Assessing Drug Release from Manipulated Abuse Deterrent Formulations
Tóm tắt
There is a need to develop in vitro
dissolution methods that discriminate for particle size of the manipulated abuse
deterrent formulation (ADF) and that can be used for in
vivo predictive models since dissolution methods developed for intact
formulation might not be suitable for manipulated ones. A vertical diffusion cell
(VDC) and United States Pharmacopeia (USP) Apparatus 1, 2, and 4 were evaluated for
measuring the dissolution of intact and manipulated metoprolol succinate tablets
with abuse deterrent-like properties. These tablets were physically manipulated to
produce fine (106–500 μm) and coarse (500–1000 μm) powder samples. The VDC method
was not able to discriminate the effect of particle size on drug release with varied
stirring rate (200 to 800 rpm), molecular weight cut-off (MWCO, 3–5 kDa to
12–14 kDa) of the diffusion membrane, or composition and ionic strength (0.45% and
0.9%) of receiver medium. Standard and modified USP Apparatus 1 and 2 methods were
assessed; however, large variations (RSD > 20%) were observed with USP Apparatus
1 for manipulated product dissolution and floating powder samples caused failure of
auto-sampling when using standard USP Apparatus 2. For the USP Apparatus 4
dissolution method, packing configuration (1, 3, 8 layers and blend), ionic strength
of dissolution medium (0.017, 0.077, and 0.154 M additional NaCl), and flow rate (4,
8, 16 mL/min) were studied to discriminate the effect of particle size on release.
The USP Apparatus 4 dissolution method was optimized by using a packaging
configuration of 8 layers with 8 mL/min flow rate which exhibited low variability
and complete drug release and it could be used for in
vivo predictive models. The dissolution method variables can be
optimized for a specific product for desirable reproducibility and discriminatory
power when using USP Apparatus 4.
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