Pemetrexed disodium liposome injection

A technology of pemetrexed disodium lipid and metrexed disodium lipid, which is applied in the field of medicine, can solve the problems of increased impurity content of freeze-dried powder injections, undisclosed improvements, toxic and side effects, etc., and achieves increased electrostatic repulsion, inhibited Gathering effect

Inactive Publication Date: 2013-04-17
海南路易丹尼生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The stability of pemetrexed disodium is relatively poor, and it is easy to degrade under high temperature and oxidative conditions, and produces impurities that may cause toxic and side effects. It is not suitable for making injections that require high-temperature sterilization, so pemetrexed disodium is usually Made into freeze-dried powder injection, but the existing freeze-dried powder injection of pemetrexed disodium is in the process of transportation and storage, and also often causes the impurity content in the freeze-dried powder injection to increase significantly because the temperature control is not strict, and Neither prior art nor public common sense discloses suggestions for improving the above deficiencies

Method used

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  • Pemetrexed disodium liposome injection
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  • Pemetrexed disodium liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Example 1 Preparation of Pemetrexed Disodium Liposome Injection

[0064] The ingredients and their weights are as follows:

[0065]

[0066] The following process is used to prepare pemetrexed disodium liposome injection:

[0067] (1) Dissolve 70g distearoylphosphatidylglycerol, 280g dipalmitoylphosphatidylcholine and 70g cholesterol in 1000ml of a mixed organic solvent of ethanol and tert-butanol with a volume ratio of 2:1, and stir to dissolve; Put the above solution in an eggplant-shaped bottle, and remove the organic solvent under reduced pressure in a 60°C water bath to form a uniform transparent film on the bottle wall;

[0068] (2) Under the protection of nitrogen, add 5000ml of an aqueous solution containing 10g pemetrexed disodium (calculated as pemetrexed) and 50gPEG600 into the bottle, stir to elute the phospholipid membrane and fully swell and hydrate. After hydration is complete Perform 5 times of gradient homogenization at 200 bar to 800 bar and filter with 0.22...

Embodiment 2

[0070] Example 2 Preparation of Pemetrexed Disodium Liposome Injection

[0071] The ingredients and their weights are as follows:

[0072]

[0073]

[0074] The following process is used to prepare pemetrexed disodium liposome injection:

[0075] (1) Dissolve 80g distearoylphosphatidylglycerol, 320g dipalmitoylphosphatidylcholine and 80g cholesterol in 1000ml of a mixed organic solvent of ethanol and tert-butanol with a volume ratio of 2:1, and stir to dissolve; Put the above solution in an eggplant-shaped bottle, and remove the organic solvent under reduced pressure in a 60°C water bath to form a uniform transparent film on the bottle wall;

[0076] (2) Under the protection of nitrogen, add 5000ml of an aqueous solution containing 20g pemetrexed disodium (calculated as pemetrexed) and 60gPEG600 to the bottle, stir to elute the phospholipid membrane and fully swell and hydrate. After the hydration is complete Perform 5 times of gradient homogenization at 200 bar to 800 bar and filte...

Embodiment 3

[0078] Example 3 Preparation of Pemetrexed Disodium Liposome Injection

[0079] The ingredients and their weights are as follows:

[0080]

[0081] The following process is used to prepare pemetrexed disodium liposome injection:

[0082] (1) Dissolve 100g distearoylphosphatidylglycerol, 400g dipalmitoylphosphatidylcholine and 100g cholesterol in 1000ml of a mixed organic solvent of ethanol and tert-butanol with a volume ratio of 2:1, and stir to dissolve; Put the above solution in an eggplant-shaped bottle, and remove the organic solvent under reduced pressure in a 60°C water bath to form a uniform transparent film on the bottle wall;

[0083] (2) Under the protection of nitrogen, add 8000ml of aqueous solution containing 50g pemetrexed disodium (calculated as pemetrexed) and 100g PEG600 into the bottle, stir to elute the phospholipid membrane and fully swell and hydrate, and the hydration is complete Then, perform 5 times of gradient homogenization at 200 bar to 800 bar, and filter...

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Abstract

The invention discloses pemetrexed disodium liposome injection which is mainly made of pemetrexed disodium and a preparation method thereof, distearoyl phosphatidyl glycerol, dipalmitoyl phosphatidyl choline, PEG600, cholesterol and mannitol. The liposome injection has the advantages that the particle size of liposome is small, the liposome is uniformly distributed, the encapsulation efficiency is high, the leakage rate is low, the stability is good, the solubility of the pemetrexed disodium and the quality of injection products are improved, the toxic and side effect is reduced, and the curative effect is improved.

Description

Technical field [0001] The invention relates to a liposome injection and a preparation method thereof, in particular to a pemetrexed disodium liposome injection and a preparation method thereof, and belongs to the technical field of medicine. Background technique [0002] The pemetrexed disodium described herein has the chemical name N-[4-[2-(2-amino-4,7-dihydro-4-carbonyl-1H-pyrrole[1,3-d]-pyrimidine -5-yl)ethyl]benzoyl]-L glutamic acid disodium salt 2.5 hydrate, or pemetrexed disodium 2.5 hydrate. The molecular formula is C 20 H 19 N 5 Na 2 O 6 ·2.5H 2 The structural formula of O is as follows: [0003] [0004] Pemetrexed is an antifolate preparation with a pyrropyrimidine group as its core structure. It inhibits cell replication by disrupting the normal folate-dependent metabolic process in cells, thereby inhibiting tumor growth. Exosome studies have shown that pemetrexed can inhibit the biosynthesis of thymidylate synthase, dihydrofolate reductase and glycinamide nucleotides...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/519A61K47/34A61K47/28A61P35/00
Inventor 王平
Owner 海南路易丹尼生物科技有限公司
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