Pemetrexed disodium injection solution and preparation method thereof

A technique for pemetrexed disodium and injections, which is applied in the field of pemetrexed disodium injections and its preparation, can solve the problems of failure to achieve targeted drug delivery, slow down of elimination speed, etc., and achieve simple and reliable production technology, including The effect of high sealing rate and relaxed storage conditions

Inactive Publication Date: 2016-12-07
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the pemetrexed disodium liposome injection disclosed in CN201210551378.1 has the technical effect of "slowing down the elimination speed in the body, prolonging the distribution time in the systemic circulation, achieving a partial sustained release effect, and increasing the bioavailability", but still Did not achieve the effect of targeted drug delivery

Method used

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  • Pemetrexed disodium injection solution and preparation method thereof
  • Pemetrexed disodium injection solution and preparation method thereof
  • Pemetrexed disodium injection solution and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Prescription

[0031]

[0032] The preparation process is as follows:

[0033] Dissolve pemetrexed disodium, phospholipids, cholesterol and vitamin E in methanol according to the formula and mix them evenly; use a rotary evaporator to remove the methanol in the solution under reduced pressure to form a lipid film; dissolve PEG300 in 10ml of water for injection, and mix with water The lipid film was hydrated, and the hydration temperature was 40°C to obtain the pemetrexed disodium liposome suspension; after the hydration was complete, the liposomes were prepared with a high-pressure homogenizer until the average particle size was 130 ± 10nm, and the liposomes were Particle size and uniformity are detected with a multi-angle nanoparticle analyzer; the concentration that is constant with water for injection and adjusted to is a 2.0mg / ml solution, and the pemetrexed disodium liposome suspension is micronized with a 0.22 micron aperture. Filter and sterilize through the ...

Embodiment 2

[0035] Prescription

[0036]

[0037] The preparation process is as follows:

[0038] Dissolve pemetrexed disodium, phospholipids, cholesterol and vitamin E in methanol according to the formula and mix them evenly; use a rotary evaporator to remove the methanol in the solution under reduced pressure to form a lipid film; dissolve PEG300 in 10ml of water for injection, and mix with water The lipid film was hydrated, and the hydration temperature was 30°C to obtain the pemetrexed disodium liposome suspension; after the hydration was complete, the liposomes were prepared with a high-pressure homogenizer until the average particle size was 120 ± 10nm, and the liposomes were Particle size and uniformity are detected with a multi-angle nanoparticle analyzer; the concentration that is constant with water for injection and adjusted to is a 2.0mg / ml solution, and the pemetrexed disodium liposome suspension is micronized with a 0.22 micron aperture. Filter and sterilize through the po...

Embodiment 3

[0040] Prescription

[0041]

[0042] The preparation process is as follows:

[0043] Dissolve pemetrexed disodium, phospholipids, cholesterol and vitamin E in methanol according to the formula and mix them evenly; use a rotary evaporator to remove the methanol in the solution under reduced pressure to form a lipid film; dissolve PEG300 in 10ml of water for injection, and mix with water The lipid film was hydrated, and the hydration temperature was 50°C to obtain the pemetrexed disodium liposome suspension; after the hydration was complete, the liposomes were prepared with a high-pressure homogenizer until the average particle size was 110 ± 10nm, and the liposomes were Particle size and uniformity are detected with a multi-angle nanoparticle analyzer; the concentration that is constant with water for injection and adjusted to is a 2.0mg / ml solution, and the pemetrexed disodium liposome suspension is micronized with a 0.22 micron aperture. Filter and sterilize through the ...

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Abstract

The invention relates to a pemetrexed disodium injection solution and a preparation method thereof. The injection solution contains pemetrexed disodium, neutral phospholipid, charged phospholipid, cholesterol, an antioxidant and a suspending agent. The injection solution provided by the invention has appropriate particle size distribution, is high in encapsulation efficiency and good in stability, and can be distributed in cancerization organs in a targeting manner, the curative effect of the pemetrexed disodium is improved, and the toxic and side effects are reduced.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an injection of pemetrexed disodium and a preparation method thereof. Background technique [0002] Pemetrexed disodium (Pemetrexed disodium), the chemical name is N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidine) -5-Alkyl)ethyl]benzoyl]-L-glutamate disodium. [0003] Pemetrexed disodium is a multi-target folic acid antagonist developed by Eli Lilly and Company for the treatment of tumors. It can be used in combination with cisplatin to treat inoperable malignant pleural mesothelioma. At present, pemetrexed disodium is the world's It is the only drug for the treatment of malignant pleural mesothelioma (MPM), and it is also used for the second-line treatment of metastatic non-small cell lung cancer. Pemetrexed alone or combined with chemotherapy has obvious therapeutic effects on a variety of tumors, especially for patients who have failed previous treatm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/519A61K47/24A61K47/22A61K47/34A61K47/28A61P35/00
CPCA61K9/127A61K9/0019A61K31/519A61K47/10A61K47/22A61K47/24A61K47/28
Inventor 吕慧李巍李琴姜涛冯芮茂
Owner JIANGSU HANSOH PHARMA CO LTD
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