Composition for injection containing fosaprepitant dimeglumine and preparation method thereof

A kind of technology of fosaprepitant dimeglumine and sharpitant dimeglumine, which is applied to the freeze-dried preparation of fosaprepitant dimeglumine for injection and the field of preparation thereof, and can solve the time-consuming and time-consuming freeze-drying process. energy and other problems, to achieve the effect of stable product quality, simple and controllable process, and energy saving

Active Publication Date: 2014-09-17
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The freeze-drying process adopted by this method consumes time and ener

Method used

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  • Composition for injection containing fosaprepitant dimeglumine and preparation method thereof
  • Composition for injection containing fosaprepitant dimeglumine and preparation method thereof
  • Composition for injection containing fosaprepitant dimeglumine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Each 1000 vials of lyophilized preparation contains

[0050]

[0051] Add water for injection to the total volume of the solution (2500ml)

[0052]Add lactose, edetate disodium, and Tween-80 into water for injection (above 50°C) accounting for 80% of the total volume of the solution, dissolve, adjust the pH value to 7.0-8.5, and obtain a solution of excipients, cool to 20- 30°C, standby; add fosaprepitant dimeglumine to the auxiliary material solution to dissolve, keep the liquid at 10-30°C, adjust the pH value to 8.4, add activated carbon for decarburization, and add ethanol to account for 2% of the total volume of the solution 5%, dilute to the full volume with water for injection, filter aseptically through a 0.22um filter membrane, fill the filtrate in a vial with a half stopper and send it to a freeze-drying box, close the box door, and close the suction valve. Turn on the freezer, wait for the temperature of the product to reach below -40°C, and keep it warm f...

Embodiment 2

[0055] Each 1000 vials contains the following ingredients before lyophilization

[0056]

[0057]

[0058] Add water for injection to the total volume of dosing (1917ml)

[0059] Add lactose, edetate disodium, and Tween-80 into water for injection (above 50°C) accounting for 80% of the total volume of the solution, dissolve, adjust the pH value to 7.0-8.5, and obtain a solution of excipients, cool to 20- 30°C, standby; Fosaprepitant dimeglumine is added to the auxiliary material solution to dissolve, the liquid is kept at 10-30°C, and the pH value is adjusted to 8.6. After adding activated carbon for decarburization, the amount of ethanol added accounts for 2% of the total volume of the solution. 10%, dilute to the full volume with water for injection, filter aseptically through a 0.22um filter membrane, fill the filtrate in a vial and put it into a freeze-drying box, close the door tightly, and close the suction valve. Turn on the freezer, wait for the temperature of t...

Embodiment 3

[0062] Each 1000 vials contains the following ingredients before lyophilization

[0063]

[0064] Add water for injection to the total volume of the solution (2500ml)

[0065] Add lactose, edetate disodium, and Tween-80 into water for injection (above 50°C) accounting for 80% of the total volume of the solution, dissolve, adjust the pH value to 7.0-8.5, and obtain a solution of excipients, cool to 20- 30°C, standby; add fosaprepitant dimeglumine to the auxiliary material solution to dissolve, keep the liquid at 10-30°C, adjust the pH value to 8.4, add activated carbon for decarburization, and add ethanol to account for 2% of the total volume of the solution 10%, dilute to the full volume with water for injection, filter aseptically through a 0.22um filter membrane, fill the filtrate in a vial and put it into a freeze-drying box, close the door tightly, and close the suction valve. Turn on the freezer, wait for the temperature of the product to reach below -40°C, and keep i...

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Abstract

The invention provides a pharmaceutical composition containing fosaprepitant dimeglumine and a preparation method thereof. The pharmaceutical composition is composed of fosaprepitant dimeglumine, lactose, disodium edentate and tween-80, wherein a mass ratio among the fosaprepitant dimeglumine, the disodium edentate, the tween-80 and the lactose is 188-245.3:14.4-18.8:57.5-75:287.5-375. The composition is prepared in an aqueous containing alcohol in a freeze-drying manner. The preparation method is simple and controllable in processes and can reduce energy consumption. The pharmaceutical composition, prepared by the preparation method in the invention, is stable in quality and can ensure safety of clinical medication.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a freeze-dried preparation of fosaprepitant dimeglumine for injection and a preparation method thereof. Background technique [0002] The chemical name of fosaprepitant dimeglumine is: [3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethylphenyl)ethoxy] -3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-one-1H-1,2,4-triazol-1-yl]phosphate Di(N-methyl-D-glucosamine) salt, the chemical structure is shown in formula-I. [0003] [0004] Fosaprepitant dimeglumine for injection is a chemotherapeutic antiemetic drug, and it is suitable for the prevention and treatment of acute and severe complications caused by initial and repeated administration of moderate and large doses of emetic anticancer chemotherapy drugs (including high doses of cisplatin) when used in combination with other antiemetic drugs. and late nausea and vomiting. Fosaprepitant dimeglumine is ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/675A61K47/10A61P1/08
Inventor 赵小伟宗在伟杜有国刘小东
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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