Dosing heads for apparatus for dispensing a defined amount of dry powder concurrently to a plurality of spaced apart dose receiving containers include a plurality of spaced apart elongate channels having a channel length with an upper end defining an entry orifice and a lower end defining an exit port. In use, the dosing heads are aligned with a dry powder bed residing above and in communication with the dosing head and at least one vibration source in communication with the dosing head channels configured to controllably apply a vibration flow signal. When the vibration flow signal is applied to the dosing head channels, dry powder from the dry powder bed flows through the elongate channels and out the exit port and when the flow signal is removed, dry powder does not flow through the dosing head elongate channels.
Methods of fabricating and operating dry powder inhalers that include dose disks and airway channel disks with sealant layers, the airway channel disks forming radially-extending discrete, typically dose-specific, airway channels serially forming a portion of the inhalation pathway to deliver dry powder to a user using the inhalers.
Disclosed is a process for preparing a treprostinil salt. The process involves the step of dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution. The treprostinil solution is reacted with an aqueous basic solution containing an alkali metal cation to form treprostinil salt. Allowing crystallization of the treprostinil salt to take place, and then collecting the treprostinil salt formed.
A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (Formula (1)) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (1a): (Formula (Ia)) to form the m-hydroxy-substituted benzaldehyde of formula (1b): (Formula (Ib)) and then reacting compound (1b) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula (1).
C07C 45/61 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups
C07C 45/67 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton
C07C 45/71 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction with functional groups containing oxygen only in singly bound form being hydroxy groups
C07C 47/575 - Compounds having —CHO groups bound to carbon atoms of six-membered aromatic rings containing ether groups, groups, groups, or groups
Urea compositions useful for treatment of dermatological conditions. The compositions may include greater than about 50 wt-% urea, and methods of making such compositions are provided.
Disclosed is a process for preparing a treprostinil salt. The process involves the step of dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution. The treprostinil solution is reacted with an aqueous basic solution containing an alkali metal cation to form treprostinil salt. Allowing crystallization of the treprostinil salt to take place, and then collecting the treprostinil salt formed.
A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (see formula 1) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (Ia): (see formula Ia) to form the m-hydroxy-substituted benzaldehyde of formula (Ib): see formula Ib) and then reacting compound (Ib) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula 1
C07C 47/575 - Compounds having —CHO groups bound to carbon atoms of six-membered aromatic rings containing ether groups, groups, groups, or groups
C07C 45/64 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by introduction of functional groups containing oxygen only in singly bound form
C07C 45/67 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton
16.
SYNTHESIS OF TREPROSTINIL AND INTERMEDIATES USEFUL THEREIN
Treprostinil is prepared by a process which involves Pauson - Khan cyclization of an an alkene-substituted, alkyne-substituted benzene corresponding to formula: (see above formula) where PMB represents para-methoxybenzyl protecting group and R1 and R2 are alcohol protecting groups. Following cyclization, the resulting compound can be subjected to several chemical transformations followed by alkylation, hydrolysis and salt formation to yield treprostinil sodium. The use of para-methoxybenzyl group as the phenolic protecting group confers several process advantages that result in simplified purification of the final product and improved yields.
