Improving cyclodextrin complexation of a new antihepatitis drug with glacial acetic acid

Jennifer L.H. Johnson, Yan He, Akash Jain, Samuel H. Yalkowsky

Research output: Contribution to journalReview articlepeer-review

8 Scopus citations

Abstract

The purpose of this study was to develop and evaluate a solid nonaqueous oral dosage form for a new hepatitis C drug, PG301029, which is insoluble and unstable in water. Hydroxypropyl-β-cyclodextrin (HPβCD) and PG301029 were dissolved in glacial acetic acid. The acetic acid was removed by rotoevaporation such that the drug exists primarily in the complexed form. The stability of formulated PG301029 was determined upon dry storage and after reconstitution in simulated intestinal fluid (SIF), simulated gastric fluid (SGF), and water. Formulated PG301029 was found to be stable upon storage and can be reconstituted with water to a concentration 200 times that of the intrinsic solubility. Once reconstituted, the powder dissolves rapidly and PG301029 remains stable for 21 hours in SGF, SIF, and water. The unique use of acetic acid and HPβCD results in a solid dosage form of PG301029 that is both soluble and stable in water.

Original languageEnglish (US)
Article number18
Pages (from-to)E1-E6
JournalAAPS PharmSciTech
Volume7
Issue number1
StatePublished - Feb 24 2006

Keywords

  • Acetic acid
  • Complexation
  • Hydroxypropyl-β-cyclodextrin
  • Oral formulation
  • PG301029
  • Solid dose
  • Solubility
  • Stability

ASJC Scopus subject areas

  • Pharmaceutical Science

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