Method for increasing the solubility and stability of chloramphenicol, by the formation of inclusion complexes with cyclodextrins, solutions containing said inclusion complex, and process for the preparation of these solutions

摘要

The present invention relates to a method for increasing the solubility and stability of chloramphenicol, characterized by adding chloramphenicol to a solution containing a cyclodextrin, preferably β- dimethylcyclodextrin or β-hydroxypropylcyclodextrin, so as to obtain an inclusion complex between the chloramphenicol and said cyclodextrin. The invention also relates to a solution, preferably a collyrium containing chloramphenicol, a cyclodextrin, and ophthalmologically acceptable vehicles and adjuvants. More concretely, a collyrium solution of the invention will contain from 0.5 to 1.0% (w/v) of chloramphenicol, from 3.0 to 15.0% (w/v) of a suitable cyclodextrin, from 0.5 to 1.0% (w/v) of boric acid, from 0.05 to 0.20% (w/v) of sodium borate, from 0.001 to 0.003% (w/v) of phenylmercury nitrate, and make-up water. The invention also relates to a process for the preparation of said solution.