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Stable mycophenolate mofetil for injection, and preparation method thereof

A technology of mycophenolate mofetil and water for injection, which is applied in the field of mycophenolate mofetil for injection and its preparation, can solve the problems of accelerated degradation and unstable storage of mycophenolate mofetil for injection, and avoid The effect of reducing curative effect, convenient operation and simple process

Active Publication Date: 2017-07-14
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Mycophenolate mofetil is easy to degrade in water, especially when the temperature is increased, its degradation is accelerated; meanwhile, mycophenolate mofetil for injection is unstable during storage, and the preparations made by the prior art are all cannot solve the above problems

Method used

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  • Stable mycophenolate mofetil for injection, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Add 2000ml of water for injection pre-cooled to room temperature into the dispensing tank, add 250.0g of mycophenolate mofetil, 2.5g of citric acid, and 8012.5g of polysorbate in the prescribed amount, stir and mix well, and adjust the pH of the solution with 1M hydrochloric acid to 3.4. Add 30.0 g of disodium tetraborate, set the volume to 2500 ml, stir the solution until it becomes a colorless clear liquid; filter, fill, freeze-dry, and visually inspect to obtain the finished product.

[0024] The freeze-drying process is:

[0025] Pre-freezing: Raise the temperature of the slab to 30°C and keep it warm for 30 minutes; then lower the temperature of the slab to -45°C in 210 minutes and keep it warm for 390 minutes;

[0026] Sublimation drying: pump the vacuum in the box to 80mTorr, and keep it at -35°C for 30 minutes; use 150 minutes to raise the temperature of the plate layer to -17.5°C, and hold it for 540 minutes;

[0027] Re-drying: take 150 minutes to raise the t...

Embodiment 2

[0029] Add 2000ml of water for injection pre-cooled to room temperature into the dispensing tank, add 250.0g of mycophenolate mofetil, 2.5g of citric acid, and 8012.5g of polysorbate in the prescribed amount, stir and mix well, and adjust the pH of the solution with 1M hydrochloric acid to 3.4, add 50.0 g of disodium tetraborate, set the volume to 2500 ml, stir the solution until it becomes a colorless clear liquid; filter, fill, freeze-dry, and visually inspect to obtain the finished product.

[0030] The freeze-drying process is:

[0031] Pre-freezing: Raise the temperature of the slab to 40°C and keep it warm for 40 minutes; then lower the temperature of the slab to -35°C in 270 minutes and keep it warm for 450 minutes;

[0032] Sublimation drying: pump the vacuum in the box to 120mTorr, and keep it at -35°C for 90 minutes; take 210 minutes to raise the temperature of the plate layer to -12.5°C, and hold it for 660 minutes;

[0033] Re-drying: take 210 minutes to raise the...

Embodiment 3

[0035] Add 2000ml of water for injection pre-cooled to room temperature into the dispensing tank, add 250.0g of mycophenolate mofetil, 2.5g of citric acid, and 8012.5g of polysorbate in the prescribed amount, stir and mix well, and adjust the pH of the solution with 1M hydrochloric acid to 3.0, add 40.0g of disodium tetraborate, set the volume to 2500ml, stir the solution to a colorless and clear liquid; filter, fill, freeze-dry, and visually inspect to obtain the finished product.

[0036] The freeze-drying process is:

[0037] Pre-freezing: Raise the temperature of the slab to 35°C and keep it warm for 35 minutes; then use 240 minutes to lower the temperature of the slab to -40°C and hold it for 420 minutes;

[0038] Sublimation drying: pump the vacuum in the box to 100mTorr, and keep it at -40°C for 60 minutes; use 180 minutes to raise the temperature of the plate layer to -15°C, and hold it for 600 minutes;

[0039] Re-drying: take 180 minutes to raise the temperature of ...

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Abstract

The present invention relates to a stable mycophenolate mofetil freeze-drying composition for injection, wherein the composition is prepared from mycophenolate mofetil, citric acid, polysorbate 80, disodium tetraborate, a pH value adjuster, and water for injection. The preparation method comprises: adding a prescription amount of mycophenolate mofetil, citric acid and polysorbate 80 to a proper amount of water for injection, uniformly stirring and mixing, adjusting the pH value of the solution to 2.6-3.4 with 1 M hydrochloric acid, adding a prescription amount of disodium tetraborate, carrying out volume metering to achieve the total amount, stirring the solution until achieving a colorless and clear liquid, filtering, filling, carrying out freeze drying, and carrying out visual inspection so as to obtain the finished product. According to the present invention, the product is stable, such that the safety risk caused by the treatment effect reducing and the impurity increasing due to the drug degradation can be avoided; and the method has characteristics of simple process and simple operation, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a stable injection of mycophenolate mofetil and a preparation method thereof. Background technique [0002] About 70,000 people around the world receive organ transplants every year, most of which are kidney transplants. In China, more than 5,000 patients receive kidney transplants every year. How to improve the long-term survival rate of transplanted organs has always been a major problem in the medical field. The human immune system has the ability to recognize "self" and "non-self". Usually, it only produces an immune response to foreign antigens, but immune tolerance to self-antigens. Therefore, the immune system's rejection of allografted organs hinders the success of organ transplantation. Although the immunosuppressive regimen composed of macrolide antibiotic structure immunosuppressants, calcineurinase inhibitors, and adrenal cortex hormones has bee...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/5377A61K47/02A61K47/12A61K47/26A61P37/06
CPCA61K9/0019A61K9/19A61K31/5377A61K47/02A61K47/12A61K47/26
Inventor 张贵民董其松任英
Owner SHANDONG NEWTIME PHARMA
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