Mct. Deilarduya et al., DISSOLUTION RATE OF POLYMORPHS AND 2 NEW PSEUDOPOLYMORPHS OF SULINDAC, Drug development and industrial pharmacy, 23(11), 1997, pp. 1095-1098
This study reports the enhancement of sulindac dissolution rate by usi
ng the acetone and chloroform solvated forms. The intrinsic dissolutio
n rates of polymorphs I and II and the influence of crystal habit on t
he drug dissolution process have also been studied. The dissolution pr
operties were studied by calculating the intrinsic dissolution rate (k
) by linear regression analysis from the amount dissolved versus time.
The results indicated that the intrinsic dissolution rates of solvate
s in acetone and chloroform were much higher (k = 0.076 mg min(-1)cm(-
2), respectively) than those of polymorphs I and II (k = 0.036 mg min(
-1)cm(-2)). However, the dissolution rates of the two solvates were fo
und to be essentially the same and independent of the solvent nature.
The intrinsic dissolution rates of form II recrystallized in methanol
and ethanol differed (k = 0.031 and 0.036 mg min(-1)cm(-2), respective
ly), which confirms the influence of crystal habit on sulindac dissolu
tion rate. No significant difference in dissolution profiles were obse
rved between forms I and II, in agreement with the similar values effu
sion temperature (187 and 183 degrees C, respectively).