Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach.

Madan, JR; Kamate, VJ; Dua, K; Awasthi, R

Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach.

Madan, JR Kamate, VJ Dua, K

Awasthi, R

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Publication Type:: Journal Article
Citation:: Polim Med, 2017, 47 (2), pp. 83 - 90
Issue Date:: 2017-07

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Field	Value	Language
dc.contributor.author	Madan, JR	en_US
dc.contributor.author	Kamate, VJ	en_US
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159	en_US
dc.contributor.author	Awasthi, R	en_US
dc.date.issued	2017-07	en_US
dc.identifier.citation	Polim Med, 2017, 47 (2), pp. 83 - 90	en_US
dc.identifier.issn	0370-0747	en_US
dc.identifier.uri	http://hdl.handle.net/10453/126706
dc.description.abstract	BACKGROUND: Nevirapine, an antiviral drug, is a potent reverse transcriptase inhibitor (NNRTI). It is used in combination with nucleoside analogues for treatment of HIV type-1 (HIV-1) infection and AIDS. Nevirapine is a BCS class II drug which shows dissolution rate limited absorption. OBJECTIVES: The aim of the present research was to provide a fast dissolving solid dispersion of nevirapine. MATERIAL AND METHODS: The solubility of nevirapine was initially determined individually in four hydrotropic agents - namely urea, lactose, citric acid and mannitol - at a concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. The highest solubility was obtained in the 40% citric acid solution. Then different combinations of 2 and 3 hydrotropic agents in different ratios were used to determine solubility, so that the total concentration of hydrotropic agents was always 40%. RESULTS: The highest solubility was obtained in a solution of lactose and citric acid at the optimum ratio of 15:25. This optimized combination was utilized in preparing solid dispersions by a common solvent technique using distilled water as a solvent. The solid dispersions were evaluated for XRD, DSC and FTIR to show no drug-hydrotrope interaction. CONCLUSIONS: It was concluded that the concept of mixed hydrotropic solid dispersion is a safe, novel and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs by dissolving the drug in a nonionized form. The enhancement in solubility of nevirapine using hydrotropy is a clear indication of its potential to be used in the future for other poorly water-soluble drugs in which low bioavailability is a major concern.	en_US
dc.language	eng	en_US
dc.relation.ispartof	Polim Med	en_US
dc.relation.isbasedon	10.17219/pim/77093	en_US
dc.subject.mesh	Mannitol	en_US
dc.subject.mesh	Citric Acid	en_US
dc.subject.mesh	Urea	en_US
dc.subject.mesh	Nevirapine	en_US
dc.subject.mesh	Lactose	en_US
dc.subject.mesh	Biological Availability	en_US
dc.subject.mesh	Solubility	en_US
dc.title	Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach.	en_US
dc.type	Journal Article
utslib.citation.volume	2	en_US
utslib.citation.volume	47	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	closed_access
pubs.issue	2	en_US
pubs.publication-status	Published	en_US
pubs.volume	47	en_US

Abstract:

BACKGROUND: Nevirapine, an antiviral drug, is a potent reverse transcriptase inhibitor (NNRTI). It is used in combination with nucleoside analogues for treatment of HIV type-1 (HIV-1) infection and AIDS. Nevirapine is a BCS class II drug which shows dissolution rate limited absorption. OBJECTIVES: The aim of the present research was to provide a fast dissolving solid dispersion of nevirapine. MATERIAL AND METHODS: The solubility of nevirapine was initially determined individually in four hydrotropic agents - namely urea, lactose, citric acid and mannitol - at a concentration of 10, 20, 30 and 40% w/v solutions using purified water as a solvent. The highest solubility was obtained in the 40% citric acid solution. Then different combinations of 2 and 3 hydrotropic agents in different ratios were used to determine solubility, so that the total concentration of hydrotropic agents was always 40%. RESULTS: The highest solubility was obtained in a solution of lactose and citric acid at the optimum ratio of 15:25. This optimized combination was utilized in preparing solid dispersions by a common solvent technique using distilled water as a solvent. The solid dispersions were evaluated for XRD, DSC and FTIR to show no drug-hydrotrope interaction. CONCLUSIONS: It was concluded that the concept of mixed hydrotropic solid dispersion is a safe, novel and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs by dissolving the drug in a nonionized form. The enhancement in solubility of nevirapine using hydrotropy is a clear indication of its potential to be used in the future for other poorly water-soluble drugs in which low bioavailability is a major concern.

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http://hdl.handle.net/10453/126706