Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast.

Madan, JR; Pawar, AR; Patil, RB; Awasthi, R; Dua, K

Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast.

Madan, JR Pawar, AR Patil, RB Awasthi, R Dua, K

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Publication Type:: Journal Article
Citation:: Polim Med, 2018, 48 (1), pp. 17 - 24
Issue Date:: 2018-01

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Field	Value	Language
dc.contributor.author	Madan, JR	en_US
dc.contributor.author	Pawar, AR	en_US
dc.contributor.author	Patil, RB	en_US
dc.contributor.author	Awasthi, R	en_US
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159	en_US
dc.date.issued	2018-01	en_US
dc.identifier.citation	Polim Med, 2018, 48 (1), pp. 17 - 24	en_US
dc.identifier.issn	0370-0747	en_US
dc.identifier.uri	http://hdl.handle.net/10453/130682
dc.description.abstract	BACKGROUND: Solid dispersions are among the techniques successfully employed to enhance the dissolution of poorly water-soluble drugs. Microwave (MW)-assisted evaporative crystallization has been used to prepare solid dispersions of drugs and polymers. OBJECTIVES: The aim of the study was to investigate the solubility of apremilast (APM) in water by exploring the effect of MW-assisted solid dispersion technology. MATERIAL AND METHODS: In the present study, solid dispersions of APM, a poorly water-soluble drug, were prepared. The solid dispersions were prepared using the conventional method (CM) and the MW-based solvent evaporation technique. Microwave energy was used to enhance the solubility and dissolution rate of APM. The physical mixture and solid dispersions were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Apremilast tablets containing MW-assisted solid dispersions were prepared by the direct compression technique and compared with the marketed formulation (Aprezo tablets). RESULTS: The results obtained confirmed the conversion of crystalline APM to an amorphous form. The XRPD pattern of the MW-assisted formulation at a 2:1 ratio suggests the amorphous structure of APM within the formulation. Based on solubility studies results, Syloid® 244FP was selected as the best carrier. The dissolution study results suggested that the APM tablet prepared using MW-assisted solid dispersions at a 2:1 carrier/drug ratio improved the APM dissolution rate compared to the marketed formulation. CONCLUSIONS: Based on the results, it can be concluded that the MW-assisted solid dispersion technique may be an effective approach to enhancing the dissolution profile of other poorly water-soluble drugs.	en_US
dc.language	eng	en_US
dc.relation.ispartof	Polim Med	en_US
dc.relation.isbasedon	10.17219/pim/99801	en_US
dc.subject.mesh	Thalidomide	en_US
dc.subject.mesh	Tablets	en_US
dc.subject.mesh	Calorimetry, Differential Scanning	en_US
dc.subject.mesh	Spectroscopy, Fourier Transform Infrared	en_US
dc.subject.mesh	Solubility	en_US
dc.subject.mesh	Microwaves	en_US
dc.title	Preparation, characterization and in vitro evaluation of tablets containing microwave-assisted solid dispersions of apremilast.	en_US
dc.type	Journal Article
utslib.citation.volume	1	en_US
utslib.citation.volume	48	en_US
utslib.location.activity	Poland	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	open_access
pubs.issue	1	en_US
pubs.publication-status	Published	en_US
pubs.volume	48	en_US

Abstract:

BACKGROUND: Solid dispersions are among the techniques successfully employed to enhance the dissolution of poorly water-soluble drugs. Microwave (MW)-assisted evaporative crystallization has been used to prepare solid dispersions of drugs and polymers. OBJECTIVES: The aim of the study was to investigate the solubility of apremilast (APM) in water by exploring the effect of MW-assisted solid dispersion technology. MATERIAL AND METHODS: In the present study, solid dispersions of APM, a poorly water-soluble drug, were prepared. The solid dispersions were prepared using the conventional method (CM) and the MW-based solvent evaporation technique. Microwave energy was used to enhance the solubility and dissolution rate of APM. The physical mixture and solid dispersions were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM). Apremilast tablets containing MW-assisted solid dispersions were prepared by the direct compression technique and compared with the marketed formulation (Aprezo tablets). RESULTS: The results obtained confirmed the conversion of crystalline APM to an amorphous form. The XRPD pattern of the MW-assisted formulation at a 2:1 ratio suggests the amorphous structure of APM within the formulation. Based on solubility studies results, Syloid® 244FP was selected as the best carrier. The dissolution study results suggested that the APM tablet prepared using MW-assisted solid dispersions at a 2:1 carrier/drug ratio improved the APM dissolution rate compared to the marketed formulation. CONCLUSIONS: Based on the results, it can be concluded that the MW-assisted solid dispersion technique may be an effective approach to enhancing the dissolution profile of other poorly water-soluble drugs.

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