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High optical purity trans-dextro oxaliplatin lyophilized powder injection and preparation method thereof

A freeze-dried powder injection, optical purity technology, applied in the field of medicine, can solve the problems affecting the safety of drug use, the levorotatory isomer has no drug activity and toxicity, and achieves the effects of overcoming risks, high optical purity, and good stability.

Active Publication Date: 2012-09-12
QILU PHARMA HAINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The L-isomer has no drug activity and high toxicity, which can seriously affect the drug safety of the drug. Therefore, it is necessary to strictly control the optical purity of oxaliplatin to ensure the drug safety of oxaliplatin freeze-dried powder injection

Method used

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  • High optical purity trans-dextro oxaliplatin lyophilized powder injection and preparation method thereof
  • High optical purity trans-dextro oxaliplatin lyophilized powder injection and preparation method thereof
  • High optical purity trans-dextro oxaliplatin lyophilized powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: The freeze-dried powder injection of trans-dextrooxaliplatin is made from the following components:

[0043] Trans-D-oxaliplatin 50mg, glycine 120mg, the optical purity of oxaliplatin is 100%.

[0044] Preparation:

[0045] (1) Dissolve 50mg of trans-D-oxaliplatin with an optical purity of 100% and 120mg of glycine in 10ml of water for injection, sterilize and filter, divide into 25mL glass bottles, and half add lyophilized rubber stoppers;

[0046](2) Put the packaged liquid medicine bottle on the shelf in the freeze-drying box for pre-freezing; first cool down the temperature of the plate layer to 5°C, keep it for 2 hours, and then quickly cool it down to -50°C within 60 minutes, After pre-freezing for 6 hours, carry out sublimation drying;

[0047] (3) When the vacuum degree in the drying oven reaches below 10Pa, the temperature of the shelf is slowly raised to 0°C in 120 minutes for sublimation drying, and the vacuum is controlled below 30Pa during t...

Embodiment 2

[0050] Embodiment 2: The freeze-dried powder injection of trans-dextro-oxaliplatin is made from the following components:

[0051] Trans-D-oxaliplatin 50mg, trehalose 135mg, the optical purity of trans-D-oxaliplatin is 99.99%.

[0052] Preparation:

[0053] (1) Dissolve 50mg of trans-D-oxaliplatin with an optical purity of 99.99% and 135mg of trehalose in 10ml of water for injection, sterilize and filter, divide into 25mL glass bottles, and half add lyophilized rubber stoppers ;

[0054] (2) Put the packaged liquid medicine bottle on the shelf in the freeze-drying box for pre-freezing: first cool down the temperature of the plate layer to 0°C, keep it for 2 hours, and then quickly cool it down to -60°C within 60 minutes , after pre-freezing for 4 hours, carry out sublimation drying;

[0055] (3) When the vacuum degree in the drying oven reaches below 30Pa, the temperature of the shelf is slowly raised to 0°C in 120 minutes for sublimation drying, and the vacuum is controlle...

experiment example 1

[0058] Experimental example 1, resolubility test

[0059] The trans-dex-oxaliplatin freeze-dried powder injection obtained in Examples 1 and 2 was detected, and the results are shown in Table 1 below:

[0060] Table 1. Reconstitution of lyophilized powder injection

[0061]

[0062] The above data show that the trans-D-oxaliplatin freeze-dried powder injection with high optical purity provided by the present invention has good reconstitution properties.

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Abstract

The invention relates to a high optical purity trans-dextro oxaliplatin lyophilized powder injection and a preparation method thereof. The lyophilized powder injection contains high optical purity trans-dextro oxaliplatin with treatment effective dose and pharmaceutically acceptable lyophilized excipient, and does not contain animal-based auxiliary lactose, wherein the optical purity of the trans-dextro oxaliplatin is not lower than 99.95 percent; the pharmaceutically acceptable lyophilized excipient is one or more of cane sugar, trehalose, glycine, histidine, dextran, polyethylene glycol andcyclodextrin. The preparation method of the lyophilized powder injection comprises the following steps: dissolving raw and auxiliary materials in water; subpackaging, pre-freezing, lyophylizing, performing analytic drying; infiltering nitrogen into subpackaged bottles after the lyophilization is completed; and pressing plugs and caps. The high optical purity trans-dextro oxaliplatin lyophilized powder injection is used for preparing an anti-cancer medicament, and can be applied in a parenteral way after being re-dissolved with a compatible solution.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a trans-dex-oxaliplatin freeze-dried powder injection with high optical purity, a preparation method and an application thereof. Background technique [0002] Oxaliplatin, chemical name: trans-dextro-1,2-cyclohexanediamino oxaliplatin, has the chemical structure shown in formula I, and is the third generation of platinum-based anti-cancer drugs after cisplatin and carboplatin The drug was first developed by Debiopharm in Switzerland and first launched in France in October 1996, and was approved by the US FDA in August 2002. The drug is safe to use, has low adverse reactions, and mild hematological toxicity. The chemotherapy regimen composed of other antineoplastic drugs is effective and well tolerated. It is mainly suitable for patients with metastatic colorectal cancer after failure of fluorouracil treatment. Platinum and carboplatin have a significant curative effect on colorec...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/282A61P35/00
Inventor 王晶翼谭永利杨清敏张明会
Owner QILU PHARMA HAINAN
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