Enhancement of solubility and dissolution of indomethacin and phenylbutazone by cholic and deoxycholic acid conjugates

Abstract

Amino acids, cysteine and phenylalanine were conjugated with bile acids, cholic and deoxycholic acid to prepare cysteinocholic acid [N- (3α, 7α, 12α - trihydroxy - 24 - oxocholan - 24 - y1) cysteine], phenylalanocholic acid [N - (3α, 7α, 12α - trihydroxy- 24-oxocholan-24-y1) phenylalanine], cysteinodeoxycholic acid [N- (3α, 12α-dihydroxy-24-oxocholan-24-y1) cystiene] and phenylalanodeoxycholic acid [N- (3α, 12α -dihydroxy-24-oxocholan-24-y1) phenylalanine]. Subsequently, they were converted into their sodium salt. These compounds were evaluated for their surfactant properties mainly solubilization and dissolution enhancing properties. The drugs selected or this study were poorly water soluble non-steroidal anti-inflammatory drugs, indomethacin and phenylbutazone. All the biosurfactants enhanced the solubility and dissolution of both the drugs.