Hovione Scientia Limited

Hovione Inter Limited

Hovione International Limited

Constanca Cacela

Zita Mendes

Ana Fernandez Casares

Gloria Ten Figas

Peter Villax

Luis Sobral

Filipe Gaspar

Marcio Temtem

Eunice Costa

Marco Gil

Ricardo Mendonca

The present invention concerns new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.

Polymorphic forms of minocycline base and processes for their preparation

Described are new forms of crystalline minocycline base. In particular, two new crystalline polymorphic forms, designated Form IV and Form V of minocycline base are provided. These are characterized by XRD, FTIR and TGA. Processes for preparing the new polymorphic forms and their use in pharmaceutical compositions are also provided. Form IV and Form V are prepared by dissolving and/or suspending minocycline base in an organic solvent followed by crystallization.

A new scalable process to control the particle size and the particle size distribution, comprising 5 steps: (i) suspension preparation in a mixture of solvents in which the API and/or excipient is partially soluble in one of the solvents; (ii) particle size reduction of the suspension; (iii) aging; (iv) stopping the aging by solvent removal; and (v) optionally, a step of isolating the processed ingredients in the form of powder.

Assisted particle size reduction process

A process for reducing the particle size of an active pharmaceutical ingredient (API) while maintaining its polymorphic form, comprises the step of processing the active pharmaceutical ingredient by cavitation at elevated pressure. The process preferably comprises the step of isolating the processed active ingredient in the form of powder, wherein the isolation step comprises filtration or spray drying. Particles produced by the process of the invention typically have a span value of less than 2.5.

Process for particle processing of active pharmaceutical ingredients

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Lisbon, Portugal

Constanca Cacela