Session Speaker
The New Approach to Affect the Bioavailibility of Solid Drugs
Valeriy Komarov
Russia
The bioavailability and farmacokinetics of solid-state particles for
drug applications prepared from metastable solid-phases is discussed
in the context of drug delivery systems. Metastable solid-phases are
prepared by drug or joint drug and exipients vapor deposition on solid
surface. Stability at storage of final powders was more than 1-2 years.
Since most drugs are solids, drug design must consider solid state
properties such as supramolecular structure, the degree and type of
dispersivity, and drug and excipient combination efficiency. Modification
of these properties may influence the physico-chemical properties
and, as a consequence, bioavailability of the drug.
Main advantages of this approach rather to the most common approaches
for drug modification, first off all, high universality of technology
and ability to solve the problems inaccessible to other approaches,
are discussed. For poorly soluble drugs micronization without exipients
at certain conditions increased Cmax and decreased Tmax in 2-3 times
and at joint micronization usual exipients got ability to considerably
change the bioavailability of drugs. The bioavailability of water
soluble drugs could be increased in several times or at other conditions
of micronization rate and level of drug absorbsion could be strongly
reduced, that is necessary for creation of medicinal forms of the
prolonged action.
Examples involving different drugs are presented, which led to the
formation new polymorphs, new size distribution, new kind of joint
solid state with exipients that sharply change physico-chemical behaviour
and farmacokinetic properties and could be used to create new drug
formulations with enhanced bioavailability or prolonged action.
References:
1. Sergeev, G. B., Komarov, V. S., Mol. Cryst. Liq. Cryst., Vol. 456,
pp. 107-115, 2006.
2. Komarov,V. S. (2008). WO 2008/010741 A1.
3. Komarov,V. S. (2008). WO 2008/030134 A1.
4. Komarov, V. S., Morozov, Y.N, Zuev, A.P. (2008). Patent RU23 31409.
5. Komarov, V. S. (2009). Patent RU2347565.
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