In vitro evaluation and pharmacokinetics in dogs of solid dispersion pellets containing Silybum marianum extract prepared by fluid-bed coating.

Abstract:

:The solid dispersion of a poorly water-soluble Silybum marianum extract (SME) was prepared by a one-step fluid-bed coating technique depositing onto non-pareil pellets. In vitro evaluation indicated that this technique was highly efficient and reproducible producing pellets with acceptable appearance, flowability, friability, uniformity of drug content and enhanced dissolution. Physical characterization by DSC, powder X-ray diffractometry and FT-IR suggested the formation of a solid dispersion and possible interaction between PVP and the flavonolignans. Stress testing showed that the drug content and dissolution profiles of the SME solid dispersion pellets were sensitive to heat and humidity, while they are not affected under accelerated and long-term testing conditions. The relative bioavailability of solid dispersion pellets in dogs based on quantification of silibinin was about five-fold that of the SME suspension confirming enhanced oral bioavailability. It was concluded that the solid dispersion pellets prepared by fluid-bed coating showed favorable in vitro characteristics and enhanced oral bioavailability.

journal_name

Planta Med

journal_title

Planta medica

authors

Sun N,Zhang X,Lu Y,Wu W

doi

10.1055/s-2008-1034294

subject

Has Abstract

pub_date

2008-02-01 00:00:00

pages

126-32

issue

2

eissn

0032-0943

issn

1439-0221

journal_volume

74

pub_type

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