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Butylphthalide- and edaravone-containing compound injection and preparation method thereof

A technology of injection and butylphthalide, which is applied in the field of medicine, can solve problems such as unadjusted dosage, elevated ALT or AST, and increased liver adverse reactions, so as to reduce the metabolic burden of the liver, reduce the dosage of the drug, and improve the quality of the liver. The effect of reducing the recurrence rate of adverse reactions

Active Publication Date: 2012-07-04
SHIJAZHUANG ZHONGSHUO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Compared with the butylphthalide soft capsule group and the edaravone group, the above-mentioned administration method did not adjust the dosage accordingly. While receiving synergistic effects in the curative effect, the adverse reactions of the liver also increased correspondingly.
[0012] The reasons for the increase of liver adverse reactions are as follows: 1. The first-pass effect of butylphthalide soft capsules is obvious when taken orally. The absolute bioavailability is about 6-7%, and the maximum is no more than 10%. For the course of treatment, the dosage is 600 mg per day, and about 550 mg of the main drug is first-pass decomposed in the liver, which will virtually increase the burden on the liver, cause liver damage and lead to an increase in ALT or AST; 2. Edaravone itself has Hepatotoxicity, as indicated in the drug instructions, the incidence of liver adverse reactions after medication exceeds 5%

Method used

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  • Butylphthalide- and edaravone-containing compound injection and preparation method thereof
  • Butylphthalide- and edaravone-containing compound injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 50g of racemic butylphthalide, 50g of edaravone, 300g of hydroxypropyl-β-cyclodextrin, 900g of sodium chloride, 20g of sodium bisulfite, 200ml of absolute ethanol.

[0036] Preparation:

[0037] Step a, inclusion:

[0038] ① Prepare the absolute ethanol solution of racemic butylphthalide for subsequent use;

[0039] ②Take 2L of water for injection, heat it to 45°C, add hydroxypropyl-β-cyclodextrin, stir to dissolve completely, then add the solution obtained in step ① at 0.5ml / min, and stir until it becomes clear and transparent without oil drops exist, then add water for injection to 80L, and the resulting solution is ready for use;

[0040] Step b, preparation of compound solution: add disodium hydrogen phosphate and sodium dihydrogen phosphate (ratio 1:1) to the solution obtained in step a, add appropriate amount of phosphoric acid to control pH4.0, then add 20g of sodium bisulfite, chloride Sodium 900g, stir to make it dissolve completely, finally add edaravone, s...

Embodiment 2

[0044] D-butylphthalide 25g, Edaravone 25g, hydroxypropyl-β-cyclodextrin 800g, sodium chloride 700g, L-cysteine ​​10g, absolute ethanol 200ml.

[0045] Preparation:

[0046] Step a, inclusion:

[0047] ①Prepare the dehydrated ethanol solution of D-butylphthalide for subsequent use;

[0048] ②Take 4L of water for injection, heat to 50°C, add hydroxypropyl-β-cyclodextrin, stir to dissolve completely, then add the solution obtained in step ① at 5ml / min, and stir until it becomes clear and transparent without oil droplets. Then add water for injection to 60L, and the resulting solution is ready for use;

[0049]Step b. Prepare compound solution: add disodium hydrogen phosphate and sodium dihydrogen phosphate (ratio 5:1) to the solution obtained in step a, add appropriate amount of phosphoric acid to control pH4.5, then add 10g of L-cysteine, Sodium chloride 700g, stir to make it dissolve completely, finally add Edaravone, stir to make it dissolve completely in the solution, the...

Embodiment 3

[0053] 50g of L-butylphthalide, 25g of Edaravone, 800g of hydroxypropyl-β-cyclodextrin, 855g of sodium chloride, 50g of acetylcysteine, 500ml of absolute ethanol.

[0054] Preparation:

[0055] Step a, inclusion:

[0056] ①Prepare the dehydrated ethanol solution of L-butylphthalide for subsequent use;

[0057] ②Take 4L of water for injection, heat to 50°C, add hydroxypropyl-β-cyclodextrin, stir until it dissolves completely, then add the solution obtained in step ① at 10ml / min, stir until it becomes clear and transparent, without oil droplets, Then add water for injection to 60L, and the resulting solution is ready for use;

[0058] Step b. Prepare compound solution: add disodium hydrogen phosphate and sodium dihydrogen phosphate (ratio 10:1) to the solution obtained in step a, add appropriate amount of phosphoric acid to control pH3.0, then add acetylcysteine ​​50g, chlorine Sodium chloride 855g, stir to make it dissolve completely, finally add Edaravone, stir to make it d...

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Abstract

The invention relates to a butylphthalide- and edaravone-containing compound injection and a preparation method thereof. The injection of every 100 ml contains 25-50 mg of active ingredient butylphthalide, 12.5-50 mg of edaravone, as well as absolute ethyl alcohol, hydroxypropyl-beta-cyclodextrin, an osmotic pressure regulator, an antioxidant and the like. With the adoption of the butylphthalide- and edaravone-containing compound injection, the administration dosage is greatly lowered, the burden of liver metabolism is reduced, and the incidence rate of liver adverse reactions is lowered. According to determination, with the adoption of the butylphthalide- and edaravone-containing compound injection, the administration dosage of the edaravone can be reduced by at least 20%, besides, the compound injection has a better curative effect, and the incidence rate of the liver adverse reactions is also remarkably lowered.

Description

technical field [0001] The invention relates to a compound drug injection and a preparation method thereof, in particular to a compound injection containing butylphthalide and edaravone and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Butylphthalide is celery seed extract, which has been artificially synthesized, including butylphthalide racemate, L-butylphthalide and D-butylphthalide. Its structure is as follows: [0003] [0004] At room temperature, butylphthalide is a yellow liquid, stable in nature, not easy to degrade, and insoluble in water. Clinical research results show that butylphthalide can improve the damage of central nervous system function in patients with acute ischemic stroke, and can promote the functional recovery of patients. Animal pharmacodynamic studies suggest that this product can block multiple pathological links of brain damage caused by ischemic stroke, has a strong anti-cerebral i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4152A61K31/365A61P9/10A61P25/00
Inventor 杨丽英田建宣刘福利赵晓雷张伟锋李志永孙丽亚李巍岳丽娜沈芳汪泳
Owner SHIJAZHUANG ZHONGSHUO PHARMA CO LTD
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