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Mechanism studies on solubility enhancement of ibuprofen by complexation with nicotinamide
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Pei-ya SHEN1, Hai-tao DOU1, Shuai QIAN1, Jian-jun ZHANG2, Yuan GAO1, *
Acta Pharmaceutica Sinica | 2019, 54(1) : 41 - 47
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Acta Pharmaceutica Sinica | 2019, 54(1): 41-47
• Special Reports: Promoting the Dissolution of Poorly Soluble Drugs •
Mechanism studies on solubility enhancement of ibuprofen by complexation with nicotinamide
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Pei-ya SHEN1, Hai-tao DOU1, Shuai QIAN1, Jian-jun ZHANG2, Yuan GAO1, *
Affiliations
  • 1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 211198, China
  • 2. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 211198, China
Published: 2019-01-12 doi: 10.16438/j.0513-4870.2018-0786
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The aim of this study is to investigate the effect of nicotinamide (NIC) on the solubility/dissolution of a poorly soluble drug ibuprofen (IBU), and to explore the mechanism of the formed soluble complex by complexation model, fluorescence quenching and Raman spectroscope. The results showed that NIC could significantly improve the solubility of IBU, and exhibited an Ap type complexation profile. The calculated complexation constants of K1:1 and K1:2 were 0.24 and 4.00, respectively. In the solution, the fluorescent intensity of IBU gradually decreased with the increase of NIC, exhibiting the typical fluorescence-quenching phenomenon. The Raman spectrum showed stretching vibrations, bending vibrations, and rocking vibrations ascribed to benzene ring of IBU and pyridine ring of NIC disappeared or significantly shifted, suggested that the soluble complex was formed by dipole-dipole interaction force between the benzene group on IBU and pyridine group on NIC, resulting in the aqueous solubility enhancement of IBU. In comparison to IBU alone, the physical mixture of IBU and NIC showed significantly higher dissolution rate (1.6-fold) and extent.

ibuprofen  /  nicotinamide  /  complex  /  solubility  /  fluorescence
Pei-ya SHEN, Hai-tao DOU, Shuai QIAN, Jian-jun ZHANG, Yuan GAO. Mechanism studies on solubility enhancement of ibuprofen by complexation with nicotinamide[J]. Acta Pharmaceutica Sinica, 2019 , 54 (1) : 41 -47 . DOI: 10.16438/j.0513-4870.2018-0786
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Article Info
doi: 10.16438/j.0513-4870.2018-0786
  • Receive Date：2018-08-27
  • Online Date：2026-01-26
  • Published：2019-01-12
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  • Received：2018-08-27
  • Revised：2018-10-29
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Affiliations
    1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 211198, China
    2. Department of Pharmaceutics, 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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