Abstract: The present application relates to an extended-release tablet for oral administration of Clarithromycin. The tablet comprises a water soluble diluent and an acidic compound wherein the acidic compound is used to increase the dissolution rate of Clarithromycin. The tablet is free from polymers or may comprise polymer that is insufficient to function as a release controlling agent.

Abstract: An antibiotic product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours after the initial release of antibiotic. In one embodiment, there is a delayed release dosage form, as well as two or more delayed sustained release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: A biocompatible putty formulation suitable for insertion within chronic and acute wounds of humans and animals, the formulation containing a topical antibiotic, a biocompatible humectant, a biocompatible viscosity-building agent, and at least 5% water, by weight, the humectant and the viscosity-building agent intimately mixed within the formulation, the formulation adapted whereby the formulation remains a solid over the entire temperature range of 20° C. to 35° C.

Abstract: Extracorporeal systems and methods for treating blood-borne diseases in a subject or for developing drugs to treat blood-borne diseases include various environmental and treatment modules that can be tailored to a specific disease or infection. In certain embodiments of the systems and methods, a blood sample is treated with hydrostatic pressure, a pulsed electrical field, a pharmaceutical agent, microwave, centrifugation, sonification, radiation, or a combination thereof, under environmental conditions that are effective for the treatment.

Abstract: The compound 3?-N-demethyl-4?-O-(2-diethylaminoethanoyl)-6-O-methyl-9a-aza-9a-homoerythromycin A, having the Formula (I): or a salt thereof, compositions comprising the compound, its use in the treatment of neutrophil dominated inflammatory diseases, and methods for its preparation.

Abstract: A preparation method of drug loaded emulsion is disclosed. The method comprises the steps of: preparing a non-self emulsifying O/W blank emulsion having no active ingredients; then, adding therapeutically effective amount of active ingredients to the 0/W blank emulsion, adjusting pH to distribute the active ingredients through the membrane to obtain the desired emulsion.

Abstract: Described herein are formulations and methods for treating diseases caused by infectious pathogens, including mycobacterium avium complex, mycobacterium tuberculosis, Nocardia, Plasmodium falcium, and Plasmodium berghei.

Abstract: Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder.

Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.

Abstract: The present invention provides macrocyclic compounds useful as therapeutic agents of the formula: or a pharmaceutically acceptable salt, ester, N-oxide, or prodrug thereof, wherein T, R1, R2, R3, D, E, F, and G are as defined herein. More particularly, these compounds are useful as anti-infective, antiproliferative, anti-inflammatory and prokinetic agents.

Abstract: The present invention provides glycorandomaized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.

Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.

Abstract: Compounds of Formula I or II, and methods of making and using thereof, are described herein. M represents a macrolide subunit, n is a C1-6 group, optionally containing one or more heteroatoms, D is an alkyl or aryl group, A is a linking group connected to D, B is an alkyl, alkylaryl or alkylheteroaryl spacer group, ZBG is a Zinc Binding Group, R1, R2 and R4 are independently are selected from hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkanoate group, a C2-6 carbamate group, a C2-6 carbonate group, a C2-6 carbamate group, or a C2-6 thiocarbamate group, R3 is hydrogen or —OR5, R5 is selected from a group consisting of Hydrogen, a C1-6 alkyl hgroup, a C2-6 alkenyl group, a C2-6 alkynyl group, C1-6 alkanoate group, C2-6 carbamate group, C2-6 carbonate group, C2-6 carbamate group, or C2-6 thiocarbamate group.

Abstract: A process for the preparation of a composition intended for the oral administration of active principles with unacceptable taste, which comprises from about 15% to about 30% of organoleptically unpleasant active ingredient (principle) that is mixed with from about 60% to about 80% of an ester of glycerol or of a fatty acid, to which a wax is optionally added and to which a surfactant is added, and in that it is prepared by a spray-cooling process which can produce a particle size of less than 350 ?m.

