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Medicinal composition solution and preparation method and use thereof

A composition and drug technology, applied in the field of medicine, can solve problems such as degradation and difficulty in preparation, and achieve the effect of inhibiting lipid peroxidation, not easy to degrade, and rapid onset of action

Inactive Publication Date: 2011-02-09
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Terisravone is insoluble or insoluble in water, so it is difficult to prepare injections containing Terisravone; at the same time, Terisravone contains structures that are easily oxidized, such as aromatic amines, and is very stable in a solid state, but its aqueous solution In contact with air, it is prone to oxidation-reduction reaction and degradation

Method used

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  • Medicinal composition solution and preparation method and use thereof
  • Medicinal composition solution and preparation method and use thereof
  • Medicinal composition solution and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] In a nitrogen environment at 70°C, the antioxidant and L-arginine are dissolved in water according to the following weight ratio, and then Terisravone is added for dissolution to prepare a Terasylravone pharmaceutical composition solution, which The weight ratio is:

[0026] Teri Rabone 3g

[0027] L-Arginine 6g

[0028] Sodium thiosulfate 0.5g

[0029] Add water for pharmaceuticals to 1000ml

Embodiment 2

[0031] According to the following weight ratio:

[0032] Teri Rabone 3g

[0033] L-Arginine 6g

[0034] Sodium thiosulfate 0.5g

[0035] Add water for injection to 800ml

[0036] Add 0.5 g of sodium thiosulfate to 800 ml of water for injection at 80°C under nitrogen gas for 10 minutes, stir to dissolve, then add 6 g of L-arginine, and stir until completely dissolved. Add 3 g of Teriravone and stir until completely dissolved to obtain the pharmaceutical composition solution.

[0037] Add 1 g of activated carbon to the above-mentioned pharmaceutical composition solution, stir for 10 minutes, keep it at 70° C. for 20 minutes, and adjust the total amount to 1000 ml. The resulting solution was filtered with a membrane filter (0.45 μm in pore size) under a nitrogen atmosphere, and the pH was adjusted to 8.6 with hydrochloric acid. After the solution was clear and qualified, it was filled in an ampoule with a volume of 5 ml, replaced with nitrogen to remove air, and sterilized af...

Embodiment 3

[0045] According to the following weight ratio:

[0046] Teri Rabone 3g

[0047] L-Arginine 6g

[0048] Sodium thiosulfate 1g

[0049] Add water for injection to 800ml

[0050] Add 1.0 g of sodium thiosulfate to 800 ml of water for injection at 80° C. under nitrogen gas for 10 minutes, stir to dissolve, then add 6 g of L-arginine, and stir until completely dissolved. Add 3 g of Teriravone and stir until completely dissolved to obtain the pharmaceutical composition solution.

[0051] Add 1 g of activated carbon to the above pharmaceutical composition solution, stir for 10 minutes, keep it at 65° C. for 20 minutes, and adjust the total amount to 1000 ml. The resulting solution was filtered with a membrane filter (0.45 μm in pore size) under a nitrogen atmosphere, and the pH was adjusted to 8.6 with hydrochloric acid. After the solution was clear and qualified, it was filled in an ampoule with a volume of 5 ml, replaced with nitrogen to remove the air, and sterilized after fu...

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Abstract

The invention relates to medicinal composition solution. The medicinal composition solution comprises 2-methy-5-imido-benzo-[d][1,3] oxazine [5-b] pyrazole, arginine, an antioxidant and a solvent, wherein the weight ratio of the 2-methy-5-imido-benzo-[d][1,3] oxazine [5-b] pyrazole, the arginine, the antioxidant to the solvent is 1:0.5 to 15:0.1 to 1.5:10 to 400; and the solvent is pharmaceutical water. The medicinal composition has high water dissolubility, and is difficult to degrade under the protection of the antioxidant. The medicinal composition solution has stable injection exposure, has stable effect of inhibiting coloring change, is not hemolytic, does not separate crystal in serum out and is safe to use.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a 2-methyl-5H-benzo[d]pyrazole[5,1-b][1,3]oxamate for the treatment of cerebral apoplexy, traumatic brain injury and traumatic shock. The pharmaceutical composition solution of oxazine-5 imine and its preparation method and application. Background technique [0002] The application number is 200910129816.3 Chinese patent application "2-methyl-5-imino-benzo [d] [1,3] oxazine [5-b] pyrazole compound and its preparation method and use" (hereinafter referred to as Teriravone) discloses a compound with brain neuroprotection, Terreravone has a strong ability to scavenge oxygen free radicals, alleviates free radical damage, and inhibits lipid peroxidation. Its effective dose is 3mg / kg. Terrebone as a raw material can significantly improve the neurological deficit symptoms of cerebral ischemia-reperfusion animals in a dose-dependent manner, reduce the size of cerebral infarction, reduc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5365A61K9/08A61P25/00A61P17/02A61P9/00A61K47/18A61K47/04A61P39/06A61P9/10
Inventor 李振霞苏国强徐晓琳曹瑞山王芳牛佰慧纪存朋
Owner QINGDAO HUANGHAI PHARM CO LTD
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