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The Effect of the Molecular Weight of Polyvinylpyrrolidone and the Model Drug on Laser-Induced In Situ Amorphization

Hempel, Nele-Johanna (författare)
Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
Merkl, Padryk (författare)
Karolinska Institutet
Knopp, Matthias Manne (författare)
Univ Copenhagen, Dept Pharm, Bioneer FARMA, DK-2100 Copenhagen, Denmark.
visa fler...
Berthelsen, Ragna (författare)
Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
Teleki, Alexandra (författare)
Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab
Hansen, Anders Kragh (författare)
Tech Univ Denmark, Dept Photon Engn, DK-4000 Roskilde, Denmark.
Sotiriou, Georgios A. (författare)
Karolinska Institutet
Löbmann, Korbinian (författare)
Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark.
visa färre...
Karolinska Institutet Univ Copenhagen, Dept Pharm, DK-2100 Copenhagen, Denmark (creator_code:org_t)
2021-07-01
2021
Engelska.
Ingår i: Molecules. - : MDPI. - 1431-5157 .- 1420-3049. ; 26:13
  • Tidskriftsartikel (refereegranskat)
Abstract Ämnesord
Stäng  
  • Laser radiation has been shown to be a promising approach for in situ amorphization, i.e., drug amorphization inside the final dosage form. Upon exposure to laser radiation, elevated temperatures in the compacts are obtained. At temperatures above the glass transition temperature (T-g) of the polymer, the drug dissolves into the mobile polymer. Hence, the dissolution kinetics are dependent on the viscosity of the polymer, indirectly determined by the molecular weight (M-w) of the polymer, the solubility of the drug in the polymer, the particle size of the drug and the molecular size of the drug. Using compacts containing 30 wt% of the drug celecoxib (CCX), 69.25 wt% of three different M-w of polyvinylpyrrolidone (PVP: PVP12, PVP17 or PVP25), 0.25 wt% plasmonic nanoaggregates (PNs) and 0.5 wt% lubricant, the effect of the polymer M-w on the dissolution kinetics upon exposure to laser radiation was investigated. Furthermore, the effect of the model drug on the dissolution kinetics was investigated using compacts containing 30 wt% of three different drugs (CCX, indomethacin (IND) and naproxen (NAP)), 69.25 wt% PVP12, 0.25 wt% PN and 0.5 wt% lubricant. In perfect correlation to the Noyes-Whitney equation, this study showed that the use of PVP with the lowest viscosity, i.e., the lowest M-w (here PVP12), led to the fastest rate of amorphization compared to PVP17 and PVP25. Furthermore, NAP showed the fastest rate of amorphization, followed by IND and CCX in PVP12 due to its high solubility and small molecular size.

Ämnesord

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)

Nyckelord

in situ amorphization
near-IR laser radiation
amorphous solid dispersion
plasmonic photothermal nanoparticles
dissolution kinetics

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