A miniaturized in vitro release method for investigating drug-release mechanisms.

Abstract:

:We have evaluated a miniaturized in vitro method, based on the μDISS Profiler™ technique that enables on-line monitoring of drug release from a 21 μl sample with 10 ml of release medium. Four model drugs in eight clinically used formulations, including both solid and non-solid drug delivery systems, were investigated. The acquired data were compared with historical in vitro release data from the same formulations. Use of the Weibull function to describe the in vitro drug-release profiles allowed discrimination between the selected formulations with respect to the drug-release mechanisms. Comparison of the release data from the same formulation in different in vitro set-ups showed that the methodology used can affect the mechanism of in vitro release. We also evaluated the ability of the in vitro methods to predict in vivo activity by comparing simulated plasma concentration-time profiles acquired from the application of the biopharmaceutical software GI-Sim to the in vitro observations. In summary, the simulations based on the miniaturized-method release data predicted the plasma profiles as well as or more accurately than simulations based on the historical release data in 71% of the cases and this miniaturized in vitro method appears to be applicable for both solid and non-solid formulations.

journal_name

Int J Pharm

authors

Ahnfelt E,Sjögren E,Axén N,Lennernäs H

doi

10.1016/j.ijpharm.2015.03.076

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

339-49

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(15)00303-8

journal_volume

486

pub_type

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