Dissolution rate improvement of telmisartan through modified MCC pellets using 32 full factorial design

Abstract

Microcrystalline cellulose (MCC) is the most widely used excipient for the production of pellets but it retards the release of poorly water soluble drugs. The present investigation reports incorporation of camphor, cross carmellose sodium (CCS) and spray dried lactose (SDL) into MCC pellets to enhance the dissolution rate of telmisartan. A full factorial design (3) was used in the study. Concentration of camphor and CCS was selected as independent variables whereas percentage porosity and percentage drug release at 60 min were selected as dependent variables. Pellets were produced by extrusion-spheronization technique and evaluated for percentage yield, particle size analysis, flow characteristics, percentage porosity, drug content and drug release. Contour plots and 3-D surface plots were presented for graphical expression of the results. Pellet formulations exhibited acceptable morphological, flow and mechanical properties. As against to 38.54% drug release after 60 min with MCC pellets, pellets prepared with optimized formulation, composed of proper combination of MCC, SDL, camphor and CCS, released 100% drug after 60 min. Our study underlines the fact that dissolution of telmisartan from MCC pellets can be successfully enhanced by incorporating water soluble excipient, disintegrant and pore formers.

Hot-Melt Extruded Amorphous Solid Dispersion for Solubility, Stability, and Bioavailability Enhancement of Telmisartan

“…Specifically, sodium hydroxide, (NaOH, a strong alkalizer), povidone (K25, widely used as binder and tablet disintegrant), and meglumine (a solubilizing agent) which could have resulted in higher solubility, therefore, enhanced the dissolution profile of the commercial formulation compared to the F8 tablets. Addition of a few excipients such as strong alkalizer (NaOH), super disintegrant, or solubilizing agents may increase the release kinetics of TEL from the F8 tablets as reported in the prior literature [ 30 , 42 ]. However, the study aims to address the stability issue observed with the marketed formulation (MICARDIS ® ) and meanwhile, enhance the solubility and bioavailability of poorly soluble TEL.…”

Development of Liquisolid Tablets of Chlorpromazine using 32 Full Factorial Design

“…4, Y = b 0 +b 1 X 1 +b2X 2 +b 12 X 1 X 2 +b 11 X 1 2 +b 22 X 2 2 , where, Y is the measured response associated with each factor level combination; b 0 is an intercept; b 1 to b 22 are regression coefficients computed from the observed experimental values of Y, and X 1 and X 2 are the coded levels of independent variables. The terms X 1 X 2 and Xi 2 (i = 1, and 2) represent the interaction and quadratic terms, respectively [21] . The dependent and independent variables selected are shown in Table 2 along with their low, medium and high levels.…”

Physical characterization of multiparticulate systems

“…Obtention of immediate-release systems, with a focus on masking drug flavor (Hamedelniel, Bajdik, Pintye-Hódi, 2010;Issa et al, 2012b;Patel, Patel, Patel, 2010);  Controlled-release (Abbaspour, Sadeghi, Garekani, 2008;Bialleck, Rein, 2011;Cantor, Hoag, Augsburger, 2009a;Cantor, Hoag, Augsburger, 2009b;Franc et al, 2015;Ghanam, Kleinebudde, 2011;Ghosh, Chakraborty, 2013;Han et al, 2013;Heckötter et al, 2011;Hung et al, 2015;Ríos, Ghaly, 2015;Roblegg et al, 2011;Szkutnik-Fiedler et al, 2014;Wang et al, 2015;Xu, Liew, Heng, 2015;You et al, 2014);  Improvement in dissolution of poorly soluble drugs (Abdalla, Mader, 2007;Abdalla, Klein, Mader, 2008;Chopra, Venkatesan, Betageri, 2013;Ibrahim, El-Badry, 2014;Lu et al, 2009;Patel et al, 2016);  Gastro-retentive systems/ floating systems (Amrutkar, Chaudhari, Patil, 2012;Li et al, 2014;Pagariya, Patil, 2013;Qi et al, 2015;Zhang et al, 2012);  Enteric release/gastro-resistant systems (Andreo-Filho et al, 2009;Ghanam, Kleinebudde, 2011;Pund et al, 2010);  Improvement of plant extract or active ingredient stability (Araújo-Junior et al, 2013;Beringhs et al, 2012;Bu...…”