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Aprepitant emulsion

A kind of aprepitant emulsion, emulsion technology, applied in emulsion delivery, drug combination, organic active ingredients and other directions, can solve problems such as increased technical requirements, increased emulsion viscosity, increased technological difficulty, etc., to overcome technical difficulties, Increased stability and easy filtration and sterilization

Pending Publication Date: 2020-07-10
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the high emulsifier content, the viscosity of the emulsion increases, not only the production cost increases, but also the technical requirements increase and the process difficulty increases

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] Table 2

[0072] Element Dosage (g) Concentration (wt%) weight ratio to aprepitant Aprepitant 2.34g 0.721 1 egg yolk lecithin 32.5g 10 13.9:1 ethanol 9g 2.773 3.8:1 Soybean oil 30.6g 9.429 13.1:1 sodium oleate 1.8g 0.555 0.77:1 sucrose 18g 5.546 7.7:1 Water for Injection 230.3g 70.976 98.4:1 Absolute ethanol* 30g / /

[0073] *Solvent added in formulation but removed during preparation of oil phase;

[0074] Preparation Process:

[0075] 1) Mix 2.34g of aprepitant and 32.5g of egg yolk lecithin, add 30g of ethanol, fill with nitrogen protection, and dissolve the mixture by heating and stirring for 30min at 65°C and 200rpm; place the mixture on a rotary evaporator , 65 ° C under reduced pressure rotary steaming for 10 min to remove ethanol; add 9 g of ethanol and 30.6 g of soybean oil for injection to the resulting solution, fill with nitrogen protection, continue heating and stirring at ...

Embodiment 2

[0082] table 3

[0083] Element Dosage (g) Concentration (wt%) weight ratio to aprepitant Aprepitant 2.34g 0.721 1 egg yolk lecithin 29.2g 9 12.5:1 ethanol 9g 2.773 3.8:1 Soybean oil 30.6g 9.429 13.1:1 sodium oleate 1.8g 0.555 0.77:1 sucrose 18g 5.546 7.7:1 Water for Injection 233.5g 71.976 99.8:1 Absolute ethanol* 30g / /

[0084] *Solvent added in formulation but removed during preparation of oil phase;

[0085] Preparation Process:

[0086] 1) Mix 2.34g of aprepitant and 29.2g of egg yolk lecithin, add 30g of ethanol, fill with nitrogen protection, and dissolve the mixture by heating and stirring for 30min at 65°C and 200rpm; place the mixture on a rotary evaporator , 65 ° C under reduced pressure rotary steaming for 10 min to remove ethanol; add 9 g of ethanol and 30.6 g of soybean oil for injection to the resulting solution, fill with nitrogen protection, continue heating and stirring at 6...

Embodiment 3

[0102] table 5

[0103] Element Dosage (g) Concentration (wt%) weight ratio to aprepitant Aprepitant 2.34g 0.721 1 egg yolk lecithin 32.5g 10 13.8:1 Soybean oil 30.6g 9.429 13.1:1 sodium oleate 1.8g 0.555 0.77:1 sucrose 18g 5.546 7.7:1 Water for Injection 239.3g 73.749 102.3:1 Absolute ethanol* 30g / /

[0104] *Solvent added in formulation but removed during preparation of oil phase;

[0105] Preparation Process:

[0106] 1) Mix 2.34g of aprepitant and 32.5g of egg yolk lecithin, add 30g of ethanol, fill with nitrogen protection, and dissolve the mixture by heating and stirring for 30min at 65°C and 200rpm; place the mixture on a rotary evaporator , 65 ° C under reduced pressure rotary steaming for 30 min, remove ethanol; add 30.6 g of soybean oil for injection to the resulting solution, fill with nitrogen protection, continue heating and stirring at 65 ° C and 200 rpm for 10 min to prepare the oil ph...

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Abstract

The invention discloses a stable aprepitant emulsion for injection. The aprepitant emulsion comprises aprepitant, an emulsifier, a co-emulsifier, injection oil, a tension adjusting agent, a pH value adjusting agent and injection water, wherein the weight ratio of the emulsifier to the aprepitant is (12-1)-(14:1); the content of the emulsifier is 9-10wt%; and the pH value is within 8.0-9.5. The medicine preparation is a stable oil-in-water emulsion, has a small particle size and good physical stability, and is applicable to non-oral treatment on patients suffering from high / medium vomiting cancer chemotherapy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a stable aprepitant emulsion for injection and a preparation process. Background technique [0002] The chemical name of aprepitant is 5-[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluoro Phenyl)morpholin-4-ylmethyl]-3,4-dihydro-2H-1,2,4-triazol-3-one has a chemical structure shown in formula I: [0003] [0004] Aprepitant is a typical representative of NK-1 receptor antagonist antiemetic drugs, which is used to prevent acute or delayed nausea and vomiting caused by highly emetogenic chemotherapy. Its effect of reducing nausea and vomiting is superior to other drugs; it has no serious adverse reactions and has good safety. In China, aprepitant is only available in oral capsules, but due to the nausea and vomiting experienced by chemotherapy patients, its compliance is poor when taken orally, and the absorption and bioavailabil...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/24A61K47/10A61K31/5377A61P1/08
CPCA61K9/0019A61K9/107A61K47/24A61K47/10A61K31/5377A61P1/08
Inventor 乔建斌王栋海周志超杨清敏张明会
Owner QILU PHARMA
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