Uses of deferiprone and formulation thereof in preparing medicament for preventing and treating cardiotoxicity induced by anthracyclines

A technology of cardiotoxicity and anthracyclines, which is applied in the field of medicine, can solve the problems of no reports on the development of deferiprone cardioprotective agent preparations, etc., and achieve the effects of reducing myocardial peroxidative damage, improving therapeutic index, and reducing cardiotoxicity

Inactive Publication Date: 2009-01-28
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there has been no report about the effect of deferiprone on myocardial contractility damage induced by doxorubicin in vitro and the effect on cardiotoxicity of doxorubicin in vivo; Report on formulation development

Method used

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  • Uses of deferiprone and formulation thereof in preparing medicament for preventing and treating cardiotoxicity induced by anthracyclines
  • Uses of deferiprone and formulation thereof in preparing medicament for preventing and treating cardiotoxicity induced by anthracyclines
  • Uses of deferiprone and formulation thereof in preparing medicament for preventing and treating cardiotoxicity induced by anthracyclines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Deferiprone (Deferiprone) prevents and treats cardiotoxicity in rats caused by doxorubicin (DOX)

[0057] 1.1 Establishment of doxorubicin heart failure model and dose setting of deferiprone The experiment lasted for 10 weeks, the drug was stopped at the 8th week, and the observation continued for 2 weeks. Get 72 rats, divide into 6 groups at random according to body weight, administer according to the following method:

[0058] Adriamycin group: intraperitoneal injection of 2.5 mg / kg (4.31 μmol / kg) of adriamycin, once a week, for 8 consecutive weeks.

[0059] Blank control group: intraperitoneal injection of equal volume of normal saline, 5 days a week, for 8 consecutive weeks.

[0060] Deferiprone treatment group: Different doses of deferiprone were administered 5 days a week for 8 consecutive weeks. in:

[0061] Deferiprone group 1: the treatment was the same as that of the doxorubicin group, and a low dose of deferiprone 1.71 mg / kg was given intraperito...

Embodiment 2

[0103] Accurately weigh deferiprone, lactic acid-glycolic acid copolymer (PLGA) and / or polylactic acid (PLA) according to a certain proportion, dissolve them in an appropriate amount of dichloromethane, put them in an oil bath at 37°C, and evaporate the solvent to make a self-made extruder Extrusion. After drying in a vacuum oven at room temperature to constant weight, it was cut into small rods with a diameter×length of 2mm×20mm, and the average weight of the preparation was 84.23±11.01mg to obtain the implant of the present invention.

Embodiment 3

[0105] Prevention and treatment of deferiprone biodegradable implants on cardiotoxicity induced by doxorubicin in rats

[0106] 3.1 Grouping and administration

[0107] The experiment was divided into 4 groups and lasted 30 days. Table 3 is the dosage regimen of each group.

[0108] table 3

[0109]

[0110] After administration, the general situation was observed, and the changes in body weight and survival rate were recorded. Animals that died during the experiment were weighed and dissected in time. The experiment was ended on the 30th day after administration, and the ascites volume and liver and kidney edema were recorded after the animals were sacrificed by bloodletting; the left ventricular muscle at the apex of the heart was fixed with 10% formaldehyde for pathological examination.

[0111] 3.2 Effect of deferiprone implant on the survival rate of doxorubicin-administered rats

[0112] After the implantation operation, there was no redness, swelling and exudati...

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Abstract

The invention belongs to the field of medicine, which relates to Deferiprone and a novel medicated purpose of a Deferiprone preparation, in particular to Deferiprone (1,2- dimethyl-3-hydroxide radical-4-pyridine, Deferiprone) and the application of the Deferiprone preparation in the prevention and curing of Anthracycline medicine heart toxicity. The invention researches the preventing and curing function of the Deferiprone to bandicoot heart toxicity caused by Adriamycin from the cell level, the tissue level and the whole level and prepares biodegradable type Deferiprone implant, Deferiprone troche, capsule, oral liquor and injection that can release medicine continuously. An experimental result proves that the Deferiprone and the Deferiprone preparation can not only improves the cardiac muscle shrinkage functions and protects the myocardial cell organ structure, but also complexes free iron ions directly, reduces the heart toxicity and other side and toxic effects caused by the Anthracycline medicine obviously and the mortality rate caused by the Anthracycline medicine.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new medicinal application of deferiprone and its preparation. It specifically relates to the application of deferiprone (Deferiprone) and its preparations in preventing and treating cardiotoxicity of anthracyclines. Background technique [0002] Anthracyclines play an important role in the chemotherapy of tumors and have the advantages of broad spectrum and high efficiency. Their main mechanism of action is to directly intercalate between DNA base pairs, interfere with the transcription process, prevent the formation of mRNA, and inhibit the proliferation of tumor cells. . It inhibits both DNA synthesis and RNA synthesis, so it has effects on all stages of the cell cycle, and is a non-specific drug for the cell cycle. However, the dose-cumulative cardiotoxicity of anthracyclines limits their clinical application and increases the pain and burden of patients. Taking Doxorubicin (DOX) as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4412A61K9/08A61K9/10A61K9/20A61K9/48A61P9/00A61P39/02
Inventor 陆伟跃徐凌洁何萍魏刚俸灵林
Owner FUDAN UNIV
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