Crystal Forms of Anti-HIV Drugs: Role of Recrystallization

Developing a model-driven workflow for the digital design of small-scale batch cooling crystallisation with the antiviral lamivudine

“…XRPD also confirmed the presence of the most thermodynamically stable form, form II. 11 Later data collected in this study showed that form I, on the other hand, had a crystallisation exotherm at 139.1 °C (Fig. S1 in the ESI †) and melting endotherm at 178.8 °C with TGA data showing approximately 2% mass loss (Fig.…”

“…9 Lamivudine has been shown to produce three crystalline forms, form I, which is a 0.2 hydrate that exhibits needle geometry, and two anhydrous forms, form II, and III which typically adopt bipyramidal 10 and needle morphologies, respectively. 11 Existing patents state that form I and form II are preferred in solid oral dosing. 12 Therefore, the objective of the crystallisation is the purification and management of physical attributes to ease downstream processing.…”

The effect of efflux bomb and the transmural potential difference in the permeation of azidothymidine across the small intestine of the rat

“…Solid dispersion technology has been applied to develop formulations with a high drug loading (e.g. Zidovudine Tablets USP 300 mg per tablet) or containing drugs with a high tendency to crystallize 10 . However, the aim of this study was to improve the AZT permeation rate using Pluronic P-407 as an inhibitor of ABC transporters and PLDLA 30/70 to decrease the solubility of zidovudine and to prevent the re-crystallization with a crystal lattice different.…”