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Pomalidomide crystal and preparation method thereof

The technology of pomalidomide crystal and pomalidomide is applied in the field of pomalidomide crystal form and its preparation, which can solve the difference of microscopic crystal structure, appearance, physical and chemical properties and biological activity, and influence on drug stability and solubility. and bioavailability

Active Publication Date: 2014-03-12
CHONGQING TAIHAO PHARM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Different crystal forms of the same compound have the same chemical composition but different microscopic crystal structures, which lead to differences in their appearance, physicochemical properties and biological activities
These characteristics directly affect the preparation performance of the drug, and will affect the stability, solubility and bioavailability of the drug, which in turn will affect the quality, safety, effectiveness and application of the drug

Method used

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  • Pomalidomide crystal and preparation method thereof
  • Pomalidomide crystal and preparation method thereof
  • Pomalidomide crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of pomalidomide crystal form

[0040] Add 180 mL of DMSO to 5 g of crude pomalidomide, stir at room temperature to dissolve, then add 200 mL of water to the solution, crystals precipitate out, stir and mix well, let stand at room temperature for 10 h, filter with suction, and dry the filter cake under reduced pressure to obtain crystallized pomalidomide Methamide 4.5g. HPLC detection purity ≥ 99.82%.

Embodiment 2

[0041] Embodiment 2: Preparation of pomalidomide crystal form

[0042] Add 90 mL of DMSO to 3 g of crude pomalidomide, stir at room temperature to dissolve, then add 250 mL of water to the solution, crystals precipitate out, stir and mix well, let stand at room temperature for 5 hours, filter with suction, and dry the filter cake under reduced pressure to obtain crystallized pomalidomide Methamide 2.75g. HPLC detection purity ≥ 99.73%. HPLC detection chart see figure 2 , and the analysis results are shown in Table 1.

[0043] Table 1 pomalidomide crystal form HPLC detection and analysis results

[0044] Peak ID

Embodiment 3

[0045] Embodiment 3: Preparation of pomalidomide crystal form

[0046] Add 30 mL of DMSO to 2 g of crude pomalidomide, stir at room temperature to dissolve, then add 250 mL of water to the solution, crystals precipitate out, stir and mix well, let stand at room temperature for 12 hours, filter with suction, and dry the filter cake under reduced pressure to obtain crystalline pomalidomide Methamide 1.75g. HPLC detection purity ≥ 99.85%.

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Abstract

The invention relates to the field of pharmaceutical chemistry, and discloses a novel pomalidomide crystal and a preparation method thereof. The novel pomalidomide crystal disclosed by the invention has the advantages of good crystal stability, high bioavailability, excellent property in the aspects of oral absorption and enhancement of immune response mediated by a T cell and a natural killer cell, weak toxicity and good storage and treatment stability and can be used for preparing pharmaceutical for treating multiple myeloma.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a crystal form of pomalidomide and a preparation method and application thereof. Background technique [0002] Pomalidomide, trade name Pomalyst, Chinese chemical name: 3-amino-N-(2,6-dioxo-3-piperidinyl) phthalimide, molecular formula C 13 h 11 N 3 o 4 , which has a structure as shown in formula I: [0003] [0004] Pomalidomide is a new type of immunomodulator developed by Celgene Pharmaceuticals. It is a thalidomide analogue and the third of its kind to be marketed after thalidomide and lenalidomide. Immunomodulators. Pomalidomide can enhance the immune response mediated by T cells and natural killer cells, while inhibiting the production of pro-inflammatory cytokines (such as TNF-α) by monocytes. In addition, pomalidomide can inhibit the proliferation of tumor cells and induce apoptosis, and it also has a strong inhibitory effect on the proliferation of lenalidomid...

Claims

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Application Information

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IPC IPC(8): C07D401/04A61K31/4439A61P35/00
CPCC07D401/04
Inventor 李靖王信见夏雪峰吴进
Owner CHONGQING TAIHAO PHARM CO LTD
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