Extruded Soluplus/SIM as an oral delivery system: characterization, interactions, in vitro and in vivo evaluations.

Abstract:

:The aim of this study was to obtain a stable, amorphous solid dispersion (SD) with Soluplus, prepared by hot-melt extrusion (HME) as an effective and stable oral delivery system to improve the physical stability and bioavailability of the poorly water-soluble simvastatin (SIM), a drug with relatively low Tg. The drug was proved to be miscible with Soluplus by calculation and measurements. The solubility, dissolution, thermal characteristics, interactions and physical stability of the SIM/Soluplus SDs were investigated. The crystal state of simvastatin in the SD was found to change from crystalline to amorphous form during the HME process and also hydrogen bonds were observed between SIM and the extruded Soluplus. The phase solubility showed the solubilization effect of Soluplus was strong and spontaneous. The equilibrium solubility illustrated that Soluplus/SIM SDs gained much higher solubility than its corresponding physical mixtures (PMs). Both of the dissolution profiles and in-vivo performance showed that the SIM/Soluplus SD obtained a marked enhancement, compared with the PM. There was a little change in the SIM/Soluplus SD during a 3-month storage period (40 °C, 75%), indicating the good physicochemical stability. The extruded Soluplus system prepared by HME is a good alternative for the water-insoluble SIM to improve the stability and bioavailability.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Zhang Y,Liu Y,Luo Y,Yao Q,Zhong Y,Tian B,Tang X

doi

10.3109/10717544.2014.960982

subject

Has Abstract

pub_date

2016-07-01 00:00:00

pages

1902-11

issue

6

eissn

1071-7544

issn

1521-0464

journal_volume

23

pub_type

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