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  • The dissolution enhancement of piroxicam in its physical mixtures and solid dispersion formulations using gluconolactone and glucosamine hydrochloride as potential carriers.

The dissolution enhancement of piroxicam in its physical mixtures and solid dispersion formulations using gluconolactone and glucosamine hydrochloride as potential carriers.

Pharmaceutical development and technology (2014-01-08)
Hiba Al-Hamidi, Wasfy M Obeidat, Ali Nokhodchi
ABSTRACT

The solid dispersion technique is one of the most effective methods for improving the dissolution rate of poorly water-soluble drugs; however this is reliant on a suitable carrier and solvent being selected. The work presented explores amino sugars (d-glucosamine HCl and d-gluconolactone) as potential hydrophilic carriers to improve dissolution rate of a poorly water-soluble drug, piroxicam, from physical mixtures and solid dispersion formulations. Solid dispersions of the drug and carrier were prepared using different ratios by the conventional solvent evaporation method. Acetone was used as solvent in the preparation of solid dispersions. Physical mixtures of piroxicam and carrier were also prepared for comparison. The properties of all solid dispersions and physical mixtures were studied using a dissolution tester, Fourier transform infrared, XRD, SEM and differential scanning calorimetry. These results showed that the presence of glucosamine or gluconolactone can increase dissolution rate of piroxicam compared to pure piroxicam. Glucosamine or Gluconolactone could be used as carrier in solid dispersion formulations and physical mixtures to enhance the dissolution rate. Solid state studies showed that no significant changes occurred for piroxicam in physical mixtures and solid dispersion.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Acetone, purum, ≥99.0% (GC)
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.9%
Sigma-Aldrich
N,N′-Disuccinimidyl carbonate, ≥95%
Sigma-Aldrich
N,N′-Disuccinimidyl carbonate, purum, ≥95.0% (NMR)
Sigma-Aldrich
D-(+)-Glucosamine hydrochloride, ≥99%, crystalline
Sigma-Aldrich
D-(+)-Glucosamine hydrochloride, ≥99%, BioReagent, suitable for cell culture
Sigma-Aldrich
D-(+)-Glucosamine hydrochloride, Vetec, reagent grade, ≥99%
Sigma-Aldrich
Acetone, puriss., meets analytical specification of Ph. Eur., BP, NF, ≥99% (GC)
Sigma-Aldrich
Acetone, ACS reagent, ≥99.5%
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.8%
Sigma-Aldrich
Acetone, HPLC Plus, for HPLC, GC, and residue analysis, ≥99.9%
Sigma-Aldrich
Acetone, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.5% (GC)
Sigma-Aldrich
Acetone, suitable for HPLC, ≥99.9%
Sigma-Aldrich
Gluconolactone, meets USP testing specifications
Sigma-Aldrich
D-(+)-Gluconic acid δ-lactone, ≥99.0%
Supelco
Glucosamine hydrochloride, Pharmaceutical Secondary Standard; Certified Reference Material
Supelco
Acetone solution, certified reference material, 2000 μg/mL in methanol: water (9:1)
USP
Glucosamine hydrochloride, United States Pharmacopeia (USP) Reference Standard
Glucosamine for system suitability, European Pharmacopoeia (EP) Reference Standard
Glucosamine hydrochloride, European Pharmacopoeia (EP) Reference Standard