Enhancement of Solubility of Tadalafil by Cocrystal Approach

Abstract

Cocrystallization is an emerging method to optimize physicochemical properties of pharmaceutically active compounds including dissolution rate and stability. The main aim of this study was to increase the solubility by cocrystal approach and characterize the cocrystals (1:1) involving tadalafil and salicylic acid which were prepared by solvent evaporation method (crystal form I), neat grinding method (crystal form II), co-grinding method (crystal form III). The prepared cocrystals were characterized by X-Ray Diffraction studies, Fourier Transfoorm Infrared Spectrophotometry, microscopic studies, solubility and dissolution studies. The prepared cocrystals showed increased solubility than the pure drug

Physicochemical Characterization and <i>In Vitro</i> Dissolution Test of Quercetin-Succinic Acid Co-crystals Prepared Using Solvent Evaporation

“…6 Co-crystal formers are commonly inert or exhibit no pharmacology activity. 7 Succinic acid (S) is a co-crystal former that is freely soluble in aqueous medium. It has been reported the cocrystals of S and sildenafil citrate with 1:1 molar ratio increase the solubility of sildenafil citrate by 5-fold.…”

Solid Dosage Form Development of Glibenclamide-Aspartame Cocrystal Using the Solvent Evaporation Method to Increase the Solubility of Glibenclamide

“…Samples were mixed with potassium bromide crystal and crushed until homogeneous, and then compressed to a pressure of 20 psi. The infrared spectrum was obtained using an infrared spectrophotometer in a range of wavenumbers (400-4000 cm-1) using FT-IR [8,9,16]…”

Selection of effective cocrystals former for dissolution rate improvement of active pharmaceutical ingredients based on lipoaffinity index

“…Furthermore DSR enhancement was also studied for Exemestane and Megestrol acetate acting as antineoplastics (Shiraki et al, 2008). Such interest was also focused on some cardiovascular agents including Cilnidipine, Felodipine, Irbesartan, Telmisartan, Apixaban, Ezetimibe, Fenofibrate, Olanzapine, Sildenafil, Tadalafil (Arafa et al, 2016;Chadha et al, 2014;Chen et al, 2016;Info, 2013;Khor et al, 2016;Nijhawan et al, 2015;Punita et al, 2016;Renkoğlu et al, 2015;Shewale et al, 2015;Shiraki et al, 2008;Sugandha et al, 2014;Vinesha et al, 2013;Žegarac et al, 2014). There are also single studies devoted to antiallergics as Fexofenadine (Mounika et al, 2015), antidiabetic agents as Gliclazide (Prawiro et al, 2016), AMG 517, Danazol, Famotidine (Bak et al, 2008;Childs et al, 2013;Shi et al, 2013), sodium channel blockers as 4-(4-…”