C07C 49/755 - Unsaturated compounds containing a keto group being part of a ring containing ether groups, groups, groups, or groups a keto group being part of a condensed ring system with two or three rings, at least one ring being a six-membered aromatic ring
C07C 41/08 - Preparation of ethers by addition of compounds to unsaturated compounds by addition of organic compounds only to carbon-to-carbon triple bonds
C07C 43/215 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring having unsaturation outside the six-membered aromatic rings
C07C 43/23 - Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
C07C 45/50 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reaction with carbon monoxide by oxo-reactions
C07C 45/67 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by isomerisationPreparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by reactions not involving the formation of C=O groups by change of size of the carbon skeleton
C07C 49/84 - Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
C07C 51/367 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reactions not involving formation of carboxyl groups by introduction of functional groups containing oxygen only in singly bound form
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
Goods & Services
Topical and skin preparations, face creams, body lotions, body moisturizers; skin creams, lotions, nail creams, moisturizing creams and lotions; face and body cleansers, cleansing lotions; alpha hydroxyl acid face creams; alpha hydroxyl face and body cleansers, wrinkle-removing skin care preparations and moisturizers; creams for the prevention and treatment of skin conditions and aging conditions; anti-aging eye creams, dermatological lotions, creams and gels; creams, lotions and gels to improve the appearance of fine lines; skin peeling creams; and cosmetics and toiletries.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical and medicated preparations and substances for the prevention, treatment and/or alleviation of dermatological diseases, disorders and conditions; pharmaceutical and medicated preparations, namely, ointments, creams, gels, lotions, suspensions and solutions for the prevention, treatment and/or alleviation of dermatological diseases, disorders and conditions; oral and topical antibiotics; topical anesthetics; topical corticosteroid preparations; [ medicated pads for the treatment of skin warts; ] medicated preparations for vaginal use, namely, antifungals and anti-infective preparations; sterile surgical lubricant; [ medicinal preparation for use as an antispasmodic and anti-secretory agent; ] pharmaceutical preparations for use as an ear water drying aid
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical and medicated preparations and substances for the prevention, treatment and/or alleviation of dermatological diseases, disorders and conditions; pharmaceutical and medicated preparations, namely, ointments, creams, gels, lotions, suspensions and solutions for the prevention, treatment and/or alleviation of dermatological diseases, disorders and conditions; oral and topical antibiotics; topical anesthetics; topical corticosteroid preparations; [ medicated pads for the treatment of skin warts; ] medicated preparations for vaginal use, namely, antifungals and anti-infective preparations; sterile surgical lubricant; [ medicinal preparation for use as an antispasmodic and anti-secretory agent; ] pharmaceutical preparations for use as an ear water drying aid
20.
TUBULAR DRY POWDER FEEDERS WITH AXIALLY APPLIED VIBRATION FOR DRY POWDER FILLING SYSTEMS
Tubular dry powder feed systems with an in-line actuator that applies a flow vibration signal axially. The flow vibration signal can be a harmonic or non-harmonic signal, such as a sinusoidal, saw tooth, square wave or other signal and may be frequency or amplitude modulated.
B65B 1/26 - Reducing volume of filled material by pneumatic means, e.g. suction
B67C 3/00 - Bottling liquids or semiliquidsFilling jars or cans with liquids or semiliquids using bottling or like apparatusFilling casks or barrels with liquids or semiliquids
F42B 33/02 - Filling cartridges, missiles, or fuzesInserting propellant or explosive charges
B05B 5/08 - Plant for applying liquids or other fluent materials to objects
21.
DIRECT FILL DRY POWDER SYSTEMS WITH DOSING HEADS CONFIGURED FOR ON/OFF CONTROLLED FLOW
Apparatus for dispensing a defined amount of dry powder concurrently to a plurality of spaced apart dose receiving containers include: (a) a dosing head comprising a support body with a plurality of spaced apart elongate channels having a channel length with an upper end defining an entry orifice and a lower end defining an exit port; (b) a dry powder bed residing above and in communication with the dosing head; and (c) at least one vibration source in communication with the dosing head channels configured to controllably apply a vibration flow signal, wherein, when the vibration flow signal is applied to the dosing head channels, dry powder from the dry powder bed flows through the elongate channels and out the exit port and when the flow signal is removed, dry powder does not flow through the dosing head elongate channels.
B65B 1/24 - Reducing volume of filled material by mechanical compression
B67C 3/00 - Bottling liquids or semiliquidsFilling jars or cans with liquids or semiliquids using bottling or like apparatusFilling casks or barrels with liquids or semiliquids
F42B 33/02 - Filling cartridges, missiles, or fuzesInserting propellant or explosive charges
B65B 1/02 - Machines characterised by the incorporation of means for making the containers or receptacles
B05B 1/00 - Nozzles, spray heads or other outlets, with or without auxiliary devices such as valves, heating means
22.
