Solubility Measurement of Crystal Form II and Form V Ticagrelor in Several Pure Organic Solvents

Abstract

Ticagrelor (TCG) is a P2Y12 platelet inhibitor and has several crystal forms including Form II and Form V. In this work, it has been confirmed that Form II TCG would gradually transform to Form V in selected solvents. According to the crystal form stability, a dynamic method was adopted to measure the solubility of Form II TCG in six pure solvents (n-propanol, isopropanol, n-butanol, 2-butanol, ethyl acetate, and isopropyl acetate). The solubility of Form V TCG in 12 pure solvents (methanol, ethanol, n-propanol, isopropanol, n-butanol, 2-butanol, methyl acetate, ethyl acetate, isopropyl acetate, acetone, 2-butanone, and cyclohexanone) was measured by a static method. The solubility measurement temperature range was from 273.15 to 313.15 K. The experimental solubility data were correlated by the modified Apelblat model and the λh model. It was shown that the calculated solubility was consistent with the experimental data.

Solubility Measurement of the Crystal Form 1 and Form 4 Nirmatrelvir in Six Mono-Solvents and Two Binary Solvent Mixtures

“…In order to accurately determine the solid–liquid equilibrium point, EasyViewer was introduced to monitor the dissolution process. A similar experimental apparatus has been reported in our previous work . The high-resolution images caught by EasyViewer were analyzed by iC Vision 8.0.31 software to provide more information about suspension particles, such as turbidity and particle morphology.…”

“…A similar experimental apparatus has been reported in our previous work. 12 The high-resolution images caught by EasyViewer were analyzed by iC Vision 8.0.31 software to provide more information about suspension particles, such as turbidity and particle morphology. The experiment apparatus is shown in Figure 4.…”

A Study on the Crystal Transformation Relationships of Valacyclovir Hydrochloride Polymorphs: Sesquihydrate, Form I, and Form II

“…The solubility of SH, Form I, and Form II in different aqueous ethanol at 60 °C was measured, as shown in Figure 25. [11] It was found that with the decrease of ethanol content, the solubility difference between SH and Form I increased, which meant that the driving force of the transformation expended, so the transformation was accelerated. It followed the general law of SMT.…”