Terfenadine-beta-Cyclodextrin inclusion complex with antihistaminic activity enhancement

Drug Development and Industrial Pharmacy
H G ChoiC K Kim

Abstract

Terfenadine, an antihistaminic drug, has relatively low bioavailability after oral administration due to its limited solubility in water. To enhance the antihistaminic activity of terfenadine, the terfenadine-beta-cyclodextrin (1:2) inclusion complex was prepared by the neutralization method. The solubility and dissolution of the inclusion complex were carried out, and its antihistaminic activity was then evaluated and compared with terfenadine powder by the passive subcutaneous anaphylaxis method in rats. The formation constant of the inclusion complex was higher at lower pH, while its formation ratio was 1:2 irrespective of pH. For terfenadine, it improved the solubility 200 times and the dissolution rate 5 times. It gave a low histamine level at 30 min, followed by a sustained low level until 60 min, while terfenadine powder gave a low histamine level at 60 min, suggesting that it had faster and more effective antihistaminic activity than terfenadine powder in rats due to fast dissolution and absorption of terfenadine. It is concluded that this inclusion complex enhanced the antihistaminic activity of terfenadine following the enhanced solubility and dissolution of terfenadine.

References

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Citations

Dec 16, 2005·AAPS PharmSciTech·Rajeswari ChallaR K Khar
Feb 2, 2010·Biological & Pharmaceutical Bulletin·Dong Xun LiHan-Gon Choi
Apr 1, 2010·Journal of Pharmacy & Bioallied Sciences·Gaurav TiwariAwani K Rai
Jun 5, 2012·Journal of Microencapsulation·Roshan PradhanJong Oh Kim
Oct 11, 2012·Drug Development and Industrial Pharmacy·Gun Gook KimHan-Gon Choi
Oct 7, 2005·Drug Development and Industrial Pharmacy·Chul Soon YongHan-Gon Choi
Oct 22, 2014·Pharmaceutical Development and Technology·Mehdi RahimiAliasghar Behnamghader
May 31, 2012·International Journal of Pharmaceutics·Young Keun ChoiChul Soon Yong
Nov 30, 2004·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Chul Soon YongHan-Gon Choi
May 22, 2007·Journal of Cardiovascular Pharmacology·Ann MikhailZhi Su
Mar 21, 2007·Archives of Pharmacal Research·Balakrishnan PrabagarChul Soon Yong
May 4, 2012·Archives of Pharmacal Research·Hyung Hee BaekChul Soon Yong
May 28, 2009·Archives of Pharmacal Research·Young-Joon ParkHan-Gon Choi
Dec 12, 2012·Pharmaceutical Research·Alan B WattsRobert O Williams
May 7, 2011·Archives of Pharmacal Research·Hyung Hee BaekChul Soon Yong
May 7, 2011·Archives of Pharmacal Research·Si-Young JungHan-Gon Choi
Jun 5, 2014·Archives of Pharmacal Research·Roshan PradhanJong Oh Kim

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Anaphylaxis

Anaphylaxis is a serious allergic reaction that is rapid in onset and may cause death.