Decataxel self-microemulsifying composition and preparation method thereof

Abstract

The invention belongs to the field of medicinal preparations, and relates to a decataxel self-microemulsifying composition for injection and a preparation method thereof. The decataxel self-microemulsifying preparation comprises the following components by weight percentage: 1 to 20 percent of decataxel, 5 to 60 percent of oil phase, 10 to 90 percent of emulsifier, 1 to 30 percent of coemulsifier, and 0 to 10 percent of additive. The preparation method comprises the following steps: mixing the decataxel, the oil phase, the emulsifier, the coemulsifier and a stabilizer; performing ultrasonic treatment; stirring the mixture at a temperature of between 20 and 80 DEG C to ensure that the mixture is completely dissolved; and mixing evenly to obtain the composition. The self-microemulsion can be directly used and can also be diluted into products of any steady concentration to use by adding the moisture in any proportion. The composition reaches a human body through injection or oral administration, can spontaneously form a microemulsion with nanometer particle size when encountering body fluid, obviously improve the solubility of medicaments, increase the stability of the medicaments, and improve the bioavailability. The composition has the advantages of simple preparation process, high production efficiency, steady product quality, and easy industrialized large-scale production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a docetaxel self-microemulsion composition and a preparation method thereof. Background technique [0002] Docetaxel (docetaxel) is a new generation of taxane antineoplastic drugs developed in recent years. It is a mitosis inhibitor. Docetaxel is a semi-synthetic new antitumor drug. It is suggested that docetaxel can inhibit the growth of SPC Al lung adenocarcinoma cells, and the inhibitory effect is enhanced with the increase of the dose, which is related to the drug-induced cell GZM phase arrest. Studies on Lewis lung cancer in vivo have shown that docetaxel inhibits the growth of tumor tissue by inducing G2M phase arrest and apoptosis in Lewis lung cancer cells. The mechanism of action of docetaxel is similar to that of paclitaxel, but its antitumor activity is 1.3 to 12 times that of paclitaxel, and it has obvious curative effects on breast cancer, non-small cell lun...

AI Technical Summary

Problems solved by technology

[0003] Docetaxel is poorly soluble in water. Even if it is prepared as an injection, it has relatively large toxic and side effects in clinical application and is likely to cause more complications, such as allergic reactions, bone marrow suppression, neurotoxicity, cardiovascular toxicity, hair loss, etc. , while the drug metabolizes rapidly in the body, long-term use is required

Attempts to modify its structure to reduce adverse effects have not made much progress so far

[0004] At present, docetaxel is mainly prepared from Tween 80 and ethanol, etc., which have toxic and side effects on the human body after injection. Especially before using docetaxel injection, you must first take anti-allergic drugs or inject anti-allergic drugs to help Relieve the severe allergies and other toxic and side effects caused by

Images