A kind of romidepsin acetate crystal form and preparation method thereof

A technology of romidepsin and acetate, which is applied in the field of romidepsin acetate crystal form and its preparation, can solve instability, few reports of romidepsin salt crystal form, romidepsin Poor solubility and other problems, to achieve the effect of improving solubility and stability

Active Publication Date: 2022-04-19
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The present invention aims at the defects of poor solubility and instability of romidepsin, few crystal forms of romidepsin salt, etc., and provides a crystal form of romidepsin acetate and a preparation method thereof

Method used

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  • A kind of romidepsin acetate crystal form and preparation method thereof
  • A kind of romidepsin acetate crystal form and preparation method thereof
  • A kind of romidepsin acetate crystal form and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0083] At a constant temperature of 25°C, weigh 4g of romidepsin and dissolve it in 10ml of acetic acid, and ultrasonically assist in dissolving. After 24 hours, crystals were found to be precipitated, and romidepsin acetate crystals were obtained by filtration to obtain romidepsin acetate crystal form with a purity of 99.1% and a yield of 85.5%.

Embodiment 2

[0085] At a constant temperature of 70°C, weigh 5.5g of romidepsin and dissolve it in 10ml of acetic acid, and ultrasonically assist the dissolution. After the romidepsin is completely dissolved, filter through filter paper to obtain a clear solution, and then place the solution at room temperature at 25°C. After 48 hours, crystals were found to be precipitated, and romidepsin acetate crystals were obtained by filtration to obtain romidepsin acetate crystal form with a purity of 99.3% and a yield of 80.5%. Use it for XRPD, DSC, and single crystal detection, see the XRPD spectrum figure 1 , IR spectrum see figure 2 , see the DSC spectrum image 3 , the ellipsoid diagram of the three-dimensional structure of the molecule is shown in Figure 4 , the unit cell packing projection along the a-axis is shown in Figure 5 , the XRPD of the initial romidepsin acetate crystal form and the XRPD of the sample after 60 days see Figure 6 , the comparison of its XRPD pattern with the ro...

Embodiment 3

[0087] At a constant temperature of 45°C, weigh 4.5g of romidepsin and dissolve it in 10ml of acetic acid, and ultrasonically assist the dissolution. After the romidepsin is completely dissolved, filter through filter paper to obtain a clear solution, and then place the solution at room temperature at 10°C. After 48 hours, crystals were found to be precipitated, and romidepsin acetate crystals were obtained by filtration to obtain romidepsin acetate crystal form with a purity of 99.2% and a yield of 87.3%.

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Abstract

The invention discloses a crystal form of romidepsin acetate and a preparation method thereof. The romidepsin acetate crystal form of the present invention improves the solubility and stability of romidepsin, can expand the application of romidepsin in the field of tumor treatment and HIV treatment, and can also provide more romidepsin The development of octyl acetate dosage forms provides a research basis.

Description

technical field [0001] The invention relates to a crystal form of romidepsin acetate and a preparation method thereof. Background technique [0002] Romidepsin (also known as FK228, FR901228, trade name Istodax) is a class of cyclic peptide antitumor antibiotics, originally by Ueda (J.Antibiot.1994, 47 (3): 301-310) from a strain It was isolated from Chromobacterium violaceum WB968. Romidepsin is a cyclic peptide structure, and each amino acid or amino acid derivative is connected by a peptide bond, and there is a disulfide bond structure in the structure, and the disulfide bond is the reason why romidepsin acts as a histone deacetylase inhibitor (HDACi ) plays a key role, when romidepsin enters the cell, its disulfide bond can be reduced to a sulfhydryl group by reduced glutathione, at this time the sulfhydryl group and the Zn 2+ Coupling, thereby inhibiting HDAC activity. [0003] [0004] The chemical structure of romidepsin [0005] Romidepsin inhibits the growth ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K5/103C07K1/30
Inventor 熊磊胡海峰陈昌发
Owner SHANGHAI INST OF PHARMA IND CO LTD
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