Abstract
Introduction of matrix type sustained release systems were a breakthrough for novel oral drug delivery systems. Present research focuses on the development and evaluation of Fentanyl citrate sustained release formulations. It is a potent, sparingly soluble synthetic opioid analgesic with rapid onset and short duration of action. Considering the half-life of the drug which is 1.5 h, there is a strong clinical need and market potential for delivery systems that will deliver drug in controlled and prolonged manner. A number of strategies were planned for formulation development and evaluation such that they demonstrate robust stability and in vitro-in vivo performance using putative hydrophilic polymer HPMC (HPMCK 15M) in combination with hydrophobic polymer Ethyl cellulose N10. A Central composite design was employed to get an optimum formulation suitable for once a day administration. Effects of formulation variables, hydrodynamic conditions and agitational variations on drug release profile were also investigated. Drug release mechanisms using various mathematical kinetic models are discussed. The developed matrix tablets were successfully prepared without the need for functional coating thus promising to be a cost effective formulation with high commercial probability.
Highlights
Sustained release matrix tablets are relatively easy to fabricate by incorporating drug molecules in slowly disintegrating or inert porous materials, versatile, effective and at low cost (Basak, Reddy, & Mani, 2006; Kumar, Bhowmik, Srivastava, Paswan, & Dutta, 2012; Patel, Panchal, Patel, Brahmbhatt, & Suthar, 2011)
Hydrophilic polymer matrix is widely used in case of sustained release formulations of water insoluble drug (Reddy, Mutalik, & Reddy, 2003)
Sustained release matrix tablets of this opioid were prepared by wet granulation technique using Central composite design (CCD), where the effect of independent variables, HPMCK 15M and Ethyl cellulose on dependent response variables such as percent drug released at 2, 12 and 24 h were considered to get an optimized formulation for once a day administration and the selection for it was made on the basis of T50%
Summary
Sustained release matrix tablets are relatively easy to fabricate by incorporating drug molecules in slowly disintegrating or inert porous materials, versatile, effective and at low cost (Basak, Reddy, & Mani, 2006; Kumar, Bhowmik, Srivastava, Paswan, & Dutta, 2012; Patel, Panchal, Patel, Brahmbhatt, & Suthar, 2011). These delivery systems are designed to achieve therapeutically effective concentrations of drug in the systemic circulation over an extended period of time, achieving better patient compliance and allowing reduction of both the total dose of drug administered and the incidence of adverse effects (Perucca, 2009). The technique requires minimum experimentation and time, proving to be far more effective and lucrative than the conventional methods of formulating sustained release dosage forms (Singh, Dahiya, Saharan, & Ahuja, 2005b)
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