Eutectic crystal of temozolomide and baicalein as well as preparation method for eutectic crystal

A technology of temozolomide and baicalein, applied in the field of chemical medicine, to achieve the effect of improving oral half-life, simple preparation method, and improving stability
CN108623601AActive Publication Date: 2018-10-09TIANJIN UNIVERSITY OF TECHNOLOGY
3 Cites 1 Cited by

Patent Information

Authority / Receiving Office
CN Β· China
Current Assignee / Owner
TIANJIN UNIVERSITY OF TECHNOLOGY
Publication Date
2018-10-09

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention relates to eutectic crystal of temozolomide and baicalein as well as a preparation method for the eutectic crystal. Specifically, an X-ray powder diffraction pattern of the eutectic crystal has characteristic peaks with 2 theta value being 7.7 + / -0.2 degree, 8.6+ / -0.2 degree, and 12.7+ / -0.2 degree. The eutectic crystal provided by the invention has obvious advantages in stability, solubility, pharmacokinetic properties and the like of two pharmaceutical ingredients in comparison with existing temozolomide and baicalein bulk drugs, has an important value in developing drug combination of two drugs.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to the field of chemical medicine, in particular to a co-crystal of temozolomide and baicalein and a preparation method thereof. Background technique

[0002] Temozolomide (TMZ) is an alkylating agent antitumor drug containing an imidazole tetrazine ring, and its chemical name is 3,4-dihydro-3-methyl-4-oxoimidazole[5,1-d] And 1,2,3,5-tetrazine-8-carboxamide, its chemical structure is:

[0003]

[0004] Temozolomide is a prodrug and has no activity itself. It is converted into the active compound MITC (5-(3-methyltriazen-1-yl) imidazole-4-amide) by non-enzymatic pathway at physiological pH level, the latter It is further hydrolyzed into AIC (5-amino-imidazol-4-amide) and methyl diazonium ions, and then methyl diazonium ions act on the O6 and N7 sites on guanine to methylate DNA, making it impossible to combine with thymus Pyrimidine pairing produces cytotoxicity and exerts antitumor activity. The drug can pass through the blo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More