69 results about "Anti histamines" patented technology

Systems for the treatment of nasal tissue, particularly the nasal turbinates, are described. One method for reducing the size of the inferior nasal turbinate is to apply ultrasound energy to the tissue regions beneath the surface of the turbinate tissue. One instrument may be used to deliver ultrasound energy and provide an infusion or injection of a fluid directly into the turbinate being treated, e.g., to bulk up the size of the turbinate to ensure that the ultrasound energy is properly delivered directly into the intended turbinate tissue. Fluids containing anesthetics, fluids infused with analgesics, etc. may be used for pain management while other medications, such as non-steroidal drugs, steroidal drugs, anti-inflammatory drugs, anti-histamines, anti-bacterial drugs, etc., can also be used. Such assemblies can also be utilized with other instruments as a system. For example, such a probe can be used with nasal speculums or imaging instrument in treating tissue.

Apparatus and methods for the treatment of nasal tissue, particularly the nasal turbinates, are described herein. One method for reducing the size of the inferior nasal turbinate is to apply ultrasound energy to the tissue regions beneath the surface of the turbinate tissue. One instrument may be used to deliver ultrasound energy and to provide an infusion or injection of a fluid directly into the turbinate being treated. The injected fluid can be used to bulk up the size of the turbinate to ensure that the ultrasound energy is properly delivered directly into the intended turbinate tissue. Accordingly, fluids containing anesthetics, fluids infused with analgesics, etc. may be used for pain management while other medications, such as non-steroidal drugs, steroidal drugs, anti-inflammatory drugs, anti-histamines, anti-bacterial drugs, etc., can also be used.

A nasal spray apparatus for simultaneously administrating metered amounts of multiple medicaments includes chambers for separately storing incompatible medicaments, such as an antihistamine and a steroid. Reciprocal piston pumps allow the medications to be sprayed into the user's nasal cavity. Two pumps can be used to separately transfer the medicaments to a receptacle where they can be initially mixed just prior to administration. A small volume receptacle is used to reduce the amount of mixture remaining after each stroke of the nasal spray apparatus. A check valve can be associated with each pump to further reduce medicament mixtures from cross contamination within storage chamber preparations. Collapsible components, including collapsible storage chambers or balloon capacitors can be employed to compensate for vacuums and back pressures as the medicaments are pumped to a spray nozzle.

Hypodermic syringes with multiple needles are used to practice a method of calming psychiatric patients. In accordance with one embodiment of the invention generally used to calm violent adult patients, the syringe has a first barrel containing an antipsychotic, a second barrel containing a sedating antihistamine and a third barrel containing an antianxiety sedative. Each barrel also has a separate projecting needle and contains a piston. A common operator, preferably in the form of a plunger simultaneously pushes all of the pistons so that the patient receives three injections simultaneously. For children, a second embodiment of the syringe includes two barrels instead of three, each barrel containing a separate medication. In each embodiment the syringe is packaged in a manually openable plastic envelope with a safety cap over the needles.

Aerosol spray formulations capable of delivering high concentrations of active agent-containing materials and / or excipient are described herein. The formulation contains a carrier fluid, a propellant, and a therapeutic, prophylactic, consmeticeutical and / or inert solid suspended, dissolved, or dispersed in the formulation. The active ingredient may be any pharmaceutically active agent, but is preferably an antibiotic, an antihistamine, an anesthetic, an anti-inflammatory, and / or an astringent. In one embodiment, the active agent is an antifungal agent. In another embodiment, the active agent is a consmeticeutical. The active agent can optionally be dispersed on, or associated with, a carrier powder. The carrier fluid is a highly volatile silicone liquid, which evaporates in less than 10 minutes, preferably less than 5 minutes, after application of the formulation to the patient's skin. The formulation may also contain one or more pharmaceutically acceptable excipients such as antioxidants, stabilizers, perfumes, colorants, viscosifiers, emulsifiers, surfactants, and combinations thereof. The formulation can be packaged in a conventional aerosol spray can.

