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Preparation of tadalafil-dapoxetine coamorphous complex with evaluation of dissolution and physical stability
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Ya-jing SHEN1, Lei QIN1, Wei-li HENG2, Jian-jun ZHANG2, Shuai QIAN1, Yuan GAO1, *
Acta Pharmaceutica Sinica | 2018, 53(7) : 1162 - 1168
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Acta Pharmaceutica Sinica | 2018, 53(7): 1162-1168
• ORIGINAL ARTICLES·Pharmaceutics •
Preparation of tadalafil-dapoxetine coamorphous complex with evaluation of dissolution and physical stability
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Ya-jing SHEN1, Lei QIN1, Wei-li HENG2, Jian-jun ZHANG2, Shuai QIAN1, Yuan GAO1, *
Affiliations
  • 1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
  • 2. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
Published: 2018-07-12 doi: 10.16438/j.0513-4870.2018-0260
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Tadalafil (TD), a phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction, has a low oral bioavailability due to its extremely poorly aqueous solubility. The aim of this study was to enhance its solubility and dissolution by coamorphization with dapoxetine (DP), a selective serotonin reuptake inhibitor to manage premature ejaculation. Coamorphous TD-DP (molar ratio, 1:1) was prepared by solvent-evaporation method and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared spectroscopy (FTIR). The supersaturated dissolution of TD from coamorphous TD-DP was investigated in various aqueous media and compared to that of crystalline TD. In addition, physical stability of coamorphous system was also evaluated under the conditions of 40℃/75% relative humidity (RH) and 25℃/60% RH for 90 days. DSC thermogram and PXRD pattern indicated the formation of the coamorphous TD-DP. In comparison to original TD crystal, the dissolution of TD from coamorphous system were significantly enhanced in various media (water, 0.01 mol·L-1 HCl and pH 4.5 phosphate buffer). In addition, no crystallization phenomenon of the prepared coamorphous system was observed until 90 days' storage under 25℃/60% RH. However, when temperature and humidity were increased to 40℃/75% RH, the coamorphous TD-DP was recrystallized easily.

tadalafil  /  dapoxetine  /  coamorphous  /  dissolution rate  /  physical stability
Ya-jing SHEN, Lei QIN, Wei-li HENG, Jian-jun ZHANG, Shuai QIAN, Yuan GAO. Preparation of tadalafil-dapoxetine coamorphous complex with evaluation of dissolution and physical stability[J]. Acta Pharmaceutica Sinica, 2018 , 53 (7) : 1162 -1168 . DOI: 10.16438/j.0513-4870.2018-0260
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Year 2018 volume 53 Issue 7
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Article Info
doi: 10.16438/j.0513-4870.2018-0260
  • Receive Date：2018-03-27
  • Online Date：2026-01-15
  • Published：2018-07-12
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History
  • Received：2018-03-27
  • Revised：2018-05-02
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Affiliations
    1. Department of Traditional Chinese Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China
    2. Department of 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
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Family		 属数
Number of
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Number of
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Percentage of
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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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