Influence of Polymer Molecular Weight on Drug-Polymer Solubility: A Comparison between Experimentally Determined Solubility in PVP and Prediction Derived from Solubility in Monomer

Journal of Pharmaceutical Sciences
Matthias Manne KnoppThomas Rades

Abstract

In this study, the influence of polymer molecular weight on drug-polymer solubility was investigated using binary systems containing indomethacin (IMC) and polyvinylpyrrolidone (PVP) of different molecular weights. The experimental solubility in PVP, measured using a differential scanning calorimetry annealing method, was compared with the solubility calculated from the solubility of the drug in the liquid analogue N-vinylpyrrolidone (NVP). The experimental solubility of IMC in the low-molecular-weight PVP K12 was not significantly different from that in the higher molecular weight PVPs (K25, K30, and K90). The calculated solubilities derived from the solubility in NVP (0.31-0.32 g/g) were found to be lower than those experimentally determined in PVP (0.38-0.40 g/g). Nevertheless, the similarity between the values indicates that the analogue solubility can provide valuable indications on the solubility in the polymer. Hence, if a drug is soluble in an analogue of the polymer, it is most likely also soluble in the polymer. In conclusion, the solubility of a given drug-polymer system is determined by the strength of the drug-polymer interactions rather than the molecular weight of the polymer. Therefore, during the first screenin...Continue Reading

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Citations

Jan 31, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Malte Bille RaskThomas Rades
Jan 31, 2016·Advanced Drug Delivery Reviews·Teófilo VasconcelosBruno Sarmento
Nov 6, 2015·Journal of Pharmaceutical Sciences·Matthias Manne KnoppThomas Rades
Feb 24, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Matthias Manne KnoppPeter Langguth
Jul 28, 2015·Molecular Pharmaceutics·Matthias Manne KnoppThomas Rades
Jun 1, 2016·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Nicolas GautschiMartin Kuentz
Aug 11, 2016·Pharmaceutical Research·Tochukwu C OkwuosaMohamed A Alhnan
Mar 27, 2018·Chemphyschem : a European Journal of Chemical Physics and Physical Chemistry·Connor P CallawaySeung Soon Jang
Sep 28, 2018·Drug Development and Industrial Pharmacy·Vahid Jouyban-GharamalekiElaheh Rahimpour
Aug 14, 2019·AAPS PharmSciTech·Nitin SalunkhePrafulla Choudhari
Sep 3, 2019·Chemical & Pharmaceutical Bulletin·Shin-Ichiro KimuraHiromu Kondo
Nov 9, 2020·AAPS PharmSciTech·Athira R NairSwapnil J Dengale
Jan 2, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Nele-Johanna HempelKorbinian Löbmann
Mar 4, 2021·Molecular Pharmaceutics·Alex MathersMichal Fulem
May 28, 2021·Molecular Pharmaceutics·Samarth D ThakoreArvind K Bansal
May 23, 2021·Journal of Pharmaceutical Sciences·Nele-Johanna HempelKorbinian Löbmann
Nov 24, 2018·Journal of the American Chemical Society·Maximilian KarlThomas Rades
Sep 26, 2020·Molecular Pharmaceutics·Anasuya SahooRonald A Siegel

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