Topical skin care composition comprising an extract of Citrus Jabara, topical compositions having anti-histamine activity, and methods and regimens for treating skin with compositions containing an extract of Citrus Jabara.

Compositions and methods can be used for tolerizing the immune system. The compositions can be physiologically acceptable and can include any of a wide variety of allergens that are designed to be administered in escalating doses to, for example, an infant. The compositions can include other active ingredients (e.g., one or more of a steroid, vitamin, mineral, vasodilator, hormone, decongestant, anticholinergic agent, leukotriene inhibitor, immunomodulator, mast cell stabilizer, expectorant, immune suppressant, anti-histamine, or anti-inflammatory agent) and / or a carrier.

A drug delivery system is disclosed. The drug delivery system includes a recognitive polymeric hydrogel through which a drug is delivered by contacting biological tissue. The recognitive polymeric hydrogel is formed using a bio-template, which is a drug or is structurally similar to the drug, functionalized monomers, preferably having complexing sites, and cross-linking monomers, which are copolymerized using a suitable initiator. The complexing sites of the recognitive polymeric hydrogel that is formed mimic receptor sites of a target biological tissue, biological recognition, or biological mechanism of action. A system in accordance with some embodiments is a contact lens for delivering a drug through contact with an eye. In some embodiments, the drug is an anti-microbial, such as an anti-fungal agent for treatment of large animals. In some embodiments, a comfort molecule hyaluronic acid (HA) is delivered. In some embodiments, ketotifen fumarate (anti-histamine) and / or diclofenac sodium (anti-inflammatory) are delivered.

The invention discloses an alcohol dehydrogenase, a gene thereof, a recombinant expression vector and a recombinant expression transformant respectively containing the gene, a recombinase of the alcohol dehydrogenase, and an application of the alcohol dehydrogenase in asymmetric reduction synthesis of chiral diaryl secondary alcohol as a catalyst, and belongs to the technical field of bioengineering. The alcohol dehydrogenase is from Kluyveromyces sp. CCTCCM2011385, has a carbonyl group reduction function, and also has a hydroxy group oxidation function. Extra addition of glucose dehydrogenase and other enzymes used for cofactor circulation is not needed when the alcohol dehydrogenase is used in the reduction of diaryl ketone into the chiral diaryl secondary alcohol as a biocatalyst, and the alcohol dehydrogenase has the advantages of high catalysis efficiency, mild reaction conditions, easy product recovery and low cost, so the alcohol dehydrogenase has very good application and exploitation prospect in the production of antihistamine medicines.

The invention discloses an alcohol dehydrogenase mutant, an encoding gene thereof, and an application thereof in the preparation of chiral diaryl alcohol. The mutant is obtained through substituting serine in the 237th position of alcohol dehydrogenase from Kluyveromyces sp.CCTCC M2011385 and with the amino acid sequence represented by SEQ ID No.1 with alanine. The alcohol dehydrogenase mutant has greatly higher reduction activity and stereoselectivity than wild enzymes. The mutant is especially suitable for asymmetric reduction of diaryl ketone to prepare chiral diaryl alcohol, and can be used to synthesize various antihistamine medicines. The alcohol dehydrogenase mutant has good industrial application prospect.

The invention discloses an alcohol dehydrogenase mutant and an application thereof to synthesis of chiral biaryl alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant has excellent catalytic activity and stereoselectivity and can be used for efficient catalysis for preparation of a series of R-configuration and S-configuration chiral biaryl alcohols. Alcohol dehydrogenase can be applied to synthesis of various chiral biaryl alcohol intermediates of antihistamine drugs by being coupled with glucose dehydrogenase or formate dehydrogenase. Compared withthe existing reports, a method for preparing the chiral biaryl alcohols from alcohol dehydrogenase through asymmetric catalytic reduction has the advantages of simple operation, high substrate concentration, complete reaction and high product purity, and has broad industrial application prospect.

