RESEARCH ARTICLE


Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique



Pankaj V. Dangre*, Vikesh B. Sormare, Mangesh D. Godbole
Department of Pharmaceutics, Kamla Nehru College of Pharmacy, Butibori, Nagpur-441108, Maharashtra, India


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© 2017 V. Dangre et al.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

* Address correspondence to this author at the Kamla Nehru College of Pharmacy, Butibori, Nagpur, Maharashtra, India; Tel:+91 9960160479; E-mail: pankaj_dangre@rediffmail.com


Abstract

Background:

Bosentan monohydrate (BM), a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH). It is poorly soluble in water, and having absolute bioavailability of 50%.

Objective:

The aim of the present work is to develop and evaluate the solid dispersions (SD) of a poorly water soluble drug bosentan monohydrate (BM).

Method:

Solid dispersions (SDs) systems of BM were prepared with Hydroxy propyle β-cyclodextrin (HPβ-CD) and Polyethylene glycol (PEG-4000) polymers using a spray drying technique.

Result:

The significant rise in a saturation solubility 174.23±1.36 mg/mL; and drug dissolution 95.11±1.22%; was observed with optimized formulation (SD 6). The solid state characterization of optimized formulation (SD 6) by SEM, DSC, and XRPD revealed the absence of crystalline nature of BM in solid dispersion. High dissolution rate of solid dispersion (SD 6) compared with pure drug indicated the increase in dissolution characteristics.

Conclusion:

In conclusion, our studies illustrated that spray drying technique could be useful large scale producing method to prepare the solid dispersion of bosentan with HP β-CD, which can improve the solubility as well as stability of the formulation.

Keywords: Bosentan monohydrate, Solid dispersion, Hydroxy propyle β-cyclodextrin, Polyethylene glycol, Spray drying.