Unlock instant, AI-driven research and patent intelligence for your innovation.

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, which can solve the inconvenience of production and affect the filtration speed and filling accuracy , hemolytic reactions, etc.

Active Publication Date: 2021-08-31
SHANDONG NEWTIME PHARMA
View PDF7 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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
Comparison scheme
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) Mix 0.5L of tert-butanol with 2.5L of water for injection, heat to 60°C, weigh 200g of fosaprepitant dimeglumine, add it, set the stirring speed to 80r / min, and stir until clear;

[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 needles, heat to 50 ° C and stir for 15 minutes, decarbonize and filter until clarified;

[0033] (3) Mix the solutions (1) and (2), add water for injection to constant volume, cool to room temperature, sterilize and filter, fill, put into a lyophilizer to lyophilize, and the lyophilization curve is: cool the shelf to - Keep at 40°C for 4 hours to freeze the medicinal solution; turn on the vacuum pump to make the vacuum in the freeze-drying box to 20Pa; heat the shelf to -10°C for 2 ho...

Embodiment 2

[0036] fosaprepitant dimeglumine 200g citric acid 7g sodium citrate 8g Water for Injection Add to 5L

[0037] Preparation Process:

[0038] (1) Mix 0.3L of tert-butanol with 3.0L of water for injection, heat to 50°C, weigh the prescribed amount of fosaprepitant dimeglumine, add it, set the stirring speed to 60r / min, and stir until clear;

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

[0040](3) Mix the solutions (1) and (2), add water for injection to constant volume, cool to room temperature, sterilize and filter, fill, put into a lyophilizer to lyophilize, and the lyophilization curve is: cool the shelf to - Keep at 45°C for 4 hours to freeze the medicinal liquid; turn on the vacuum pump to make the vacuum in the freeze-drying box to 60Pa; heat the shelf to ...

Embodiment 3

[0043] fosaprepitant dimeglumine 200g citric acid 10g sodium citrate 10g Water for Injection Add to 5L

[0044] Preparation Process:

[0045] (1) Mix 0.4L of tert-butanol with 2.6L of water for injection, heat to 45°C, weigh the prescribed amount of fosaprepitant dimeglumine, add it, set the stirring speed to 70r / min, and stir until clear;

[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 needles, heat to 60°C and stir for 15 minutes, decarbonize and filter until clarified;

[0047] (3) Mix the solutions (1) and (2), add water for injection to constant volume, cool to room temperature, sterilize and filter, fill, put into a lyophilizer to lyophilize, and the lyophilization curve is: cool the shelf to - Keep at 45°C for 6 hours to freeze the medicinal solution; turn on the vacuum pump to make the vacuum in the freeze-drying box 100Pa; heat the shelf ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a freeze-dried powder injection of fosaprepitant dimeglumine for injection and a preparation method thereof. The powder injection is composed of the active ingredient fosaprepitant dimeglumine and a stabilizer, avoiding the use of Tween 80 and lactose, and improving the safety of the product. In the preparation process, tert-butanol-water is used to form a co-solvent to increase the solubility of fosaprepitant dimeglumine, so that it reaches the concentration required for the preparation, which meets the production needs, and avoids the generation of foam during the preparation process, which improves the sterilization Filtration speed and filling volume accuracy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a fosaprepitant dimeglumine freeze-dried powder injection and a preparation method thereof. Background technique [0002] Fosaprepitant Dimeglumine (Fosaprepitant Dimeglumine), is the prodrug of aprepitant (aprepitant), which is rapidly converted into aprepitant in the body after injection, which can increase the angina of the 5-HT3 receptor blocker. Antiemetic effects of dansetron and the glucocorticoid dexamethasone in suppressing cisplatin-induced emesis in the acute and late phases. [0003] Fosaprepitant dimeglumine was approved for marketing in the United States in January 2008. Its product name is EMEND. Its dosage form is sterile freeze-dried powder for injection, with two specifications of 115mg and 150mg. It is also available in Sweden, Czech Republic and Portugal. and the United Kingdom, the trade name is IVEMEND. According to the FDA ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/675A61K47/10A61K47/12A61P1/08
CPCA61K9/0019A61K9/19A61K31/675A61K47/10A61K47/12
Inventor 陈小兵王赛琪赵静赵震震董其松
Owner SHANDONG NEWTIME PHARMA