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Effect of crystal form and filler on the compressibility of clarithromycin
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Heng-qing ZHU1, Xiao-fang GAO2, Dao-yi ZHENG2, Wen-hui MENG2, Zun-ting PANG1, Yuan GAO1, *
Acta Pharmaceutica Sinica | 2021, 56(11) : 3166 - 3172
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Acta Pharmaceutica Sinica | 2021, 56(11): 3166-3172
• Original Articles •
Effect of crystal form and filler on the compressibility of clarithromycin
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Heng-qing ZHU1, Xiao-fang GAO2, Dao-yi ZHENG2, Wen-hui MENG2, Zun-ting PANG1, Yuan GAO1, *
Affiliations
  • 1. School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China
  • 2. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China
Published: 2021-11-12 doi: 10.16438/j.0513-4870.2021-0600
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Clarithromycin (CLA) belongs to the second generation macrolide antibiotic. The commercial crystal form of CLA is form Ⅱ, and it exhibits the poor compressibility during the tablet pressing process. Since the crystal form of drugs has a significant effect on their mechanical properties, from the perspective of crystallography, this study investigated the difference of the compressibility between CLA form Ⅰ and form Ⅱ, and analyzed the mechanism that led to such difference. On the other hand, from the perspective of pharmaceutics, we also studied the effect of filler on the compressibility of form Ⅱ. It was found that CLA form Ⅰ had improved plastic deformation than form Ⅱ because of the slip planes in its crystal structure leading to the better compressibility. Moreover, microcrystalline cellulose, pre-gelatinized starch and lactose monohydrate could improve the compressibility of form Ⅱ, and microcrystalline cellulose showed the best effect. We improve the compressibility of CLA from crystal form and filler, and also lay a foundation for the development of CLA solid preparations.

clarithromycin  /  compressibility  /  polymorphism  /  slip plane  /  filler
Heng-qing ZHU, Xiao-fang GAO, Dao-yi ZHENG, Wen-hui MENG, Zun-ting PANG, Yuan GAO. Effect of crystal form and filler on the compressibility of clarithromycin[J]. Acta Pharmaceutica Sinica, 2021 , 56 (11) : 3166 -3172 . DOI: 10.16438/j.0513-4870.2021-0600
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Article Info
doi: 10.16438/j.0513-4870.2021-0600
  • Receive Date：2021-04-22
  • Online Date：2025-12-18
  • Published：2021-11-12
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History
  • Received：2021-04-22
  • Revised：2021-06-23
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Affiliations
    1. School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China
    2. School of Pharmacy, China Pharmaceutical University, Nanjing 211198, 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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