Methopterin intralipid, its freeze drying agent, preparation method and application thereof

A technology of methotrexate and fat emulsion, applied in anti-inflammatory agents, pharmaceutical formulations, emulsion delivery, etc., which can solve problems such as restrictions on widespread use, trouble and confusion in clinical medication, and no indications for treating rheumatic diseases

Active Publication Date: 2008-12-10
叶志中 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

thus limiting its widespread use
[0005] At present, there are MTX tablets and powder injections produced in China. They have no indications for treating rheumatic diseases,

Method used

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  • Methopterin intralipid, its freeze drying agent, preparation method and application thereof
  • Methopterin intralipid, its freeze drying agent, preparation method and application thereof
  • Methopterin intralipid, its freeze drying agent, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 100ml of methotrexate fat emulsion contains:

[0037] Methotrexate for injection 500mg, soybean oil for injection 4g,

[0038] Egg yolk lecithin for injection 2g, maltose 8g,

[0039] Glycerin 2g,

[0040] Adjust pH to 6.5 with hydrochloric acid,

[0041] The dosage of water for injection is added to the total volume of methotrexate fat emulsion to 100ml.

[0042] The preparation method of the above-mentioned 100ml methotrexate fat emulsion is as follows: at 40 ° C, 500mg of methotrexate for injection and 4g of soybean oil for injection are heated and mixed to obtain an oil phase; 2g of egg yolk lecithin for injection is dispersed into 80ml containing In the glycerol aqueous solution of 8g maltose (containing glycerol 2g), obtain water phase, wherein water is water for injection; at 40 ℃, water phase and oil phase are mixed, in high-speed homogenizer (Zhejiang Jintan Instrument Factory) with 15000 rev / Stir at a high speed of 10 minutes, mix for 10 minutes to prepare ...

Embodiment 2

[0044] The methotrexate fat emulsion prepared in Example 1 was subpackaged under aseptic conditions, and 1ml was injected into 5ml bottles respectively, and the lyophilizer (RL-20MB, manufactured by Kyowa Vacuum Co., Ltd.) was used in- Pre-freeze at 40°C for 2 hours, then perform primary drying under reduced pressure at 0°C for 10 hours, and then perform secondary drying at 25°C under reduced pressure for 5 hours to obtain the present invention of methotrexate lyophilisate. The obtained freeze-dried agent is dissolved in 1 ml of water for injection (regenerated into 1 ml of fat emulsion), and the dissolution is completed soon. The particle size of the emulsion particles is more than 90% of 5-70 nm as measured by a photometer.

Embodiment 3

[0046] 100ml of methotrexate fat emulsion contains:

[0047] Methotrexate for injection 500mg, soybean oil for injection 6g,

[0048] Egg yolk lecithin for injection 4g, oleic acid 240mg,

[0049] Glycerin 2g, Vitamin E 20mg

[0050] Maltose 5g,

[0051] Adjust pH to 7.4 with hydrochloric acid,

[0052] The amount of water for injection was added to a total volume of 100 ml.

[0053] The preparation method of the above-mentioned 100ml methotrexate fat emulsion is as follows: at 40° C., the methotrexate for injection, soybean oil for injection, oleic acid and vitamin E are heated and mixed to obtain an oil phase; the egg yolk lecithin for injection is dispersed In 80ml of maltose-containing glycerol aqueous solution, the water phase is obtained, wherein the water is water for injection; the remaining steps are the same as those in Example 1. Measured by high pressure liquid chromatography, containing 5.0 mg / ml of methotrexate, and measured by light scattering photometer, t...

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Abstract

The invention relates to methotrexate intralipid, a freeze-dried agent, a preparation method and an application thereof. The methotrexate intralipid consists of methotrexate active ingredient, oil for injection, emulsifying agent, stabilizing agent, isotonic adjustment agent, antioxidant, amylose, water for injection and pH modifying agent. The methotrexate intralipid of the invention is freeze-dried to obtain the freeze-dried agent of the methotrexate intralipid. The methotrexate intralipid and the freeze-dried agent of methotrexate intralipid can be applied to the medicines for treating a tumor and rheumatoid diseases.

Description

technical field [0001] The present invention relates to a preparation whose active ingredient is methotrexate, a preparation method and application thereof. Background technique [0002] Methotrexate (MTX) has been used to treat malignant tumors as early as 50 years ago, and has been approved by the U.S. Food and Drug Administration as a disease-modifying antirheumatic drug for the treatment of rheumatoid disease through small-dose discontinuous administration for more than 20 years. It is effective for rheumatic diseases such as arthritis, spondyloarthropathy, and systemic lupus erythematosus. [0003] The pharmacological effects of methotrexate are as follows: ① Combines with dihydrofolate reductase (DHFR) and inhibits the activity of this enzyme, resulting in the stop of the synthesis of purine metabolites; it can also prevent the conversion of glycine into serine, homocysteine Amino acid is converted to methionine, which inhibits DNA and protein synthesis. It is cytotox...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/519A61P35/00A61P29/00A61P19/02
Inventor 叶志中高洁生高戈尹志华
Owner 叶志中
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