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Crystal form of 7-ethyl-10-hydroxycamptothecin and its preparation method and application
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A technology of hydroxycamptothecin and crystal form, which is applied in the field of medicinal chemistry and can solve the problem of low solubility of polymorphs
Active Publication Date: 2016-06-15
SHANDONG UNIV
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However, the polymorphic form of 7-ethyl-10-hydroxycamptothecin is not very soluble
Method used
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Embodiment 1
[0057] Examples 1-5 are the preparation of crystalline form II of 7-ethyl-10-hydroxycamptothecin, and examples 6-10 are the preparation of crystalline form III of 7-ethyl-10-hydroxycamptothecin.
[0058] Embodiment 1, the preparation of 7-ethyl-10-hydroxycamptothecin crystal form II
[0059] Weigh 50mg of 7-ethyl-10-hydroxycamptothecin into a reaction flask, add 20ml of a mixed solvent of methanol: chloroform with a volume ratio of 1:1, stir to dissolve, evaporate the solvent at 10-20°C, and separate the solid by filtration , and the solid was vacuum-dried at 50°C to constant weight to obtain crystalline form II of 7-ethyl-10-hydroxycamptothecin.
Embodiment 2
[0060] Example 2, Preparation of 7-ethyl-10-hydroxycamptothecin crystal form II
[0061] Weigh 30mg of 7-ethyl-10-hydroxycamptothecin into a reaction bottle, add 210ml of methanol solvent, stir to dissolve, evaporate the solvent at 10-20°C, filter and separate the solid, and dry the solid under vacuum at 50°C to constant weight , that is, 7-ethyl-10-hydroxycamptothecin crystal form II.
Embodiment 3
[0062] Example 3, Preparation of 7-ethyl-10-hydroxycamptothecin crystal form II
[0063] Weigh 50mg of 7-ethyl-10-hydroxycamptothecin into a reaction flask, add 12ml of a mixed solvent of methanol: chloroform with a volume ratio of 1:1, stir at room temperature, filter and separate the solid, and dry the solid in vacuum at 50°C to Constant weight to obtain 7-ethyl-10-hydroxycamptothecin crystal form II.
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Abstract
The invention relates to 7-ethyl-10-hydroxycamptothecine crystal forms II and III, and a preparation method and application thereof. The crystal form II uses Cu-K alpha radiation; the X-ray powder diffraction represented by 2theta angle has characteristic peaks when the diffraction angle is 5.64, 10.80, 12.55, 13.48, 17.09, 17.65, 18.21, 18.79, 24.52 and 26.84 degrees; and the error range of 2theta is + / -0.2 degree. The crystal form III uses Cu-K alpha radiation; the X-ray powder diffraction represented by 2theta angle has characteristic peaks when the diffraction angle is 4.58, 9.34, 10.42, 11.12, 12.30, 13.40, 14.40, 16.34, 16.86, 17.20, 17.70, 18.72, 19.32, 21.48, 22.44, 24.90, 25.40, 25.68 and 27.44 degrees; and the error range of 2theta is + / -0.2 degree. The two crystal forms of 7-ethyl-10-hydroxycamptothecine have high solubility and favorable stability.
Description
technical field [0001] The invention relates to two new crystal forms of 7-ethyl-10 hydroxycamptothecin and a preparation method thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Irinotecan (mnotecan, CPT-11) is a semi-synthetic water-soluble derivative of camptothecin. Its antitumor activity is higher than that of camptothecin, and its side effects are lower than that of camptothecin. The anti-tumor mechanism of irinotecan is mainly to inhibit the activity of topoisomerase-I, which affects DNA replication and leads to cell death. CPT-11 is an important drug for the treatment of small-cell lung cancer (SCLC). In 2010, the National Comprehensive Cancer Network (NCCN) in the United States recommended CPT-11 as the first-line treatment drug for advanced SCLC, and it can also be used for second-line treatment. . Irinotecan is an ester prodrug, which is mainly metabolized by carboxylesterase into 7-ethyl-10-hydroxycamptothecin (SN-3...
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