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Platinum anticancer oxaliplatin composition

A technology for oxaliplatin and anticancer drugs, which is applied in the field of medicine and can solve the problems of easy moisture absorption and deterioration of loading capacity, poor fluidity, and differences.

Inactive Publication Date: 2015-11-18
QINGDAO HUAZHICAO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At the same time, oxaliplatin has a strong hygroscopic ability, especially after the powder injection is prepared, the hygroscopic ability becomes stronger, the fluidity becomes worse, it is easy to absorb moisture and deteriorate, and there is a difference in filling capacity

Method used

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  • Platinum anticancer oxaliplatin composition
  • Platinum anticancer oxaliplatin composition
  • Platinum anticancer oxaliplatin composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1: Preparation of Oxaliplatin Crystals

[0024] Take the oxaliplatin raw material, add in the mixed solvent A of N,N-dimethylformamide and N-methylacetamide whose volume is 8 times the weight of oxaliplatin at 30°C, N,N-dimethylformamide Methyl formamide, N-methyl acetamide volume ratio is 4:1, obtains solution; Then in the horizontal direction of the liquid surface of gained solution, applying magnetic field intensity is the constant magnetic field of 1.0T, and under the condition of this constant magnetic field to Chloroform whose volume is 8 times the weight of oxaliplatin was added dropwise to the solution; after the dropwise addition, the temperature was lowered to -10°C, allowed to stand for 2 hours, filtered, washed, and vacuum-dried to obtain the oxaliplatin crystals.

[0025] The X-ray powder diffraction pattern obtained by the Cu-Kα ray measurement of the prepared oxaliplatin crystal is as follows: figure 1 Shown, its purity as determined by high pe...

Embodiment 2

[0026] Example 2: Preparation of Oxaliplatin Compositions

[0027] The composition is: 1 part by weight of oxaliplatin crystal prepared by the present invention, and 0.03 part by weight of sodium dihydrogen phosphate.

[0028] The preparation method is:

[0029] (1) Weigh oxaliplatin crystals and sodium dihydrogen phosphate in proportion and mix them thoroughly;

[0030] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0031] Example 3: Preparation of Oxaliplatin Compositions

[0032] The composition is: 1 part by weight of oxaliplatin crystal prepared by the present invention, and 0.04 part by weight of sodium dihydrogen phosphate.

[0033] The preparation method is:

[0034] (1) Weigh oxaliplatin crystals and sodium dihydrogen phosphate in proportion and mix them thoroughly;

[0035] (2) Dispense into sterilized vials and stopper them.

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Abstract

The invention discloses a platinum anticancer oxaliplatin composition, belonging to the technical field of medicines. The composition comprises oxaliplatin and sodium dihydrogen phosphate, wherein oxaliplatin is a crystal. An X-ray powder diffraction pattern obtained through measurement by using a Cu-Kalpha ray is shown in a drawing 1 in the specification. A new crystal form of oxaliplatin provided by the invention is different from the crystal structure of the prior art. Through experimental verification, the compound in the new crystal form has high purity, good flowability and stability and low impurity content, has low possibility of moisture absorption and is safe and reliable to apply clinically. Powder injections prepared by utilizing the compound in the new crystal form have good stability after undergoing compatibility with solvents, have low content of insoluble particles and are very suitable to apply clinically.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a platinum anticancer drug oxaliplatin composition. Background technique [0002] Oxaliplatin is the third-generation platinum anticancer drug after cisplatin and carboplatin. It has broad-spectrum antitumor activity both in vivo and in vitro, and is also cytotoxic to cisplatin-resistant tumor cells. A synergistic cytotoxic effect of the combination of oxaliplatin and 5-fluorouracil was observed in both in vivo and in vitro studies. Oxaliplatin has few adverse reactions, no renal toxicity of cisplatin, and no myelosuppression of carboplatin. Its main site of action is DNA. By forming a conjugate with DNA, preventing its replication and transcription, it achieves the effect of killing tumor cells. Purpose, and the spectrum of anti-tumor activity has a significant inhibitory effect on colorectal cancer, non-small cell lung cancer, gastric cancer, ovarian cancer, and a variety of cel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/282C07F15/00A61P35/00
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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