Crystal structure, dissolution and hygroscopicity of a novel cocrystal hydrate of berberine hydrochloride with L(+)-lactic acid.

Berberine hydrochloride (BCl) is commercially used to treat diarrhea, diabetes, hyperlipidemia, and cancer. However, BCl suffers from solid state instability, low aqueous solubility, low dissolution rate, and poor bioavailability, which limit its potential application in clinical medicine. In this work, we report a novel cocrystal hydrate of BCl with L(+)-lactic acid (BCl-LA-H₂O), designed to improve its physicochemical properties, thus promoting its application in the pharmaceutical industry. As a result, the cocrystal strategy improved the solubility, dissolution, melting point, and hygroscopicity of BCl, which indicated that the BCl-LA-H₂O can be used as a better solid form.