DISSOLUTION RATE OF POLYMORPHS AND 2 NEW PSEUDOPOLYMORPHS OF SULINDAC

Citation
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
Citations number
19
Categorie Soggetti
Chemistry Medicinal","Pharmacology & Pharmacy
ISSN journal
03639045
Volume
23
Issue
11
Year of publication
1997
Pages
1095 - 1098
Database
ISI
SICI code
0363-9045(1997)23:11<1095:DROPA2>2.0.ZU;2-D
Abstract
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).