Debiopharm S.a.

Debio Recherche Pharmaceutique S.a.

Romano Deghenghi

Piero Orsolini

Rolland-Yves Mauvernay

Francesco Maria Veronese

Luciana Sartore

A pharmaceutical composition for the sustained release of a peptide wherein the composition includes a polylactide polymer, a polymer of lactic acid and glycolic acid, or a mixture of such polymers and a therapeutically active peptide in the form of its pamoate, tannate or stearate salt. The composition when placed in an aqueous physiological environment releases the peptide in a continuous manner for a period of at least about one week.

Sustained and controlled release of water insoluble polypeptides

Biologically active drug polymer derivatives and method for preparing

There is disclosed a pharaceutical composition for sustained and controlled release of drug over an extended period of time comprising a polylactide, a copolymer of lactic and glycolic acid, a mixture of such polymers and a water-insoluble peptide which, when placed in an aqueous physiologically-type environment releases the peptide in continuous manner for a period of at least one week, and with an initial release for the first twenty-four hours of not more than 30% of the total amount released. There is thus provided the control of the release pattern and in general a decrease of the initial burst effect.

The microencapsulation of medicamentous water-soluble substances is carried out by phase separation. The operations of the hardening step take place at a temperature comprised between about 0.degree. and about 25.degree. C., the non-solvent used during this step being an aliphatic fluorinated or fluorohalogenated hydrocarbon or a mixture of such hydrocarbons. Further, the non-solvent is used in an excess with respect to the volume of solvent and non-solvent resulting from the phase-separation step.

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Lausanne, Switzerland

Romano Deghenghi