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Effect of different preparation processes on the properties of aprepitant solid dispersions
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Bing-xi WANG1, Ting CHEN2, Jing YANG3
Chinese Journal of New Drugs | 2023, 32(21) : 2191 - 2197
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Chinese Journal of New Drugs | 2023, 32(21): 2191-2197
Effect of different preparation processes on the properties of aprepitant solid dispersions
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Bing-xi WANG1, Ting CHEN2, Jing YANG3
Affiliations
  • 1Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
  • 2Shanghai Zhitong Biomedical Technology Co., Ltd., Shanghai 201203, China
  • 3East China University of Science and Technology, Shanghai 200237, China
Published: 2023-11-15
Outline
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Objective:

To establish an analytical method for determination of the content and dissolution of aprepitant, prepare aprepitant solid dispersion by three different preparation methods (hot-melt extrusion, solvent-melt method and spray drying method), and investigate the effects of different processes on the physical stability of the solid dispersions.

Methods:

The effects of different preparation processes on the stability of aprepitant solid dispersions were measured in terms of water content, moisture attraction, residual microcrystals, aprepitant content, related impurities, and in vitro release.

Results:

Among the three different processes, the aprepitant solid dispersion prepared by hot-melt extrusion had low water content, poor moisture attraction, drug in amorphous form, good in vitro dissolution behavior, able to dissolve and release in acid solution, resistant to crystallization and precipitation behavior due to pH change and maintained high supersaturation after transit to the intestine.

Conclusion:

Hot-melt extrusion is the optimal preparation method for solid dispersions composed of crystallization inhibitor HPMCAS and dissolution enhancer PVP K30.

aprepitant  /  solid dispersion  /  preparation process  /  in vitro dissolution
Bing-xi WANG, Ting CHEN, Jing YANG. Effect of different preparation processes on the properties of aprepitant solid dispersions[J]. Chinese Journal of New Drugs, 2023 , 32 (21) : 2191 -2197 .
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Year 2023 volume 32 Issue 21
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Article Info
  • Online Date：2026-03-05
  • Published：2023-11-15
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History
  • Accepted：2023-04-10
Affiliations
    1Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
    2Shanghai Zhitong Biomedical Technology Co., Ltd., Shanghai 201203, China
    3East China University of Science and Technology, Shanghai 200237, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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