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Fosaprepitant dimeglumine freeze-dried powder injection and preparation method thereof

A technology of fosaprepitant dimeglumine and freeze-dried powder injection, which is applied in the field of fosaprepitant dimeglumine freeze-dried powder injection and its preparation, can solve the problem of affecting the filtration speed and filling accuracy, and affecting the medication Safety, production inconvenience and other issues, to achieve the effect of improving sterilization filtration speed and filling volume accuracy, ensuring drug stability, and avoiding foam generation

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

However, Tween 80 is prone to hemolysis reaction, which affects the safety of medication, and as a surfactant, it produces serious foam during stirring, which affects the filtration speed and filling accuracy, and brings a lot of inconvenience to production.
[0009] (2) Fosaprepitant dimeglumine has good compatibility with lactose, but poor compatibility with other excipients such as mannitol and dextran. However, lactose is prone to lactose intolerance for certain populations, especially Asian populations. Affect drug safety

Method used

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  • Fosaprepitant dimeglumine freeze-dried powder injection and preparation method thereof
  • Fosaprepitant dimeglumine freeze-dried powder injection and preparation method thereof
  • Fosaprepitant dimeglumine freeze-dried powder injection and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Fosaprepitant dimeglumine 200g Citric acid 5g Sodium citrate 5g Water for Injection Add to 5L

[0030] Preparation Process:

[0031] (1) 0.5L of tert-butanol is mixed with 2.5L of water for injection, heated to 60°C, and 200g of fosaprepitant dimeglumine is weighed and added thereto, and the stirring speed is set to 80r / min, and stirred until clarification;

[0032] (2) Weigh 5 g of citric acid and 5 g of sodium citrate, add 1.5 L of water for injection to dissolve, add 15 g of activated carbon for injection, heat to 50 ° C and stir for 15 minutes, decarbonize and filter to clarify;

[0033] (3) Mix the solutions (1) and (2), add water for injection to volume, cool to room temperature, sterilize, filter, fill, and freeze-dry in a freeze-drying machine. The freeze-drying curve is: the shelf is cooled to - 40°C and maintained for 4 hours to freeze the medicinal liquid; turn on the vacuum pump to make the vacuum in the freeze-drying box 20...

Embodiment 2

[0036] Fosaprepitant dimeglumine 200g Citric acid 7g Sodium citrate 8g Water for Injection Add to 5L

[0037] Preparation Process:

[0038] (1) 0.3L of tert-butanol is mixed with 3.0L of water for injection, heated to 50° C., and the recipe quantity Fosaprepitant dimeglumine is weighed and added therein, and the stirring speed is set to 60r / min, and stirred until clarification;

[0039] (2) Weigh 7g of citric acid and 8g of sodium citrate, add 1.5L water for injection to dissolve, add 15g of activated carbon for injection, heat to 55°C and stir for 15 minutes, decarbonize and filter to clarify;

[0040](3) Mix the solutions (1) and (2), add water for injection to volume, cool to room temperature, sterilize, filter, fill, and freeze-dry in a freeze-drying machine. The freeze-drying curve is: the shelf is cooled to - 45°C and hold for 4 hours to freeze the medicinal liquid; turn on the vacuum pump to make the vacuum in the freeze-drying box 60Pa...

Embodiment 3

[0043] Fosaprepitant dimeglumine 200g Citric acid 10g Sodium citrate 10g Water for Injection Add to 5L

[0044] Preparation Process:

[0045] (1) 0.4L of tert-butanol is mixed with 2.6L of water for injection, heated to 45°C, and the recipe quantity Fosaprepitant dimeglumine is weighed and added therein, and the stirring speed is set to 70r / min, and stirred until clarification;

[0046] (2) Weigh 10 g of citric acid and 10 g of sodium citrate, add 1.5 L of water for injection to dissolve, add 15 g of activated carbon for injection, heat to 60 ° C and stir for 15 minutes, decarbonize and filter to clarify;

[0047] (3) Mix the solutions (1) and (2), add water for injection to volume, cool to room temperature, sterilize, filter, fill, and freeze-dry in a freeze-drying machine. The freeze-drying curve is: the shelf is cooled to - 45 ℃ and maintain for 6 hours to make the liquid freeze solid; turn on the vacuum pump to make the vacuum in the freez...

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Abstract

The present invention relates to a fosaprepitant dimeglumine freeze-dried powder injection and a preparation method thereof, wherein the fosaprepitant dimeglumine freeze-dried powder injection comprises an active component fosaprepitant dimeglumine and a stabilizer so as to avoid the use of Tween 80 and lactose and improve the product safety. According to the present invention, during the preparation process, the solubility of fosaprepitant dimeglumine is increased by using the tert butyl alcohol-water cosolvent, such that the concentration required by the preparation is achieved so as to meet the production requirement; and the generation of foams is avoided during the preparation process, such that the sterilization and filtration rate and the filling accuracy are improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a freeze-dried powder injection of fosaprepitant dimeglumine and a preparation method thereof. Background technique [0002] Fosaprepitant Dimeglumine (Fosaprepitant Dimeglumine), is a prodrug of aprepitant (aprepitant), it is rapidly converted into aprepitant in the body after injection, which can increase the 5-HT3 receptor blocker Antiemetic effects of dansetron and the glucocorticoid dexamethasone, inhibition of cisplatin-induced emesis in the acute and late phases. [0003] Fosaprepitant dimeglumine was approved for marketing in the United States in January 2008, and its trade name is EMEND. The dosage form is sterile lyophilized powder for injection. and the UK marketed under the trade name IVEMEND. According to FDA instructions, its prescription contains lactose, polysorbate-80, disodium edetate, hydrochloric acid / sodium hydroxide and othe...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/675A61K47/10A61K47/12A61P1/08
CPCA61K9/0019A61K9/19A61K31/675A61K47/10A61K47/12
Inventor 张贵民赵震震董其松
Owner SHANDONG NEWTIME PHARMA
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