The present invention generally relates to the transdermal delivery of various compounds. In some aspects, transdermal delivery may be facilitated by the use of a hostile biophysical environment. One set of embodiments provides a composition for topical delivery comprising an H1 antihistamine and / or a salt thereof, and optionally, a hostile biophysical environment and / or a nitric oxide donor. In some cases, the composition may be stabilized using a combination of a stabilization polymer (such as xanthan gum, KELTROL® BT and / or KELTROL® RD), propylene glycol, and a polysorbate surfactant such as Polysorbate 20, which combination unexpectedly provides temperature stability to the composition, e.g., at elevated temperatures such as at least 40° C. (at least about 104° F.), as compared to compositions lacking one or more of these.

The invention provides a preparing method of red ginseng extract, whose technical characteristic is as follows: the dry red ginseng taproot is broken into meal, through dipping, ultrasound extract, filtering and decompression to be condensed to extract. The process is suitable for industrial production. The drug composite taking red ginseng extract as effective ingredient to prepare skincare cosmetic is characterized in that: the red ginseng contains AFG which is the basic active ingredient of cosmetic. The invention provides the specific embodiment of multiple skincare cosmetics such as semitransparent microemulsion astringent, nutritive lotion cream, face cream and hair conditioner etc., simultaneously expounding the cleaning function of different ingredients of red ginseng WSP to superoxide anion and the anti histamine liberation function of red ginseng WSP.

A composition for topical treatment of dermatitis is provided. The composition includes one or more anti-histamines or a pharmaceutically acceptable salt thereof; one or more polysaccharides; and one or more Group 1, 2, or 13 metal hydroxides. The dermatitis may be a poison ivy, poison oak, poison sumac, diaper rash, eczema, lichen simplex chronicus, rashes, dermatoses, seborrheic dermatitis, psoriasis, atopic dermatitis, or the combination thereof A method of treatment of dermatitis is also provided.

The invention discloses an alcohol dehydrogenase mutant and application thereof to synthesis of diaryl chiral alcohol and belongs to the technical field of biological engineering. The alcohol dehydrogenase mutant disclosed by the invention has good catalytic activity and stereoselectivity, and a series of chiral diaryl alcohol with R- and S- configurations can be prepared through efficient catalysis. According to the alcohol dehydrogenase mutant, alcohol dehydrogenase is coupled with glucose dehydrogenase or formate dehydrogenase, and can be used for synthesizing various antihistamine drugs, i.e., a chiral diaryl alcohol intermediate. Compared with an existing report, a method for preparing the diaryl chiral alcohol through asymmetric catalysis of the alcohol dehydrogenase has the advantages of simplicity in operation, high substrate concentration, complete reaction and high product purity and has a very good industrial application prospect.

The present invention describes novel nitrosated and / or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and / or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and / or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and / or preventing renal toxicity; and for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2.

An oral rinse formulation for the treatment or prophylaxis of mucositis or stomatitis comprises one or more of the following components in combination with pharmaceutically acceptable excipients or additives: a) at least one corticosteroid; b) at least one anti-histamine; c) at least one topical anaesthetic; and, d) at least one anti-fungal antibiotic agent. A stable nystatin containing formulation is also provided comprising a buffering agent, a preservative, a chelating agent and an anti-oxidant.

An oral rinse formulation for the treatment or prophylaxis of mucositis or stomatitis comprises one or more of the following components in combination with pharmaceutically acceptable excipients or additives: a) at least one corticosteroid; b) at least one anti-histamine; c) at least one topical anaesthetic; d) at least one antibiotic agent; and, e) at least one anti-fungal antibiotic agent. A method of treating or preventing mucositis or stomatitis using such formulation is provided.

A nasal spray composition for treating mucosal inflammation associated with rhinitis, sinusitis, or both can include a decongestant and at least one therapeutic agent. The therapeutic agent is selected from the group consisting of an anti-inflammatory agent and an anti-histamine agent. The nasal spray composition is non-habituating and is administered intranasally to a subject in need thereof.

