Sustained-release gel injection loaded with platinum compound and alkyl agent

Abstract

A sustained-release gel injection comprises cisplatin, carboplatin, nedaplatin, oxaliplatin or satraplatin, stines, amphiphilic block copolymer and solvent. The stines are selected from carmustine, mimustine, ambnmustine, bendamustine, galamustine, fotemustine, estramustine, lomustine, semustine, SarCNU, ranimustine, tallimustine and spiromustine; the amphiphilic block copolymer is selected from glycolide-lactide copolymer and polyethylene glycol-glycolide-lactide copolymer; and the gel injection has a temperature sensitive gelatinization characteristic, isa fluid liquid at room temperature, and automatically becomes non-flowing biodegradable water insoluble gel in warm-blooded animals. The preparation can locally slowly release at tumor foci and maintain effective drug concentration for several weeks to several months; has effects on killing tumor cells, thereby effectively inhibiting tumor angiogenesis, reducing systemic toxicity of drug, and enhancing the treatment effect of chemotherapy and radiotherapy (particularly radioactive particles).

Description

A sustained-release gel injection containing platinum compounds and alkylating agents (1) Technical field The invention relates to a sustained-release gel injection loaded with a platinum compound and an alkylating agent and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "Intratumoral placement of carmustine plus systemic carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (KongQetal., JSurgOncol.1998Oct; 69 (2): 76 -82). In addition, blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma ...

AI Technical Summary

Problems solved by technology

However, the operation of solid drug implantation is more complicated and traumatic. In addition to easily causing various complications such as bleeding, infection, and decreased immunity, it can also cause or accelerate the spread and metastasis of tumors.

In addition, it is difficult to effectively and evenly contact the irregular tumor cavity by placing solid drug implants after surgery, so the therapeutic effect needs to be further improved

In addition, tumor cells have strong self-protection, regulation and repair functions. Single drug therapy may have a certain effect in the early stage, but most patients develop drug resistance during treatment or after short-term chemotherapy, and the latter is often the result of tumor treatment failure. main reason

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