3 results about "Lafutidine" patented technology

This invention discloses a lafutidine pharmaceutical composition containing the following components by weight percentage: lafutidine 5-10%; lactose 35-70%; microcrystalline cellulose 5-20%; corn starch 5-20%; croscarmellose sodium 1-10%; hydroxypropyl cellulose 1-10%; colloidal silica 0.1-5%; and magnesium stearate 0.1-5%. The lafutidine pharmaceutical composition provided by this invention is suitable for direct powder compression, which simplifies the process and reduces costs compared to wet granulation for preparing lafutidine tablets. Under various influencing factors, the lafutidine tablets of this invention exhibit stable quality, and the trends of various test indicators are consistent with the original formulation.

The invention discloses a high-stability lafutidine tablet and a production process thereof, and relates to the technical field of medicine preparation. According to the invention, the solid dispersion system of lafutidine is prepared, so that the dissolution rate of lafutidine is increased, and the bioavailability is improved; through the synergistic effect of dry rolling and a stabilizer, the dry rolling densifies a solid dispersion system, improves the particle density, increases the intermolecular Van der Waals force, reduces the porosity and improves the stability of a microstructure; the particle size is controlled within the range of 50-70 meshes through screening, so that the uniformity of the system can be ensured, and the stability of the lafutidine can be remarkably improved; the high-stability lafutidine tablet is prepared by carrying out phenolation modification on vitamin C, endowing the characteristics of swallowing free radicals and absorbing ultraviolet rays and enhancing the antioxidant activity of the vitamin C, compounding phenolic vitamin C, tocopherol and mannitol to obtain a stabilizer, and improving the compatibility and flowability of the stabilizer and lafutidine.

This invention belongs to the field of medicinal chemistry and relates to a method for preparing lafutidine. The method involves an aminolysis reaction of the compound shown in Formula 2 with a primary amine compound in an organic solvent, followed by the addition of a base to the resulting reaction solution for further deprotection. The resulting compound, shown in Formula 4, undergoes a condensation reaction with the compound shown in Formula 5 to obtain lafutidine. Compared with existing technologies, the lafutidine preparation method provided by this invention has advantages such as low production cost, good safety, high purity, and suitability for industrial production.