Solubilization of NSC-639829

被引：26

作者：

Jain, N

Yang, G

Tabibi, SE

Yalkowsky, SH

机构：

[1] Univ Arizona, Coll Pharm, Dept Pharm Practice & Sci, Tucson, AZ 85721 USA

[2] NCI, Pharmaceut Resources Branch, NIH, Bethesda, MD 20892 USA

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2001年 / 225卷 / 1-2期

关键词：

solubilization; NSC-639829; dimethyl aniline;

D O I：

10.1016/S0378-5173(01)00773-6

中图分类号：

R9 [药学];

学科分类号：

1007 [药学];

摘要：

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 pK(a) 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 (SBE beta CD) carried a negative charge enhanced solubilities of more than a million-fold were observed for the drug. (C) 2001 Elsevier Science B.V. All rights reserved.

引用

页码：41 / 47

页数：7

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