Abstract: Disclosed is a preparation method for an SGLT2 inhibitor intermediate V, the method comprising: adding a compound IV to a solvent, and in the presence of a catalytic reagent, carrying out heat preservation reaction with a fluorination reagent. The preparation process for the intermediate V is simple in operations, mild in reaction conditions and high in safety, facilitates quality control and is suitable for industrial production. In addition, the intermediate V prepared by the method is high in purity, has few side reaction product monofluoro-impurity shown as structural Formula V?, is easy to purify, and is applicable to quality research on active pharmaceutical ingredients and preparations of the SGLT2 inhibitor.
Abstract: A gas layer is formed in a tablet core of the film-coated tablet after being immersed in acid. A mixture containing a permeation enhancer, a gas generating agent, and drug ingredients is compressed into a tablet. Then, the tablet is coated with a semipermeable film. After the film-coated tablet is immersed in acid for several seconds or longer, gas is generated from the tablet core to form a gas layer in the tablet core. Therefore, the tablet core becomes a two-layered structure, and the tablet floats. One of the layers is the gas layer. During a research process, the tablet core generates gas and expands, causing the film to rupture. After the film is ruptured, the tablet core can continue to float, and the drug release rate is related to the composition of the tablet core and is not affected by the film.