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Rheology guided the preparation of suvorexant-copovidone solid dispersions via hot melt extrusion technology
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Peng ZHAO1, 2, Cong-hui LI2, Si-yi SHUAI2, Bing YANG2, Hui ZHANG2, Nan LIU2, Zeng-ming WANG2, Yong-jun WANG1, *, Ai-ping ZHENG2, *
Acta Pharmaceutica Sinica | 2024, 59(8) : 2396 - 2403
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Acta Pharmaceutica Sinica | 2024, 59(8): 2396-2403
Original Articles
Rheology guided the preparation of suvorexant-copovidone solid dispersions via hot melt extrusion technology
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Peng ZHAO1, 2, Cong-hui LI2, Si-yi SHUAI2, Bing YANG2, Hui ZHANG2, Nan LIU2, Zeng-ming WANG2, Yong-jun WANG1, *, Ai-ping ZHENG2, *
Affiliations
  • 1. Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China
  • 2. State Key Laboratory of National Security Specially Needed Medicines, Academy of Military Medical Sciences, Beijing 100850, China
Published: 2024-08-12 doi: 10.16438/j.0513-4870.2024-0019
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The rheological properties of drug and carrier materials have a wide range of guiding significance for the formulation and process development of solid dispersions. In this study, the rheological properties of materials with different drug carrier ratios were systematically studied with suvorexant as the model drug and copovidone as the carrier material, which provided a sufficient basis for determining the formulation and process of solid dispersions. The optimal suvorexant-copovidone ratio obtained by oscillating temperature scanning was 1∶4. If the ratio is greater than 1∶ 4, the glass transformation temperature of the material will increase significantly, and the solubilization effect of the solid dispersion will show a downward trend. The results of oscillation temperature scanning and oscillation temperature sweep can show that when the extrusion temperature is greater than 150 ℃, the viscosity of the material is less than 10 000 Pa·s, and the melt can be extruded smoothly, and the best extrusion temperature of 160-180 ℃ can be obtained by combining the dissolution results. Finally, the dissolution of suvorexant tablets guided by rheological property studies in multiple media is similar to that of the commercially available tablets Belsomra. Therefore, rheological studies can screen and optimize the formulation and process of suvorexant solid dispersions at the mechanism level, which is of great significance to improve the success rate of R & D and shorten the R & D cycle of solid dispersions prepared by hot melt extrusion.

rheology  /  hot melt extrusion  /  suvorexant  /  solid dispersion  /  glass transition temperature  /  viscosity
Peng ZHAO, Cong-hui LI, Si-yi SHUAI, Bing YANG, Hui ZHANG, Nan LIU, Zeng-ming WANG, Yong-jun WANG, Ai-ping ZHENG. Rheology guided the preparation of suvorexant-copovidone solid dispersions via hot melt extrusion technology[J]. Acta Pharmaceutica Sinica, 2024 , 59 (8) : 2396 -2403 . DOI: 10.16438/j.0513-4870.2024-0019
Year 2024 volume 59 Issue 8
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Article Info
doi: 10.16438/j.0513-4870.2024-0019
  • Receive Date:2024-01-09
  • Online Date:2025-11-26
  • Published:2024-08-12
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History
  • Received:2024-01-09
  • Revised:2024-04-18
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Affiliations
    1. Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China
    2. State Key Laboratory of National Security Specially Needed Medicines, Academy of Military Medical Sciences, Beijing 100850, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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