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Aprepitant intravenous injection emulsion as well as preparation method and application thereof

A technology of aprepitant and water for injection, applied in the field of pharmacy, can solve problems such as injection site pain and neuritis, achieve good fluidity, good stability, and improve the safety of clinical use

Pending Publication Date: 2019-02-22
GUANGZHOU HANFANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical intravenous ethanol may cause pain at the injection site, neuritis and other adverse reactions

Method used

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  • Aprepitant intravenous injection emulsion as well as preparation method and application thereof
  • Aprepitant intravenous injection emulsion as well as preparation method and application thereof
  • Aprepitant intravenous injection emulsion as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0041] In the aprepitant intravenous emulsion of this embodiment, every 1000 mL of the emulsion contains: 1.3 g of aprepitant, 100.0 g of refined soybean oil, 12 g of refined egg yolk lecithin, 2.5 g of oleic acid, an appropriate amount of 0.1N NaOH, and 25 g of glycerin , dilute to 1000mL with water for injection. Wherein, the proportion of refined soybean oil as the oil phase is 10%.

[0042] The preparation method of the present embodiment aprepitant intravenous emulsion is:

[0043] (1) Weigh the prescribed amount of refined soybean oil, refined egg yolk lecithin and oleic acid, stir to dissolve the emulsifier, add the prescribed amount of aprepitant, and heat in a water bath to 70°C as the drug-loaded oil phase for use;

[0044] (2) Weigh the prescribed amount of glycerin and add it to 800mL water for injection, and heat it in a water bath to 70°C as the water phase;

[0045] (3) Slowly add the oil phase to the water phase, keep the temperature at 70°C, shear at 8,000 r...

Embodiment 2

[0050] In the aprepitant intravenous emulsion of this embodiment, every 1000mL of the emulsion contains: 13g of aprepitant, 150g of refined olive oil, 50g of refined egg yolk lecithin, 2.5g of oleic acid, appropriate amount of 0.1N NaOH, 25g of glycerin, injection Dilute to 1000mL with water. Wherein, the proportion of refined olive oil as the oil phase is 15%.

[0051] The preparation method of the present embodiment aprepitant intravenous emulsion is:

[0052] (1) Weigh the prescribed amount of refined olive oil, refined egg yolk lecithin and oleic acid, stir to dissolve the emulsifier, add the prescribed amount of aprepitant, and heat to 75°C in a water bath as the drug-loaded oil phase;

[0053] (2) Weigh the prescribed amount of glycerin and add it to 700mL water for injection, and heat it in a water bath to 75°C as the water phase;

[0054] (3) Slowly add the oil phase to the water phase, maintain the temperature at 75°C, shear at 15,000 rpm for 5 minutes at high speed...

Embodiment 3

[0059] In the aprepitant intravenous injection emulsion of this embodiment, every 1000mL emulsion contains: 20g of aprepitant, 100g of refined soybean oil, 100g of refined olive oil, 100g of egg yolk phosphatidylcholine, 5g of sodium oleate, 0.1N NaOH Appropriate amount, glycerin 25g, water for injection and dilute to 1000mL. Wherein, the proportion of refined soybean oil and refined olive oil as the oil phase is 20%.

[0060] The preparation method of the present embodiment aprepitant intravenous emulsion is:

[0061] (1) Weigh the prescribed amount of refined olive oil, refined soybean oil, and egg yolk phosphatidylcholine, stir to dissolve the emulsifier, add the prescribed amount of aprepitant, and heat in a water bath to 75°C as the drug-loaded oil phase;

[0062] (2) Weigh the prescribed amount of glycerin and sodium oleate, add it to 800mL water for injection, and heat it in a water bath to 75°C as the water phase;

[0063] (3) Slowly add the oil phase to the water ph...

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Abstract

The invention relates to aprepitant intravenous injection emulsion as well as a preparation method and an application thereof, and belongs to the technical field of pharmaceutics. The aprepitant intravenous injection emulsion is prepared from components in percentage by mass as follows: 0.05%-3% of aprepitant, 5%-30% of an oil phase solvent, 1.2%-18% of an emulsifier, 0.03%-0.6% of a stabilizer and 1%-5% of an isoosmotic adjusting agent, the injection emulsion further contains a pH regulating agent and the balance of water for injection, and pH value of the injection emulsion is 5.5-8.0. The aprepitant intravenous injection emulsion contains no low-carbon chain alcohol such as ethanol and the like, meanwhile, the quality requirement for a marketed product can be met by technological innovation and adjustment, and clinical use safety of the aprepitant intravenous injection emulsion is greatly improved; direct intravenous injection is utilized during clinical using, and dilution is not needed; the aprepitant intravenous injection emulsion can be used for treating acute and tardive nausea and vomiting caused by high-dose cis-platinum combined high-dose sensitizing cancer chemotherapy,and nausea and vomiting in early stage and middle stage of tumor chemotherapy are reduced.

Description

technical field [0001] The invention relates to an aprepitant intravenous injection emulsion and a preparation method and application thereof, belonging to the technical field of pharmacy. Background technique [0002] According to the latest data released by WHO in 2017, 8.8 million people die from cancer every year worldwide, accounting for nearly one-sixth of the total number of deaths worldwide each year. There are more than 14 million new cases of cancer each year, and this number is expected to increase to more than 210 million by 2030. [0003] Currently, chemotherapy is considered to be one of the most important methods of cancer treatment. But when it comes to chemotherapy, it is its strong side effects of nausea and vomiting (Chemotherapy Induced Nausea and Vomiting, CINV). According to surveys, about 75% of chemotherapy drugs can cause symptoms such as nausea and vomiting, and about 70% to 80% of chemotherapy patients experience nausea and vomiting. Therefore, ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/24A61K47/12A61K31/5377A61P35/00A61P1/08
CPCA61K9/0019A61K9/107A61K31/5377A61K47/12A61K47/24A61P1/08A61P35/00
Inventor 袁诚许文东唐顺之何劼牛亚伟傅玉萍王国财关伟键牟肖男李遥
Owner GUANGZHOU HANFANG PHARMA
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