Process for activation of drugs in a vibrational mill
AssigneeEurand Pharmaceuticals Ltd.
InventorsLuca Dobetti, Massimo Bresciani
Life of this patent
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Abstract
A process is described for the activation (increase in solubility and bioavailability) of drugs. The process, carried out in a vibrational mill, is characterised by the use of given proportions between the physical mixture made up of drug and pharmaceutical carrier and the empty volume among the grinding means contained inside the mill. The process leads to obtaining powders for pharmaceutical use in which the drug has a high and constant degree of activation; this result is obtainable irrespective of the nature of the drug and carrier used, and of their weight ratio.
Claims9
A process for the preparation of drug-carrier composites, performed by co-grinding of a drug-carrier mixture in a vibrational mill, said process being characterised in that:
- the vibrational mill contains grinding means of a cylindrical shape, with flat or convex bases, said grinding means having:
- diameter and height, independently of one another, of between 0.4 cm and 3 cm, a dimensional ratio (rd) of between 0.5 and 2, and a curvature ratio (rc) of between 0 and 0.5;
- a volume of drug-carrier mixture of between 35% and 100% of the empty volume comprised between the grinding means (interstitial volume Vi) is used.
The process according to claims 14, where the carrier is a solid substance for pharmaceutical use chosen among cross-linked polymers, linear polymers, and non-polymeric carriers.
The process for the preparation of a given number (n) of drug-carrier batches with a constant degree of activation, performed by means of n cycles of co-grinding of the corresponding drug-carrier mixtures in a vibrational mill, said process being characterised in that:
- the vibrational mill contains grinding means having a cylindrical shape, with flat or convex bases, having:
- diameter and height, independently of one another, of between 0.4 cm and 3 cm, a dimensional ratio (rd) of between 0.5 and 2, and a curvature ratio (rc) of between 0 and 0.5.
- a volume of drug-carrier mixture of between 35% and 100% of the empty volume comprised between the grinding means (interstitial volume VI) is used, and in which the interstitial volume Vi is determined only once and is used as a reference for all the n grinding cycles.
Dependencies are inferred from the claim text.