DIRECT FILL DRY POWDER SYSTEMS WITH DOSING HEADS CONFIGURED FOR ON/OFF CONTROLLED FLOW
Apparatus for dispensing a defined amount of dry powder concurrently to a plurality of spaced apart dose receiving containers include: (a) a dosing head comprising a support body with a plurality of spaced apart elongate channels having a channel length with an upper end defining an entry orifice and a lower end defining an exit port; (b) a dry powder bed residing above and in communication with the dosing head; and (c) at least one vibration source in communication with the dosing head channels configured to controllably apply a vibration flow signal, wherein, when the vibration flow signal is applied to the dosing head channels, dry powder from the dry powder bed flows through the elongate channels and out the exit port and when the flow signal is removed, dry powder does not flow through the dosing head elongate channels.
B65B 1/24 - Reducing volume of filled material by mechanical compression
B05B 1/00 - Nozzles, spray heads or other outlets, with or without auxiliary devices such as valves, heating means
B65B 1/02 - Machines characterised by the incorporation of means for making the containers or receptacles
B67C 3/00 - Bottling liquids or semiliquidsFilling jars or cans with liquids or semiliquids using bottling or like apparatusFilling casks or barrels with liquids or semiliquids
F42B 33/02 - Filling cartridges, missiles, or fuzesInserting propellant or explosive charges
23.
Tubular dry powder feeders with axially applied vibration for dry powder filling systems
Tubular dry powder feed systems in communication with a hopper of dry powder are configured with an in-line actuator that applies a flow vibration signal axially. The flow vibration signal can be a harmonic or non-harmonic signal, such as a sinusoidal, saw tooth, square wave or other signal and may be frequency or amplitude modulated.
Dry powder inhalers with rotatable piercing mechanisms facilitate the use of dose container assemblies having dose containers arranged in concentric rows. A piercing mechanism is operably associated with the dose container assembly and is configured to pierce sealants that seal a dose container. The piercing mechanism is rotatable such that it can serially alternate between the two rows of dose containers. The piercing mechanism includes a rotatable drum, an elongate piercing member, and a biasing member operably associated with the piercing member. The rotatable drum has an open end, an opposite closed end, and a cylindrical wall that extends from the closed end and terminates at the open end. The closed end includes an aperture formed therein in a location adjacent to the wall. The elongate piercing member is extended and retracted through the aperture to pierce the sealants of a dose container.
The present invention refers to a method for treating cancerous or precancerous lesions of the skin by administering a pharmaceutically effective amount of a polyphenol to a patient as well as to the production of a medicament thereto.
A61K 36/00 - Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.
Ready-to-use bivalirudin compositions, methods of using the ready-to-use bivalirudin compositions, and methods of preparing the ready-to-use bivalirudin compositions. The ready-to-use bivalirudin compositions comprise bivalirudin and one or more stabilizing agents. The one or more stabilizing agents may be buffering agents having a pKa of about 2.5 to about 6.5, pH-adjusting agents, polymers, preservatives, antioxidants, sugars or polyols, or a combination thereof. The ready-to-use bivalirudin compositions may also comprise [9-10]-cycloimido bivalirudin, [11-12]-cycloimido bivalirudin, or a combination thereof. The method of using the ready-to-use bivalirudin compositions comprises administering the ready-to-use compositions to a patient in need thereof. Further, the method of preparing the ready-to-use bivalirudin compositions comprises mixing bivalirudin with one or more stabilizing agents.
Dry powder inhalers and methods are provided that facilitate deagglomeration of powdered medicament during inspiration. A dry powder inhaler includes a dry powder medicament container assembly, and an elongated dry powder delivery tube having an inlet at one end that communicates with a dose container, and an outlet or inhalation port that extends from the inhaler housing at an opposite end. The delivery tube includes one or more apertures adjacent the inlet that cause cyclonic or turbulent airflow through the delivery tube. The inner surface of the delivery tube has a polygonal configuration and the cyclonic air stream bounces off the polygonal inner surface numerous times as the air stream flows through the delivery tube. Another dry powder inhaler includes a deagglomeration chamber with a polygonal inner surface. An air stream containing dry powder medicament is directed into the deagglomeration chamber and impacts the polygonal inner surface numerous times.
