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Pemetrexed liposome and preparation method thereof

A technology of metrexed lipid and pemetrexed, which is applied in the field of pemetrexed liposome and its preparation, and can solve the problems of poor stability of pemetrexed, toxic and side effects, and increased impurity content of pemetrexed preparations, etc.

Inactive Publication Date: 2015-04-29
XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the existing pemetrexed preparations have problems such as poor absorption in vivo, loss of liver metabolism, and reproductive toxicity. How to reduce its toxicity and improve its therapeutic effect has become the main direction of current research
[0005] In addition, pemetrexed also has the problem of poor stability. It is prone to degradation under high temperature and oxidative conditions, and also produces impurities that may cause toxic and side effects. During transportation and storage, it is often caused by insufficient temperature control. As a result, the impurity content in the pemetrexed preparation increased significantly and other problems

Method used

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  • Pemetrexed liposome and preparation method thereof
  • Pemetrexed liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment one, MTA liposome 1#

[0047] Put 37mg of liposome mixture (HSPC / chol / TPGS mass ratio is 47.4 / 42.6 / 10) in ep tube and add 0.5ml chloroform to dissolve; the mixture is placed in a rotary evaporator, at room temperature, evaporated under reduced pressure to form an organic film Add 5ml of calcium acetate aqueous solution for hydration, rotary steaming 30min, remove residual organic solvent; the liposome ice bath ultrasonic 5min that forms; Get above-mentioned liposome solution and join in the dialysis bag that molecular weight cut off is 1000, dialysate ( The volume of NS solution) is 1L, and the dialysis time is 6-8 hours. The liquid (1L*2) is changed twice to form a calcium acetate gradient and increase the monitoring of pH (pH=4.5-5.5).

[0048] The liposome solution after dialysis was taken, and the pre-prepared 5 mg / ml pemetrexed solution (dissolved in MilliQ water) was added to the final concentration of 1 mg / ml, and the solution was bathed in water at 60...

Embodiment 2

[0049] Embodiment two, MTA liposome 2#

[0050]Put 30mg of liposome mixture (HSPC / chol / TPGS mass ratio is 50 / 45 / 5) in ep tube and add 0.5ml chloroform to dissolve; the mixture is placed in a rotary evaporator, at room temperature, evaporated under reduced pressure to form an organic film Add 5ml of calcium acetate aqueous solution for hydration, rotary steaming 20min, remove residual organic solvent; the liposome ice bath ultrasonic 10min that forms; Get above-mentioned liposome solution and join in the dialysis bag that molecular weight cut off is 1000, dialysate ( The volume of NS solution) is 1L, and the dialysis time is 6-8 hours. The liquid (1L*2) is changed twice to form a calcium acetate gradient and increase the monitoring of pH (pH=4.5-5.5).

[0051] The liposome solution after dialysis was taken, and the pre-prepared 10 mg / ml pemetrexed solution (dissolved in MilliQ water) was added to the final concentration of 2 mg / ml. During the drug loading process, the solution ...

Embodiment 3

[0052] Embodiment three, MTA liposome 3#

[0053] Put 40 mg of liposome mixture (HSPC / chol / TPGS mass ratio is 44.7 / 40.3 / 15) into an ep tube and add 1 ml of chloroform to dissolve; the mixture is placed in a rotary evaporator, at room temperature, and evaporated under reduced pressure to form an organic film; Add 10ml of calcium acetate aqueous solution for hydration, rotary steam for 60min, remove residual organic solvent; sonicate the formed liposome in an ice bath for 10min; take the above liposome solution and add it to a dialysis bag with a molecular weight cut-off of 1000, dialysate (NS The volume of solution) is 1L, and the dialysis time is 6-8 hours. The liquid (1L*2) is changed twice to form a calcium acetate gradient and increase the monitoring of pH (pH=4.5-5.5).

[0054] The liposome solution after dialysis was taken, and the pre-prepared 4 mg / ml pemetrexed solution (dissolved in MilliQ water) was added to the final concentration of 2 mg / ml. During the drug loading ...

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Abstract

The invention provides a pemetrexed liposome, which is characterized by being prepared from a pemetrexed and a liposome mixture, wherein the mass ratio of the pemetrexed and the liposome mixture is 1:(0.1-10); through the prepared pemetrexed liposome, the drug resistance can be reduced by more than 60% of non-liposome pemetrexed. Known from stability test, the liposome is favorable in stability. Known from clinical trials, the efficacy of the liposome can be improved by more than 80% compared with the common preparation, the in-vivo retention time can be prolonged by more than 65%, and the targeting effect is obvious.

Description

technical field [0001] The invention belongs to the field of preparations, and in particular relates to a pemetrexed liposome and a preparation method thereof. Background technique [0002] Pemetrexed is an antifolate preparation with a pyrrolic pyrimidine group in its structure. It can inhibit the growth of tumors by destroying the normal metabolic process dependent on folic acid in cells and inhibiting cell replication. In vitro studies have shown that pemetrexed can inhibit the activities of thymidylate synthase, dihydrofolate reductase and glycinamide nucleotide formyltransferase, which are all enzymes necessary for the synthesis of folic acid and participate in the thymidine nucleogenesis. Pemetrexed enters the cell through the folic acid-carrying carrier and the folic acid-binding protein transport system on the cell membrane. [0003] Once pemetrexed is inside the cell, it is converted to the polyglutamate form by the enzyme folyl polyglutamate synthetase. Polygluta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/519A61K47/24A61K47/22A61K47/28A61P35/00
Inventor 刘艳陈婷尹又高洁陈霁晖
Owner XIN HUA HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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