Sweet Berberine

Abstract

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.

A New Co-Crystal of Synthetic Drug Rosiglitazone with Natural Medicine Berberine: Preparation, Crystal Structures, and Dissolution

“…The medicinal efficacy is affected badly by the moisture. According to reports, the berberine chloride has a hygroscopicity close to 20% in a high humidity environment with a relative humidity of 95%, which is a medium hygroscopic substance [ 24 ]. As exhibited in Figure 11 a, Rsg did not begin to absorb 0.46% water until the relative humidity reached 70%.…”

“…Due to its feasible hypoglycemic effect, berberine was used in combination with other hypoglycemic drugs to treat type 2 diabetes in clinical drug research [23]. Moreover, its chloride salt has good solubility in water [24], which meets the conditions of co-crystal formers. In this work, we seek to address the adverse properties of Rsg, such as solubility, by the technique of crystal engineering.…”

Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

“…Intrinsic dissolution rate (IDR) was determined by the rotating disc method [29,30] in a phosphate buffer at pH 6.8 to mimic duodenum pH. For each sample, approximately 20 mg of powder was compressed, using a custom-made stainless-steel die, at a force of 2000 lb against a flat stainless-steel disc for 2 min to prepare a pellet (6.39 mm in diameter).…”

Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

“…Intrinsic dissolution rate (IDR) of RTV was determined by the rotating disc method. 25,26 Dissolution medium was HCl aqueous solution with SLS (0-20 mM) at pH 1.2. Approximately 20 mg of RTV powder was compressed at a force of 2000 lb, using a custom-made stainless steel die, against a flat stainless steel disc for 2 min to prepare pellet (6.39 mm in diameter) with a visually smooth exposed surface that was coplanar with the surface of the die.…”