Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.

Abstract: The invention provides a method of making a composition for inhalation which includes the step of mixing particles of additive material having a diameter of not more than 2 ?m with active particles, wherein the additive material is suitable for promoting the dispersal of active particles upon aerolization of a dry, powder in a dry powder inhaler.

Abstract: The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R1, R2, R3, and R4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R5 is hydrogen or a C1-C7 linear or branched acyclic hydrocarbon group, or R5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.

Abstract: Disclosed herein is a cosmetic composition for the treatment of keratinous fibers, for example, human keratinous fibers, such as the hair, in the form of an aerosol comprising at least one polysaccharide of lambda-carrageenan type and carbon dioxide as propellant. Also disclosed herein is a cosmetic treatment method for keratinous fibers comprising applying such a composition to the keratinous fibers.

Abstract: Multimodal particulate formulations of medicaments and methods for their use, e.g. by nasal or pulmonary administration for the treatment of various medical conditions, are provided.

Abstract: Micronized particles of a low-dosage strength active ingredient, to be used in dry powder formulations for inhalation, with particular properties can easily and homogenously disperse in a dry powder formulation to be administered by means of a dry powder inhaler device.

Abstract: Described herein are respiratory drug condensation aerosols and methods of making and using them. Kits for delivering condensation aerosols are also described. The respiratory drug aerosols typically comprise respiratory drug condensation aerosol particles. In some variations the respiratory drug compound is selected from the group consisting of ?-adrenergics, methylxanthines, anticholinergics, corticosteroids, mediator-release inhibitors, anti-leukotriene drugs, asthma inhibitors, asthma antagonists, anti-endothelin drugs, prostacyclin drugs, ion channel or pump inhibitors, enhancers, or modulators and pharmaceutically acceptable analogs, derivatives, and mixtures thereof. Methods of treating a respiratory ailment using the described aerosols are also described. In general, the methods typically comprise the step of administering a therapeutically effective amount of respiratory drug condensation aerosol to a person with a respiratory ailment.

Abstract: A pulmonary drug delivery system is disclosed, including a breath-powered, dry powder inhaler, and a cartridge for delivering a dry powder formulation. The inhaler and cartridge can be provided with a drug delivery formulation comprising, for example, a diketopiperazine and an active ingredient, including, peptides and proteins such as insulin and glucagon-like peptide 1 for the treatment of endocrine disease, for example, diabetes and/or obesity.

Abstract: There is provided a powder formulation for nasal delivery including a protein having a molecular weight of 10 kDa or greater and chitosan or a derivative thereof or a salt of chitosan or a salt of a derivative of chitosan. Preferably the protein is human growth hormone.

Abstract: Embodiments of the invention relate to particles of active substances, methods for preparing the particles, formulations containing the particles, and metered dose inhalers containing such particles or formulations. In one embodiment, a composition of an aerosol formulation is provided and contains a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 ?m suspended in a hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v. The aerosol formulation exhibits a flocculation volume of about 85% or greater about 1 minute after mixing the particulate active substance and the hydrofluorocarbon fluid vehicle. The particulate active substance contains an alkaloid ergotamine, pharmaceutically acceptable salts thereof, analogues thereof, or derivatives thereof.

Abstract: The invention relates to a method of delivering an agent to the pulmonary system of a compromised patient, in a single breath-activated step, comprising administering a particle mass comprising an agent from an inhaler containing less than 5 milligrams of the mass, wherein at least about 50% of the mass in the receptacle is delivered to the pulmonary system of a patient. The invention also relates to receptacles containing the particle mass and the inhaler for use therein.

Abstract: A controlled release pharmaceutical composition for oral use comprising carvedilol. The composition releases carvedilol after oral administration to a mammal, including a human, in such a manner that a prolonged residence of carvedilol is obtained in the circulatory system compared with the known compositions of carvedilol. Furthermore, a composition according to the present invention makes available to the body a suitable plasma concentration of one or both of the enantiomeric species, namely R(+) and/or S(?) carvedilol for obtaining the desired therapeutic effect.

Abstract: Swellable particles for delivery of a drug or other working agent to the pulmonary system are provided. The swellable particles include a dehydrated (dry) aerodynamic particle diameter of 5 ?m or less to enable delivery to the respiratory tract, such as for example to the tracheo-bronchial airways of the upper respiratory tract and/or to the alveolic regions of the deep lung, and a hydrated particle diameter that is greater than 6 ?m volume mean diameter to retard or prevent their phagocytosis by the macrophages present in airways of the respiratory tract.

Abstract: The invention relates to pharmaceutical compositions containing combinations of formoterol and ciclesonide and the use of such pharmaceutical compositions in medicine, in particular, the prophylaxis and treatment of respiratory disease.

Abstract: The invention provides microparticles for use in a pharmaceutical composition for Pulmonary administration, each microparticle comprising a particle of an active substance having, on its surface, particles of a hydrophobic material suitable for delaying the dissolution of the active substance. The invention also provides a method for making the microparticles.

