170
that it is ideal; however, the physical mixture process does not yield
100% complexation.
∙ The physical mixture of lyophilized losartan with raw material
2-HP-β-CD led to interaction between the two molecules and
their existence in amorphous state.
∙ Finally, the physical mixture of lyophilized losartan with lyophilized 2-HP-β-CD was thermodynamically very close to their
complex, which indicates the high degree of interactions
between the molecules by utilizing these methods.
4 Notes
1. The raw materials are first subjected to lyophilization and then
physically mixed, in order to be analyzed. Lyophilization is
only possible for losartan in its salt form.
2. The complex is formed by dissolving the molecules and then
freeze-drying.
3. For losartan, this can be achieved because of the drug being
available in salt form with potassium, while this does not apply
for irbesartan.
4. The process of stirring inside the cyclodextrin solution aims to
increase the insertion of the drugs inside the cavity and lead to
complexation.
5. Single-component samples are neat 2-HP-β-CD, irbesartan,
losartan, or their lyophilized forms. Samples containing mixture of raw materials, their lyophilized forms, or combinations
of those are prepared by weighting raw material or lyophilized
2-HP-β-CD and raw material or lyophilized sartan, in 3.6:1
molar ratio, for a total of approximately 3 mg.
Cyclodextrin:sartan complex preparations have been described
previously.
6. Equilibration is considered necessary for samples that have
been previously hydrated with aqueous media; however, the
same applies for solids, because of the pressure applied during
the crucible sealing.
7. The isotherm at the analysis starting point is necessary to
ensure that the sample is at equilibrium.
8. Typically, the analysis temperature range depends on the melting points and the various thermodynamic alterations, endothermic or exothermic, that are expected for every component
that is analyzed. As a result, the range should be the same for
all samples, in order to be able to assess all types of interactions
between the components. Based on the bibliography, the
expected melting points for irbesartan and losartan, respecNikolaos Naziris et al.
that it is ideal; however, the physical mixture process does not yield
100% complexation.
∙ The physical mixture of lyophilized losartan with raw material
2-HP-β-CD led to interaction between the two molecules and
their existence in amorphous state.
∙ Finally, the physical mixture of lyophilized losartan with lyophilized 2-HP-β-CD was thermodynamically very close to their
complex, which indicates the high degree of interactions
between the molecules by utilizing these methods.
4 Notes
1. The raw materials are first subjected to lyophilization and then
physically mixed, in order to be analyzed. Lyophilization is
only possible for losartan in its salt form.
2. The complex is formed by dissolving the molecules and then
freeze-drying.
3. For losartan, this can be achieved because of the drug being
available in salt form with potassium, while this does not apply
for irbesartan.
4. The process of stirring inside the cyclodextrin solution aims to
increase the insertion of the drugs inside the cavity and lead to
complexation.
5. Single-component samples are neat 2-HP-β-CD, irbesartan,
losartan, or their lyophilized forms. Samples containing mixture of raw materials, their lyophilized forms, or combinations
of those are prepared by weighting raw material or lyophilized
2-HP-β-CD and raw material or lyophilized sartan, in 3.6:1
molar ratio, for a total of approximately 3 mg.
Cyclodextrin:sartan complex preparations have been described
previously.
6. Equilibration is considered necessary for samples that have
been previously hydrated with aqueous media; however, the
same applies for solids, because of the pressure applied during
the crucible sealing.
7. The isotherm at the analysis starting point is necessary to
ensure that the sample is at equilibrium.
8. Typically, the analysis temperature range depends on the melting points and the various thermodynamic alterations, endothermic or exothermic, that are expected for every component
that is analyzed. As a result, the range should be the same for
all samples, in order to be able to assess all types of interactions
between the components. Based on the bibliography, the
expected melting points for irbesartan and losartan, respecNikolaos Naziris et al.