TY - JOUR
T1 - Solubilization of NSC-639829
AU - Jain, Neera
AU - Yang, Gang
AU - Tabibi, S. Esmail
AU - Yalkowsky, Samuel H.
N1 - Funding Information:
The work was performed under Contract No. CM-77 109 from the National Cancer Institute.
PY - 2001/8/28
Y1 - 2001/8/28
N2 - Solubilization using pH combined with cosolvents, surfactants, and complexants are investigated for NSC-639829, an investigational anti-tumor agent. The intrinsic solubility of the drug is approximately 30 ng/ml and it has an ionizable dimethyl aniline group with an approximate base pKa of 5. Samples buffered at pH 1.0, 2.0, and 7.0 with various concentrations of the solubilizing agents were used to study the solubilization of NSC-629829 when present as charged and uncharged species. The solubilization of NSC-639829 was found to be much more effective when the drug was present primarily in ionized form. At pH values 1.0 and 2.0 where the surfactant (SLS) and complexant (SBEβCD) carried a negative charge enhanced solubilities of more than a million-fold were observed for the drug.
AB - Solubilization using pH combined with cosolvents, surfactants, and complexants are investigated for NSC-639829, an investigational anti-tumor agent. The intrinsic solubility of the drug is approximately 30 ng/ml and it has an ionizable dimethyl aniline group with an approximate base pKa of 5. Samples buffered at pH 1.0, 2.0, and 7.0 with various concentrations of the solubilizing agents were used to study the solubilization of NSC-629829 when present as charged and uncharged species. The solubilization of NSC-639829 was found to be much more effective when the drug was present primarily in ionized form. At pH values 1.0 and 2.0 where the surfactant (SLS) and complexant (SBEβCD) carried a negative charge enhanced solubilities of more than a million-fold were observed for the drug.
KW - Dimethyl aniline
KW - NSC-639829
KW - Solubilization
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U2 - 10.1016/S0378-5173(01)00773-6
DO - 10.1016/S0378-5173(01)00773-6
M3 - Article
C2 - 11489553
AN - SCOPUS:0035964467
SN - 0378-5173
VL - 225
SP - 41
EP - 47
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -