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A stable sodium folinate injection

A technology of sodium folinate and injection, applied in the directions of liquid delivery, emulsion delivery, antidote, etc., can solve the problem of not obtaining satisfactory results, and achieve the effect of reducing hydrolysis and oxidative decomposition, and preventing decomposition and deterioration.

Inactive Publication Date: 2011-11-30
CHONGQING Y S F PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, although there are many documents disclosing methods for improving the stability of tetrahydrofolate-related preparations, all of them have not obtained satisfactory results.

Method used

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  • A stable sodium folinate injection
  • A stable sodium folinate injection
  • A stable sodium folinate injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Effect of pH on Stability

[0027] According to the method of the above preparation process, when adjusting the pH, adjust to different pH values ​​in the following Table 1 to prepare the finished product, and the change of impurities after storage at 25°C for 10 days.

[0028]

[0029] Studies have shown that as the pH increases, the solubility of folinic acid increases. When the pH reaches 6.5, the drug is completely dissolved. When the pH is 7.8, it is the theoretical value for folinic acid to disodium folinate. Considering the reduction of blood vessel stimulation during injection, The pH should not be too high, and the above experiment also proves that the sodium folinate injection is relatively more stable when the pH is controlled between 6.5 and 8.5.

Embodiment 2

[0030] Embodiment 2: Sodium citrate is compared with other stabilizing agents on the influence of stability

[0031] The results are shown in the table below

[0032]

[0033] Prescription 1 used sodium citrate as a stabilizer, Prescription 2 added phosphate buffer saline, and Prescription 3 used tartaric acid instead of sodium citrate as a stabilizer.

[0034]

[0035] From the above results, after being placed at 25°C for 10 days, from the content point of view, they all decreased, and the degree of decline in prescription 1 and prescription 3 was relatively small. Therefore, it is judged that under its storage conditions (2-8°C), the change in content is acceptable.

Embodiment 3

[0036] Embodiment 3: the influence of the sodium citrate of different proportions on stability

[0037] The results are shown in the table below

[0038]

[0039] From the above results, the content ratio of the stabilizer sodium citrate to the main drug is in a linear relationship within a certain range of 0.0001: 1 to 5: 1, and the stability decreases with the reduction of the amount of sodium citrate, but without adding stabilizer When sodium citrate was added, the stability of the aqueous solution was even worse, which indicated that an appropriate amount of sodium citrate was very important for the long-term preservation of sodium folinate injection as a stabilizer. Especially when the weight ratio between the main ingredient and sodium citrate is 1:0.0005, the stability is the best.

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PUM

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Abstract

The invention relates to a stable sodium folinate injection, which contains folinic acid or its pharmaceutically acceptable salt as an active ingredient and water for injection, and it also contains leucovorin or its pharmaceutically acceptable salt as an active ingredient The weight ratio is a stabilizer of 0.0001:1-5:1, and the pH value of the injection is adjusted to 6.5-8.5 by using a pH regulator. The present invention thereby enables stable formulations of sodium folinate in high concentrations in physiologically compatible isotonic solutions.

Description

technical field [0001] The present invention relates to the preparation of aqueous solution for injection, which takes leucovorin or its pharmacologically acceptable salt as an active ingredient, in particular to a stable sodium folinate injection. Background technique [0002] Folinic acid is a known compound known by the alias 5-formyltetrahydrofolate. The calcium salt of this compound has been on the market abroad for many years, and it is mainly used clinically in combination with 5-fluorouracil as a synergist for the treatment of gastric cancer and colorectal cancer, and as a rescue drug for methotrexate overdose. Due to the presence of calcium ions, calcium folinate has poor solubility, which has certain limitations in clinical treatment. The performance is: when using clinically, 1% calcium folinate solution needs to be dissolved in 0.9% sodium chloride isotonic solution, which increases the total amount of medication and the amount of ions irrelevant to treatment; c...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/519A61K47/12A61P35/00A61P39/02
Inventor 杨杰杨玉华甘建新
Owner CHONGQING Y S F PHARMA
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