Fidia Farmaceutici S.p.a.

Cristian Guarise

Davide Renier

Devis Galesso

Monica Campisi

Carlo Pizzocaro

Mauro Pavan

Stefano Pluda

Disclosed are alkenylamides of sulfated hyaluronic acid and their use for the stabilisation and release of medicaments in the form of micellar suspensions which can be administered locally and/or locoregionally, in particular intra-articularly.

Stabilisation and controlled-release systems for medicaments unstable on sterilisation

Disclosed is grade 2 sulphated hyaluronic acid having 2 to 60% molar, preferably 15 to 35%, and even more preferably between 20 and 25%, of the carboxyl groups functionalized with dopamine conjugated directly via an amide bond or by means of a spacer having an amino group for the formation of an amide bond with the carboxyl groups of hyaluronic acid and of a carboxyl group for the formation of an amide bond with the amino group of dopamine.

Sulphated hyaluronic acids functionalised with dopamine

The present invention relates to an improved process for the production of sulfated hyaluronic acid (HA), sulfated HA-derivatives and/or mixtures thereof, having a high purity and a sulfation degree ranging from 1 to 3, which comprises the following steps: a) solubilization of HA-Na or HA-derivative-Na, in an aprotic solvent in the presence of an organic sulfonic acid; b) sulfation of the solution obtained by the addition of an excess of sulfating agents; c) precipitation in ethanol until a precipitate is obtained; d) solubilization of the precipitate thus obtained in a mixture of water and the aprotic solvent used in step a), in the presence of an excess of NaCl, with a pH adjustment within a range of 3 to 4; e) further precipitation with ethanol until a powder is obtained; f) washings of the powder coming from step c) and drying the product thus obtained under vacuum. The present invention also relates to sulfated HA, sulfated HA derivatives and/or mixtures thereof, having a high purity and sulfation degree ranging from 1 to 3, thus prepared, and the relative pharmaceutical mixtures.

Process for the production of high-purity sulfated HA

The object of the present invention is novel release systems comprising specific hyaluronic acid amides combined with therapeutically and/or biologically active proteins with a mainly hydrophobic nature, for sustained, slow release over time which increases the efficacy of the medicament and the patient's compliance.

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Abano Terme, Italy

Cristian Guarise