Taxane medicines albumin nanoparticle preparation for injection and preparation method thereof

Abstract

The invention belongs to the field of medicinal preparation, and relates to taxane medicines albumin nanoparticle preparation for injection and a preparation method of the preparation. According to the invention, the albumin nanoparticle preparation is prepared by combining the albumin with the taxane medicines to form the albumin nanoparticles by dispersing and stabilizing with the phospholipid. According to the invention, the strengthened osmosis and retention effect on the tumors by the nanoparticles are utilized, and more medicines are passively targeted and concentrated on the tumor tissues so as to improve the antitumor effect; simultaneously, due to the fact that the bioavailability in the injection way is high and the soluble albumin nanoparticle preparation for injection exists passive targeting, the administration dose can be greatly reduced, so that the medicinal concentration on the non-target parts can be effectively reduced, the toxic and side effects of the medicines can be reduced, and the good clinical application prospect can be implemented. The preparation is convenient in preparation method and is suitable for industrial mass production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an albumin nanoparticle preparation of taxane drugs for injection and a preparation method thereof. Background technique [0002] In recent years, the incidence of tumor has risen sharply, and its treatment is difficult and its mortality rate is high. It has become the second leading cause of human death. According to reports, about 6 million people die of malignant tumors in the world every year, among which about 4.5 million cancer patients in China, the mortality rate exceeds 30%, which has become a serious social problem. At present, surgery, chemotherapy, and radiotherapy are usually used in the clinical treatment of malignant tumors; for early-stage tumors, surgical resection combined with other therapies can often achieve better therapeutic effects; The development of the disease is accompanied by severe immune system suppression or toxic side effects, and it is d...

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Problems solved by technology

[0004] At present, although taxanes have good anti-tumor effects, the treatment practice shows that they still have the following defects: (1) Because the drug is poorly soluble in water (paclitaxel has a solubility of 0.0005mg / mL in water at room temperature, docetaxel Almost insoluble in water)), clinically used injections all need to add a large amount of surfactants, such as paclitaxel using CremophorEL to help dissolve, docetaxel using Tween 80 to help dissolve, etc., resulting in relatively large toxic side effects of the injection in clinical application, easy to Cause complications, such as allergic reaction, bone marrow suppression, neurotoxicity, cardiovascular toxicity, hair loss, etc.; (2) Due to the rapid distribution and metabolism of the drug after entering the body, the blood drug concentration decreases rapidly, which requires frequent administration and long-term (3) Since the drug is a cytotoxic drug and has no targeting, the drug is distributed throughout the body after conventional injection administration, resulting in systemic toxic and side effects. However, there is no attempt to modify its structure to reduce adverse reactions. Greater progress

[0013] So far, the basic and applied basic research on taxane drugs has mainly focused on their targeting research as a model drug and the research on drug combination. Literature report

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