Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology

Sultan M. Alshehri; Jun Bom Park; Bader B. Alsulays; Roshan V. Tiwari; Bjad Almutairy; Abdullah S. Alshetaili; Joseph Morott; Sejal Shah; Vijay Kulkarni; Soumyajit Majumdar; Scott T. Martin; Sanjay Mishra; Lijia Wang; Michael A. Repka

doi:10.1016/j.jddst.2015.03.003

Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology

Sultan M. Alshehri, Jun Bom Park, Bader B. Alsulays, Roshan V. Tiwari, Bjad Almutairy, Abdullah S. Alshetaili, Joseph Morott, Sejal Shah, Vijay Kulkarni, Soumyajit Majumdar, Scott T. Martin, Sanjay Mishra, Lijia Wang, Michael A. Repka

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

60 Scopus citations

Abstract

The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit® E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25% of drug loading. SEM images indicated aggregation of MA at over 30% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20% and 25% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40 °C/75% RH and 12 months at 25 °C/60% RH, respectively.

Original language	English
Pages (from-to)	18-27
Number of pages	10
Journal	Journal of Drug Delivery Science and Technology
Volume	27
DOIs	https://doi.org/10.1016/j.jddst.2015.03.003
State	Published - 1 Jun 2015
Externally published	Yes

Keywords

Hot-melt extrusion
Molecular interaction
Orally disintegrating tablets
Solid dispersion
Solubility enhancement
Taste masking effect

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10.1016/j.jddst.2015.03.003

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Alshehri, S. M., Park, J. B., Alsulays, B. B., Tiwari, R. V., Almutairy, B., Alshetaili, A. S., Morott, J., Shah, S., Kulkarni, V., Majumdar, S., Martin, S. T., Mishra, S., Wang, L., & Repka, M. A. (2015). Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology. Journal of Drug Delivery Science and Technology, 27, 18-27. https://doi.org/10.1016/j.jddst.2015.03.003

@article{cd0d9700d19a4772bd1c2a6242accb92,

title = "Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology",

abstract = "The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit{\textregistered} E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40\% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25\% of drug loading. SEM images indicated aggregation of MA at over 30\% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20\% and 25\% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40 °C/75\% RH and 12 months at 25 °C/60\% RH, respectively.",

keywords = "Hot-melt extrusion, Molecular interaction, Orally disintegrating tablets, Solid dispersion, Solubility enhancement, Taste masking effect",

author = "Alshehri, \{Sultan M.\} and Park, \{Jun Bom\} and Alsulays, \{Bader B.\} and Tiwari, \{Roshan V.\} and Bjad Almutairy and Alshetaili, \{Abdullah S.\} and Joseph Morott and Sejal Shah and Vijay Kulkarni and Soumyajit Majumdar and Martin, \{Scott T.\} and Sanjay Mishra and Lijia Wang and Repka, \{Michael A.\}",

year = "2015",

month = jun,

day = "1",

doi = "10.1016/j.jddst.2015.03.003",

language = "English",

volume = "27",

pages = "18--27",

journal = "Journal of Drug Delivery Science and Technology",

issn = "1773-2247",

publisher = "Editions de Sante",

}

Alshehri, SM, Park, JB, Alsulays, BB, Tiwari, RV, Almutairy, B , Alshetaili, AS, Morott, J, Shah, S, Kulkarni, V, Majumdar, S, Martin, ST, Mishra, S, Wang, L & Repka, MA 2015, 'Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology', Journal of Drug Delivery Science and Technology, vol. 27, pp. 18-27. https://doi.org/10.1016/j.jddst.2015.03.003

TY - JOUR

T1 - Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology

AU - Alshehri, Sultan M.

AU - Park, Jun Bom

AU - Alsulays, Bader B.

AU - Tiwari, Roshan V.

AU - Almutairy, Bjad

AU - Alshetaili, Abdullah S.

AU - Morott, Joseph

AU - Shah, Sejal

AU - Kulkarni, Vijay

AU - Majumdar, Soumyajit

AU - Martin, Scott T.

AU - Mishra, Sanjay

AU - Wang, Lijia

AU - Repka, Michael A.

PY - 2015/6/1

Y1 - 2015/6/1

N2 - The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit® E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25% of drug loading. SEM images indicated aggregation of MA at over 30% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20% and 25% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40 °C/75% RH and 12 months at 25 °C/60% RH, respectively.

AB - The objective of this study was to enhance the solubility as well as to mask the intensely bitter taste of the poorly soluble drug, Mefenamic acid (MA). The taste masking and solubility of the drug was improved by using Eudragit® E PO in different ratios via hot melt extrusion (HME), solid dispersion technology. Differential scanning calorimetry (DSC) studies demonstrated that MA and E PO were completely miscible up to 40% drug loads. Powder X-ray diffraction analysis indicated that MA was converted to its amorphous phase in all of the formulations. Additionally, FT-IR analysis indicated hydrogen bonding between the drug and the carrier up to 25% of drug loading. SEM images indicated aggregation of MA at over 30% of drug loading. Based on the FT-IR, SEM and dissolution results for the extrudates, two optimized formulations (20% and 25% drug loads) were selected to formulate the orally disintegrating tablets (ODTs). ODTs were successfully prepared with excellent friability and rapid disintegration time in addition to having the desired taste-masking effect. All of the extruded formulations and the ODTs were found to be physically and chemically stable over a period of 6 months at 40 °C/75% RH and 12 months at 25 °C/60% RH, respectively.

KW - Hot-melt extrusion

KW - Molecular interaction

KW - Orally disintegrating tablets

KW - Solid dispersion

KW - Solubility enhancement

KW - Taste masking effect

UR - http://www.scopus.com/inward/record.url?scp=84941645173&partnerID=8YFLogxK

U2 - 10.1016/j.jddst.2015.03.003

DO - 10.1016/j.jddst.2015.03.003

M3 - Article

AN - SCOPUS:84941645173

SN - 1773-2247

VL - 27

SP - 18

EP - 27

JO - Journal of Drug Delivery Science and Technology

JF - Journal of Drug Delivery Science and Technology

ER -

Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology

Abstract

Keywords

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