Anticancer composition loaded with melphalan and carmustine

Abstract

An anticancer composition carrying melphalan and carmustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from the melphalan, ifosfamide, 4H-peroxycyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of polyphosphate esters such as p(LAEG-EOP), p(DAPG-EOP) and the like, copolymer of the polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, or copolymer or polyblend of poly(erucic acid dimmer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composition is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The anticancer composition can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.

Description

(1) Technical field

[0001] The invention relates to an anticancer composition containing nitrosourea drugs and an alkylating agent, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing nitrosourea drugs and alkylating agents locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can prolong the drug release time and Can increase drug sensitivity. (2) Background technology

[0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. 参见(中国专利申请号200510042234.3,03148624.X,200510042236.2,96116041.1,97107078.4,200510042260.6,200510042261.0,200510042262.5,200510042263.X;美国专利US5651986,RE37410)。

[0003] However, the sustained-release excipients used in the above-mentioned and other existing pharmaceutical preparations more or less cause sud...