Debio Recherche Pharmaceutique S.a.

Asta Medica, Aktiengesellschaft

Debiopharm S.a.

Frederic Heimgartner

Piero Orsolini

Peter P Speiser

Edith Heimgartner

Urs Schleuniger

A composition designed for the sustained and controlled release of medicamentous peptide substances having the formula (I):

Composition for the sustained and controlled release of medicamentous

The process is aimed at providing a composition designed for the sustained and controlled release of medicamentous peptide substances, obtained in the form of microspheres of a biodegradable polymeric material incorporating said medicamentous substance. It consists in converting first a water-soluble peptide or peptide salt into a water-insoluble peptide, respectively peptide salt. The following steps include preparing an organic-aqueous emulsion and then extracting the organic solvent in an excess of aqueous medium.

Process for the preparation of microspheres made of a biodegradable

A pharmaceutical composition is prepared in the form of microparticles or of an implant comprising a biodegradable polymer selected from poly-1,4-butylene succinate, poly-2,3-butylene succinate, poly-1,4-butylene fumarate and poly-2,3-butylene succinate, incorporating as the active substance the pamoate, tannate, stearate or palmitate of a natural or of a synthetic peptide comprising 3 to 45 amino acids, such as LH-RH, somatostatin, GH-RH or calcitonin, or one of their synthetic analogues or homologues. The preparation comprises dry blending the ingredients in the form of powders, pre-compressing and preheating the mixture and then extruding the pre-compressed and pre-heated mixture. The product resulting from the extrusion step can then be comminuted and finally sieved.

Process for preparing a pharmaceutical composition

The ultracentrifugal disintegrator includes a device for cooling the annular zone (7), extending from the outer face (8) of the rotor (4) to the inner face (9) of the sieve (5), by feeding a gaseous coolant to the upper part of the zone (7), vertically with respect to the zone (7). Such a disintegrator is used for the cryocomminution of heat sensitive material.

Ultracentrifugal disintegrator and its use for the cryocomminution of

The pharmaceutical composition is intended in particular for the sustained and controlled release of an effective dose of a medicinal substance. It comprises, as a carrier for the medicinal substance, a biodegradable polymer or copolymer or a mixture of biodegradable polymers and/or copolymers derived from a dicarboxylic acid selected from the acids of the Krebs cycle, and from an aliphatic diol containing 4 carbon atoms or from cyclohexane-1,4-dimethanol.

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Martigny, Switzerland

Frederic Heimgartner