Formulation and solid state characterization of carboxylic acid-based co-crystals of tinidazole: An approach to enhance solubility.

Madan, JR; Dagade, RH; Awasthi, R; Dua, K

Formulation and solid state characterization of carboxylic acid-based co-crystals of tinidazole: An approach to enhance solubility.

Madan, JR Dagade, RH Awasthi, R Dua, K

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Publication Type:: Journal Article
Citation:: Polim Med, 2018, 48 (2), pp. 99 - 104
Issue Date:: 2018-07

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Field	Value	Language
dc.contributor.author	Madan, JR	en_US
dc.contributor.author	Dagade, RH	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	2018-07	en_US
dc.identifier.citation	Polim Med, 2018, 48 (2), pp. 99 - 104	en_US
dc.identifier.issn	0370-0747	en_US
dc.identifier.uri	http://hdl.handle.net/10453/136661
dc.description.abstract	BACKGROUND: Tinidazole (TNZ) is an anti-parasite drug used in the treatment of a variety of amebic and parasitic infections. It has low solubility in aqueous media and is categorized under Class II of the Biopharmaceutical Classification System. OBJECTIVES: The aim of this research was to study the potential for enhancing the solubility of TNZ using carboxylic acid co-crystals. MATERIAL AND METHODS: The solubility of TNZ was determined individually using 6 carboxylic acids for forming co-crystals at a 1:1 stoichiometric ratio. Three carboxylic acids - namely tartaric acid (TA), oxalic acid (OA) and glutaric acid (GA) - resulted in the formation of co-crystals with enhanced solubility. An equilibrium solubility study of TNZ co-crystals at 1:1.5 and 1:2 stoichiometric ratios was also carried out. The co-crystals which developed were evaluated using X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC) to study the drug-co-crystal former interactions. RESULTS: The solubility of TNZ in distilled water was found to be 0.014 mg/mL. The highest enhancement ratio was obtained with TNZ and TA at a ratio of 1:1. Differential scanning calorimetry thermograms suggested that the drug and carboxylic acids had undergone interactions such as hydrogen bonding. The XRD and DSC results confirmed the formation of co-crystals. CONCLUSIONS: It was concluded that the results of enhanced solubility of TNZ using co-crystals is a clear indication of the potential for co-crystals to be used in the future for other poorly water-soluble drugs, considering that co-crystals are a safe and cost-effective approach.	en_US
dc.language	eng	en_US
dc.relation.ispartof	Polim Med	en_US
dc.relation.isbasedon	10.17219/pim/105609	en_US
dc.subject.mesh	Carboxylic Acids	en_US
dc.subject.mesh	Tinidazole	en_US
dc.subject.mesh	Calorimetry, Differential Scanning	en_US
dc.subject.mesh	Crystallization	en_US
dc.subject.mesh	Spectroscopy, Fourier Transform Infrared	en_US
dc.subject.mesh	Solubility	en_US
dc.title	Formulation and solid state characterization of carboxylic acid-based co-crystals of tinidazole: An approach to enhance solubility.	en_US
dc.type	Journal Article
utslib.citation.volume	2	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	2	en_US
pubs.publication-status	Published	en_US
pubs.volume	48	en_US

Abstract:

BACKGROUND: Tinidazole (TNZ) is an anti-parasite drug used in the treatment of a variety of amebic and parasitic infections. It has low solubility in aqueous media and is categorized under Class II of the Biopharmaceutical Classification System. OBJECTIVES: The aim of this research was to study the potential for enhancing the solubility of TNZ using carboxylic acid co-crystals. MATERIAL AND METHODS: The solubility of TNZ was determined individually using 6 carboxylic acids for forming co-crystals at a 1:1 stoichiometric ratio. Three carboxylic acids - namely tartaric acid (TA), oxalic acid (OA) and glutaric acid (GA) - resulted in the formation of co-crystals with enhanced solubility. An equilibrium solubility study of TNZ co-crystals at 1:1.5 and 1:2 stoichiometric ratios was also carried out. The co-crystals which developed were evaluated using X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC) to study the drug-co-crystal former interactions. RESULTS: The solubility of TNZ in distilled water was found to be 0.014 mg/mL. The highest enhancement ratio was obtained with TNZ and TA at a ratio of 1:1. Differential scanning calorimetry thermograms suggested that the drug and carboxylic acids had undergone interactions such as hydrogen bonding. The XRD and DSC results confirmed the formation of co-crystals. CONCLUSIONS: It was concluded that the results of enhanced solubility of TNZ using co-crystals is a clear indication of the potential for co-crystals to be used in the future for other poorly water-soluble drugs, considering that co-crystals are a safe and cost-effective approach.

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http://hdl.handle.net/10453/136661