Sustained-release injection containing octadecyl dimethyl-4-piperidine phosphate

Abstract

A sustained release anti-cancer injection with edelfosine consists of the edelfosine with effective anti-cancer amount and an amphiphilic block copolymer hydrogel, wherein, part or the whole of the edelfosine is encapsulated in sustained release microsphere and exists singly in the form of the sustained release microsphere or microsphere and micro-powder in the sustained release injection. The amphiphilic block copolymer hydrogel is selected from PLGA-polyethylene glycol-PLGA, sustained release gel has temperature-sensitive gelation property; and the sustained release gel is flowable fluid in an environment below body temperature, and can automatically change into biodegradable and absorbable non-flowable water-insoluble gel in bodies of warm blooded animals, thus causing the drug to be slowly released in the local part of tumor; the sustained release microsphere is favorable to the stable and sustained release of the drug, the dual sustained release is beneficial to controlling tumor cells in dormancy stage, the drug in the form of the micro-powder in the sustained release gel is favorable to the relatively quick release, thus being beneficial to controlling cells with quicker proliferation. The sustained release anti-cancer injection with edelfosine can be used together with radiotherapeutic particles, chemotherapeutic drugs, etc.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release injection, which belongs to the technical field of medicines. Specifically, the invention relates to a sustained-release gel formulation capable of stably releasing edelfosine to the local solid tumors, and it is mainly a sustained dual-release gel formulation containing sustained-release microspheres. Gel injection, the sustained-release gel preparation is an aqueous solution at room temperature, and can be transformed into a semi-solid or solid gel in warm-blooded animals. The sustained-release gel and sustained-release microspheres can slowly release edelfosine locally on the tumor for several months. (2) Background technology [0002] Phosphoinositide 3-kinase (PI3K) inhibitors have a significant inhibitory effect on the growth of a variety of tumor cells. However, the therapeutic effect of intravenous application on solid tumors is not obvious. The fundamental problem lies in traditional che...

AI Technical Summary

Problems solved by technology

Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or dissemination

In addition, organic solvents or high heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients

[0005] Solid implants cannot effectively cover the irregular tumor cavity after tumor resection, so the residual tumor cells cannot be effectively removed after surgery, and postoperative recurrence cannot be effectively controlled