Loaded aprepitant nanocrystal lipid microcapsule and preparation method thereof

An aprepitant nanometer and lipid microcapsule technology, applied in the field of medicine, can solve the problems of poor absorption, low solubility of aprepitant, low bioavailability, etc., and achieves low preparation cost, good in vivo absorption, and high biological The effect of utilization

Active Publication Date: 2016-04-06
FUREN PHARMA GROUP +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the low solubility of aprepitant, poor absorption, low bioavailability, and the shortcomings of the aprepitant suspension prepared by other methods, and to provide a lipid microparticle containing aprepitant nanocrystals. Capsule new dosage form; Another object is to provide its preparation method

Method used

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  • Loaded aprepitant nanocrystal lipid microcapsule and preparation method thereof
  • Loaded aprepitant nanocrystal lipid microcapsule and preparation method thereof
  • Loaded aprepitant nanocrystal lipid microcapsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] After mixing 20 mg of aprepitant and 10 mg of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, add an appropriate amount of deionized water and grind in a P7 miniature planetary high-energy ball mill for 60 minutes (grinding for 15 minutes, intermittent 10 minutes, cycled 4 times), the aprepitant nanocrystal suspension was obtained, and the concentration of aprepitant was 0.5 mg / ml. The average particle size of the aprepitant nanocrystals was determined to be 280nm. Dissolve 200mg of soybean lecithin in an appropriate amount of absolute ethanol, add the above-mentioned aprepitant nanocrystal suspension to emulsify, freeze-dry to make aprepitant nanocrystal lipid microcapsules, and measure its average particle size to be 130 μm .

Embodiment 2

[0022] Disperse 50 mg of aprepitant and 18850 mg of poloxamer in an appropriate amount of deionized water, and use an M-110L high-pressure micro-fluidic nano-homogenizer to homogenize for 10 cycles under the pressure of 9000 PSI to obtain aprepitant nanocrystal suspension agent, the concentration of aprepitant is 0.5mg / ml. The average particle size of the aprepitant nanocrystals was determined to be 380nm. Dissolve 300mg soybean lecithin and 200mg lecithin in an appropriate amount of absolute ethanol, add the above-mentioned aprepitant nanocrystal suspension to emulsify, freeze-dry to make aprepitant nanocrystal lipid microcapsules, and measure the average The particle size is 150 μm.

Embodiment 3

[0024] Aprepitant 20mg and polyvinylpyrrolidone K2515mg were mixed evenly and pulverized by a high-speed airflow mill, and then dispersed in an appropriate amount of deionized water to obtain aprepitant nanocrystal suspension. The concentration of aprepitant was 1.0mg / ml. The average particle size of the aprepitant nanocrystals was determined to be 475nm. Dissolve 100mg soybean phospholipid and 50mg hydrogenated phospholipid in an appropriate amount of absolute ethanol, add the above-mentioned aprepitant nanocrystal suspension to emulsify, spray dry to make aprepitant nanocrystal lipid microcapsules, and measure the average The particle size is 420 μm.

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Abstract

The invention relates to a loaded aprepitant nanocrystal lipid microcapsule and a preparation method thereof, and belongs to the technical field of a medicine. The microcapsule is prepared by the method comprising the following steps: preparing an aprepitant nanocrystal from aprepitant by virtue of a grinding process, high-speed air jet pulverization or high-pressure homogenization, then mixing and emulsifying the aprepitant nanocrystal with phospholipid, removing a liquid phase and drying so as to obtain the aprepitant nanocrystal lipid microcapsule. The prepared loaded aprepitant nanocrystal lipid microcapsule can improve the stability of the aprepitant nanocrystal and the lipid loaded nanocrystal can increase the speed and the amount of being absorbed by gastrointestinal mucosa of a body, so that the effects of relatively high bioavailability and accelerated development of efficacy are achieved; and the preparation method of the loaded aprepitant nanocrystal lipid microcapsule is mild in condition, simple and controllable, low in preparation cost and is suitable for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a lipid microcapsule carrying aprepitant nanocrystals, and also relates to a preparation method of the lipid microcapsule. Background technique [0002] Aprepitant is clinically used for acute and delayed nausea or vomiting after chemotherapy. It is the first neurokinin-1 (neurokinin-1, NK-1) receptor antagonist approved by the US FDA. Substance P can be blocked by binding to NK-1 receptors, thereby treating vomiting, depression and other related diseases mediated by substance P. However, the solubility of aprepitant in water is only 0.55 μg / m1, the gastrointestinal absorption is low, and the oral bioavailability is low, which limits the efficacy of aprepitant. Therefore, it is necessary to study an effective dosage form and technology to improve the oral absorption of aprepitant. [0003] Nanocrystal technology, which reduces drug crystals to nanoscale, is a novel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/5377A61K47/24A61P1/08A61P25/24
CPCA61K9/5015A61K31/5377
Inventor 朱松林肖艳孟庆乐赵永星崔浩陈永强方水霞潘娜陈水库梁倩罗峰刘金霞岳晓慧
Owner FUREN PHARMA GROUP
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