Oxaliplatin crystal compound and freeze-dried powder injection

An oxaliplatin and compound technology, which is applied in the field of oxaliplatin crystalline compounds and freeze-dried powder injections, can solve the problems of poor solubility and poor reconstitution performance of oxaliplatin, and achieves improved drug safety performance and improved dissolution. good performance

Active Publication Date: 2014-05-07
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, oxaliplatin has poor solubility in water, especially after the preparation of injections, the reconstitution performance is poor

Method used

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  • Oxaliplatin crystal compound and freeze-dried powder injection
  • Oxaliplatin crystal compound and freeze-dried powder injection
  • Oxaliplatin crystal compound and freeze-dried powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]Take 100g of crude oxaliplatin, add a water:methanol solution with a volume ratio of 1300ml of crude oxaliplatin, and heat to reflux; after the crude oxaliplatin is dissolved, add 0.5 times of activated carbon for decolorization 30min, filter, add dropwise to the filtrate with a volume of oxaliplatin crude product weight 180ml and a volume ratio of 2.5:7.5 ether: isobutanol solution under stirring, the stirring is 23rmp, and the dropping is controlled dropping time 4 Add dropwise at a constant rate of about 1 minute; after dropping, stir and cool down, the stirring and cooling down is 10 minutes at 18rmp to 38°C, then 13rmp to 17°C for 15 minutes, let stand for 19 hours, filter, and use 6:4 ether : Washing with isobutanol solution and drying to obtain 97.8 g of the oxaliplatin crystalline compound, HPLC content 99.72%, mp 172.3-172.8°C.

[0038] Measured by powder X-ray diffraction method, the X-ray powder diffraction pattern represented by 2θ±0.2° diffraction angle is a...

Embodiment 2

[0040] Take 100g of crude oxaliplatin, add a water:methanol solution with a volume ratio of 1200ml of crude oxaliplatin, and heat to reflux; after the crude oxaliplatin is dissolved, add 0.3 times of activated carbon to decolorize 30min, filter, add dropwise to the filtrate with a volume ratio of 2.5:7.5 ether: isobutanol solution with a volume ratio of 180ml of oxaliplatin crude product weight under stirring, the stirring is 20rmp, and the dropping is controlled dropping time 3.5 Add dropwise at a constant speed in about 1 minute; after dropping, stir and cool down, the stirring and cooling down is 10 minutes at 19rmp to 38°C, then 15min at 14rmp to 19°C, let stand for 18 hours, filter, and use 6:4 ether : Washing with isobutanol solution and drying to obtain 98.1 g of the oxaliplatin crystalline compound, HPLC content 99.51%, mp 172.2-173.0°C.

[0041] Measured by powder X-ray diffraction method, the X-ray powder diffraction pattern represented by 2θ±0.2° diffraction angle i...

Embodiment 3

[0043] Take 100g of crude oxaliplatin, add a water:methanol solution with a volume ratio of 1400ml of crude oxaliplatin, and heat to reflux; after the crude oxaliplatin is dissolved, add 0.2 times of activated carbon to decolorize 40min, filter, add dropwise to the filtrate under stirring, the volume ratio is 2.5:7.5 ether: isobutanol solution, the volume ratio of oxaliplatin crude product weight 160ml, described stirring is 20rmp, and described dropwise is to control dropping time 5 Add dropwise at a constant speed in about 1 minute; after dropping, stir and cool down. The stirring and cooling is to cool down to 37°C for 10 minutes under stirring at a rotating speed of 20rmp, and then cool down to 15°C for 15min under stirring at a rotating speed of 15rmp, let stand for 19 hours, filter, and use 6:4 ether : Washing with isobutanol solution and drying to obtain 95.2 g of the oxaliplatin crystalline compound, HPLC content 99.74%, mp 172.2-172.7°C.

[0044] Measured by powder X-...

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PUM

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Abstract

The invention relates to an oxaliplatin crystal compound. The oxaliplatin crystal compound is measured by using a powder X-ray diffraction measurement method. Characteristic diffraction peaks are shown at positions of 6.5 degrees, 9.8 degrees, 11.2 degrees, 13.7 degrees, 17.5 degrees, 18.5 degrees, 19.7 degrees, 22.4 degrees, 23.2 degrees, 26.8 degrees, 27.1 degrees, 33.8 degrees, 35.2 degrees, 36.9 degrees and 43.8 degrees in an X-ray powder diffraction pattern shown by a diffraction angle of 2theta+ / -0.2 degree. The oxaliplatin crystal compound is good in dissolubility.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an oxaliplatin crystal compound and its freeze-dried powder injection. Background technique [0002] Oxaliplatin, English name: Oxaliplatin, molecular formula: C 8 h 12 N 2 o 4 Pt, oxaliplatin (L-OHP) chemical name: L-trans diaminocycloethane oxalate platinum, is a platinum anticancer drug for the treatment of malignant tumors, preclinical drug efficacy, dosage and toxicology studies have shown that: L- OHP is a new generation of platinum-based anticancer drug with high anti-pain activity, low toxicity and high safety. Its structural formula is: [0003] [0004] Oxaliplatin is the third-generation platinum-based anticancer drug developed by Debiopharm in Switzerland. It is a new type of platinum-containing anti-tumor drug developed after cisplatin and carboplatin. Platinum anticancer drugs with broad-spectrum antitumor activity both inside and outside. Its anti-tumor spectrum is...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/282A61K9/19A61P35/00
Inventor 马鹰军钟正明
Owner HAINAN JINRUI PHARMA CO LTD
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