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

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

Active Publication Date: 2011-04-06
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, and the powder injections have been issued a document to stop using them, which brings trouble and confusion to clinical medication. It is urgent to change the status quo

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] 500mg of methotrexate for injection, 4g of soybean oil for injection,

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

[0039] 2g of glycerin,

[0040] Adjust the pH to 6.5 with hydrochloric acid,

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

[0042] The preparation method of the above-mentioned 100ml methotrexate fat emulsion is as follows: at 40°C, 500mg methotrexate for injection and 4g soybean oil for injection are heated and mixed to obtain an oil phase; 2g egg yolk lecithin for injection is dispersed to 80ml containing 8g of maltose in a glycerol aqueous solution (containing 2g of glycerol) to obtain a water phase, where the water is water for injection; mix the water phase with the oil phase at 40°C, and use a high-speed homogenizer (Zhejiang Jintan Instrument Factory) at 15,000 rpm Stir at a high speed for 10 minutes and mix for 10 minutes to ...

Embodiment 2

[0044] The methotrexate fat emulsion prepared in Example 1 was dispensed under aseptic conditions, and 1 ml was injected into a 5 ml bottle, and the freeze dryer (RL-20MB, manufactured by Kyowa Vacuum Co., Ltd.) was used to- Perform pre-freezing at 40°C for 2 hours, then perform primary drying under reduced pressure at 0°C for 10 hours, and then perform secondary drying under reduced pressure at 25°C for 5 hours to obtain the present invention Lyophilized methotrexate. The obtained lyophilized agent is dissolved in 1ml water for injection (regenerated into 1ml fat emulsion), and the dissolution is completed soon. The re-dissolved fat emulsion is determined by high pressure liquid chromatography and contains 5mg / ml of methotrexate. As measured by the photometer, the particle size of the emulsion particles is greater than 90% of 5-70 nm.

Embodiment 3

[0046] 100ml of methotrexate fat emulsion contains:

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

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

[0049] Glycerin 2g, Vitamin E 20mg

[0050] Maltose 5g,

[0051] Adjust the pH to 7.4 with hydrochloric acid,

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

[0053] The preparation method of the above-mentioned 100ml methotrexate fat emulsion is as follows: at 40°C, heat and mix methotrexate for injection, soybean oil for injection, oleic acid, and vitamin E to obtain an oil phase; disperse egg yolk lecithin for injection Into 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 in Example 1. Measured by high pressure liquid chromatography, containing 5.0 mg / ml of methotrexate, measured by a light scattering photometer, the particle size of the emulsion parti...

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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 invention relates to a preparation whose active ingredient is methotrexate, its preparation method and application. Background technique [0002] Methotrexate (MTX) has been used to treat malignant tumors as early as 50 years ago. In the past 20 years, it has been approved by the US Food and Drug Administration as a disease-improving anti-rheumatic drug for the treatment of rheumatism through small doses of discontinuous administration. Arthritis, spondyloarthropathy, systemic lupus erythematosus and other rheumatic diseases are effective. [0003] The pharmacological effects of methotrexate are as follows: ① Combine with dihydrofolate reductase (DHFR) and inhibit the activity of the enzyme, leading to the stop of the synthesis of purine metabolites; it can also prevent the conversion of glycine to serine, homocysteine The amino acid is converted to methionine, which inhibits DNA and protein synthesis. It is cytotoxic when used in large doses. It is used...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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