Sweet Berberine

Berberine is a drug with an intense bitter taste. The high aqueous solubility of its chloride salt, which is commonly used in commercial drug products of berberine, worsens the challenge of taste masking. We have approached this drug delivery challenge by forming salts with the sweeteners acesulfame and saccharine, through the anion exchange reaction. In addition to the intrinsic sweetness of the two counterions, both salts also exhibit reduced aqueous solubility, which further alleviates the problem of bitter taste of the drug by limiting dissolution of berberine. Moreover, both salts exhibit good tableting performance. They are also non-hygroscopic and stable against high humidity and temperature. The stability against humidity variations makes the two sweet salts more amenable for tablet development over the chloride salt, which undergoes complex hydration/dehydration phase changes when relative humidity varies. Collectively, the two novel solid phases of berberine are sweet and exhibit superior properties for developing pharmaceutically elegant drug products.