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Pharmaceutics 2018, 10(1), 35; https://doi.org/10.3390/pharmaceutics10010035

Orally Disintegrating Tablets Containing Melt Extruded Amorphous Solid Dispersion of Tacrolimus for Dissolution Enhancement

1
Institute of Chemical and Engineering Sciences, 1, Pesek Road Jurong Island, Singapore 627833, Singapore
2
Department of Chemical and Biomolecular Engineering, National University of Singapore, Singapore 117585, Singpore
3
Department of Pharmacy, National University of Singapore, Singapore 117559, Singpore
*
Authors to whom correspondence should be addressed.
Received: 9 February 2018 / Revised: 9 March 2018 / Accepted: 10 March 2018 / Published: 16 March 2018
(This article belongs to the Special Issue Dissolution Enhancement of Poorly Soluble Drugs)
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Abstract

In order to improve the aqueous solubility and dissolution of Tacrolimus (TAC), amorphous solid dispersions of TAC were prepared by hot melt extrusion with three hydrophilic polymers, Polyvinylpyrrolidone vinyl acetate (PVP VA64), Soluplus® and Hydroxypropyl Cellulose (HPC), at a drug loading of 10% w/w. Molecular modeling was used to determine the miscibility of the drug with the carrier polymers by calculating the Hansen Solubility Parameters. Powder X-ray diffraction and differential scanning calorimetry (DSC) studies of powdered solid dispersions revealed the conversion of crystalline TAC to amorphous form. Fourier transform Infrared (FTIR) spectroscopy results indicated formation of hydrogen bond between TAC and polymers leading to stabilization of TAC in amorphous form. The extrudates were found to be stable under accelerated storage conditions for 3 months with no re-crystallization, indicating that hot melt extrusion is suitable for producing stable amorphous solid dispersions of TAC in PVP VA64, Soluplus® and HPC. Stable solid dispersions of amorphous TAC exhibited higher dissolution rate, with the solid dispersions releasing more than 80% drug in 15 min compared to the crystalline drug giving 5% drug release in two hours. These stable solid dispersions were incorporated into orally-disintegrating tablets in which the solid dispersion retained its solubility, dissolution and stability advantage. View Full-Text
Keywords: melt extrusion; amorphous solid dispersion; dissolution enhancement; tacrolimus; orally-disintegrating tablets melt extrusion; amorphous solid dispersion; dissolution enhancement; tacrolimus; orally-disintegrating tablets
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Ponnammal, P.; Kanaujia, P.; Yani, Y.; Ng, W.K.; Tan, R.B.H. Orally Disintegrating Tablets Containing Melt Extruded Amorphous Solid Dispersion of Tacrolimus for Dissolution Enhancement. Pharmaceutics 2018, 10, 35.

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