In situ measurement of solvent-mediated phase transformations during dissolution testing

Jaakko Aaltonen, Paula Heinänen, Leena Peltonen, Hanna Kortejärvi, Veli Pekka Tanninen, Leena Christiansen, Jouni Hirvonen, Jouko Yliruusi, Jukka Rantanen

    Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

    Kuvaus

    In this study, solvent-mediated phase transformations of theophylline (TP) and nitrofurantoin (NF) were measured in a channel flow intrinsic dissolution test system. The test set-up comprised simultaneous measurement of drug concentration in the dissolution medium (with UV-Vis spectrophotometry) and measurement of the solid-state form of the dissolving solid (in situ with Raman spectroscopy). The solid phase transformations were also investigated off-line with scanning electron microscopy. TP anhydrate underwent a transformation to TP monohydrate, and NF anhydrate (form beta) to NF monohydrate (form II). Transformation of TP anhydrate to TP monohydrate resulted in a clear decrease in the dissolution rate, while the transformation of NF anhydrate (form II) to NF monohydrate (form II) could not be linked as clearly to changes in the dissolution rate. The transformation of TP was an order of magnitude faster than that of NF. The presence of a water absorbing excipient, microcrystalline cellulose, was found to delay the onset of the transformation of TP anhydrate. Combining the measurement of drug concentration in the dissolution medium with the solid phase measurement offers a deeper understanding of the solvent-mediated phase transformation phenomena during dissolution. (c) 2006 Wiley-Liss, Inc.
    Alkuperäiskielienglanti
    LehtiJournal of Pharmaceutical Sciences
    Vuosikerta95
    Sivut2730-2737
    Sivumäärä8
    ISSN0022-3549
    DOI - pysyväislinkit
    TilaJulkaistu - 2006
    OKM-julkaisutyyppiA1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä, vertaisarvioitu

    Lainaa tätä

    Aaltonen, Jaakko ; Heinänen, Paula ; Peltonen, Leena ; Kortejärvi, Hanna ; Tanninen, Veli Pekka ; Christiansen, Leena ; Hirvonen, Jouni ; Yliruusi, Jouko ; Rantanen, Jukka. / In situ measurement of solvent-mediated phase transformations during dissolution testing. Julkaisussa: Journal of Pharmaceutical Sciences. 2006 ; Vuosikerta 95. Sivut 2730-2737.
    @article{4efa91f5da794fe4bde7566dd01a84c4,
    title = "In situ measurement of solvent-mediated phase transformations during dissolution testing",
    abstract = "In this study, solvent-mediated phase transformations of theophylline (TP) and nitrofurantoin (NF) were measured in a channel flow intrinsic dissolution test system. The test set-up comprised simultaneous measurement of drug concentration in the dissolution medium (with UV-Vis spectrophotometry) and measurement of the solid-state form of the dissolving solid (in situ with Raman spectroscopy). The solid phase transformations were also investigated off-line with scanning electron microscopy. TP anhydrate underwent a transformation to TP monohydrate, and NF anhydrate (form beta) to NF monohydrate (form II). Transformation of TP anhydrate to TP monohydrate resulted in a clear decrease in the dissolution rate, while the transformation of NF anhydrate (form II) to NF monohydrate (form II) could not be linked as clearly to changes in the dissolution rate. The transformation of TP was an order of magnitude faster than that of NF. The presence of a water absorbing excipient, microcrystalline cellulose, was found to delay the onset of the transformation of TP anhydrate. Combining the measurement of drug concentration in the dissolution medium with the solid phase measurement offers a deeper understanding of the solvent-mediated phase transformation phenomena during dissolution. (c) 2006 Wiley-Liss, Inc.",
    author = "Jaakko Aaltonen and Paula Hein{\"a}nen and Leena Peltonen and Hanna Kortej{\"a}rvi and Tanninen, {Veli Pekka} and Leena Christiansen and Jouni Hirvonen and Jouko Yliruusi and Jukka Rantanen",
    year = "2006",
    doi = "10.1002/jps.20725",
    language = "English",
    volume = "95",
    pages = "2730--2737",
    journal = "Journal of Pharmaceutical Sciences",
    issn = "0022-3549",
    publisher = "Wiley",

