Novel crystal form for temozolomide, method for preparing temozolomide and medicinal composition of temozolomide

Abstract

The invention provides a novel crystal form for temozolomide, a method for preparing the temozolomide and a medicinal composition of the temozolomide. The novel crystal form for the temozolomide is characterized in that: Cu is used for radiation, and diffraction peaks of 2 theta represented by degrees exist at 8.2+ / -0.2 and 6.0+ / -0.2 in an X-ray diffraction pattern. The invention has the advantages that: a temozolomide crystal-shaped object which is suitable for industrialized production is provided; and the problems in the prior art are solved. The preparation process is simple and easy to operate, the industrialized production is convenient to operate, the quality is controllable, and the yield is stable. The crystal-shaped object obtained by the preparation process can remarkably improve the appearance and color and luster of products; the temozolomide M crystal-shaped object prepared by the method has high stability and can be stored for a long time; and in the method, the crystal-shaped object is prepared by using an organic solvent with lower toxicity, so the potential influence effect of the positioning of organic residue on human bodies is reduced to a certain degree. The advantages ensure that the invention is beneficial to the remarkable improvement on the quality of the products and is more suitable for industrialized production.

Description

Technical field [0001] The invention relates to a crystal form of temozolomide, a preparation method and a composition thereof, and belongs to the technical field of medicine. Background technique [0002] The chemical name of temozolomide is 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide, chemical structure: [0003] [0004] Temozolomide (trade name Temodal TM ) Was developed by M.F.G Stevens, E.S Newlands, etc., and transferred to Schering-Plough for production in 1992. It was approved under the unanimous recommendation of the European Union CPMP in October 1997, and Temozolomide capsules were marketed in Europe in 1998. In January 1999, the US FDA expert advisory group unanimously recommended that the approval of temozolomide should be accelerated and it was approved by the FDA for listing in the US on August 11, 1999. At the same time, the company has submitted listing applications to 16 countries including Canada, Australia, New Zealand, Switzerlan...

AI Technical Summary

Problems solved by technology

[0011] (2) It is difficult for a single impurity to reach less than 0.1%;

[0012] (3) The amount of solvent is large, the crystallization time is long, and the yield is low;

[0013] (4) The operation is cumbersome and requires column purification, which is not suitable for industrial production;

[0014] It is difficult to control the single impurity in the above temozolomide crystal forms below 0.1%, and it is difficult to meet the quality requirements of injection raw materials. It also fails to meet the relevant technical requirements of ICH, the EU quality research technical guidance principle, and the refined yield is also low. ,high cost

Images