68 results about "Rebamipide" patented technology

The present invention provides a combination of rebamipide and a tear-retaining agent as a medicament for the treatment of anterior eye diseases.

The invention discloses a preparation method of high-purity rebamipide. During synthesis process of a rebamipide crude product, the rebamipide crude product is precipitated out, in the form of a rebamipide salt solid, directly from a reaction solution. Thus, effective separation of impurities from a product is realized. A rebamipide salt crude product has good quality and high purity. Without further refining, dissociating is carried out directly by an acid-alkali method so as to obtain a high-purity rebamipide finished product. By the above method to obtain rebamipide, operational steps and refining frequency are minimized, and production efficiency is raised remarkably. In addition, a solvent used is cheap and easily available, and it is beneficial to realize industrial production.

The invention provides an improved process for preparing rebamipide that is useful as a medicament, which makes it possible to prepare rebamipide with high purity and high yield. The invention is an improved process for preparing rebamipide of the formula (1), comprising subjecting a carbostyril amino acid compound of the formula (5) or a salt thereof containing a compound of the formula (11) as an impurity to a reduction treatment in the presence of hydrogen and a catalyst in a basic aqueous solution, thereby selectively reducing the impurity compound (11) to transform into the carbostyril amino acid compound (5); and then acylating the compound (5) in a basic aqueous solution to give rebamipide (1).

The present invention relates to an eye drop composition for treating dry eye syndrome, characterized in that the eye drop composition remains stable during storage without precipitation occurring andcontains a safe ingredient for use as an eye drop, by solubilizing rebamipide that is a poorly soluble compound, and a method for producing the same. The eye drop composition for treating dry eye syndrome of the present invention includes a base for solubilizing rebamipide, and is characterized by containing a stabilizer for maintaining a supersaturated stabilized state, a specific type of bufferfor maintaining biocompatible pH of 7 to 8 and an osmotic agent. A method for producing the same comprises the steps of: adding a base to rebamipide or a pharmaceutically acceptable salt thereof anda stabilizer and dissolving the same in water to obtain an aqueous eye drop solution of pH of 10 to pH of 11; adding at least one osmotic agent selected from a buffer and a nonionic osmotic agent to the eye drop solution and dissolving the same; and after adjusting the pH to 7 to 8 with an acid, filtering the solution with a syringe filter to make the same sterile. The produced eye drop is in theform of an aqueous solution, is stable when frozen, refrigerated, and at room temperature, and includes a therapeutic agent for dry eye syndrome which is stable even when cross-stored in a refrigerator or at room temperature, or at a refrigerating temperature or room temperature.