New crystal from of pentostatin, and preparation method and application of same

A pentostatin and crystal form technology, which is applied in the field of chemical pharmacy, can solve the problems of unfavorable crystal form stability preparation storage stability, poor fluidity of needle-like crystals, affecting the operability of preparations, etc., to reduce the decline in curative effect Effects of risk and safety risks, reduced sieving time, improved uniformity and stability

Active Publication Date: 2018-09-28
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Needle crystals generally have poor fluidity, low bulk density, and are difficult to filter and dry, which affects the operability of preparation processing; in addition, needle crystals need to be pulverized before they can be used in solid dosage form pharmaceutical preparations, and pulverization will affect the crystal form. Destruction, which is not conducive to the stability of the crystal form and the storage stability of the preparation

Method used

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  • New crystal from of pentostatin, and preparation method and application of same
  • New crystal from of pentostatin, and preparation method and application of same
  • New crystal from of pentostatin, and preparation method and application of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 0.2g crude pentostatin (HPLC purity> 95%) dissolved in 20mL methanol, heated to 50°C, dissolved, filtered, added 80ml methyl acetate with stirring, crystallized at 20°C for 6h, controlled the stirring speed at 170rpm / min, filtered, and dried under vacuum at 35°C to obtain 0.08g Lump crystals are easy to filter, and the purity detected by HPLC is 99.7%.

[0049] The X-ray powder diffraction and DSC spectra of this crystal are detailed in Figure 1-2 In the present invention, it is named pentostatin crystal form I.

Embodiment 2

[0051] 0.2g crude pentostatin (HPLC purity> 95%) dissolved in 10mL methanol, warmed to 60℃, dissolved, filtered, added 60ml methyl acetate with stirring, crystallized at 25℃ for 24h, controlled the stirring speed at 170rpm / min, filtered and dried under vacuum at 35℃ to obtain 0.11g Lump crystals are easy to filter, and the purity detected by HPLC is 99.5%. After measuring the X-ray powder diffraction pattern (XRD), it is confirmed that it is pentostatin crystal form I.

Embodiment 3

[0053] 0.2g crude pentostatin (HPLC purity> 95%) dissolved in 12mL methanol, heated to 55℃, dissolved, filtered, added 120ml methyl acetate with stirring, crystallized at 30℃ for 8h, controlled the stirring speed at 170rpm / min, filtered, and dried under vacuum at 35℃ to obtain 0.14g Lump crystals are easy to filter, and the purity detected by HPLC is 99.1%. After measuring the X-ray powder diffraction pattern (XRD), it is confirmed that it is pentostatin crystal form I.

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PUM

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Abstract

The invention relates to a new crystal from (I) of pentostatin, and a preparation method and an application of same. The new crystal from (I) has good solubility and is improved in bioavailability during intestinal absorption and oral taking. The crystal from (I) has high product purity, excellent physical and chemical properties, excellent chemical stability, and processing reproducibility (filtration, drying and tabletting). The crystallization process is simple and is convenient to carry out, is low in pollution, and can achieve industrial production.

Description

Technical field [0001] The invention relates to the field of chemical pharmacy. More specifically, the present invention relates to a new crystal form of pentostatin, a method for preparing the crystal form, and its medical use. technical background [0002] Pentostatin was isolated from Streptomyces antiboticus culture medium by Woo et al. in 1974. It is a very strong adenosine deaminase (ADA) inhibitor. Pentostatin has a high affinity for ADA. It can bind tightly to ADA, inhibit the activity of ADA, and increase the level of cell deoxyadenosine triphosphate (dATP). dATP blocks DNA synthesis by inhibiting ribonucleotide reductase. In addition, pentostatin can inhibit RNA synthesis and enhance DNA damage. In February 1998, the US FDA officially approved the marketing of pentostatin (trade name Nipent) for injection, which is mainly used for stem cell leukemia (Hairy cell leukemia, HCL), chronic lymphocytic leukemia (Chronic lymphocytic leukemia, CLL), and mycosis fungus Treatm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/23C07H1/06A61K31/7056A61P35/00A61P35/02
CPCC07B2200/13C07H1/06C07H19/23
Inventor 李娜张亮陈连蔚应雪肖苏笛
Owner ZHEJIANG HISUN PHARMA CO LTD
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