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Improving In Vitro Performance of Roflumilast by Polymeric Carrier Systems

Author(s): M. Idrees, A. Afzal, M. Sarfraz*, M. Farooq, N. Koser, R. Kulsoom and R. Kausar
Faculty of Pharmacy, 1Faculty of Allied Health Sciences, University of Lahore, Lahore, Punjab 54600, 2ILM College of Pharmaceutical Sciences, Sargodha, Sargodha 40100, Pakistan

Correspondence Address:
M. Sarfraz, Faculty of Pharmacy, 1Faculty of Allied Health Sciences, University of Lahore, Lahore, Punjab 54600, Pakistan, E-mail:

Roflumilast, a selective phosphodiesterase 4 inhibitor, was approved by the European Medicines Agency Committee for Medicinal Products for Human Use in 2010 for the treatment of severe chronic obstructive pulmonary disease. However, low solubility of Roflumilast is a question mark to design a suitable dosage form to get therapeutic objectives. The aim of this work was to enhance solubility of the drug to develop fast release oral tablet. Drug-polymer binary system was developed at 1:1 w/w ratio followed by development of immediate release tablet by direct compression method. Drug-polymer compatibility studies were assessed by Fourier-transform infrared spectroscopy, X-ray Diffraction, thermogravimetric analysis, and scanning electron microscopic studies. Pre and Post-compression tests and in vitro dissolutions studies in acidic (pH 1.2) and PBS pH 6.8 were performed to evaluate in vitro performance of the developed formulations. In vitro kinetic models were applied and similarity and difference factors were computed in comparison with reference product (marketed brand). Drug content was found between 95.37 to 99.57 in the developed formulations. Drug-polymer compatibility results demonstrated good compatibility among drug, polymers and other excipients. The micromeretic parameters and post compression studies results were in acceptable limit for all the developed formulations. Fast drug release behavior was observed in acidic medium. The results suggested that similarity factor (f2) values of the developed formulations were within acceptable limit (50-100). The developed binary systems may apply to overcome solubility issues of biopharmaceutical classification system class II drugs. The developed formulations are easy to scale-up.

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