Sterile lyophilized preparation containing fosaprepitant, and preparation method thereof

A freeze-dried preparation, fosaprepitant dimeglumine technology, applied in the field of medicine, can solve the problems affecting the quality of life of patients, reducing treatment compliance, potential safety hazards, etc., and achieves accelerated experiments with good stability, safe use, and avoidance of The effect of security risks

Active Publication Date: 2012-10-31
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented new type of drug called Fosapertam (FOSP) can help treat cancer better than other drugs currently available on market today. It's easy to make it right before going through clinic trials because there are no harmful side effect or complications associated with current therapies like anthracycline agents that target DNA replication.

Problems solved by technology

This patents discusses different ways how cancer causes symptoms like nausebility due to chemical therapy drug usage. One method involves controlling these side effects through adjustments made based upon patient's needs. Another approach focuses on improving the dosage administered while avoiding harmful side effects associated with current methods.

Method used

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  • Sterile lyophilized preparation containing fosaprepitant, and preparation method thereof
  • Sterile lyophilized preparation containing fosaprepitant, and preparation method thereof
  • Sterile lyophilized preparation containing fosaprepitant, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Embodiment 1. prepare 1000 bottles of sterile lyophilized preparations containing 115mg fosaprepitant per bottle

[0056] formula:

[0057] Fosaprepitant dimeglumine 188g, polysorbate-80 57.5g, edetate disodium 14.4g, mannitol 287.5g, sodium hydroxide / hydrochloric acid (acidity regulator), add water for injection to a total of 4000mL.

[0058] Preparation Process:

[0059] 1) Liquid preparation: Weigh according to the formula, stir and dissolve 188g of fosaprepitant dimeglumine, 57.5g of polysorbate-80, 14.4g of edetate disodium, and 287.5g of mannitol in an appropriate amount of sterile water for injection Add sterile water for injection to 4000mL, adjust the pH value to 9.2 with 2mol / L sodium hydroxide solution and 0.1mol / L hydrochloric acid, then pass the liquid medicine through a sterile microporous filter membrane with a pore size of 0.22 microns, and pack 1000 Bottles are half-stoppered with halogenated butyl rubber and placed in a freeze dryer. Bacteria and end...

Embodiment 2

[0068] Embodiment 2. prepare 1000 bottles of sterile freeze-dried preparations containing 120mg fosaprepitant per bottle

[0069] formula:

[0070] Fosaprepitant dimeglumine 196.2g, polysorbate-20 65g, edetate disodium 16.5g, glucose 325g, sodium bicarbonate, add water for injection to a total of 5000mL.

[0071] Preparation Process:

[0072] 1) Liquid preparation: Weigh according to the formula, stir and dissolve 196.2 g of fosaprepitant dimeglumine, 65 g of polysorbate-20, 16.5 g of edetate disodium, and 325 g of glucose in an appropriate amount of sterile water for injection, Add sterile water for injection to 5000mL, adjust the pH value to 8.3 with 1mol / L sodium bicarbonate, then pass the liquid medicine through a sterile microporous filter membrane with a pore size of 0.22 microns, pack into 1000 bottles, and half stopper with halogenated butyl rubber Then put it into the freeze dryer, and the bacteria and endotoxins are strictly controlled during the whole process;

...

Embodiment 3

[0081] Embodiment 3. prepare 1000 bottles of sterile freeze-dried preparations containing 130mg fosaprepitant per bottle

[0082] formula:

[0083] Fosaprepitant dimeglumine 212.6g, polyethylene glycol 70g, triethanolamine 17.2g, sorbitol 332g, sodium hydroxide / hydrochloric acid, add water for injection to a total of 5000mL.

[0084] Preparation Process:

[0085] 1) Liquid preparation: Weigh according to the formula, stir and dissolve 212.6g of fosaprepitant dimeglumine, 70g of polyethylene glycol, 17.2g of triethanolamine, and 332g of sorbitol in an appropriate amount of sterile water for injection, add sterile Water for injection to 5000mL, adjust the pH value to 7.2 with 2mol / L sodium hydroxide solution / 0.1mol / L hydrochloric acid, then pass the liquid medicine through a sterile microporous filter membrane with a pore size of 0.22 microns, pack into 1000 bottles, half-stoppered and halogenated Put the butyl rubber stopper into the freeze dryer, and the bacteria and endotox...

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Abstract

The invention provides a sterile lyophilized preparation containing fosaprepitant, and a preparation method thereof. According to the invention, an effective dosage of fosaprepitant dimeglumine is adopted as an effective component, and auxiliary materials such as a solubilizer, a complexing agent, a lyophilization excipient, and an acidity adjusting agent are contained in the preparation. The lyophilization excipient does not comprise lactose, and is selected from one or a combination of mannitol, glucose, dextran, sorbitol, arginine, and glycine. The components are dissolved in injection water. The solution is sterilized, filtered, sub-packaged, and lyophilized. The prepared sterile lyophilized preparation has excellent high-temperature stability, illumination stability, and accelerated-experiment stability. When in use, the sterile lyophilized preparation provided by the invention is added into a solvent, so that an injection solution with an appropriate concentration is prepared and can be used. The preparation has good treatment effect upon chemotherapy-induced nausea and vomiting. With the form of injection medication, patient compliance is improved. The preparation process of the lyophilized preparation is simple. The lyophilized preparation is suitable for industrialized productions.

Description

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Claims

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Application Information

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Owner QILU PHARMA
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