Abstract: Compositions for nasal administration, which comprise a pharmaceutical, a physiologically active peptide, or a peptide-related compound, and as the carrier thereof, crystalline cellulose with a specific particle diameter and/or partially pregelatinized starch are provided. Such compositions improve the in vivo absorption efficiency of pharmaceuticals.

Abstract: Pharmaceutical formulations comprising beclometasone dipropionate and a salt of formoterol exhibit improved stability and are useful in pressurized metered dose inhalers (pMDIs).

Abstract: Compositions which contain an active ingredient, a propellant containing a hydrofluoroalkane (HFA), a co-solvent, and a low-volatility component are useful for administering the active ingredient via an aerosol.

Abstract: A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period of time that is less than 60 minutes.

Abstract: The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.

Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass medium average diameter predominantly between 1 to 5 ?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.

Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, from the peptide or protein. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration. The formulations include microparticles formed of (i) the active agent, which may be charged or neutral, and (ii) a transport enhancer that masks the charge of the agent and/or that forms hydrogen bonds with the target biological membrane in order to facilitate transport. In one embodiment, insulin is administered via the pulmonary delivery of microparticles comprising fumaryl diketopiperazine and insulin in its biologically active form. This method of delivering insulin results in a rapid increase in blood insulin concentration that is comparable to the increase resulting from intravenous delivery.

Abstract: A stable suspension aerosol formulation of epinephrine is suitable for administration through inhalation comprising a therapeutically effective amount of epinephrine, hydrofluorocarbon propellant, co-solvent, surfactant, and antioxidant. The suspension aerosol formulation further comprises [pre-] pre-micronized epinephrine suspended in an alcohol/surfactant solution with hydrofluoroalkane propellant. The suspension formulation provides a highly efficient delivery of drug microparticles into the respirable region of patients' lungs and has the following advantages: lower dosage requirement, minimum alcohol content, with less impurities generated during storage, improved efficacy and safety, and exhibits no ozone depleting potential compared to a formulation containing chlorofluorocarbon.

Abstract: A fosfomycin plus tobramycin combination formulation for delivery by aerosolization is described. The concentrated fosfomycin tobramycin combination formulation containing an efficacious amount of fosfomycin plus tobramycin is able to inhibit susceptible bacteria. Fosfomycin and tobramycin are formulated separately in a dual ampoule such that when reconstituted, the pH is between 4.5 and 8.0 or as a dry powder. The method for treatment of respiratory tract infections by a formulation delivered as an aerosol having mass median aerodynamic diameter predominantly between 1 to 5?, produced by a jet or ultrasonic nebulizer (or equivalent) or dry powder inhaler.

Abstract: Disclosed are propellant gas formulations containing at least one suspended active substance which contains chemically bound water, water and the propellant TG 227 or TG 134 a.

Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.

Abstract: A dry powder pharmaceutical composition comprising (i) a medicament particle fraction comprising medicament particles with an aerodynamic diameter no greater than 10 ?m; and (ii) at least 50% of a non-respirable excipient fraction comprising low density excipient particles with an aerodynamic diameter greater than 10 ?m and a geometric diameter greater than 30 ?m. In additional embodiments of the invention, the pharmaceutical composition includes a respirable excipient fraction comprising excipient particles with an aerodynamic diameter no greater than 10 ?m. In a preferred embodiment of the invention, the non-respirable excipient particles include pores adapted to receive a portion of the respirable excipient fraction and/or the medicament fraction.

Abstract: A device comprising an inhaler suitable for administration of a stable dry powder blend is described, which contains a blend comprising a thyroid hormone, in particular levothyroxine sodium, and other additives such as lactose particles, sodium starch glycolate, magnesium stearate, and talc silicified.

Abstract: A method of manufacturing heat-sensitive pharmaceutical powder is disclosed. The original pharmaceutical substances are dissolved in a solution or suspended in a suspension, which is sprayed through an atomizing nozzle and frozen in a cold gas phase or liquid nitrogen atomized directly in the spray-freeze chamber or gas jacket at the same time (for cooling purposes). The particles are freeze-dried at roughly atmospheric pressure in a down-stream fluid flow with exit filter thereby to remove moisture entrapped on or inside the frozen particles. The system has applicability for forming other powders.

Abstract: Compositions, methods and systems are provided for pulmonary or nasal delivery of two or more active agents via a metered dose inhaler. In one embodiment, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium.

Abstract: The invention involves methods and formulations for treating or preventing rhinosinusitis, including but not limited to, bacterial-induced, viral-induced and/or fungus-induced rhinosinusitis in mammals, and/or rhinosinusitis not induced by an infective agent, such as bacteria, fungus or virus. In one embodiment, the formulation of the present invention comprises an anti-inflammatory agent (e.g. fluticasone propionate) having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.

Abstract: Disclosed are in vitro methods for evaluating the in vivo redispersibility of dosage forms of poorly water-soluble active agents. The methods utilize media representative of in vivo human physiological conditions.

Abstract: Nano-constructscomprising nanoshells and methods of using the nano-constructs for treating or ameliorating a medical condition are provided.

Abstract: The present invention relates to a stable liquid formulation comprising desoximetasone, isopropyl myristate, a C2-C4 alcohol and a stabilizing agent. Specifically, the present invention provides a liquid formulation comprising: a) about 0.01 wt % to about 2.5 wt % desoximetasone; b) about 10 wt % to about 70 wt % isopropyl myristate; c) about 20 wt % to about 70 wt % C2-C4 alcohol; and d) a stabilizing agent selected from the group consisting of an oleaginous vehicle and a propellant, wherein the stabilizing agent is in an amount sufficient to reduce the formation of less than about 1 wt % 17-carboxy-9?-fluoro-11?-hydroxy-16a-methyl-androsta-1,4-diene-3-one under an accelerated storage condition.

Abstract: The present invention relates to active substances in particulate form, to methods for preparing them and to their uses. The present invention provides particulate powders, such as might be of use for delivery using a dry powder inhaler (DPI) or similar delivery device, having properties which may be beneficial to the DPI delivery process.

Abstract: The invention provides a dry powder inhalation composition comprising medicament particles and a mixture of lactose particles with a VMD of between about 70 and about 120 microns and a diameter of less than 250 microns, the mixture being characterized in that up to 96% by weight of the lactose particles are less than 150 microns in diameter and wherein up to 25% by weight of the lactose particles are less than 5 microns in diameter. The compositions provide for a more accurate, uniform and consistent dispersion when used with, for example, a multidose dry powder inhaler. Also disclosed are methods for use of the compositions of the invention.

Abstract: Particles having a tap density of less than 0.4 g/cm3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.

Abstract: Swellable particles for delivery of a drug or other working agent to the pulmonary system are provided. The swellable particles include a dehydrated (dry) aerodynamic particle diameter of 5 ?m or less to enable delivery to the respiratory tract, such as for example to the tracheo-bronchial airways of the upper respiratory tract and/or to the alveolic regions of the deep lung, and a hydrated particle diameter that is greater than 6 ?m volume mean diameter to retard or prevent their phagocytosis by the macrophages present in airways of the respiratory tract.

Abstract: A pharmaceutical aerosol formulation comprising particles of (a) formoterol or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof and (b) mometasone or a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof dispersed in a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof, and a bulking agent having a mass median diameter of less than one micron.

Abstract: Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMDd greater than the Volume Mean Diameter VMDw of particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.

Abstract: A respiratory dispersion for pulmonary delivery comprises one or more bioactive agents, a suspension medium, and a plurality of perforated microstructures having a mean aerodynamic diameter of less than 5 ?m. The suspension medium comprises at least one propellant and permeates the perforated microstructures.

Abstract: A dry powder suitable for inhalation n a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period of time that is less than 60 minutes.

Abstract: A method of forming and resulting nano-structured composite includes atomizing a mixture of an amount of each of aminopropyltriethoxysilane, AgNO3, DI water, and ethanol in a carrier gas; heating the atomized droplets at a selected temperature for a time sufficient to reduce the Ag to its elemental form in a silica matrix; and outputting the nano structured composite particles. A predetermined heating time is from about 0.01 to about 40 seconds and a selected heating temperature is from about 200 to about 800° C. The nano structured composite includes a plurality of nano particles at a contact surface of the composite, dispersed throughout and at a contact surface of the composite, or dispersed throughout the composite.

Abstract: The present invention provides novel condensation aerosols for the treatment of disease and/or intermittent or acute conditions. These condensation aerosols have little or no pyrolysis degradation products and are characterized by having an MMAD of between 1-3 microns. These aerosols are made by rapidly heating a substrate coated with a thin film of drug having a thickness of between 0.05 and 20 ?m, while passing a gas over the film, to form particles of a desirable particle size for inhalation. Kits comprising a drug and a device for producing a condensation aerosol are also provided. The device contained in the kit typically, has an element for heating the drug which is coated as a film on the substrate and contains a therapeutically effective dose of a drug when the drug is administered in aerosol form, and an element allowing the vapor to cool to form an aerosol. Also disclosed, are methods for using these aerosols and kits.

Abstract: The invention therefore relates to protein-containing powders, wherein the proportion of phenylalanine is at least 30% (w/w), or at least 40% (w/w). It has been shown that phenylalanine-containing powders, particularly after spray drying, are very suitable in terms of their aerodynamic characteristics and protein stabilization for preparing powders or protein compositions with improved aerodynamic properties. The main component is phenylalanine and the optional further component is an excipient which has good water-solubility compared with phenylalanine, preferably a sugar or a polyol.

Abstract: A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes.

Abstract: The present invention includes a method for delivering medications deeper into the lungs and to the medications' pulmonary targets, which include bronchioles and alveoli. A first particularly preferred embodiment of the invention describes the use of two steps for delivery of a medication. In a first step, an aerosolized therapeutic composition or medication is administered into a patient's respiratory tract, wherein the patient may be any animal or human subject. Following the first step, an aerosolized surfactant is administered into the patient's respiratory tract that facilitates delivery of the aerosolized medication of the first step to the medication's pulmonary target. Another embodiment of the present invention contemplates an apparatus for the delivery of an aerosolized surfactant used that facilitates delivery of previously inhaled aerosolized medication.

Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.