Slow release injection containing mtrosourea medicament and topoisomerase inhibitor

Abstract

Disclosed is a slow release injection containing nitrosourea drugs and / or topoisomerase depressant, which comprises slow release microspheres and dissolvent, the slow release microspheres include nitrosourea drugs selected from Nimustine, Carmustine, and / or topoisomerase depressant anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, PLGA and poly(dodecanedioic acid-tetradecanedioic acid), the topoisomerase depressant is selected from camptothecine, monohydric camptothecine, Topotecan, Lartotecan, Irinotecan, Etoposide or Teniposide, the anticancer composition can also be prepared into slow release implanting agent for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Description

(1) Technical field

[0001] The invention relates to a slow-release injection containing nitrosourea drugs and topoase inhibitors and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology

[0002] As a class of commonly used chemotherapeutic drugs, nitrosourea drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs.

[0003] 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 camptothecin plus systemic camptothecin in the treatment of brain tumors in rats" "Journ...