Thus 1:2:0.30 proportion of solid dispersions of Acetazolamide with EPO and POL, denoted as ACEL(0.30) was supposed to have optimised based on maximum intrinsic solubility, faster dissolution rate and maximum amorphisation yet thermal stability of ACT in solid dispersions and was subsequently subjected to accelerated stability study. Physical stability and solubility attributes of amorphous

form of ACT in optimised proportion of ACEL during stability study for 3 months denoted as ACEL3(0.30) and for 6 months denoted as ACEL6(0.30) were reviewed in VX-770 in vivo the following manner. FT-IR spectrum (Fig. 2) revealed insignificant change in position and intensity of the principal peaks. It depicted that neither ACEL3 nor ACEL6 involved any further interactions between the drug and polymer–plasticiser molecules CB-839 manufacturer over the period of its storage. XRPD profile (Fig. 4) of ACEL3(0.30) and ACEL6(0.30) were similar to that of its

initial profile and did not show recurrence of any additional principal diffraction peaks. DSC thermogram (Fig. 3) of ACEL3(0.30) and ACEL6(0.30) also showed absence of an endotherm corresponding to melting of crystalline ACT. Thus, optimised proportion of ACEL did not show any tendency of spontaneous recrystallisation of ACT. Such stabilisation was reported to have resulted

from either a micro-solvent effect due to polymers or a conformational effect.2 Such stabilisation of amorphous system only in 1:2:0.30 proportion ACEL had contributed to an unaltered intrinsic solubility (Table 1) and indifferent pattern of drug release (Fig. 5) in comparison with initial samples. In conclusion, the present study demonstrates that intrinsic solubility until and in vitro dissolution rate of Acetazolamide could be enhanced when coprocessed with a polymethacrylate solubiliser as Eudragit® EPO by hot melt extrusion technique at temperature below melting point of ACT. It could be achieved through a number of influencing factors such as size reduction, increased surface area and better wettability of drug particles in solid dispersions. Furthermore, the skillful choice of a plasticiser, Poloxamer-237 in optimised proportion with a polymer was found to have major impact on the relevant characteristics of the extrusion process and the extrudates. ACEL(0.30) effectively decreased melt viscosity and the temperature needed to extrude the blend and hence facilitated the extrusion process. Evaluation of physical characteristics of these extrudates suggested formation of completely amorphous system without sign of thermal degradation at the processing temperature.