Debio Recherche Pharmaceutique S.a.

Debiopharm S.a.

Asta Medica, Aktiengesellschaft

Debio Recherche Pharmaceutique

Piero Orsolini

Frederic Heimgartner

Romano Deghenghi

Rolland-Yves Mauvernay

Robert Gurny

Francesco Maria Veronese

Alexandra Rothen-Weinhold

Fr&eacute;d&eacute;ric Heimgartner

Thomas R Tice

Andrew V Schally

Paolo Ferruti

Peter P Speiser

Oddone Schiavon

Paolo Caliceti

Luciana Sartore

Edith Heimgartner

Evelyne Vuaridel

Urs Schleuniger

Biologically active drug polymer derivatives, namely peptides or protein derivatives, are useful medicaments and are represented by the generic formula: RO&mdash;(CH &mdash;CH O) &mdash;(CO)&mdash;NH&mdash;X&mdash;(CO)&mdash;NH&mdash;Z wherein R represents a lower alkyl group, n is an integer between 25 and 250, X when combined with adjcacent NH and CO groups represents a dipeptide residue, and Z when combined with the adjacent group represents a biologically active peptide or protein.

Biologically active conjugates having a detectable reporter moiety and method of identification of the derivative

The present invention relates to a process for the preparation of microparticles, with an extremely high encapsulation rate, comprising a water-soluble substance in a biodegradable polymer, said water-soluble substance and said biodegradable polymer being first incorporated in an organic liquid phase comprising at least one organic non-water miscible solvent. The organic phase is poured into an aqueous liquid phase having a volume which is sufficient to dissolve said organic solvent, said aqueous phase containing a surfactant, the resulting organic-aqueous phase being homogenised in order to perform in one single step the microparticle formation and the organic solvent removal. The thus obtained microparticles show surprisingly good agent retention qualities.

Process for microencapsulation of water soluble substances

The present invention relates to a non crosslinked block polymer. It also relates to a process for the preparation thereof and to the use thereof particularly in pharmaceutical compositions. The block polymer according to the invention contains sequences of polyethylene glycol linked to sequences of polyester and/or polycarbonate. The polyester sequences are selected in particular from polyfumarate, polymaleate and polysuccinate sequences.

Non cross-linked block polyetherester, preparation and uses

The present intention relates to an implant for the controlled release of at least one pharmaceutically active principle comprising a core containing at least one active principle and a sheath surrounding said core, wherein said sheath is composed of at least one polymeric film applied around said core. It also relates to a process for the preparation of such an implant, characterised by the production of a core containing at least one active principle, preparation of at least one polymeric film, application of the polymeric film(s) around said core by juxtaposition and/or superposition thereof, and sterilisation of the implant thus obtained.

Implants for controlled release of pharmaceutically active principles and method for making same

Pharmaceutical composition for the controlled release of at least one water-insoluble active principle, containing a homopolymer of D,L-lactic acid or of L-lactic acid of low molecular weight combined with said active principle, wherein the molecular weight of the homopolymer of D,L-lactic acid is between approximately 2,000 and 6,000 daltons or the molecular weight of the homopolymer of L-lactic acid is about 4,000 daltons.

Pharmaceutical compositions for the sustained release of insoluble active principles

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

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

Biologically active drug polymer derivatives and method for preparing

A method for preparing a pharmaceutical composition in the form of microparticles, the composition thus obtained and its use for preparing injectable suspensions.

Pharmaceutical composition in the form of microparticles

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 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

Piero Orsolini