Abstract: The present invention is directed to nanoparticulate carvedilol compositions having improved pharmacokinetic profiles, improved bioavailability, dissolution rates and efficacy. In one embodiment, the nanoparticulate carvedilol composition has an effective average particle size of less than about 2000 nm.

Abstract: This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity, and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: The present invention provides a composition comprising cephalosporin useful in the treatment and prevention of a bacterial infection. In one embodiment, the composition comprises nanoparticulate particles comprising cephalosporin and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. In another embodiment, the composition comprises a modified release composition that, upon administration to a patient, delivers cephalosporin in a bimodal, multimodal or continuous manner. The invention also relates to dosage forms containing such compositions, and to methods for the treatment and prevention of a bacterial infection.

Abstract: The present invention is directed to compositions and methods comprising nanoparticulate aripiprazole, or salts or derivatives thereof, having improved bioavailability, faster rates of absorption and a faster onset of therapeutic effect. The nanoparticulate aripiprazole compositions are proposed to have an average effective particle size of less than about 2000 nm, and may be useful for the treatment of diseases and disorders of the central nervous system, including mental diseases and disorders.

Abstract: The present invention is directed to compositions comprising zonisamide, or a salt or derivative thereof, and at least one nanoparticulate NSAID. The zonisamide and NSAID combination preferably includes nanoparticulate NSAID particles of the composition with an effective average particle size of less than about 2000 nm. The zonisamide and NSAID combination is useful in the treatment of migraine and acute migraine pain and related conditions.

Abstract: The invention relates to a multiparticulate modified release composition comprising a fluorocytidine derivative, preferably capecitabine, and a modified release component comprising a modified release coating, a modified release matrix material, or both. Following oral delivery, the composition in operation delivers the fluorocytidine derivative in a pulsatile manner at about six to about twelve hours after administration.

Abstract: The present invention is directed to compositions comprising nanoparticulate tadalafil, or a salt or derivative thereof, having improved bioavailability, faster rates of absorption and a faster onset of therapeutic effect. The nanoparticulate tadalafil particles of the composition are proposed to have an effective average particle size of less than about 2000 nm and may be useful in the treatment of sexual dysfunction and vascular-, pulmonary- and cardiac-related diseases and conditions.

Abstract: Nanoparticulate compositions comprising a corticosteroid and a leukotriene receptor antagonist are described. The compositions are useful in the prophylaxis and chronic treatment of asthma in adults and pediatric patients and for the relief of allergic conjunctivitis, symptoms of seasonal allergic rhinitis in adults and pediatric patients. Combining a leukotriene receptor antagonist with a corticosteroid in a particle size ranges of less than 2000 nm in a single formulation results in improved efficacy. In addition, patient compliance is enhanced since only one dosage form is needed. Furthermore, local administration of the leukotriene receptor antagonist results in less liver toxicity since the liver will be exposed to lower amounts of drug than happens following oral administration. The drug compositions according to the invention can be formulated into inhalation, nasal, or ocular formulations.

Abstract: The invention is directed to compositions comprising at least one nanoparticulate H1-histamine receptor antagonist, such as ebastine or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate H1-histamine receptor antagonist particles, such as ebastine, have an effective average particle size of less than about 2000 nm and are useful in the treatment of seasonal and perennial allergic rhinitis and related diseases.

Abstract: The present invention relates to nanoparticulate benidipine compositions having improved bioavailability. The compositions comprise benidipine particles having an effective average particle size of less than about 2000 nm and may be useful in the prevention and treatment of hypertension, renal parenchymal hypertension and angina pectoris.

Abstract: The present invention is directed to compositions comprising nanoparticulate macrolides such as clarithromycin, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate macrolide particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of infection and related diseases.

Abstract: The present invention is directed to compositions comprising a nanoparticulate clopidogrel, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate clopidogrel particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the prevention and treatment of pathologies induced by platelet aggregation. The clopidogrel particles may also be formulated as a controlled release polymeric coating or matrix drug delivery system.

Abstract: The present invention is directed to compositions comprising a nanoparticulate clopidogrel and aspirin combination, or salts or derivatives thereof, having improved clopidogrel bioavailability. The nanoparticulate clopidogrel particles, and optionally the nanoparticulate aspirin particles, of the composition have an effective average particle size of less than about 2000 nm and are useful in the prevention and treatment of pathologies induced by platelet aggregation. The clopidogrel and aspirin particles may also be formulated as a controlled release polymeric coating or matrix drug delivery system.

Abstract: The invention is directed to compositions comprising a nanoparticulate acetaminophen composition, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate acetaminophen particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of aches and pain, and in the reduction of fever and related conditions.

Abstract: The present invention is directed to a nanoparticulate compositions of imatinib mesylate, or a salt or derivative thereof, having improved pharmacokinetic profiles and reduced fed/fasted variability. The nanoparticulate imatinib mesylate particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of chronic myeloid leukemia, gastrointestinal stromal tumors and related diseases.

Abstract: The invention relates to a controlled release composition comprising acylanilide, and preferably bicalutamide, for use, in particular, in combination therapy with a luteinizing hormone-releasing hormone (LHRH) analogue for the treatment of stage D2 metastatic carcinoma of the prostate. The controlled release composition comprises an immediate release component and a modified release component or formulation. The immediate release component comprises a first population of bicalutamide. The modified release formulation preferably comprises a second population of acylanilide bicalutamide, and a controlled release constituent. The controlled release formulation is preferably in the form of an erodable formulation, a diffusion controlled formulation or an osmotic controlled formulation. The combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or bi-modal manner.

Abstract: The invention relates to nanoparticulate lipase inhibitor compositions having improved pharmacokinetic profiles. The nanoparticulate lipase inhibitor compositions have an effective average particle size of less than about 2000 nm and are useful in the treatment of obesity and related diseases.

Abstract: The present invention is directed to nanoparticulate quinazoline derivative compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The nanoparticulate quinazoline derivative particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of hyperproliferative disorders, such as cancer and other neoplastic diseases. The compositions may include quinazolinamine derivatives such as erlotinib or a salt thereof.

Abstract: The invention relates to a multiparticulate modified release composition that, upon administration to a patient, delivers at least one active ingredient in a bimodal or multimodal manner. The multiparticulate modified release composition comprises a first component and at least one subsequent component; the first component comprising a first population of active ingredient containing particles and the at least one subsequent component comprising a second population of active ingredient containing particles wherein the combination of the components exhibit a bimodal or multimodal release profile. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition.

Abstract: Compositions comprising a nanoparticulate corticosteroid and an antihistamine are described. The compositions are useful in the prophylaxis and chronic treatment of asthma in adults and pediatric patients and for the relief of allergic conjunctivitis, symptoms of seasonal allergic rhinitis in adults and pediatric patients. Combining an antihistamine with a nanoparticulate corticosteroid in a single formulation results in improved efficacy.