Preparation and application of novel antithrombotic polymer nano-drug

Abstract

The invention relates to a novel antithrombotic polymer nano-drug. The novel antithrombotic polymer nano-drug is prepared by connecting a hydrophobic antithrombotic substance with a hydrophilic antithrombotic substance by means of a simple chemical reaction; the novel antithrombotic polymer nano-drug can be separately used as a polymer nano-drug, and can be also prepared into a polymer nano-drug composition by being physically coated with other pharmaceutically active or pharmacologically active molecules so as to improve the antithrombotic activity of the pharmaceutically active or pharmacologically active molecules. The antithrombotic polymer nano-drug not only improves the water solubility and stability of the hydrophobic antithrombotic substance, prolongs the action time of the hydrophobic antithrombotic substance and increases the concentration of the drug reaching the part with thrombus, but also reduces the bleeding risk of heparin of the hydrophilic antithrombotic substance and derivatives thereof and realizes the cooperative utilization of two different action mechanisms, thus giving play to higher antithrombotic activity. By adding corresponding medical auxiliary materials, the antithrombotic polymer nano-drug and a composition thereof can be prepared into corresponding preparations used for injection, oral administration or ophthalmic drug delivery. The preparation method of the novel antithrombotic polymer nano-drug is simple and lower in cost, thus being suitable for large-scale continuous production.

Description

technical field [0001] The invention relates to the preparation and application of a novel antithrombotic polymer nano drug. Background technique [0002] Diseases that seriously endanger human health, especially the eyes, heart and brain, and blood vessels of the elderly, are closely related to thrombosis. After entering the 21st century, thrombosis has become the world's largest cause of death, and thrombosis is a group A multifactorial change process in which genetic and environmental factors interact and influence each other. The main characteristics of common clinical thrombosis patients are familial heredity, recurrence, severity of symptoms, abnormal thrombosis site, and younger onset time. [0003] The formation of thrombus is generally the cause or complication of various diseases, such as blindness, pulmonary thromboembolism, atherosclerosis, coronary heart disease, cerebrovascular disease, deep vein embolism after surgery or trauma, etc. Among them, fundus venou...

AI Technical Summary

Problems solved by technology

However, the existing antithrombotic drugs still have one or another problem in terms of safety, such as the side effects of the following four typical antithrombotic drugs: ① antiplatelet drug aspirin, adverse reactions mainly include bleeding, gastrointestinal irritation And diarrhea, rash, etc., especially when large doses are required, the side effects are more obvious and inevitable

②Urokinase and other traditional thrombolytic drugs are more likely to cause bleeding complications and cause adverse reactions in the skin, spirit, blood, cardiovascular, urinary and other systems

Especially anticoagulant antithrombotic drugs, bleeding side effects are more prominent, ③ warfarin, the most important oral anticoagulant drug, but its adverse reactions are easily affected by many factors, such as drugs, diet, environment, genetics, and disease status Both will interfere with the efficacy of warfarin, and its dosage and bleeding adverse reactions are closely related to genetic factors, so individual differences are relatively large

④Heparin, a typical anticoagulant drug, acts through anticoagulant factors II and Xa to inhibit the formation of thrombus, but it is very easy to cause bleeding side effects, so it is generally only used as an auxiliary drug for antithrombotic therapy

However, there are significant differences between the LMWH prophylaxis and postoperative DVT control groups produced by various manufacturers, so the dosage should be different for each drug.

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