An insight into carvedilol solid forms: effect of supramolecular interactions on the dissolution profiles

Abstract

Carvedilol polymorph III, with higher melting point and dissolution rate than polymorph II, presents a potential strategy for carvedilol development.

Development of carvedilol-cyclodextrin inclusion complexes using fluid-bed granulation: a novel solid-state complexation alternative with technological advantages

“…Powder X-ray diffraction analyses showed complete amorphisation of CARV : HPbCD and CARV : HPcCD when prepared at pH 2.2 by SD technique. This indicates that the drug, in its protonated form acquired at such low pH, [35] could have been included in the cyclodextrins. Nevertheless, the sorption phenomenon on the cyclodextrin surface cannot be ruled out.…”

Combining Nuclear Magnetic Resonance Spectroscopy and Density Functional Theory Calculations to Characterize Carvedilol Polymorphs

“…The experimental data were compared with the pattern simulated from the single-crystal structures previously published and the high crystallographic purity of polymorphs II and III and hydrate could be confirmed. 11 The minor differences between experimental and calculated data can be attributed to preferred orientation and thermal contraction.…”

“…ethyl]amino]-2-propanol forms II and III crystallize in the centrosymmetric monoclinic space group with four molecules (comprising two pairs of enantiomeric molecules) per unit cell 11 and the hydrate form contains two independents carvedilol molecules (molecules A and B) and one water molecule in the asymmetric unit. 13 C and 15 N CP MAS NMR spectra obtained for Carvedilol form II, form III and hydrate are depicted in Figures 3 and 4, respectively.…”

“…4; Table 2). CAR II and CAR III show a typical case of conformational polymorphism 11 and the 13 C CP MAS data suggest that this technique can distinguish active pharmaceutical ingredients with conformational polymorphism properties. The 13 C assignments of hydrate form ( Table 2) Table 2).…”

“…CAR is practically insoluble in water and its solubility is pH dependent, which limits not only its bioavailability, but also a pharmaceutical formulation in the desired manner. 7,8 Concerning carvedilol polymorphism, three anhydrous forms were described in the literature: forms I, 9 II, 10 and III, 11 and one hydrate form. 12 CAR II is the unique that was characterized by 13 C solid-state nuclear magnetic resonance (SSNMR) spectroscopy.…”