Mefenamic acid solid dispersions: impact of formulation composition on processing parameters, product properties and performance

Elke Prasad; John Robertson; Gavin W. Halbert

doi:10.1016/j.ijpharm.2022.121505

Mefenamic acid solid dispersions: impact of formulation composition on processing parameters, product properties and performance

Elke Prasad, John Robertson, Gavin W. Halbert

Strathclyde Institute Of Pharmacy And Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

14 Citations (Scopus)

25 Downloads (Pure)

Abstract

The objective of this study was to develop an immediate release (IR), crystalline solid dispersion (CSD) formulation of Mefenamic acid (MFA) by hot-melt-extrusion (HME) and assess the impact of drug loading on process parameters, product physico-chemical properties and product performance. An HME process to produce a range of MFA-Soluplus®-Sorbitol polymer matrix CSD formulations was developed based on rheological screening assays of physical mixtures (PM). The impact of drug loading on process parameters was compared to the impact of drug loading on the physico-chemical properties of formulations. Based on process and product data, three groupings of API drug loading were identified: sub-saturated, saturated, and supersaturated systems. CSD formulations were obtained for 20 - 50% (w/w) drug loading containing the stable polymorphic form I of MFA. CSD formulations predominantly improved the consistency of the product performance. An Amorphous Solid Dispersion (ASD) was obtained for 10% (w/w) drug loading, exhibiting faster drug release even at physiologically relevant pH. This study illustrates the impact of drug loading on process and product characteristics and how a better understanding of maximum API solubility in a given polymer system can improve targeted formulation development.

Original language	English
Article number	121505
Number of pages	15
Journal	International Journal of Pharmaceutics
Volume	616
Early online date	10 Feb 2022
DOIs	https://doi.org/10.1016/j.ijpharm.2022.121505
Publication status	Published - 25 Mar 2022

Keywords

extrusion
solid dosage forms
oral drug delivery
solid dispersion
dissolution
formulation

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10.1016/j.ijpharm.2022.121505Licence: CC BY 4.0

Prasad-etal-IJP-2022-Mefenamic-acid-solid-dispersionsFinal published version, 7.42 MBLicence: CC BY 4.0

Future Continuous Manufacturing and Advanced Crystallisation Research Hub (CMAC Hub)
Florence, A. (Principal Investigator), Brown, C. (Co-investigator), Halbert, G. (Co-investigator), Johnston, B. (Co-investigator), Markl, D. (Co-investigator), Nordon, A. (Co-investigator), Price, C. J. (Co-investigator), Sefcik, J. (Co-investigator) & Ter Horst, J. (Co-investigator)
EPSRC (Engineering and Physical Sciences Research Council)
1/01/17 → 30/09/24
Project: Research
Cancer Research UK Formulation - PhD Studentship
Halbert, G. (Principal Investigator), Dick, L. (Co-investigator), Elliott, M. (Co-investigator) & Ford, S. (Co-investigator)
Cancer Research UK CRUK
1/10/15 → 31/03/22
Project: Research - Studentship

Data for: "Mefenamic acid solid dispersions: Impact of formulation composition on processing parameters, product properties and performance"
Prasad, E. (Creator), Robertson, J. (Contributor) & Halbert, G. (Contributor), University of Strathclyde, 25 Oct 2021
DOI: 10.15129/8597108f-6daa-43e1-8d2d-796b97c36f3a
Dataset

Cite this

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title = "Mefenamic acid solid dispersions: impact of formulation composition on processing parameters, product properties and performance",

abstract = "The objective of this study was to develop an immediate release (IR), crystalline solid dispersion (CSD) formulation of Mefenamic acid (MFA) by hot-melt-extrusion (HME) and assess the impact of drug loading on process parameters, product physico-chemical properties and product performance. An HME process to produce a range of MFA-Soluplus{\textregistered}-Sorbitol polymer matrix CSD formulations was developed based on rheological screening assays of physical mixtures (PM). The impact of drug loading on process parameters was compared to the impact of drug loading on the physico-chemical properties of formulations. Based on process and product data, three groupings of API drug loading were identified: sub-saturated, saturated, and supersaturated systems. CSD formulations were obtained for 20 - 50% (w/w) drug loading containing the stable polymorphic form I of MFA. CSD formulations predominantly improved the consistency of the product performance. An Amorphous Solid Dispersion (ASD) was obtained for 10% (w/w) drug loading, exhibiting faster drug release even at physiologically relevant pH. This study illustrates the impact of drug loading on process and product characteristics and how a better understanding of maximum API solubility in a given polymer system can improve targeted formulation development.",

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T2 - impact of formulation composition on processing parameters, product properties and performance

AU - Prasad, Elke

AU - Robertson, John

AU - Halbert, Gavin W.

PY - 2022/3/25

Y1 - 2022/3/25

N2 - The objective of this study was to develop an immediate release (IR), crystalline solid dispersion (CSD) formulation of Mefenamic acid (MFA) by hot-melt-extrusion (HME) and assess the impact of drug loading on process parameters, product physico-chemical properties and product performance. An HME process to produce a range of MFA-Soluplus®-Sorbitol polymer matrix CSD formulations was developed based on rheological screening assays of physical mixtures (PM). The impact of drug loading on process parameters was compared to the impact of drug loading on the physico-chemical properties of formulations. Based on process and product data, three groupings of API drug loading were identified: sub-saturated, saturated, and supersaturated systems. CSD formulations were obtained for 20 - 50% (w/w) drug loading containing the stable polymorphic form I of MFA. CSD formulations predominantly improved the consistency of the product performance. An Amorphous Solid Dispersion (ASD) was obtained for 10% (w/w) drug loading, exhibiting faster drug release even at physiologically relevant pH. This study illustrates the impact of drug loading on process and product characteristics and how a better understanding of maximum API solubility in a given polymer system can improve targeted formulation development.

AB - The objective of this study was to develop an immediate release (IR), crystalline solid dispersion (CSD) formulation of Mefenamic acid (MFA) by hot-melt-extrusion (HME) and assess the impact of drug loading on process parameters, product physico-chemical properties and product performance. An HME process to produce a range of MFA-Soluplus®-Sorbitol polymer matrix CSD formulations was developed based on rheological screening assays of physical mixtures (PM). The impact of drug loading on process parameters was compared to the impact of drug loading on the physico-chemical properties of formulations. Based on process and product data, three groupings of API drug loading were identified: sub-saturated, saturated, and supersaturated systems. CSD formulations were obtained for 20 - 50% (w/w) drug loading containing the stable polymorphic form I of MFA. CSD formulations predominantly improved the consistency of the product performance. An Amorphous Solid Dispersion (ASD) was obtained for 10% (w/w) drug loading, exhibiting faster drug release even at physiologically relevant pH. This study illustrates the impact of drug loading on process and product characteristics and how a better understanding of maximum API solubility in a given polymer system can improve targeted formulation development.

KW - extrusion

KW - solid dosage forms

KW - oral drug delivery

KW - solid dispersion

KW - dissolution

KW - formulation

U2 - 10.1016/j.ijpharm.2022.121505

DO - 10.1016/j.ijpharm.2022.121505

M3 - Article

SN - 0378-5173

VL - 616

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

M1 - 121505

ER -

Mefenamic acid solid dispersions: impact of formulation composition on processing parameters, product properties and performance

Abstract

Keywords

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Projects

Future Continuous Manufacturing and Advanced Crystallisation Research Hub (CMAC Hub)

Cancer Research UK Formulation - PhD Studentship

Datasets

Data for: "Mefenamic acid solid dispersions: Impact of formulation composition on processing parameters, product properties and performance"

Cite this