Izvorni znanstveni članak

https://doi.org/10.2478/acph-2019-0009

Solubilization of ibuprofen for freeze dried parenteral dosage forms

MAJA PRESKAR ; Krka d.d. Novo mesto, SI- 8000 Novo mesto, Slovenia
TOMISLAV VRBANEC ; Krka d.d. Novo mesto, SI- 8000 Novo mesto, Slovenia
FRANC VREČER ; Krka d.d. Novo mesto, SI- 8000 Novo mesto, Slovenia; University of Ljubljana, Faculty of Pharmacy, SI- 1000, Ljubljana, Slovenia
PRIMOŽ ŠKET ; Slovenian NMR Center, National Institute of Chemistry, SI-1000 Ljubljana, Slovenia
JANEZ PLAVEC ; Slovenian NMR Center, National Institute of Chemistry, SI-1000 Ljubljana, Slovenia
MIRJANA GAŠPERLIN ; University of Ljubljana, Faculty of Pharmacy, SI- 1000, Ljubljana, Slovenia

Sažetak

Ibuprofen, a weakly acidic non-steroidal anti-inflammatory drug having poor aqueous solubility, is a challenging drug for the development of pharmaceutical formulations, resulting in numerous research attempts focusing on improvement of its solubility and consequently bioavailability. Most studies have been done for solid dosage forms, with very little attention paid to parenterals. Hence, the main purpose of the present study was to enhance ibuprofen solubility as a result of formulation composition and the freeze drying process. Moreover, the purpose was to prepare a freeze dried dosage form with improved ibuprofen solubility that could, after simple reconstitution with water for injection, result in an isotonic parenteral solution. Solubility of ibuprofen was modified by various excipients suitable for parenteral application. Drug interactions with selected excipients in the final product/lyophilisate were studied by a combined use of XRPD, DSC, Raman and ssNMR. Analyses of lyophilized samples showed solubility enhancement of ibuprofen and in situ formation of an ibuprofen salt with the alkaline excipients used.

Ključne riječi

ibuprofen; solubility enhancement; freeze drying; physico-chemical characterization

Hrčak ID:

206639

URI

https://hrcak.srce.hr/206639

Datum izdavanja:

31.3.2019.

Posjeta: 2.637 *