Liquid micellar preparation for increasing active closed-loop rate of camptothecin derivatives as well as preparation method and applications of preparation

Abstract

The invention belongs to the technical field of drugs, and in particular relates to a liquid micellar preparation for increasing the active closed-loop rate of camptothecin derivatives as well as a preparation method and applications of the preparation. The preparation disclosed by the invention is prepared from a amphiphilic copolymer, medicament molecules and an aqueous medium, wherein the amphiphilic copolymer is taken as a carrier material, the medicament molecules of active-dose camptothecin derivatives are physically loaded in a micellar form, and the aqueous medium is taken as a main dissolvent. The main body structure of the carrier material takes polyethylene glycol as a hydrophilic segment and takes polyester, poly-amino acid or polyether as a hydrophobic segment, and the medicament molecules are one or more of camptothecin, 10-hydroxycamptothecine, 9-nitrocamptothecin, 9-aminocamptothecin, 7-ethyl-10-hydroxycamptothecine, Topotecan, Irinotecan, Rubitecan, Exatecan, Belotecan, Karenitecin, Chimmitecan, Gimatecan, and the like. The micellar preparation can significantly improve the active closed-loop rate of the camptothecin medicament, enhances the medicament effect, and can effectively reduce the general reaction of the medicament, and therefore, the preparation is expected to be used in the cancer treatment of different stages.

Description

technical field

[0001] The invention belongs to the technical field of medicines, and in particular relates to a micellar preparation capable of increasing the active ring-closing rate of camptothecin derivatives, a preparation method and application thereof. Background technique

[0002] Camptothecin is an active molecule of anticancer drugs isolated from camptotheca in our country in the 1960s. Due to its poor water solubility and high toxicity and side effects, some functional groups are usually modified on active non-sensitive sites to improve drug efficacy and water solubility. At present, two camptothecin derivatives, irinotecan (CPT-11) and topotecan (Topotecan) have been approved by the State Food and Drug Administration for clinical use, and have been widely used in gastric cancer, esophageal cancer, and pancreatic cancer. and colon cancer treatment. But almost all camptothecin drugs are facing a serious problem - the instability of their own structure. as attach...

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