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Edaravone composition for injection

A technology of edaravone and its composition, which is applied in the field of pharmaceuticals and pharmaceutical manufacturing, can solve the problems of low absolute bioavailability, short maintenance time in the body, and strong first-pass effect, so as to improve bioavailability and reduce first-pass effect, the effect of enhancing the therapeutic effect

Inactive Publication Date: 2013-09-18
HAINAN WEI KANG PHARMA QIANSHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although MT has a variety of physiological functions and pharmacological effects, it has unstable oral absorption kinetics, rapid distribution and clearance, and t 1 / 2 Short (30-50min), large individual differences, strong first-pass effect, low absolute bioavailability (1%-37%), and short maintenance time in vivo (1-3h)

Method used

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  • Edaravone composition for injection
  • Edaravone composition for injection
  • Edaravone composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Embodiment 1, the preparation of edaravone composition freeze-dried powder for injection, in 1000

[0019] prescription

[0020]

[0021] 2. Preparation process

[0022] a) Add 5g of L-cysteine ​​hydrochloride-hydrate to 1500ml of water for injection, stir and add 30g of edaravone to dissolve, then add 0.6g of melatonin and stir evenly;

[0023] b) Add 1.8g of melatonin and 8.79g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 6 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0024] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 4.1, add 0.1% activated carbon and stir for 30 minutes to filter out the activated carbon, and then filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect the content of intermediates , according to Edaravone, 30mg per bottle;

[0025] d) Fill according to the test requiremen...

Embodiment 2

[0026] Embodiment two, the preparation of edaravone composition freeze-dried powder for injection, in 1000

[0027] 1. Prescription

[0028]

[0029] 2. Preparation process

[0030] a) Add 30g of Edaravone into 1500ml of water for injection and stir to dissolve, then add 1g of melatonin and stir evenly;

[0031] b) Add 3g of melatonin and 14.66g of moderately substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 6 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0032] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 4.1, add 0.1% activated carbon and stir for 30 minutes to filter out the activated carbon, and then filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect the content of intermediates , according to Edaravone, 30mg per bottle;

[0033] d) Fill according to the test requirements, put it into a freeze dryer after half-...

Embodiment 3

[0034] Embodiment three, the preparation of edaravone composition freeze-dried powder for injection, in 1000

[0035] 1. Prescription

[0036]

[0037] 2. Preparation process

[0038] a) Add 30g of Edaravone to 1500ml of water for injection and stir to dissolve, then add 0.8g of melatonin and stir evenly;

[0039] b) Add 2.4g of melatonin and 11.73g of medium-substituted hydroxypropyl-β-cyclodextrin into 500ml of water for injection, stir at 50°C for 5 hours, and detect that the encapsulation rate of melatonin is greater than 90%;

[0040] c) After mixing the solutions of groups a and b above, add HCL solution to adjust the pH value to 4.1, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect intermediates Content, according to Edaravone, 30mg per bottle;

[0041] d) Fill according to the test requirements, put it into a freeze dryer after half-tamping, cool d...

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Abstract

The invention provides an edaravone composition for injection, and relates to the technical field of medicine manufacturing. The main medicine of the composition comprises edaravone and melatonin, wherein the melatonin comprises a quick release part and a cyclodextrin-included slow release part. According to the edaravone composition for injection provided by the invention, the therapeutic effect of edaravone is improved, instability caused by oral administration of MT (Melatonin) is avoided and MT is quick to distribute and eliminate and the like, and the first pass effect of MT is reduced. The dosage of edaravone is reduced, and the side effect of edaravone is reduced. The design of dosage combining quick release and slow release is in accordance with secretion characteristic of MT, so that the problem of half-life period of MT is solved and the bioavailability of a product is improved. The melatonin combined with edaravone acted on nerve cells has the synergistic effect of preventing encephaledema, reducing the infarct volume and improving the neurological function.

Description

Technical field: [0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to an edaravone composition for injection, and more specifically, to a freeze-dried composition for injection containing edaravone and melatonin. Background technique: [0002] In 2001, Edaravone was approved for marketing in Japan. It is currently the only brain protective agent that has been proven to have clinical efficacy. clinical treatment effect. Edaravone is a brain protectant (free radical scavenger). The new free radical scavenger Edaravone generates Edaravone groups by transferring an electron to free radicals to break the lipid peroxidation reaction chain. Protect nerve cells. At present, a large number of animal experimental studies have proved that edaravone has the effects of scavenging free radicals, anti-brain edema, reducing infarct volume and improving neurological function in experimental cerebral infarction, and has the effect on vas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4152A61K9/19A61K47/48A61P25/00A61P25/28A61P11/00A61K31/4045
Inventor 汪六一汪金灿郝结兵李彪吴函峰
Owner HAINAN WEI KANG PHARMA QIANSHAN
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