Development of an intravenous formulation for the antiviral drug 9-(β-D-arabinofuranosyl)-adenine

S. D. Patel, Samuel H Yalkowsky

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

An analytical procedure for the analysis of 9-(β-D-arabinofuranosyl)-adenine (ara-A) was developed and used to determine its solubility as well as stability. A reversed-phase high performance liquid chromatographic method was used to quantitate intact drug and to determine its degradation products in aqueous solutions. The solubility of ara-A was determined in different cosolvent-water mixtures as well as in different pH-buffers. The aqueous solubility of ara-A increased exponentially with a linear increase in the volume fraction of the cosolvent. Stability studies indicate that ara-A is relatively stable in dimethylsulfoxide, dimethylacetamide, and dimethylformamide. In vitro precipitation was studied to evaluate the relative potential for precipitation of the drug on injection. Based on these findings, ara-A may be dissolved in the 70% dimethylsulfoxide-water mixture at 15 mg/ml and injected at a rate of 2 ml/min.

Original languageEnglish (US)
Pages (from-to)15-20
Number of pages6
JournalJournal of Parenteral Science and Technology
Volume41
Issue number1
StatePublished - 1987

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Adenine
Antiviral Agents
Solubility
Dimethyl Sulfoxide
Dimethylformamide
Water
Pharmaceutical Preparations
Buffers
Injections

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

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abstract = "An analytical procedure for the analysis of 9-(β-D-arabinofuranosyl)-adenine (ara-A) was developed and used to determine its solubility as well as stability. A reversed-phase high performance liquid chromatographic method was used to quantitate intact drug and to determine its degradation products in aqueous solutions. The solubility of ara-A was determined in different cosolvent-water mixtures as well as in different pH-buffers. The aqueous solubility of ara-A increased exponentially with a linear increase in the volume fraction of the cosolvent. Stability studies indicate that ara-A is relatively stable in dimethylsulfoxide, dimethylacetamide, and dimethylformamide. In vitro precipitation was studied to evaluate the relative potential for precipitation of the drug on injection. Based on these findings, ara-A may be dissolved in the 70{\%} dimethylsulfoxide-water mixture at 15 mg/ml and injected at a rate of 2 ml/min.",
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N2 - An analytical procedure for the analysis of 9-(β-D-arabinofuranosyl)-adenine (ara-A) was developed and used to determine its solubility as well as stability. A reversed-phase high performance liquid chromatographic method was used to quantitate intact drug and to determine its degradation products in aqueous solutions. The solubility of ara-A was determined in different cosolvent-water mixtures as well as in different pH-buffers. The aqueous solubility of ara-A increased exponentially with a linear increase in the volume fraction of the cosolvent. Stability studies indicate that ara-A is relatively stable in dimethylsulfoxide, dimethylacetamide, and dimethylformamide. In vitro precipitation was studied to evaluate the relative potential for precipitation of the drug on injection. Based on these findings, ara-A may be dissolved in the 70% dimethylsulfoxide-water mixture at 15 mg/ml and injected at a rate of 2 ml/min.

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