Drug–Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

Abstract

The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs.