Eurand Pharmaceuticals, Ltd.

Vectorpharma International Corporation

Leonardo Rabaglia

Fabio Carli

Luca Dobetti

Massimo Bresciani

Italo Colombo

The invention comprises a process for activating drugs by means of high-energy co-grinding of the drug with a pharmaceutical carrier, characterized by the use of a vibrational mill equipped with means that regulate the vibration frequency. The process, performed by modifying the frequency of vibration and keeping its amplitude constant, produces drug/carrier composites with a constant particle size in which the degree of drug activation increases in proportion to the frequency applied. The invention also includes a vibrational mill suitably modified to perform the process described.

Drug activation process and vibrational mill therefor

The described therapeutic compositions with controlled release of medicaments comprise a medicament loaded onto particles of a crosslinked non-ionic polymer insoluble but swellable in water, using either swelling with solutions of the medicament or high-energy co-grinding methods. The medicament-loaded particles are coated with a polymers film able to control medicament release, to obtain a prolonged release of the medicament (even exceeding 24 hours) while maintaining high bioavailability.

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Parma, Italy

Leonardo Rabaglia