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Aprepitant nanosuspension and preparation method thereof

A technology of aprepitant nanometer and nanosuspension, which is applied in the field of medicine, can solve the problems of high cost, debris pollution of grinding machines, and restrictions on the popularization and use of aprepitant, and achieves low preparation cost and high preparation method conditions. mild effect

Active Publication Date: 2013-08-21
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The aprepitant tablet currently on the market uses grinding technology to reduce the particle size of the aprepitant raw material to the nanometer level and prepare it into a nanosuspension, which improves the oral absorption of aprepitant, but the cost of this technology Very high, and there will be debris pollution from the grinder, which limits the promotion and use of aprepitant

Method used

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  • Aprepitant nanosuspension and preparation method thereof

Examples

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Effect test

Embodiment 1

[0019] Dissolve 0.1 g of aprepitant and 0.01 g of copovidone PVP S 630 in 50 mL of absolute ethanol, slowly add 0.01 g of PVP K-90 into 1000 mL of water, evaporate at 40°C, and evaporate the ethanol , to obtain aprepitant nanosuspension, the concentration of aprepitant is 0.1 mg / ml. The average particle size of the aprepitant nanosuspension was determined to be 490 nm, and the suspension remained stable within 48 h.

Embodiment 2

[0021] Dissolve 0.1 g of aprepitant and 0.05 g of copovidone PVP S 630 in 60 mL of 95% ethanol, slowly add 0.05 g of PVP K-90 into 350 mL of water, evaporate at 40°C, and evaporate the ethanol , to obtain aprepitant nanosuspension, the concentration of aprepitant is 0.3 mg / ml. Measure the average particle diameter of aprepitant nanosuspension, the result is 113 nm (the transmission electron microscope figure of aprepitant nanosuspension is shown in figure 1 ), the suspension remained stable within 48 h.

Embodiment 3

[0023] Dissolve 0.1 g of aprepitant and 0.02 g of copovidone PVP S 630 in 30 mL of absolute ethanol, slowly add 0.02 g of PVP K-90 into 200 mL of water, evaporate at 40°C, and evaporate the ethanol , to obtain aprepitant nanosuspension, the concentration of aprepitant is 0.5 mg / ml. The average particle size of the aprepitant nanosuspension was determined to be 322 nm, and the suspension remained stable within 48 h.

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Abstract

The invention belongs to the technical field of medicines, and discloses an aprepitant nanosuspension and a preparation method thereof. As aprepitant is small in solubility in water and lower in the oral bioavailability, popularization and use of aprepitant are limited. The aprepitant nanosuspension provided by the invention is characterized by comprising aprepitant, copovidone PVPS630 and povidone PVPK-90 by mass ratio of (4-10):(1-2):(1-2). The preparation method of the aprepitant nanosuspension is mild in condition and simple and controllable, and higher oral bioavailability of aprepitant is realized.

Description

technical field [0001] The invention relates to an aprepitant nano-suspension and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Aprepitant is an effective drug for chemotherapy vomiting. The solubility of aprepitant in water is very small, and the oral bioavailability is low, which limits the efficacy of aprepitant. Therefore, it is very necessary to study effective dosage forms and techniques to improve the oral absorption of aprepitant. [0003] Nanosuspension refers to a dosage form in which drug particles are dispersed in an aqueous solution containing a stabilizer with a nanoscale particle size. And it can be solidified by post-treatment processes such as spray drying and freeze drying, and further prepared into various dosage forms according to different administration routes, such as tablets, pills, capsules, etc. Since the drug in the nanosuspension is in a solid state, it can be made into a high-dose ins...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/5377A61K47/32A61P1/08
Inventor 罗瑞雪张振海
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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