Improvements in solubility and stability of thalidomide upon complexation with hydroxypropyl-β-cyclodextrin

M. Krenn, M. P. Gamcsik, Georgia Boyce Vogelsang, O. M. Colvin, K. W. Leong

Research output: Contribution to journalArticle

Abstract

Thalidomide is in clinical use for the treatment of graft-versus-host disease in leukemia patients after bone marrow transplant. Low levels of the drug in plasma after oral administration have made an intravenous thalidomide formulation desirable. Thalidomide, however, is sparingly soluble in aqueous solution (50 μg/mL) and unstable. Complexation with hydroxypropyl-β- cyclodextrin has significantly improved the aqueous solubility and stability of thalidomide. Results obtained with HPLC and 1H NMR spectrometry have demonstrated that the solubility is increased to 1.7 mg/mL and the half-life of a diluted solution is extended from 2.1 to 4.1 h. Hence, an intravenous thalidomide-hydroxypropyl-β-cyclodextrin solution has the potential to significantly improve current therapy for graft-versus-host disease by providing sustained high levels of drug in the plasma.

Original languageEnglish (US)
Pages (from-to)685-689
Number of pages5
JournalJournal of Pharmaceutical Sciences
Volume81
Issue number7
DOIs
StatePublished - 1992

Fingerprint

Thalidomide
Cyclodextrins
Complexation
Solubility
Graft vs Host Disease
Grafts
Plasmas
Transplants
Pharmaceutical Preparations
Spectrometry
Oral Administration
Half-Life
Spectrum Analysis
Bone
Leukemia
Bone Marrow
High Pressure Liquid Chromatography
Nuclear magnetic resonance
Therapeutics

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

Cite this

Improvements in solubility and stability of thalidomide upon complexation with hydroxypropyl-β-cyclodextrin. / Krenn, M.; Gamcsik, M. P.; Vogelsang, Georgia Boyce; Colvin, O. M.; Leong, K. W.

In: Journal of Pharmaceutical Sciences, Vol. 81, No. 7, 1992, p. 685-689.

Research output: Contribution to journalArticle

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