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Composition of sodium ozagrel and polyethylene glycol and preparation method thereof

A technology of ozagrel sodium and polyethylene glycol, which is applied in the field of medicine, can solve problems such as poor stability, limited dosage, and easy precipitation, and achieve improved stability in vivo, improved effectiveness, and good brain targeting Effect

Inactive Publication Date: 2010-07-21
BEIJING SIHUAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The pH value of ozagrel sodium is 8.0-9.5. It has poor stability under neutral pH conditions, is easy to precipitate, and produces isomers, which is not conducive to its long-term storage. In addition, the efficacy of its isomers is not good, thus affecting The efficacy of sodium ozagrel in the body
[0004] At the same time, as a drug acting on the brain, the permeability of the blood-brain barrier is an important factor for drug activity. The brain targeting of the existing ozagrel sodium is not ideal, and the amount of drug reaching the brain is limited, which affects its efficacy

Method used

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  • Composition of sodium ozagrel and polyethylene glycol and preparation method thereof
  • Composition of sodium ozagrel and polyethylene glycol and preparation method thereof
  • Composition of sodium ozagrel and polyethylene glycol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment O

[0060] The preparation of embodiment OJ freeze-dried powder preparation

[0061] 1. Prescription

[0062] Prescription 1:

[0063] Sodium Ozagrel 20g

[0064] PEG-40000.008g

[0065] Mannitol 4g

[0066] Add water for injection to 1000mL

[0067]

[0068] A total of 1000 bottles were made

[0069] Prescription 2:

[0070] Sodium Ozagrel 20g

[0071] PEG-4000 0.02g

[0072] Mannitol 4g

[0073] Add water for injection to 1000mL

[0074]

[0075] A total of 1000 bottles were made

[0076] Prescription 3:

[0077] Sodium Ozagrel 40g

[0078] PEG-40000.08g

[0079] Mannitol 8g

[0080] Add water for injection to 1000mL

[0081]

[0082] A total of 1000 bottles were made

[0083] Prescription 4:

[0084] Sodium Ozagrel 40g

[0085] PEG-40000.4g

[0086] Mannitol 8g

[0087] Add water for injection to 1000mL

[0088] ...

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Abstract

The invention discloses a composition of sodium ozagrel and polyethylene glycol and a preparation method thereof, belonging to the medical technical field. The weight ratio of sodium ozagrel to polyethylene glycol in the pharmaceutical composition is 1:0.002-0.1. Injections can be prepared by using the pharmaceutical composition and auxiliary material which is acceptable in pharmacy and the auxiliary material is selected from one or more of lactose, mannitol, sorbitol, dextran, citric acid-sodium citrate and sodium bicarbonate-sodium carbonate. The pharmaceutical composition is used to cure dyskinesia associated with acute thrombotic infarction and cerebral infarction.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition of sodium ozagrel and polyethylene glycol and a preparation method thereof, and the preparation of the composition for the treatment of acute thrombotic cerebral infarction and movement disorders accompanied by cerebral infarction Uses in medicine. Background technique [0002] Ozagrel Sodium (Ozagrel Sodium) is a highly effective and selective inhibitor of thromboxane synthase, through the inhibition of thromboxane A 2 (TXA 2 ) production and promote prostacyclin (PGI 2 ) to improve the imbalance between the two, and has anti-platelet aggregation and vasodilator effects. It can inhibit cerebral vasospasm, increase cerebral blood flow, improve microcirculation disorder and abnormal energy metabolism in the brain, thereby improving cerebral ischemic symptoms in patients with subarachnoid hemorrhage and ataxia in patients with cerebral thrombosis (acut...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4174A61K47/34A61K9/19A61P7/02A61P9/10A61P25/14A61K47/10
Inventor 车冯升郭维城贾中新霍彩霞孟宪慧
Owner BEIJING SIHUAN PHARMA