Preparation method of fosaprepitant dimeglumine freeze-dried preparation for injection

A technology of fosaprepitant dimeglumine and freeze-dried preparations, which is applied in the field of preparation of fosaprepitant dimeglumine freeze-dried preparations for injection, and can solve the problems of slow redissolving, slow redissolving and poor clarity of products and other problems, to achieve the effect of loose products, stable quality and good clarity

Inactive Publication Date: 2011-08-31
WUHAN LEADPHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Prepare the fosaprepitant dimeglumine preparation for injection according to the conventional method, because there is a large temperature gradient inside the product during pre-freezing, resulting in more solutes in the upper layer, higher density, lower density and loose structure, so The appearance of the product shrinks, and the reconstitution is slow and the clarity is poor
To solve this problem, proppants such as mannitol and dextran 40 can be added to the prescription. Although the appearance of the product can be slightly improved to a certain extent, it still cannot solve the problems of slow redissolution and poor clarity of the product

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Taking 100 bottles of fosaprepitant dimeglumine freeze-dried preparation for injection as an example, the specific preparation method is:

[0019] Weigh 5.75g of Tween 80, 1.44g of EDTA, 28.75g of anhydrous lactose, add 800ml of water for injection, heat and stir at 50°C to dissolve, add 18.8g of the main drug (approximately equivalent to 11.5g of fosaprepitant) , stir to completely dissolve fosaprepitant dimeglumine, let cool to room temperature, adjust the pH value to 7.5 with sodium hydroxide, filter with a 0.22 μm microporous membrane, add water to 1000ml, measure the pH value, and divide after the content is qualified. Packed, then freeze-dried at low temperature according to the following procedures:

[0020] A. Pre-freezing: firstly cool down the temperature of Fosaprepitant Dimeglumine Injection to -12°C, start freezing with temperature difference oscillation, the amplitude is -8°C to -17°C, and the time is 32 minutes, then cool down to -35°C, and then Shake an...

Embodiment 2

[0024] Prepare 0.115g fosaprepitant dimeglumine injection according to conventional methods, then carry out low-temperature freeze-drying according to the following procedures:

[0025] A. Pre-freezing: first cool down the temperature of Fosaprepitant Dimeglumine Injection to -14°C, start freezing with temperature difference oscillation, the amplitude is -8°C to -17°C, and the time is 22 minutes, then cool down to -35°C, and then Shake and freeze, the amplitude is -27°C to -37°C, the time is 42 minutes, then the temperature of the product is reduced to -52°C, and the temperature is kept for 1 hour.

[0026] B. Sublimation: After the pre-freezing process of the product is completed, start the vacuum machine to evacuate to 12 Pa, raise the temperature of the product to -35°C, and keep it warm for 6 hours; then start to fill the box with nitrogen intermittently, and control the vacuum at 17-22 Pa, shake for 1.5 hours, then raise the temperature of the product to -25°C, and keep i...

Embodiment 3

[0029] Prepare 0.115g fosaprepitant dimeglumine injection according to conventional methods, then carry out low-temperature freeze-drying according to the following procedures:

[0030] A. Pre-freezing: first cool down the temperature of Fosaprepitant Dimeglumine Injection to -14°C, start freezing with temperature difference oscillation, the amplitude is -8°C to -17°C, and the time is 42 minutes, then cool down to -36°C, and then Shake and freeze, with an amplitude of -27°C to -37°C, for 542 minutes, then the temperature of the product drops to -42°C, and keep warm for 2 hours.

[0031] B. Sublimation: After the pre-freezing process of the product is completed, start the vacuum machine to evacuate to 14 Pa, raise the temperature of the product to -35°C, and keep it warm for 7 hours; then start to fill the box with nitrogen intermittently, and control the vacuum at 17-22 Pa, shake for 1 hour, then raise the temperature of the product to -25°C, and keep it warm for 18 hours.

...

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PUM

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Abstract

A fosaprepitant dimeglumine freeze-dried preparation prepared by adopting the invention has the characteristics of porosity, stable quality, high redissolution speed, good clarity and the like. The invention provides a preparation method of a fosaprepitant dimeglumine freeze-dried preparation for injection, which comprises the following steps: (A) pre-freezing: firstly, cooling a fosaprepitant dimeglumine injection to (-12)-(-14) DEG C, and freezing through temperature oscillation; and then, cooling to (-32)-(-35) DEG C, and oscillating and freezing for 42-62 minutes; (B) sublimating: vacuumizing in a box body until the air pressure is 12-17 Pa, heating a product to (-35)-(-37) DEG C, and preserving the temperature for 8-10 hours; and intermittently injecting nitrogen gas, oscillating for 1-1.5 hours by taking air pressure (17-22 Pa) in the box body as an amplitude, heating the product to (-25)-(-29) DEG C, and preserving the temperature for 15-18 hours; and (C) drying: gradually heating the medicament to 38-42 DEG C, and preserving the temperature for 1-2 hours.

Description

technical field [0001] The invention relates to a drug fosaprepitant dimeglumine for treating vomiting caused by chemotherapy, in particular to a preparation method of a freeze-dried formulation of fosaprepitant dimeglumine for injection. Background technique [0002] Fosaprepitant dimeglumine is a substance P / neurokinin 1 (NK-1) receptor antagonist used in the treatment of chemotherapy-induced nausea and vomiting (CINV). It is suitable for intravenous injection in combination with other antiemetic drugs to prevent acute and delayed nausea and vomiting caused by initial and repeated administration of moderately emetic and high-dose emetic anticancer drug chemotherapy (including high-dose cisplatin). This product is the prodrug of aprepitant (aprepitant) oral preparation, which is rapidly converted into aprepitant in the body after injection. [0003] Prepare the freeze-dried preparation of fosaprepitant dimeglumine for injection according to the conventional method. The pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/675A61K31/5375A61P1/08
Inventor 陈洁
Owner WUHAN LEADPHARM TECH CO LTD
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