Aprepitant nanocrystal suspension and preparation method and application thereof

A nano-crystal, aprepitant technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of poor stability of aprepitant nano-crystal liquid and harsh storage conditions. And other issues

Inactive Publication Date: 2019-11-22
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the poor stability of the aprepitant nano-crystallization liquid in the prior art, the harsh storage conditions, and the existing aprepitant preparations (tablets, capsules) are difficult to bring into play its drug effect in time defect, and provide a kind of aprepitant nano crystal suspension and its preparation method and application

Method used

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  • Aprepitant nanocrystal suspension and preparation method and application thereof
  • Aprepitant nanocrystal suspension and preparation method and application thereof
  • Aprepitant nanocrystal suspension and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0135] prescription:

[0136] Aprepitant 200mg Povidone K60 200mg Sodium dodecyl sulfate 50mg Croscarmellose Sodium 2.0g pregelatinized starch 4.0g sodium benzoate 0.2g sucrose 50g strawberry flavor 2mL

[0137] Preparation process: mix the prescribed amount of aprepitant with povidone K60 and sodium lauryl sulfate, add an appropriate amount of deionized water, and place it in a high-pressure homogenizer for 10 times (homogeneous pressure 1000bar) , to get aprepitant nano crystallization liquid (A liquid). The croscarmellose sodium solution (add boiling water to make the concentration 40mg / mL), pregelatinized starch slurry (add boiling water to make the concentration 80mg / mL), syrup (sucrose is made according to the pharmaceutically acceptable process to make 75% concentration of syrup), sodium benzoate and strawberry essence were placed in a stirring device and stirred evenly to obtain a blank suspension (liquid B)...

Embodiment 2

[0139] prescription:

[0140]

[0141]

[0142] Preparation process: After mixing the prescribed amount of aprepitant and methylcellulose solution (concentration: 1mg / mL), add an appropriate amount of deionized water, and place it in an experimental ball mill. After the zirconia beads were ground for 4 hours (grinding speed 500rpm), the aprepitant nanocrystal liquid (liquid A) was obtained. Corn starch slurry (add boiling water to make up to 80mg / mL), syrup (sucrose is made into a syrup with a concentration of 75% according to a pharmaceutically acceptable process), xanthan gum, poloxamer, methyl paraben, paraben Propyl ester, citric acid and orange essence were placed in a stirring device and stirred evenly to obtain a blank suspension (liquid B). Add liquid A to liquid B, mix evenly, add deionized water to make up the volume to 400mL, place it in a colloid mill and grind for 10 minutes to obtain the final oral suspension. The average particle diameter of the obtained...

Embodiment 3

[0144] prescription:

[0145]

[0146]

[0147] Preparation process: After mixing the prescribed amount of aprepitant, povidone K30 and methylcellulose solution (concentration is 1mg / mL), after adding an appropriate amount of deionized water, homogenize 10 times in a high-pressure homogenizer ( Homogeneous pressure 1000bar), get aprepitant nano-crystallization liquid (A liquid). Hypromellose solution (add boiling water to make a concentration of 20 mg / mL), carboxymethylcellulose sodium solution (add boiling water to make a concentration of 20 mg / mL), syrup (sucrose is prepared according to a pharmaceutically acceptable process for 75 % concentration of syrup), xanthan gum, methylparaben, sodium benzoate, disodium hydrogen phosphate, mannitol and strawberry essence were placed in a stirring device and stirred evenly to obtain a blank suspension (liquid B). Add liquid A to liquid B, mix evenly, add deionized water to make up the volume to 400mL, place it in a colloid mill...

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Abstract

The invention provides an aprepitant nanocrystal suspension and a preparation method and application thereof. The preparation method of the aprepitant nanocrystal suspension comprises the following steps that an aprepitant nanocrystal solution is added into blank material fluid for mixing, and the aprepitant nanocrystal suspension is obtained; the aprepitant nanocrystal solution is prepared from aprepitant nanocrystals and a stabilizer; and the blank material fluid comprises a thickening suspending agent, and the thickening suspending agent is one or more of syrup, sorbitol, xanthan gum, Arabic gum, starch slurry, cellulose class, povidone class, Tween 80 and poloxamer. According to the provided aprepitant nanocrystal suspension, the particle diameter of the aprepitant nanocrystal suspension has no obvious difference before and after being frozen, the stability is good, and the storage condition adaptability is good; and meanwhile the dissolving-out speed of the aprepitant nanocrystalsuspension is high, the oral bioavailability is higher than that of other aprepitant bulk drugs.

Description

technical field [0001] The invention relates to an aprepitant nano crystal suspension and a preparation method and application thereof. Background technique [0002] Aprepitant was first successfully developed by Merck and Co., Ltd. of the United States, and was approved by the U.S. FDA in 2003 (trade name ), which is the world's first neurokinin NK-1 receptor blocker, is mainly used for the prevention of postoperative vomiting and the prevention and control of vomiting after chemotherapy drugs. Its antiemetic complete control rate is 14.98% higher than that of serotonin receptor antagonist drugs. However, aprepitant is almost insoluble in water (3-7 μg / mL in pH 2-10 media), and its LogP at pH 7.0 is 4.8, so it belongs to BCS class IV drug according to the biopharmaceutical classification system , that is, low solubility and low permeability drugs. Such drugs have problems such as low bioavailability, which limits the efficacy of aprepitant, so it is urgent to develop an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/32A61K47/20A61K47/38A61K47/22A61K31/5377A61P1/08
CPCA61K9/10A61K31/5377A61K47/20A61K47/22A61K47/32A61K47/38A61P1/08
Inventor 涂亮星程勐奉建芳金一
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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