamino acid compounds generally show low toxicity, high biocompatibility, easy degradation and metabolites can be absorbed by the body. These advantages make polyamino acid compounds attract attention as high-molecular pharmaceutical materials. For example, the drug release system prepared by various derivatization reactions of polyaspartic acid carboxyl side chains, especially the control or targeting of antitumor drugs covalently bonded with polyaspartic acid and daunorin or methotrexate attention due to its low toxicity. The inventor once covalently bonded L-arginine to the carboxyl group of polyaspartic acid to...

Claims

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Application Information

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IPC IPC(8): C08G69/48C08G69/10A61K31/785A61P7/02
Inventor 彭师奇赵明桂琳
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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