Improving cyclodextrin complexation of a new antihepatitis drug with glacial acetic acid
- 8 March 2006
- journal article
- Published by Springer Nature in AAPS PharmSciTech
- Vol. 7 (1) , E125-E130
- https://doi.org/10.1208/pt070118
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.Keywords
This publication has 14 references indexed in Scilit:
- Oral formulation of a novel antiviral agent, PG301029, in a mixture of Gelucire 44/14 and DMA (2∶1, wt/wt)AAPS PharmSciTech, 2005
- Improvement in solubility and dissolution rate of flavonoids by complexation with β-cyclodextrinJournal of Pharmaceutical and Biomedical Analysis, 2004
- Randomised, double blind, placebo controlled trial of interferon, ribavirin, and amantadine versus interferon, ribavirin, and placebo in treatment naive patients with chronic hepatitis CGut, 2004
- Studies on the interaction of water with ethylcellulose: Effect of polymer particle sizeAAPS PharmSciTech, 2003
- Crystal Structures ofβ-Cyclodextrin Complexes with Formic Acid and Acetic AcidJournal of inclusion phenomena and molecular recognition in chemistry, 2003
- New developments in the treatment of hepatitis CGut, 2003
- Physicochemical characterization and dissolution properties of nimesulide-cyclodextrin binary systemsAAPS PharmSciTech, 2003
- Effect of Nanonization on Absorption of 301029: Ex Vivo and In Vivo Pharmacokinetic Correlations Determined by Liquid Chromatography/Mass SpectrometryPharmaceutical Research, 2002
- Taste masking of diclofenac sodium using microencapsulationJournal of Microencapsulation, 2002
- Solubilization of cyclosporin AAAPS PharmSciTech, 2001