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Levoleucovorin freeze-dried injection agent and preparation method and pharmaceutical use thereof

A technology of leucovorin and freeze-dried powder injection, which is applied in freeze-dried delivery, drug combination, powder delivery, etc., and can solve problems such as inconvenient use, cardiac side effects, and no public reports of leucovorin

Active Publication Date: 2008-05-28
SHANGHAI HUILUN JIANGSU PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Leucovorin is generally prepared in the form of calcium salt, but the aqueous solution of calcium salt is not stable, and it is prone to precipitation, causing inconvenience in use; more importantly, because L-folinic acid is mainly used in high-dose chemotherapy, Combined use with 5-fluorouracil drugs, considering that too much calcium ions without therapeutic effect directly enter the body through injection will cause unnecessary side effects on the human heart, so the general dosage is less than 200mg / m 2 , but in most cases this dose is very insufficient for therapeutic
At present, there is no public report of levofolinic acid made into its sodium salt freeze-dried powder preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Leucovorin 100g

[0026] Mannitol 50g

[0027] Appropriate amount of sodium hydroxide (adjust the pH of sodium hydroxide solution (1mol / L) to 7.60)

[0028] Add water for injection to 3000ml

[0029] A total of 1000 bottles

[0030] Preparation method: Weigh 50g of mannitol, put it in a sterilized 5000ml container, add 2400ml of cold water for injection, stir and suspend it, weigh the prescribed amount of levofolinic acid, add it, and slowly add 1mol dropwise under full stirring About 420ml of sodium hydroxide solution per L until the solution is clear (pH7.60 or so). Add 0.3 g of activated carbon for needles, stir at room temperature for 30 minutes, filter with a sterilized 0.6 μm microporous membrane to decarbonize and filter with a 0.22 μm microporous membrane to sterilize, add water for injection to wash the filter, and add water for injection To 3000ml, adjust the pH of the solution and other items, after passing the test, put it in 10ml vials in 3ml aliquots p...

Embodiment 2

[0033] Leucovorin 200g

[0034] Mannitol 100g

[0035] Appropriate amount of sodium hydroxide (adjust the pH of sodium hydroxide solution (1mol / L) to 6.00)

[0036] Add water for injection to 6000ml

[0037] A total of 2000 bottles

[0038] Method is with embodiment 1.

[0039] The sample properties are good, but the solubility is not good.

Embodiment 3

[0041] Leucovorin 100g

[0042] Mannitol 60g

[0043] Appropriate amount of sodium hydroxide (adjust the pH of sodium hydroxide solution (1mol / L) to 7.60)

[0044] Add water for injection to 3000ml

[0045] A total of 1500 bottles

[0046] The method is the same as in Example 1, wherein the aliquots of 2ml per bottle are packed in 10ml vials.

[0047] The formability of the sample is not good and the thickness is not enough.

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PUM

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Abstract

The invention provides a freeze-dried sterile injection powder containing an active component named levorotation folinic acid; the invention contains 9-100% levorotation folinic acid, 0-91% excipients acceptable in pharmacy or / and appropriate pH moderator. The pharmaceutical excipients refer to one or a plurality of mannitol, dextran, cane sugar, lactose, gelatin and phosphate. The pH moderator refers to one or a plurality of NaOH, natronite, kalium bicarbonicum, sodium phosphate, etc. The invention also relates to the preparation of the freeze-dried sterile injection powder. The invention avoids decomposition caused by high temperature sterilization in the process of levorotation folinic acid preparation, and is suitable for mass production; the invention is low in water content and stable when placed at room temperature, so the invention is suitable for long-term storage. The sterile injection powder of the invention can be taken as a synergist or attenuation agent in tumor chemotherapy.

Description

technical field [0001] The freeze-dried powder for injection containing levofolinic acid as the active pharmaceutical ingredient and its preparation method. The drug can be used as an attenuator of certain drugs such as methotrexate in tumor chemotherapy; it can be used as a synergist and attenuator of 5-fluorouracil drugs; it can also be used for megaloblastic anemia caused by folic acid deficiency. Background technique [0002] Folinic acid is a 5-formylated derivative of the reduced tetrahydrofolate (THF) of folic acid, and is the active substance of folic acid in vivo. Currently, folinic acid commonly used clinically is the equivalent racemate of the 6-position chiral carbon, and the active form in this raceme is 6-S (Levorotatory) type folinic acid, called levofolinic acid or L-folinic acid , and its dextrorotary form has no biological activity. Therefore, the clinical use of leucovorin can reduce the dosage by half compared with the use of folinic acid while maintain...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K9/19A61K47/10A61K47/02A61P43/00A61P35/00A61P7/06
Inventor 秦继红
Owner SHANGHAI HUILUN JIANGSU PHARM CO LTD
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