Dry powder inhalers with rotatable piercing mechanisms facilitate the use of dose container assemblies having dose containers arranged in concentric rows. A piercing mechanism is operably associated with the dose container assembly and is configured to pierce sealants that seal a dose container. The piercing mechanism is rotatable such that it can serially alternate between the two rows of dose containers. The piercing mechanism includes a rotatable drum, an elongate piercing member, and a biasing member operably associated with the piercing member. The rotatable drum has an open end, an opposite closed end, and a cylindrical wall that extends from the closed end and terminates at the open end. The closed end includes an aperture formed therein in a location adjacent to the wall. The elongate piercing member is extended and retracted through the aperture to pierce the sealants of a dose container.
Dry powder inhalers are described with an inhaler body defining an enclosed cavity space and at least one of (a) an endless strip having opposing primary surfaces, the strip comprising a plurality of spaced apart blisters or dose containers holding dry powder medicament. The inhaler also has an inhalation exit flow path in the inhaler body in communication with at least one blister or at least one dose container held by the strip in a dispensing position and a piercer configured to release dry powder medicament from the blister or dose container in the dispensing position.
A dry powder inhaler includes a dose container assembly having a dose container disk with opposing upper and lower surfaces, a first row of circumferentially spaced apart dose containers at a first radius and a second row of circumferentially spaced apart dose containers at a second radius. The dose containers have dry powder therein and are sealed via a first flexible sealant over apertures in the upper surface and a second flexible sealant over apertures in the lower surface. A piercing mechanism includes two reciprocating piercers that serially alternate between the two rows of dose containers in the dose container disk. A rotatable ramp disk includes first and second sets of circumferentially spaced-apart ramp elements in staggered, concentric relationship that are configured to move the first and second piercing members between retracted and extended positions.
Inhalers with an inhaler housing having a dose container disk having inner and outer perimeters mounted in the housing. The dose container disk has a plurality of circumferentially spaced apart dose containers with dry powder therein. The inhalers also include a piercer carriage with a piercer mounted in the inhaler. The piercer carriage is in communication with a resilient member that radially biases the piercer carriage to radially travel to align the piercer with an underlying or overlying dose container.
A dry powder inhaler includes a dose container assembly having a dose container disk with opposing upper and lower surfaces, a first row of circumferentially spaced apart dose containers at a first radius and a second row of circumferentially spaced apart dose containers at a second radius. The dose containers have dry powder therein and are sealed via a first flexible sealant over apertures in the upper surface and a second flexible sealant over apertures in the lower surface. A piercing mechanism includes two reciprocating piercers that serially alternate between the two rows of dose containers in the dose container disk. A rotatable ramp disk includes first and second sets of circumferentially spaced-apart ramp elements in staggered, concentric relationship that are configured to move the first and second piercing members between retracted and extended positions.
Dry powder inhalers include radially-extending discrete, typically dose- specific, airway channels serially forming a portion of the inhalation pathway to deliver dry powder in an inhaler.
Paricalcitol, a synthetic vitamin D analog, is purified to a purity greater than 99.7% by crystallization from solution in isopropyl acetate solvent, followed by filtration and vacuum drying. Isopropyl acetate appears to be unique among commonly available and pharmaceutically acceptable solvents in its ability to precipitate paricalcitol in this high purity, essentially free of isomers thereof.
C07C 401/00 - Irradiation products of cholesterol or its derivativesVitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
C07C 37/84 - SeparationPurificationStabilisationUse of additives by physical treatment by crystallisation
38.
Pharmaceutical formulations of bivalirudin and processes of making the same
9-bivalirudin that does not exceed about 0.6%. Also, the pharmaceutical batch(es) or pharmaceutical formulation(s) may have a reconstitution time that does not exceed about 42 seconds. The method of preparing the pharmaceutical batch(es) or pharmaceutical formulation(s) may comprise dissolving bivalirudin in a solvent to form a first solution, efficiently mixing a pH-adjusting solution with the first solution to form a second solution in which the pH-adjusting solution may comprise a pH-adjusting solution solvent, and removing the solvent and the pH-adjusting solution solvent from the second solution.
9-bivalirudin that does not exceed about 0.6%. Also, the pharmaceutical batch(es) or pharmaceutical formulation(s) may have a reconstitution time that does not exceed about 42 seconds. The method of preparing the pharmaceutical batch(es) or pharmaceutical formulation(s) may comprise dissolving bivalirudin in a solvent to form a first solution, efficiently mixing a pH-adjusting solution with the first solution to form a second solution in which the pH-adjusting solution may comprise a pH-adjusting solution solvent, and removing the solvent and the pH-adjusting solution solvent from the second solution.
