Polymers in Medicine

Polim. Med.
Scopus CiteScore: 3.5 (CiteScore Tracker 3.6)
Index Copernicus (ICV 2023) – 121.14
MEiN – 70
ISSN 0370-0747 (print)
ISSN 2451-2699 (online) 
Periodicity – biannual

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Polymers in Medicine

2017, vol. 47, nr 2, July-December, p. 83–90

doi: 10.17219/pim/77093

Publication type: original article

Language: English

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Creative Commons BY-NC-ND 3.0 Open Access

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

Jyotsana R. Madan1,A,B,C,D,E,F, Virendra J. Kamate1,A,B,C,D,E,F, Kamal Dua2,3,4,A,C,D,E,F, Rajendra Awasthi5,A,C,D,E,F

1 Department of Pharmaceutics, Sinhgad Technical Education Society’s, Smt. Kashibai Navale College of Pharmacy, Pune, Maharashtra, India

2 Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Sydney, Australia

3 School of Pharmacy and Biomedical Sciences, The University of Newcastle, Newcastle, Australia

4 School of Pharmaceutical Sciences, Shoolini University, Solan, India

5 NKBR College of Pharmacy & Research Centre, Meerut, India

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.
Conclusion. 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.

Key words

nevirapine, solid dispersion, mixed hydrotropy

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