Table 2.
Solubility product (Ksp), intrinsic solubility (S0,CC), and solubility advantage ( ) of LTG cocrystals and salts.
Solid Phase | Ksp (M2) | S0,CC or S0,Salt (M) | SA |
---|---|---|---|
LTG-NCT Cocrystal | (1.4±0.4) ×10−4 | 1.2 × 10−2 | 18 |
LTG-HCl Salt | (6.7±0.53) × 10−5 a | 8.2 × 10−3 | 12 |
LTG-SAC Salt | (1.1±0.2) × 10−5 | 3.3 × 10−3 | 5 |
LTG-MP Cocrystal | (5.3±0.47) × 10−7 b | 7.3 × 10−4 | 1.1 |
LTG-PB Cocrystal | (1.2±0.5) × 10−8 | 1.1 × 10−4 | 0.2 |
Ksp of LTG-HCl was calculated from reported solubility of 0.46 mg/mL at 37°C (pH 1.2) from reference27. Ksp of the salt was estimated at 25°C from [LTGH+] and [Cl−] concentrations calculated from the dissolved salt and HCl concentrations, using a heat of solution value of 30 kJ/mol.
Steady state concentration from dissolution data in reference (3) was used to calculate the Ksp of lamotrigine-methylparaben (LTG-MP) cocrystal, where cocrystal was reported to be stable.