Oral Solubilization Technology: The Applicability of SDDs
SDD technology is most applicable to compounds with aqueous solubilities
from 100 to 0.001 µg/mL and log P values from 2 to 8.
For numerous pharmacological reasons, many active compounds have poor aqueous
solubility. A large percentage of these compounds are poorly absorbed when
dosed orally, unless their solubility is enhanced and their dissolution rate is
improved. The SDD technology offers a fully developed formulation platform
that can improve the bioavailability of these problematic low-solubility
compounds. The SDD technology expands the druggable chemical space currently
limited by traditional oral dosing constraints, such as Lipinski's "rule of
five".1 The
SDDs provide a solid, amorphous drug substance that is easily formulated as a
tablet, capsule, or oral powder. SDDs significantly improve bioavailability
for compounds outside of conventional druggable physicochemical space.
Predictive biological models have been developed to assess the suitability of
the SDD technology for specific compounds. These biomodels are based on
extensive knowledge generated from more than 13 years of development. These
biomodels are also used to generate "guidance surfaces" for oral absorption of
low-solubility compounds using SDD technology. These predictions have been
validated with numerous in vivo studies and quantitatively map the
physicochemical property space where the technology has the largest impact.
This information is used to predict the in vivo performance over a wide
range of chemical space.
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