Abstract: The present invention describes a pharmaceutical composition of biologically active peptides, associated with a controlled release system using cyclodextrins or derivatives thereof, liposomes and biodegradable polymers and/or mixtures of said systems for increasing bioavailability, duration and intensity of the biological effects of the peptide. Specifically, the present invention comprises a pharmaceutical composition, a process for preparing same, and the use of a peptide in said composition for preparing medication for intraocular hypertension or glaucoma. The present invention falls within the field of Medical Science, more specifically of preparations for medical purposes, and even more specifically of medicinal preparations containing peptides.