A kind of aseptic freeze-dried powder of fosaprepitant dimeglumine for injection and preparation process thereof

A technology for fosaprepitant dimeglumine and injection, which is applied in the field of sterile freeze-dried powder of fosaprepitant dimeglumine for injection and its preparation, can solve problems such as inability to guarantee drug stability, and achieve avoidance Allergy and hemolysis, low cost, simple and controllable preparation method

Active Publication Date: 2018-09-04
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, the main function of lactose as an excipient is to maintain the properties of the drug after freeze-drying, and has a certain stabilizing effect on the active ingredient fosaprepitant dimeglumine. In terms of maintaining the properties of the drug, the excipient commonly used in the freeze-drying process Agents mannitol, dextran, sorbitol and amino acids have similar effects, but the stability of the drug during storage cannot be guaranteed, especially the stability during long-term storage

Method used

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  • A kind of aseptic freeze-dried powder of fosaprepitant dimeglumine for injection and preparation process thereof
  • A kind of aseptic freeze-dried powder of fosaprepitant dimeglumine for injection and preparation process thereof
  • A kind of aseptic freeze-dried powder of fosaprepitant dimeglumine for injection and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021]

[0022] Weigh 180 g each of fosaprepitant dimeglumine and hydroxypropyl-β-cyclodextrin, put them into a clean container, add 200 ml of water for injection, grind for 30 minutes, add water to 4 L, and stir to dissolve. Use hydrochloric acid or sodium hydroxide solution to adjust the pH to 9.0, add 4g of activated carbon for needles, stir and absorb for 15 minutes, filter out the activated carbon for needles, sterilize and filter, divide the drug solution into vials, each bottle contains 4ml, freeze Just do it.

Embodiment 2

[0024]

[0025] Weigh 250g of fosaprepitant dimeglumine and 750g of sulfobutyl-β-cyclodextrin into a clean container, add 700ml of water for injection into it, grind for 50 minutes, add water to 6L, and stir to dissolve. Use hydrochloric acid or sodium hydroxide solution to adjust the pH to 8.0, add 6g of activated carbon for needles, stir and absorb for 15 minutes, filter out the activated carbon for needles, sterilize and filter, divide the drug solution into vials, each bottle contains 6ml, freeze Just do it.

Embodiment 3

[0027]

[0028] Weigh 200g of fosaprepitant dimeglumine and 1000g of glucosyl-β-cyclodextrin into a clean container, add 1000ml of water for injection into it, grind for 50 minutes, add water to 5L, and stir to dissolve. Use hydrochloric acid or sodium hydroxide solution to adjust the pH to 10.0, add 5g of activated carbon for needles, stir and absorb for 15 minutes, filter out the activated carbon for needles, sterilize and filter, divide the drug solution into vials, each bottle contains 5ml, freeze Just do it.

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Abstract

The invention particularly relates to a sterile freeze-dried fosaprepitant-dimeglumine powder for injection and a preparation process of the sterile freeze-dried fosaprepitant-dimeglumine powder. The sterile freeze-dried fosaprepitant-dimeglumine powder for injection comprises an active component, a solubilizing agent and a pH-value adjusting agent, wherein the active component is fosaprepitant dimeglumine. The preparation process of the sterile freeze-dried fosaprepitant-dimeglumine powder for injection is simple and feasible and is suitable for scale production. The sterile freeze-dried fosaprepitant-dimeglumine powder for injection has high quality and excellent stability and can be stored for a long time.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a sterile freeze-dried powder of fosaprepitant dimeglumine for injection and a preparation process 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. This product, like aprepitant, belongs to the human substance P / neurokinin 1 (NK-1) selective high-affinity receptor blocker, which mainly acts by blocking the nausea and vomiting signals in the brain. In animal models, aprepitant inhibits emesis induced by cytotoxic chemotherapeutic drugs such as cisplatin through central nervous effects. Animal and human positron emission tomography (PET) studies have shown that aprepitant penetrates the blood-brain barrier and occupies the brain NK-1 receptor. Animal and clinical studies have shown that aprepitant increases the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/40A61K31/675A61P1/08
Inventor 赵志全赵震震王钏舟张丽萍
Owner SHANDONG NEWTIME PHARMA
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