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Hirudin polyion micelle composition of targeted platelet

A technology of polyion and composition, which is applied in the direction of drug combination, blood disease, drug delivery, etc., and can solve the problems of changing the chemical composition of drugs and high production costs

Inactive Publication Date: 2013-07-10
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the production cost of the above method is extremely high, and the original chemical composition of the drug is changed.

Method used

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  • Hirudin polyion micelle composition of targeted platelet
  • Hirudin polyion micelle composition of targeted platelet

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the preparation of injection

[0023] Dissolve 16mg of RGD-PEG-CS in 10ml of acetic acid-sodium acetate buffer solution at pH 4.9, add 10ml of hirudin solution with a concentration of 0.2mg / mL under electromagnetic stirring, stir for 30min, and then add 5ml of hirudin solution with a concentration of 1.1mg / mL dropwise. Sodium phosphate aqueous solution, sealed and stirred for 30min. Filter with a 0.45 μm filter to obtain the platelet-targeted hirudin-polyethylene glycol-grafted chitosan polyion micelles composition.

[0024] An appropriate amount of benzyl alcohol aqueous solution is added to the obtained composition, mixed evenly, filtered, potted and sterilized by radiation.

Embodiment 2

[0025] Embodiment 2: the preparation of freeze-dried powder injection

[0026] Dissolve 32mg of RGD-polyethylene glycol grafted chitosan in 10ml of acetic acid-sodium acetate buffer solution with a pH of 4.8, add 10ml of a hirudin solution with a concentration of 0.5mg under electromagnetic stirring, and add 4mL of a solution with a concentration of 1.5mg after stirring for 45min. mg / mL sodium tripolyphosphate aqueous solution, sealed and stirred for 40min. Filter with a 0.45 μm filter to obtain the platelet-targeted hirudin-polyethylene glycol-grafted chitosan polyion micelles composition.

[0027] Add appropriate amount of glucose and mannitol into the obtained micelle composition, mix uniformly, freeze-dry, seal and sterilize by radiation.

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Abstract

The invention relates to a hirudin polyion micelle composition of a targeted platelet. The compound contains hirudin, arginine-glycine-aspartic acid-polyethylene glycol grafted chitosan and a polyion initiator. The polyion micelle composition can be prepared by a simple method, has platelet targeting, enhances the hirudin anticoagulation and the thrombus proofing activity, effectively suppresses the platelet aggregation and obviously improves the partial thromboplasting time of plasma.

Description

technical field [0001] The present invention relates to a polyionic micellar composition of arginine-glycine-aspartic acid-polyethylene glycol-chitosan (RGD-PEG-CS) loaded with hirudin targeting platelets for injection and its preparation method. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the three major fatal diseases, among which thromboembolism is the cause of many cardiovascular and cerebrovascular diseases. Due to the induction of arteriosclerosis, vascular endothelial injury, abnormal internal and external coagulation system, or abnormal hemodynamics, the components in the blood flow process form a semi-clot-like substance on the surface of the blood vessel or the intima of the heart, which is a thrombus. Aiming at various mechanisms of thrombus formation, a variety of antithrombotic drugs have come out one after another, including drugs that inhibit thrombosis (anticoagulant and antithrombotic) and platelet aggregation (antip...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K38/58A61K47/36A61P7/02
Inventor 刘艳李馨儒周艳霞王菲
Owner PEKING UNIV
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