In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release

Investigation of Dissolution Mechanism and Release Kinetics of Poorly Water-Soluble Tadalafil from Amorphous Solid Dispersions Prepared by Various Methods

“…This is probably because TAD is better wetted in the both sieve fractions of extrudates. Since their dissolution profiles overlap, they were no noteworthy differences in the porosity between both extrudates as was described e.g., in [15]. Subsequently, its release is probably retarded by the gel layer and therefore, diffusion mechanism predominated.…”

“…The powder X-ray diffraction patterns of pure TAD, K12 and K64, their PMs and SDs prepared by various method are shown in Figure 5 and Figure 6, respectively. The diffraction pattern of the TAD had sharp intensive peaks throughout its pattern suggesting that it is crystalline in nature [15]. On the contrary, the polymeric carriers showed broad amorphous bands and no sharp diffraction peaks suggesting that the Kollidons were in amorphous state.…”

“…Therefore, neither ionization nor salt formation can be applied for the enhancement of its aqueous solubility and dissolution rate and thus, it was undertaken to develop effective methods for improvement of these properties [5,14]. The transformation of pure crystalline TAD into the amorphous form is considered to be troublesome [15]. Wlodarski et al obtained the amorphous forms of TAD by amorphization methods and without excipients, i.e., by cryogenic grinding, ball milling, spray drying, freeze-drying and antisolvent precipitation.…”

“…Solid dispersion of TAD has been prepared using different methods, these include solvent evaporation method [8,10,12,18,19], spray drying [6,16,26], melting method [5,17], hot-melt extrusion [15], supercritical anti-solvent process [14,27], ball milling [26,27,28] or freeze-drying [3].…”

An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part I

“…Various reports on solubility enhancement through HME were discussed in recent reviews [3,52,63], including solid dispersions of tadalafil [67], co-amorphous system of indomethacin/arginine [68], solid crystalline suspensions of efavirenz [69], solid solutions of artesunate [70], and ternary inclusion complexes of itraconazole/cyclodextrin [71]. In this section of this review, we present new reports on HME applications for drug solubility enhancement for the readers' interest.…”