A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitationof bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula(III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine havinga high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents.

The present invention relates generally to muscarinic receptor antagonist, which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and the method for treating diseases mediated through muscarinic receptors. Also provided herein are pharmaceutical composition comprising one or more muscarinic receptor antagonists and at least one other active ingredients include, but are not limited to, corticosteroids, beta agonists, leukotriene antagonists, 5-lipoxygenase inhibitors, anti-histamines, antitussives, dopamine receptor antagonists, chemokine inhibitors, p38 MAP Kinase inhibitors, and PDE-IV inhibitors.

The present invention relates to allergy vaccines and methods of treating and / or preventing asthma, and allergic conditions. The invention is based on the discovery that inhibiting the ligand / receptor interactions involving, e.g., IgE, IL-3, IL-4, IL-5, IL-6, IL-10, IL-13, interferon-alpha, histamine, leukotriene, and their respective receptors, inhibits production of IgE thereby treating or preventing such diseases or conditions. Competitive inhibition of such receptor / ligand interactions is accomplished by immunizing a human or veterinary patient with the interleukin, interferon-alpha, histamine, leukotriene, their receptors, in any combination. Also, the invention relates to inhibiting receptor / ligand interactions involved in IgE production by competitively inhibiting such interactions by administering antibodies to the ligands, receptors, or both, as well as by administering analogs of the receptors (e.g., soluble receptors not associated with a cell).

The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and / or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal anti-inflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton-pump-inhibitors, isoprostane inhibitors, and mixtures thereof. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and / or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and / or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and / or preventing renal toxicity or other toxicities; for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.

Disclosed is a method for protecting a tree from insects by injecting the tree with a fungicide and / or an antibiotic, and applying a composition to the surface of the tree, said composition comprising water, an insect repellent, an antihistamine, and an insect poison.

A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitation of bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula (III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine having a high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents.

The invention provides a preparation method of antihistamine medicine A. A new intermediate compound shown in a formula I is prepared and can serve as a raw material for the medicine A. A preparation method of the compound in the formula I is shown as follows: a compound in a formula II and a compound in a formula III react under the catalysis of manganese dioxide and dipyridyl nickel bromide. See the formulas in the specification.

The invention discloses chiral tricyclic compounds with anti-histamine activity, a preparation method and application. The chiral tricyclic compounds with the anti-histamine activity have a structural formula, wherein when R1 is phenyl or hydroxyalkyl, ester alkyl or carboxyalkyl of C1 to C11, R2 is straight-chain alkyl of C1 to C7; R3 is hydrogen or alkyl of C1 to C4; R4 is hydrogen or alkyl of C1 to C4; R5 is hydrogen or alkyl of C1 to C4; and R6 is hydrogen or alkyl of C1 to C4. Experiments prove that the chiral tricyclic compounds with the anti-histamine activity can be competitively combined with the body H1 receptor to block the action of the histamine and the H1 receptor so as to restrain the biological effect of the histamine and play a role in allergic resistance. The experiments show that the compounds have stronger anti-histamine activity compared with a positive contrast chlorpheniramine group.

A controlled release pharmaceutical formulation for the administration of an antihistamine and decongestant to a patient wherein the formulation employs a compressed matrix core for the controlled release of a decongestant and an immediate release coating for the immediate release of the antihistamine.

The present invention relates to improved dosage forms of pharmaceuticals for treating rhinitis associated with allergies and colds. The dosage forms include an effective amount each of a non-steroidal anti-inflammatory drug, and a decongestant or an antihistamine wherein the effective amount of the decongestant or antihistamine is less than 75% of an amount present in an approved dose of the decongestant or the antihistamine relative to an amount of the NSAID corresponding to about 100% of the amount present in a normal strength dosage form of the NSAID.