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Pemetrexed disodium freeze-dried composition and preparation method thereof

A technology of pemetrexed disodium and its composition, which is applied in the field of freeze-dried pemetrexed disodium and its preparation, can solve the problems of poor stability of pemetrexed disodium, and achieve less impurities and a finished product Low moisture, good stability

Active Publication Date: 2014-12-24
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Pemetrexed disodium has poor stability and is prone to degradation under high temperature, oxidation and light conditions. Simple pemetrexed disodium will degrade in isotonic saline solution to form related substances; thus pemetrexed disodium Usually prepared as a lyophilized powder for injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Cool the water for injection to below 25°C, and add 1500 mL of water for injection into the batching tank. Open the agitator on the batching tank, add 106g mannitol in the batching tank, stir to dissolve completely; add 110.3g pemetrexed disodium (equivalent to 100g pemetrexed), stir and dissolve. Use 0.1mol / L NaOH and 0.1mol / L HCl solution to adjust the pH value of the liquid to 7.0-8.0, add 200mL of tert-butanol, add water for injection to 2000mL, add 2g of wetted activated carbon to the solution, and continue stirring for 30 minutes. The liquid medicine is decarburized, sterilized and filtered to obtain a filtrate.

[0061] The filtrate is evenly distributed in 1000 vials, and enters the box after stoppering. The product will drop from room temperature to -45°C within 5 hours, and keep the product at -45°C for 4 hours; when the temperature of the condenser reaches minus 45°C, turn on the vacuum pump. The pressure is not higher than 25Pa, and the product is heated an...

Embodiment 2

[0063] Cool the water for injection to below 25°C, and add 4800 mL of water for injection into the batching tank. Open the agitator on the batching tank, add 500g mannitol in the batching tank, stir to dissolve completely; add 551.5g pemetrexed disodium (equivalent to 500g pemetrexed), stir and dissolve. Use 0.1mol / L NaOH and 0.1mol / L HCl to adjust the pH value of the liquid to 7.0-8.0, add 300mL of tert-butanol, add water for injection to 6000mL, add 12g of wetted activated carbon, and continue stirring for 30 minutes. The liquid medicine is decarburized, sterilized and filtered to obtain a filtrate.

[0064] The filtrate is evenly distributed in 1,000 vials, and enters the box after stoppering. The product will drop from room temperature to -35°C within 5 hours, and the product will be pre-frozen at -35°C for 6 hours; when the temperature of the condenser reaches minus 45°C, turn on the vacuum pump , the pressure is not higher than 25Pa, the product is heated and sublimated...

Embodiment 3

[0072] The process of preparing the freeze-dried preparation of pemetrexed disodium and the preparation of the freeze-dried preparation in Examples 1 and 2 and Comparative Examples 1 and 2 were investigated, and the results are shown in Table-1.

[0073] Chromatographic conditions for detection of content and related substances: Octadecylsilane bonded silica gel as filler; 0.02mol / L ammonium phosphate solution-acetonitrile (86:14) as mobile phase, in which ammonium phosphate solution was adjusted to pH 4.0 with phosphoric acid; detection The wavelength is 240nm. The theoretical plate number should not be less than 2000 based on the pemetrexed disodium peak.

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PUM

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Abstract

The invention discloses a freeze-dried composition containing pemetrexed disodium and a preparation method thereof. The composition comprises pemetrexed disodium and mannitol, wherein the mass ratio of pemetrexed disodium to mannitol is 1: (0.9 to 1). The composition provided by the invention has the advantages of short freeze-drying period, small related material, and good forming appearance. The preparation method disclosed by the invention has the advantages of simpleness, practicability, and suitability for industrial mass production.

Description

technical field [0001] The invention belongs to the field of medicine, and more specifically relates to a freeze-dried composition of pemetrexed disodium and a preparation method thereof. Background technique [0002] Pemetrexed disodium is a multi-target antifolate drug, the chemical structure is shown in formula-I, and the molecular formula is C 20 h 19 N 5 Na 2 o 6 . Pemetrexed disodium is clinically used as a first-line drug for malignant pleural mesothelioma, and it is suitable for combined treatment with cisplatin in the treatment of inoperable malignant pleural mesothelioma; it is also clinically suitable for locally advanced patients who have progressed after receiving first-line chemotherapy Or the treatment of patients with metastatic non-squamous non-small cell lung cancer. [0003] Formula-I [0004] Pemetrexed disodium has poor stability and is prone to degradation under high temperature, oxidation and light conditions. Simple pemetrexed disodium will deg...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/519A61P35/00
Inventor 陈庆财李晓昕赵霞
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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