Stabilised solid drug dispersions in an organic carrier and a process for preparing the same
AssigneeEurand, Inc.
InventorsItalo Colombo, Dario Gervasoni
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AssigneeEurand, Inc.
InventorsItalo Colombo, Dario Gervasoni
Estimating the term…
New solid drug dispersions are described in which the drug is present in amorphous form and massively dispersed (in bulk) inside the particles of an organic carrier selected from cross-linked polymers and/or a complexing agents. These dispersions are obtainable by mixing together the drug and the carrier and applying an oscillating electromagnetic field to the mixture, to a frequency belonging to the microwave region; the microwaves are applied according to a specific heating cycle wherein the drug-carrier mixture is heated at a temperature higher than the melting point of the drug for at least 5 minutes. With respect to the known techniques, the present invention allows to increase in the amount of drug incorporated into the carrier in amorphous form, and to increase the physical stability of the amorphous phase. This is particularly useful in the preparation of pharmaceutical compositions based on drugs which are crystalline in nature, such as are notoriously sparingly soluble in water: thanks to the increased amounts and stability of the drug in amorphous form, the resulting formulations have a more rapid and intense effect, and are endowed with greater bioavailability.
A process for the preparation of a composite containing a drug dispersed in an organic carrier, wherein the drug is massively dispersed (in bulk) within the particles of said organic carrier and it is present in amorphous form in a quantity greater than or equal to 50%, comprising the following steps:
A composite containing a drug dispersed in carrier consisting of a water soluble complexing agent selected from cyclodextrins and maltodextrins, wherein the drug is massively dispersed (in-bulk) within the particles of said complexing agent and it is present in amorphous form in a quantity greater than or equal to 50% by weight, with respect to the total of drug present in the composite.
Dependencies are inferred from the claim text.