FIELD: medicine.
SUBSTANCE: described is a composition for delivering prodrug of aripiprazole. Composition comprises (a) a combination of aripiprazole prodrug particles having a volume size (Dv50) of less than 1000 nm, and (b) at least one surface stabilizer containing an adsorbed component which is adsorbed on the surface of prodrug particles of aripiprazole, and a free component which is capable of solubilising prodrug of aripiprazole. Ratio of the aripiprazole prodrug to the surface stabilizer ranges from 0.1:1 to 40:1, preferably 17:1. At least one surface stabilizer is carboxymethyl cellulose or polyoxyethylene sorbitol ester of fatty acids. Preferably, surface stabilizer is polysorbate 20.
EFFECT: compositions of the invention provide improved in vivo pharmacokinetic release profile of aripiprazole at the initial stage of administration and enable to achieve a therapeutic aripiprazole concentration in less than seven days.
39 cl, 26 dwg, 18 tbl, 12 ex
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