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Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development

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Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development. / Alhijjaj, Muqdad; Belton, Peter; Fabian, Laszlo; Wellner, Nikolaus; Reading, Michael; Qi, Sheng.

In: Molecular Pharmaceutics, Vol. 15, No. 12, 03.12.2018, p. 5625–5636.

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@article{06df009ea2d34f1ebda7f5ae4b694997,
title = "Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development",
abstract = "This study aimed to develop a rapid, simple and inexpensive screening method for selecting the best polymeric candidates possessing high active pharmaceutical ingredient (API) miscibility during the early stages of formulation development of solid dispersion based pharmaceutical products. A new thermal imaging based method, thermal analysis by structural characterization (TASC), was used as a thermoptometeric tool in conjunction with data analysis software to detect the melting point depression and post-melting dissolution of felodipine particles screened over thin spin-coated films of ten polymers commonly used in the pharmaceutical field. On the polymeric substrates the drug showed different degrees of melting point reduction, reflecting their different levels of polymer-drug miscibility. Using TASC to detect melting point depression is significantly (20-40 times) faster than the conventional DSC method without loss of the sensitivity of detection. The quantity of the material required for the screening is less than 1/1000th of the material used in conventional DSC tests which significantly reduce the material wastage. Isothermal TASC tests and IR imaging confirmed the occurrence of thermal dissolution of the drug in the polymer for more miscible pairs. The real-time stability tests validate the accuracy of the polymer-drug miscibility screening results. These results demonstrate TASC as a promising screening tool for rapidly selecting the polymeric excipients for pharmaceutical formulations development.",
author = "Muqdad Alhijjaj and Peter Belton and Laszlo Fabian and Nikolaus Wellner and Michael Reading and Sheng Qi",
year = "2018",
month = "12",
day = "3",
doi = "10.1021/acs.molpharmaceut.8b00798",
language = "English",
volume = "15",
pages = "5625–5636",
journal = "Molecular Pharmaceutics",
issn = "1543-8384",
publisher = "American Chemical Society",
number = "12",

}

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TY - JOUR

T1 - Novel thermal imaging method for rapid screening of drug-polymer miscibility for solid dispersion based formulation development

AU - Alhijjaj, Muqdad

AU - Belton, Peter

AU - Fabian, Laszlo

AU - Wellner, Nikolaus

AU - Reading, Michael

AU - Qi, Sheng

PY - 2018/12/3

Y1 - 2018/12/3

N2 - This study aimed to develop a rapid, simple and inexpensive screening method for selecting the best polymeric candidates possessing high active pharmaceutical ingredient (API) miscibility during the early stages of formulation development of solid dispersion based pharmaceutical products. A new thermal imaging based method, thermal analysis by structural characterization (TASC), was used as a thermoptometeric tool in conjunction with data analysis software to detect the melting point depression and post-melting dissolution of felodipine particles screened over thin spin-coated films of ten polymers commonly used in the pharmaceutical field. On the polymeric substrates the drug showed different degrees of melting point reduction, reflecting their different levels of polymer-drug miscibility. Using TASC to detect melting point depression is significantly (20-40 times) faster than the conventional DSC method without loss of the sensitivity of detection. The quantity of the material required for the screening is less than 1/1000th of the material used in conventional DSC tests which significantly reduce the material wastage. Isothermal TASC tests and IR imaging confirmed the occurrence of thermal dissolution of the drug in the polymer for more miscible pairs. The real-time stability tests validate the accuracy of the polymer-drug miscibility screening results. These results demonstrate TASC as a promising screening tool for rapidly selecting the polymeric excipients for pharmaceutical formulations development.

AB - This study aimed to develop a rapid, simple and inexpensive screening method for selecting the best polymeric candidates possessing high active pharmaceutical ingredient (API) miscibility during the early stages of formulation development of solid dispersion based pharmaceutical products. A new thermal imaging based method, thermal analysis by structural characterization (TASC), was used as a thermoptometeric tool in conjunction with data analysis software to detect the melting point depression and post-melting dissolution of felodipine particles screened over thin spin-coated films of ten polymers commonly used in the pharmaceutical field. On the polymeric substrates the drug showed different degrees of melting point reduction, reflecting their different levels of polymer-drug miscibility. Using TASC to detect melting point depression is significantly (20-40 times) faster than the conventional DSC method without loss of the sensitivity of detection. The quantity of the material required for the screening is less than 1/1000th of the material used in conventional DSC tests which significantly reduce the material wastage. Isothermal TASC tests and IR imaging confirmed the occurrence of thermal dissolution of the drug in the polymer for more miscible pairs. The real-time stability tests validate the accuracy of the polymer-drug miscibility screening results. These results demonstrate TASC as a promising screening tool for rapidly selecting the polymeric excipients for pharmaceutical formulations development.

U2 - 10.1021/acs.molpharmaceut.8b00798

DO - 10.1021/acs.molpharmaceut.8b00798

M3 - Article

VL - 15

SP - 5625

EP - 5636

JO - Molecular Pharmaceutics

JF - Molecular Pharmaceutics

SN - 1543-8384

IS - 12

ER -

ID: 144552350