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Regadenoson injection and preparation method thereof

A technology of Reganoson and injection, which is applied in the field of Reganoson injection and its preparation, can solve the problems of reducing blood calcium ions, etc., achieve the effects of reducing irritation, improving sterility, and ensuring smooth progress

Active Publication Date: 2016-10-12
NANJING HERON PHARMA SCI & TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the electronic journal of the Center for Drug Evaluation has revealed that edetate disodium in injections has the risk of reducing blood calcium ions

Method used

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  • Regadenoson injection and preparation method thereof
  • Regadenoson injection and preparation method thereof
  • Regadenoson injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Reganoson Injection (0.4mg / 5mL), 5000 vials

[0062] Prescription: Reganoson 2g, histidine 300g, L-cysteine ​​50g, tris 165g, sodium chloride 225g, hydrochloric acid to adjust the pH to 7.4, water for injection to 25L.

[0063] Preparation:

[0064] (1) Under the protection of nitrogen, dissolve histidine and L-cysteine ​​in an appropriate amount of water for injection at 65°C to make a concentrated solution with a cosolvent content of 30% (w / w), and slowly add Regano (2) Slowly lower the temperature to 45°C-50°C, add tris to dissolve, then add 70% of the prescribed amount of water for injection to dilute;

[0065] (3) Cool to 25±2°C, add sodium chloride, adjust the pH to 7.4 with hydrochloric acid, and make up the water for injection to the full amount;

[0066] (4) Use a 5000MW membrane ultrafilter to filter the medicinal solution to remove pyrogens, collect the ultrafiltrate, and then pass it through a 0.22μm polyethersulfone filter element for fine filtr...

Embodiment 2

[0069] Example 2 Reganoson Injection (0.4mg / 5mL), 5000 vials

[0070] Prescription: Reganoson 2g, histidine 400g, arginine 50g, tris 170g, sodium bisulfite 30g, sodium chloride 225g, hydrochloric acid to adjust the pH to 7.4, water for injection to 25L.

[0071] Preparation:

[0072] (1) Under the protection of nitrogen, dissolve histidine and arginine in an appropriate amount of water for injection at 65°C to make a concentrated solution with a cosolvent content of 30% (w / w), add sodium bisulfite to dissolve, and then Slowly add Reganosen, keep stirring to make it completely dissolved;

[0073] (2) Slowly lower the temperature to 45°C-50°C, add tris to dissolve, then add 70% of the prescribed amount of water for injection to dilute;

[0074] (3) Cool to 25±2°C, add sodium chloride, adjust the pH to 7.4 with hydrochloric acid, and make up the water for injection to the full amount;

[0075] (4) Use a 5000MW membrane ultrafilter to filter the medicinal solution to remove pyr...

Embodiment 3

[0078] Example 3 Reganoson Injection (0.4mg / 5mL), 5000 vials

[0079] Prescription: Regganosan 2g, histidine 400g, glycine 50g, tris 170g, sodium metabisulfite 35g, sodium chloride 225g, hydrochloric acid to adjust the pH to 7.4, water for injection to 25L.

[0080] Preparation:

[0081] (1) Under the protection of nitrogen, dissolve histidine and glycine in an appropriate amount of water for injection at 60-70°C to make a concentrated solution with a cosolvent content of 30% (w / w), add sodium metabisulfite to dissolve, and then slowly add Reginaosheng, keep warm and stir to make it completely dissolved;

[0082] (2) Slowly lower the temperature to 45°C-50°C, add tris to dissolve, then add 70% of the prescribed amount of water for injection to dilute;

[0083] (3) Cool to 25±2°C, add sodium chloride, adjust the pH to 7.4 with hydrochloric acid, and make up the water for injection to the full amount;

[0084] (4) Use a 5000MW membrane ultrafilter to filter the medicinal solu...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a novel injection of an adenosine A2A receptor agonist Regadenoson and a preparation method of the injection. The Regadenoson injection is prepared from the main drug Regadenoson, a cosolvent, an antioxidant, a stabilizer and an isoosmotic adjusting agent, wherein the cosolvent is selected from L-histidine or a combination of L-histidine and other amino acid, the stabilizer is selected from a combination of tris-hydroxymethyl aminomethane and hydrochloric acid, and sodium chloride is preferably selected as the isoosmotic adjusting agent. According to the injection, propylene glycol and phosphate buffer salt are prevented from being used, a surfactant solubilizer is not adopted, the formula and the process are simple, the injection is suitable for industrialized large-scale production, and the stability is significantly improved after high-temperature sterilization and long-term storage.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a Reganoson injection and a preparation method thereof. Background technique [0002] Regadenoson, chemical name 1-(6-amino-9-((2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran ring-yl)- 9H-purin-2-yl)-N-methyl-1H-pyrazole-4-carboxamide monohydrate, the structure is shown below, [0003] . [0004] Regadenoson (trade name Lexiscan) is a selective adenosine receptor agonist developed by CV Therapeutics, which can relax coronary arteries. This drug is used for radionuclide myocardial perfusion imaging in patients who cannot undergo exercise stress testing. Clinicians also use it for CT imaging beyond the applicable disease. [0005] Reganosen drug instructions published by the US FDA show that, in addition to the main drug Reganoson and water for injection, it also contains propylene glycol, sodium dihydrogen phosphate, disodium hydrogen phosp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/52A61K47/18A61K47/22A61K47/34A61K47/26A61K47/02A61P9/10G01N30/02
CPCA61K9/0019A61K9/08A61K31/52A61K47/02A61K47/10A61K47/18A61K47/183A61K47/22A61K47/26G01N30/02G01N2030/027
Inventor 包玉胜闵涛柏丹丹李阳史翔
Owner NANJING HERON PHARMA SCI & TECH CO LTD
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