The disclosure describes methods and inhalers that deagglomerate dry powder using inspiratory effort of a user of an inhaler. Inhaler fin and mesh configurations are described that facilitate deagglomeration. At least in steady state conditions, a dry powder and airflow pattern can be generated having turbulence with flow vortices, some of which may have a vortex having an axis of rotation that extends in an inspiratory flow direction while others may have a vortex that is substantially orthogonal to the inspiratory flow direction in an inspiratory airflow path, as an amount of dry powder travels through the inhaler to thereby deagglomerate the dry powder without trapping undue amounts of the dry powder during inhalation.
Dry powder inhalers (10) include: (a) a first generally planar spiral travel path (30) in an inhaler body, wherein the first spiral travel path has a plurality of adjacent curvilinear (30 ch) channels forming lanes with upstanding sidewalls, including an inner lane (30:) and an outer lane; and (b) a plurality of discrete sealed microcartridges (25) with substantially rigid bodies disposed in the first travel path, each comprising a pre-metered (typically dose) amount of dry powder, the microcartridges being configured to slidably advance along the first travel path toward an inhalation chamber that merges into an inhalation output port (10 p). In operation, at least one microcartridge is held in the inhalation chamber to release the dry powder therein during inhalation.
Dry powder drug containment systems with a stick substrate and at least one dry powder receptacle or container that can be detached or opened to release dry powder in an inhaler. Related inhalers and kits of sticks are described.
where R represents an aromatic ring optionally substituted with one or more electron withdrawing groups, n=0 or 1 and X is oxygen or sulphur; so as to produce a crystallizable THC carbamate of formula II:
10 alkyl group and the dotted lines indicate optional unsaturation including aromatic, separating the compound of formula II from solution in isolation of other THC derivatives, and hydrolyzing the compound of formula II to form the individual tetrahydrocannabinol isomer of interest.
Dronabinol, the tetrahydrocannabinol compound which comprises the active constituent of marijuana and is pharmaceutically useful as an antiemetic, is prepared by a process involving reaction of cis-menth-1-enc-3,8-diol with olivetol to form 1,3-dihydroxy-2-[(1R,6R)-6-(2-hydroxyprop-2-yl)-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene; and cyclizing the 1,3-dihydroxy-2-[(1R,6R)-6-(2-hydroxyprop-2-yl)-3-methylcyclohex-2-en-1-yl]-5-pentylbenzene so formed to obtain dronabinol. A novel synthesis of cis-menth-1-ene-3,8-diol is also provided.
A fluticasone lotion having improved vasoconstrictor and anti-inflammatory activity and higher than expected potency. The fluticasone lotion contains 0.05 weight percent fluticasone propionate and an oil-in-water vehicle that includes excipients. The fluticasone lotion is unexpectedly efficacious while exhibiting an improved safety profile.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations, namely, ointments in the form of creams, gels, lotions, suspensions and solutions for the treatment of dermatological and ophthalmic diseases and conditions
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
05 - Pharmaceutical, veterinary and sanitary products
39 - Transport, packaging, storage and travel services
Goods & Services
Skin care products, dermatological lotions and creams , foot care lotions and creams, tissue softener preparations. Pharmaceutical preparations; medicated skin treatment products, medicated skin treatment products in pad form used to treat skin warts; medicated dermatological products; topical ointments, creams, lotions and/or salves used to treat dryness, itching, irritation and inflammation of the skin; medical devices in the form of pads carrying medicaments for wart treatment; pharmaceutical preparations in the form of pads or patches. Distribution services to pharmacies, hospitals, drugstores, clinics and other health product retailers of pharmaceutical products.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
VETERINARY PREPARATIONS USED FOR LOCAL THERAPY FOR A VARIETY OF CUTANEOUS DISORDERS OF DOGS AND CATS, INCLUDING DISORDERS CAUSED, COMPLICATED OR THREATENED BY BACTERIAL AND/OR CANDIDAL INFECTION
