Table 2.
Formulation | Maximum dissolution (%) | DE60a (%) | RDRb (30 minutes) |
---|---|---|---|
Megestrol acetate:HPMC =1:2 | 49.5±1.9 | 46.0 | 5.6 |
Megestrol acetate:PVP K30 =1:2 | 35.6±1.6 | 32.3 | 4.0 |
Megestrol acetate:HPMC:Gelucire 44/14 =1:2:0.5 | 61.5±2.1 | 55.6 | 6.9 |
Megestrol acetate:HPMC:poloxamer 407 =1:2:0.5 | 53.9±2.1 | 49.5 | 6.0 |
Megestrol acetate:HPMC:Ryoto sugar ester L1695 =1:2:0.5 | 81.5±2.5 | 76.0 | 9.3 |
Megestrol acetate:HPMC:TPGS =1:2:0.5 | 69.3±3.2 | 65.0 | 8.0 |
Megestrol acetate:HPMC:Ryoto sugar ester L1695 =1:2:1 | 97.3±2.3 | 92.4 | 11.1 |
Raw megestrol acetate | 9.3±0.6 | 7.3 | 1.0 |
Notes:
Dissolution efficiency was calculated from the area under the dissolution profile at 60 minutes, and is expressed as the percentage of the area of the rectangle described by 100% dissolution within the same period of time;
relative dissolution rate is the ratio between the amount of drug dissolved from the solid dispersion nanoparticles and that dissolved from raw megestrol acetate after 30 minutes. Data expressed as mean ± standard deviation (n=4).
Abbreviations: SAS, supercritical antisolvent; DE, dissolution efficiency; HPMC, hydroxypropylmethyl cellulose; PVP, polyvinylpyrrolidone; TPGS, D-α-tocopheryl polyethylene glycol 1000 succinate; RDR, relative dissolution rate.