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There are many examples of varying effects of excipients on
pharmacokinetics of parenteral drugs.
http://pages.unibas.ch/diss/2005/DabsB_7289.pdf
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The following message was posted to: PharmPK
Dave,
> Does anyone have examples of IV dosed drugs whose PK characteristics/
> profile can be altered by changing the dosing formulation?
> Liposomes come to mid but are there others???
Paclitaxel is the first example that comes to mind. There has been
several approaches to develop cremophor-free formulations to get away
from cremophor, to alter clearance and drug distribution. They use
different technologies: albumin-bound nanoparticles (Abraxane),
polymeric micelle formulation (Genexol-PM), emulsion systems, other
nanoparticle formulations.
Regards,
Katya
--
Ekaterina Gibiansky
Senior Director, PKPD, Modeling & Simulation
ICON Development Solutions
Ekaterina.Gibiansky.-a-.iconplc.com
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The following message was posted to: PharmPK
"Does anyone have examples of IV dosed drugs whose PK characteristics/
profile can be altered by changing the dosing formulation?"
There are examples specially with drugs like cyclosproin, tacrolimus,
amphotericin B, doxorubicin, paclitaxel and anti-viral. Most of these
approaches are parenteral rather than oral; and rely on the disposition
kinetics of the carrier (delivery vehicle/device) per se like liposomes,
polymeric micelles, polymeric nanoparticles, hydrogels and implants.
Here
the release kinetics of drugs through these carriers dictate the PK
profile
and hence disposition kinetics of carrier comes into light. Even a
prodrug
or enzyme linked prodrug system can be fabricated towards this
direction.
It is however difficult to alter pharmacokinetics after oral delivery
except where the absorption is primarily through pathways other than
passive diffusion like using lipid-based delivery and relying on lipid
digestion or lymphatic pathway. Cyclosporin and anti-virals are prime
drugs
where such efforts have been documented in the literature.
Having said that, it is difficult to generalize and this could be
evalauted
on a case be case basis.
V. Sihorkar
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There are plenty of them.
Nanoparticles, Dendrimers, Micelles to name a few
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