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A pharmaceutical composition containing calcium levofolinate and fluorouracil

A technology of calcium levofolinate and fluorouracil, applied in the field of medicine, can solve the problems of poor water solubility, reduced volume of freeze-dried powder injection, hard shell and brittle powder, etc., and achieves the effects of fast onset, improved water solubility, and reduced toxic and side effects

Inactive Publication Date: 2015-11-25
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In order to overcome a series of problems in the prior art, the inventors creatively discovered the combined application of calcium levofolinate injection and fluorouracil injection using specific excipients, which not only completely solved the water solubility and stability of calcium levofolinate sexual problems, it is convenient for clinical use, and because stevioside is added to leucovorin calcium injection, it can enhance the anti-tumor activity of 5-fluorouracil and reduce the side effects of methotrexate more than calcium leucovorin alone.
[0012] The stevioside added in the present invention has a good solubilizing effect on calcium levofolinate, solves the problem of its poor water solubility, avoids the introduction of too many impurities, and the addition of some inorganic salt co-solvents will cause the freeze-dried powder to shrink in size At the same time, stevioside also has a good bulking effect. By adding stevioside, the prepared calcium levofolinate freeze-dried powder basically maintains the original volume, uniform color, and easy to dissolve to form clarity. The solution

Method used

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  • A pharmaceutical composition containing calcium levofolinate and fluorouracil
  • A pharmaceutical composition containing calcium levofolinate and fluorouracil
  • A pharmaceutical composition containing calcium levofolinate and fluorouracil

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1 Preparation of Calcium Levofolinate Lyophilized Powder for Injection

[0043] prescription:

[0044]

[0045] making process:

[0046] (1) First add 7200ml of water for injection into the container;

[0047] (2) Add 225g of calcium leucovorin (calculated as leucovorin) and 720g of stevioside, stir to dissolve completely, and adjust the pH to 7.7 with 1mol / L sodium hydroxide solution or 1mol / L hydrochloric acid solution;

[0048] (3) Add 2.7g of activated carbon for injection, add the remaining water for injection, set the volume to 9000ml, stir and absorb for 30 minutes;

[0049] (4) The solution is decarbonized by coarse filtration, coarsely filtered through a 0.45 μm cartridge filter, and then sterilized and filtered with a 0.22 μm microporous membrane until the visible foreign matter is qualified;

[0050] (5) Filling, 1ml / bottle or 2ml / bottle or 6ml / bottle;

[0051] (6) Freeze drying

[0052] ① During the pre-freezing period, lower the shelf tempe...

Embodiment 2

[0055] Example 2 Preparation of Calcium Levofolinate Injection

[0056] prescription:

[0057]

[0058] making process:

[0059] (1) First add 14400ml water for injection into the liquid mixing tank;

[0060] (2) Add 180g of calcium leucovorin (calculated as leucovorin) and 90g of stevioside, stir to dissolve completely, and adjust the pH to 7.6 with 1mol / L sodium hydroxide solution or 1mol / L hydrochloric acid solution;

[0061] (4) Add 5.4g of activated carbon for injection, add the remaining water for injection, set the volume to 18000ml, stir and absorb for 30 minutes;

[0062] (5) The solution is decarbonized by coarse filtration, coarsely filtered through a 0.45 μm cartridge filter, and then sterilized and filtered with a 0.22 μm microporous membrane until the visible foreign matter is qualified;

[0063] (6) Filling, 3ml / bottle or 50ml / bottle or 10ml / bottle, sealing, and sterilizing to obtain calcium levofolinate injection.

Embodiment 3

[0064] Example 3 Preparation of Fluorouracil Injection

[0065] prescription:

[0066]

[0067] making process:

[0068] (1) First add 8000ml of water for injection into the container;

[0069] (2) Add 250g of fluorouracil, stir to dissolve completely, and adjust the pH to 8.8 with 1mol / L sodium hydroxide solution;

[0070] (3) Add 5g of activated carbon for injection, add the remaining water for injection, constant volume, stir and absorb for 30 minutes;

[0071] (4) The solution is decarbonized by coarse filtration, coarsely filtered through a 0.45 μm cartridge filter, and then sterilized and filtered with a 0.22 μm microporous membrane until the visible foreign matter is qualified;

[0072] (5) Filling, 10ml / bottle, sealing, and sterilizing to obtain fluorouracil injection.

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PUM

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Abstract

The invention relates to a pharmaceutical composition containing calcium levofolinate and fluorouracil, and particularly relates to a combined application package comprising a calcium levofolinate injection and an injection containing fluorouracil. When the combined application package is in use, the calcium levofolinate injection is intravenously injected and then the fluorouracil injection is intravenously injected.

Description

technical field [0001] The invention relates to a pharmaceutical composition of calcium leucovorin and fluorouracil, in particular to a combined application package of calcium leucovorin injection and the injection containing fluorouracil, belonging to the technical field of medicine. Background technique [0002] Folinic acid is a mixture of diastereomers of 5-formyl derivatives of tetrahydrofolate (THF), and its biologically active substance is the left-handed form called levofolinic acid. Folinic acid does not need to be reduced by dihydrofolate reductase to directly participate in the biological reaction using folic acid as a carrier for transferring "one-carbon group" in vivo. L-folinic acid (L-5-leucovorin) is rapidly metabolized (5,10-methyltetrahydrofolate, 5,10-leucovorin-tetrahydrofolate) to L-5-methyltetrahydrofolate. L-5-methyltetrahydrofolate can be metabolized to 5,10-methylenetetrahydrofolate through other pathways, and 5,10-methylenetetrahydrofolate is irrev...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/519A61K9/19A61K47/26A61P35/00A61P1/00A61K31/513
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD