Solubilization of NSC-639829

Neera Jain; Gang Yang; S. Esmail Tabibi; Samuel H. Yalkowsky

doi:10.1016/S0378-5173(01)00773-6

Solubilization of NSC-639829

Neera Jain, Gang Yang, S. Esmail Tabibi, Samuel H. Yalkowsky

Pharmacology and Toxicology

Research output: Contribution to journal › Article › peer-review

35 Scopus citations

Abstract

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 (SBEβCD) carried a negative charge enhanced solubilities of more than a million-fold were observed for the drug.

Original language	English (US)
Pages (from-to)	41-47
Number of pages	7
Journal	International Journal of Pharmaceutics
Volume	225
Issue number	1-2
DOIs	https://doi.org/10.1016/S0378-5173(01)00773-6
State	Published - Aug 28 2001

Keywords

Dimethyl aniline
NSC-639829
Solubilization

ASJC Scopus subject areas

Pharmaceutical Science

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10.1016/S0378-5173(01)00773-6

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title = "Solubilization of NSC-639829",

abstract = "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.",

keywords = "Dimethyl aniline, NSC-639829, Solubilization",

author = "Neera Jain and Gang Yang and Tabibi, {S. Esmail} and Yalkowsky, {Samuel H.}",

note = "Funding Information: The work was performed under Contract No. CM-77 109 from the National Cancer Institute.",

year = "2001",

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doi = "10.1016/S0378-5173(01)00773-6",

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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

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SN - 0378-5173

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SP - 41

EP - 47

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

IS - 1-2

ER -

Solubilization of NSC-639829

Abstract

Keywords

ASJC Scopus subject areas

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