Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Standard

Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying. / Craye, Goedele; Löbmann, Korbinian; Grohganz, Holger; Rades, Thomas; Laitinen, Riikka.

I: Molecules, Bind 20, Nr. 12, 2015, s. 21532-48.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Craye, G, Löbmann, K, Grohganz, H, Rades, T & Laitinen, R 2015, 'Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying', Molecules, bind 20, nr. 12, s. 21532-48. https://doi.org/10.3390/molecules201219784

APA

Craye, G., Löbmann, K., Grohganz, H., Rades, T., & Laitinen, R. (2015). Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying. Molecules, 20(12), 21532-48. https://doi.org/10.3390/molecules201219784

Vancouver

Craye G, Löbmann K, Grohganz H, Rades T, Laitinen R. Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying. Molecules. 2015;20(12):21532-48. https://doi.org/10.3390/molecules201219784

Author

Craye, Goedele ; Löbmann, Korbinian ; Grohganz, Holger ; Rades, Thomas ; Laitinen, Riikka. / Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying. I: Molecules. 2015 ; Bind 20, Nr. 12. s. 21532-48.

Bibtex

@article{298da8bffc1d407391da5db58b32ae15,
title = "Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying",
abstract = "In this study, spray drying from aqueous solutions, using the surface-active agent sodium lauryl sulfate (SLS) as a solubilizer, was explored as a production method for co-amorphous simvastatin-lysine (SVS-LYS) at 1:1 molar mixtures, which previously have been observed to form a co-amorphous mixture upon ball milling. In addition, a spray-dried formulation of SVS without LYS was prepared. Energy-dispersive X-ray spectroscopy (EDS) revealed that SLS coated the SVS and SVS-LYS particles upon spray drying. X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that in the spray-dried formulations the remaining crystallinity originated from SLS only. The best dissolution properties and a {"}spring and parachute{"} effect were found for SVS spray-dried from a 5{\%} SLS solution without LYS. Despite the presence of at least partially crystalline SLS in the mixtures, all the studied formulations were able to significantly extend the stability of amorphous SVS compared to previous co-amorphous formulations of SVS. The best stability (at least 12 months in dry conditions) was observed when SLS was spray-dried with SVS (and LYS). In conclusion, spray drying of SVS and LYS from aqueous surfactant solutions was able to produce formulations with improved physical stability for amorphous SVS.",
author = "Goedele Craye and Korbinian L{\"o}bmann and Holger Grohganz and Thomas Rades and Riikka Laitinen",
year = "2015",
doi = "10.3390/molecules201219784",
language = "English",
volume = "20",
pages = "21532--48",
journal = "Molecules",
issn = "1420-3049",
publisher = "M D P I AG",
number = "12",

}

RIS

TY - JOUR

T1 - Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Drying

AU - Craye, Goedele

AU - Löbmann, Korbinian

AU - Grohganz, Holger

AU - Rades, Thomas

AU - Laitinen, Riikka

PY - 2015

Y1 - 2015

N2 - In this study, spray drying from aqueous solutions, using the surface-active agent sodium lauryl sulfate (SLS) as a solubilizer, was explored as a production method for co-amorphous simvastatin-lysine (SVS-LYS) at 1:1 molar mixtures, which previously have been observed to form a co-amorphous mixture upon ball milling. In addition, a spray-dried formulation of SVS without LYS was prepared. Energy-dispersive X-ray spectroscopy (EDS) revealed that SLS coated the SVS and SVS-LYS particles upon spray drying. X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that in the spray-dried formulations the remaining crystallinity originated from SLS only. The best dissolution properties and a "spring and parachute" effect were found for SVS spray-dried from a 5% SLS solution without LYS. Despite the presence of at least partially crystalline SLS in the mixtures, all the studied formulations were able to significantly extend the stability of amorphous SVS compared to previous co-amorphous formulations of SVS. The best stability (at least 12 months in dry conditions) was observed when SLS was spray-dried with SVS (and LYS). In conclusion, spray drying of SVS and LYS from aqueous surfactant solutions was able to produce formulations with improved physical stability for amorphous SVS.

AB - In this study, spray drying from aqueous solutions, using the surface-active agent sodium lauryl sulfate (SLS) as a solubilizer, was explored as a production method for co-amorphous simvastatin-lysine (SVS-LYS) at 1:1 molar mixtures, which previously have been observed to form a co-amorphous mixture upon ball milling. In addition, a spray-dried formulation of SVS without LYS was prepared. Energy-dispersive X-ray spectroscopy (EDS) revealed that SLS coated the SVS and SVS-LYS particles upon spray drying. X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) showed that in the spray-dried formulations the remaining crystallinity originated from SLS only. The best dissolution properties and a "spring and parachute" effect were found for SVS spray-dried from a 5% SLS solution without LYS. Despite the presence of at least partially crystalline SLS in the mixtures, all the studied formulations were able to significantly extend the stability of amorphous SVS compared to previous co-amorphous formulations of SVS. The best stability (at least 12 months in dry conditions) was observed when SLS was spray-dried with SVS (and LYS). In conclusion, spray drying of SVS and LYS from aqueous surfactant solutions was able to produce formulations with improved physical stability for amorphous SVS.

U2 - 10.3390/molecules201219784

DO - 10.3390/molecules201219784

M3 - Journal article

VL - 20

SP - 21532

EP - 21548

JO - Molecules

JF - Molecules

SN - 1420-3049

IS - 12

ER -

ID: 161588045