    }

    In situ measurement of solvent-mediated phase transformations during dissolution testing. / Aaltonen, Jaakko; Heinänen, Paula; Peltonen, Leena; Kortejärvi, Hanna; Tanninen, Veli Pekka; Christiansen, Leena; Hirvonen, Jouni; Yliruusi, Jouko; Rantanen, Jukka.

    julkaisussa: Journal of Pharmaceutical Sciences, Vuosikerta 95, 2006, s. 2730-2737.

    Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

    TY - JOUR

    T1 - In situ measurement of solvent-mediated phase transformations during dissolution testing

    AU - Aaltonen, Jaakko

    AU - Heinänen, Paula

    AU - Peltonen, Leena

    AU - Kortejärvi, Hanna

    AU - Tanninen, Veli Pekka

    AU - Christiansen, Leena

    AU - Hirvonen, Jouni

    AU - Yliruusi, Jouko

    AU - Rantanen, Jukka

    PY - 2006

    Y1 - 2006

    N2 - In this study, solvent-mediated phase transformations of theophylline (TP) and nitrofurantoin (NF) were measured in a channel flow intrinsic dissolution test system. The test set-up comprised simultaneous measurement of drug concentration in the dissolution medium (with UV-Vis spectrophotometry) and measurement of the solid-state form of the dissolving solid (in situ with Raman spectroscopy). The solid phase transformations were also investigated off-line with scanning electron microscopy. TP anhydrate underwent a transformation to TP monohydrate, and NF anhydrate (form beta) to NF monohydrate (form II). Transformation of TP anhydrate to TP monohydrate resulted in a clear decrease in the dissolution rate, while the transformation of NF anhydrate (form II) to NF monohydrate (form II) could not be linked as clearly to changes in the dissolution rate. The transformation of TP was an order of magnitude faster than that of NF. The presence of a water absorbing excipient, microcrystalline cellulose, was found to delay the onset of the transformation of TP anhydrate. Combining the measurement of drug concentration in the dissolution medium with the solid phase measurement offers a deeper understanding of the solvent-mediated phase transformation phenomena during dissolution. (c) 2006 Wiley-Liss, Inc.

    AB - In this study, solvent-mediated phase transformations of theophylline (TP) and nitrofurantoin (NF) were measured in a channel flow intrinsic dissolution test system. The test set-up comprised simultaneous measurement of drug concentration in the dissolution medium (with UV-Vis spectrophotometry) and measurement of the solid-state form of the dissolving solid (in situ with Raman spectroscopy). The solid phase transformations were also investigated off-line with scanning electron microscopy. TP anhydrate underwent a transformation to TP monohydrate, and NF anhydrate (form beta) to NF monohydrate (form II). Transformation of TP anhydrate to TP monohydrate resulted in a clear decrease in the dissolution rate, while the transformation of NF anhydrate (form II) to NF monohydrate (form II) could not be linked as clearly to changes in the dissolution rate. The transformation of TP was an order of magnitude faster than that of NF. The presence of a water absorbing excipient, microcrystalline cellulose, was found to delay the onset of the transformation of TP anhydrate. Combining the measurement of drug concentration in the dissolution medium with the solid phase measurement offers a deeper understanding of the solvent-mediated phase transformation phenomena during dissolution. (c) 2006 Wiley-Liss, Inc.

    U2 - 10.1002/jps.20725

    DO - 10.1002/jps.20725

    M3 - Article

    VL - 95

    SP - 2730

    EP - 2737

    JO - Journal of Pharmaceutical Sciences

    JF - Journal of Pharmaceutical Sciences

    SN - 0022-3549

    ER -