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Enhanced dissolution and intestinal absorption of adefovir dipivoxil by cocrystal formation with acetaminophen
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Pei-shen QIU1, Jing GAO2, Shuai QIAN2, Yuan-feng WEI2, Jian-jun ZHANG1, *
Acta Pharmaceutica Sinica | 2018, 53(6) : 993 - 1001
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Acta Pharmaceutica Sinica | 2018, 53(6): 993-1001
• Medicinal Chemistry Pharmaceutics •
Enhanced dissolution and intestinal absorption of adefovir dipivoxil by cocrystal formation with acetaminophen
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Pei-shen QIU1, Jing GAO2, Shuai QIAN2, Yuan-feng WEI2, Jian-jun ZHANG1, *
Affiliations
  • 1. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
  • 2. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
Published: 2018-06-12 doi: 10.16438/j.0513-4870.2018-0062
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In current study, adefovir dipivoxil (AD)-acetaminophen (AP) cocrystal (molar ratio, 1:1) was prepared by slow evaporation from acetonitrile, followed by physicochemical characterizations using differential scanning calorimetry, powder X-Ray diffraction and Fourier transform infrared spectroscopy. Molecular modeling showed that the phosphoester group of AD was connected with the amide group of AP through hydrogen bonds. In comparison to crystalline AD, the solubility and dissolution rate of AD from AD-AP cocrystal were significantly enhanced by 1.5-fold and 1.6-fold, respectively. In addition, based on the rat single-pass intestinal perfusion study, the permeabilities of AD in various intestinal sections (i.e., duodenum, jejunum, ileum and colon) were significantly improved (e.g., about 3-fold enhancement in duodenum) after cocrystallization with AP by inhibiting P-glyprotein mediated efflux of AD, which will benefit absorption in vivo and subsequent oral bioavailability of poorly permeable drug AD.

adefovir dipivoxil  /  acetaminophen  /  cocrystal  /  dissolution rate  /  intestinal permeability
Pei-shen QIU, Jing GAO, Shuai QIAN, Yuan-feng WEI, Jian-jun ZHANG. Enhanced dissolution and intestinal absorption of adefovir dipivoxil by cocrystal formation with acetaminophen[J]. Acta Pharmaceutica Sinica, 2018 , 53 (6) : 993 -1001 . DOI: 10.16438/j.0513-4870.2018-0062
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Article Info
doi: 10.16438/j.0513-4870.2018-0062
  • Receive Date：2018-01-16
  • Online Date：2026-01-15
  • Published：2018-06-12
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History
  • Received：2018-01-16
  • Revised：2018-03-08
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Affiliations
    1. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
    2. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, 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
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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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