Eurand International S.p.a.

Eurand Italia S.p.a.

Eurand, Inc.

Massimo Maria Calanchi

Luigi Giovanni Mapelli

Leonardo Gentilini

Marco Marconi

Marco Zema

Enzo Giorgetti

Gabriele Brunetti

Marco Giuseppe Raffaele Marconi

Marco Meroni

Epx European Pat Off

Stefano De Luigi Bruschi

Piergiorgio Rossi

This invention concerns wettable microcapsules ethylcellulose coated cores and to processes for their preparation; in particular, to microcapsules with ethylcellulose coats that are wettable so that they are suspendable in aqueous medium. The wettable microcapsules can be prepared by applying ethylcellulose onto drug containing core by phase separation from a solvent to provide microcapsules, optionally washing said microcapsules with a solvent in which said microcapsules are substantially insoluble and drying, (a) one or more surfactants is/are incorporated in the solvent at the phase separation step; and/or (b) one or more surfactants is/are incorporated in the solvent used to wash the microcapsules; and/or said microcapsules being coated with one or more surfactants optionally in the presence of a binder.

Wettable microcapsules having hydrophobic polymer coated cores

The invention provides a granular product useful as a pharmaceutical carrier which can be used for the preparation of pharmaceutical compositions that are capable of rapid suspension in water or aqueous media including saliva. The compositions may be used by addition to a glass of water with stirring or taken directly in the mouth. The granular product may be prepared by a process which comprises subjecting a mixture of a thickening agent and a disintegrating agent to wet granulation with an aqueous medium as wetting agent or dry granulation and preparing the pharmaceutical composition from the granular product and the pharmaceutically active ingredient. A water-soluble inert excipient, which may be a sugar, may be mixed with the granular product prior to mixing with the pharmaceutically active ingredient.

Pharmaceutical composition for rapid suspension in aqueous media

The object of the present invention is to obtain a targeted and controlled release of drugs, the pharmacological action and absorption of which takes place in the intestine and in particular in the ileum and in the colon. To achieve this objective the drug is coated with two membranes, one having pH dependent solubility and the other insoluble but permeable to intestinal juices. As long as the coated drug remains in the stomach and in the upper part of the intestinal tract, that is as long as the pH is lower than 5.5, it is not released. Only when it reaches an environment with a higher pH (small intestine and/or colon), the pH dependent membrane dissolves and the release of the drug can begin. From this moment the second membrane, pH-independent but permeable to intestinal juices, carries out its action which is to slow down and control the dissolution of the drug in the small intestine-colon tract.

Method for targeted and controlled release of drugs in the intestinal

Pharmaceutical formulations are disclosed, adapted for preparing solid oral dosage forms (tablets, capsules, lozenges, etc.) having a regular and sustained release after administration. Said formulations comprise one or more active substances and a retarding base or matrix consisting of a polysaccharide of natural origin, alone or mixed with one or more natural or synthetic polymers which may be used to modify the release pattern so as to obtain a therapeutically effective formulation.

Formulation for preparing sustained release drugs for oral administration

The invention relates to a method by which it is possible to prepare a formulation consisting of thickening or suspending agents and other excipients, having the property of dispersing and dissolving quickly in water or aqueous vehicles, without clot formation, with which it is possible to prepare an extermoraneous homogeneous suspension of solid particles and more particularly of micro-encapsulated drugs, which otherwise have the tendency to precipitate or float.

Formulation for preparing extemporaneous homogeneous microcapsule

The present invention relates to obtaining isosorbide-5-mononitrate tablets, being also of retard form, which are stable in time. Such embodiment is now possible after the discovery of the stabilizing activity of the with respect to the isosorbide-5-mononitrate with which it forms a solid solution. The use of PVP is essential so that the tablets can remain stable in time: the retard effect in turn can be obtained with the use of hydroxyalkylcelluloses.

Process for the preparation of stabilized isosorbide-5-mononitrate

The invention relates to a process for preparing microcapsules in a liquid vehicle, allowing to microencapsulate both water soluble and water insoluble substances, using either ionic or non-ionic systems, in which the membrane enclosing the core of the microcapsules is formed by a polymer selected from the group of the phthalates, and more particularly by hydroxypropylmethylcellulose phthalate.

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Sesto S. Giovanni, Italy

Massimo Maria Calanchi