Abstract: The invention provides a method of overcoming resistance to at least one antibiotic in a multidrug resistant bacterium, said method comprising contacting said bacterium with an alginate oligomer together with the antibiotic. The multidrug resistant bacterium may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with a multidrug resistant bacterium to overcome resistance to the antibiotic in said multidrug resistant bacterium. In another aspect the method can be used to combat contamination of a site with multidrug resistant bacteria, e.g. for disinfection and cleaning purposes.

Abstract: Antibacterial antisense compounds and methods of their use in treating a Mycobacterium tuberculosis infection in a mammalian host are disclosed. The compounds include an antisense oligonucleotide conjugated to a carrier peptide that significantly enhances the antibacterial activity of the oligonucleotide. The antisense oligonucleotides contain 10-20 nucleotide bases and have a targeting nucleic acid sequence complementary to a target sequence containing or within 20 bases, in a downstream direction, of the translational start codon of a bacterial mRNA that encodes a bacterial protein essential for bacterial replication, where the compound binds to a target mRNA with a Tm of between 45° to 60° C. The carrier peptide is an arginine-rich peptide containing between 6 and 14 amino acids.

Abstract: The present invention relates to co-administering a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The combination acts by interfering with the life cycle of the hepatitis C virus and is therefore useful as an antiviral therapy. As such, the combination may be used for treating or preventing Hepatitis C infections in patients. The invention also relates to compositions comprising the combination of inhibitors. The invention also relates to kits and pharmaceutical packs comprising a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The invention also relates to processes for preparing these compositions, combinations, kits, and packs.

Abstract: The invention relates to a method of using ulipristal acetate or a metabolite thereof for providing contraception or for treating a patient's condition, comprising providing a patient with ulipristal acetate or a metabolite thereof, and informing the patient or a medical care worker that ulipristal acetate or a metabolite thereof affects activity of a cytochrome p450 isozyme, and that administration of ulipristal acetate or a metabolite thereof with a substance that affects activity of a cytochrome p450 isozyme can affect plasma concentration, safety, efficacy or any combination thereof of ulipristal acetate or a metabolite thereof, the substance, or both.

Abstract: The invention provides a method to improve the efficacy of an antibiotic to inhibit the growth of Acinetobacter, said method comprising using said antibiotic together with an alginate oligomer. The Acinetobacter may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with Acinetobacter. In another aspect the method can be used to combat Acinetobacter contamination of a site e.g., for disinfection and cleaning purposes.

Abstract: Pharmaceutical compositions comprised of low-solubility and/or acid-sensitive drugs and neutralized acidic polymers are disclosed.

Abstract: New macrolide general compounds of formula I with improved activity making them useful for inhibiting human phosphodiesterase 4 and treating chronic obstructive pulmonary disease (COPD).

Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.

Abstract: An anti-infective composition for inhalation, containing, at least an effective amount of an antimicrobial aminoglycoside compound or a salt thereof; and an effective amount of a biofilm modifier which is a macrolide compound or salt thereof.

Abstract: A method of treatment for a pelvic tissue infection by vaginally administering an antibiotic and a prostaglandin to a patient is disclosed. A method of reducing surgical trauma resulting from a gynaecological operation by administering vaginally a composition comprising an antibiotic and a prostaglandin to a patient is also disclosed.

Abstract: A poorly soluble drug containing microsphere with improved bioavailability, an oral formulation comprising the same, and a method of preparing the same are provided, wherein the poorly soluble drug containing microsphere is a solid dispersion wherein the poorly soluble drug is dispersed in the water-soluble polymer carrier in a noncrystalline form by spray drying, thus increasing bioavailability of the poorly soluble drug.

Abstract: Azithromycin has increased efficacy in treating acne and other skin conditions when administered systemically at low doses, below those previously known to produce a clinical antibiotic effect.

Abstract: Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.

Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.

Abstract: The present invention relates to the preparation of compositions comprising benzoyl peroxide, with or without other additional active ingredients. The process involves introducing benzoyl peroxide, along with any other active ingredients present, into a fatty substance that contains and protects the ingredients that would otherwise be unstable when in contact with one another. The composition is designed to allow all ingredients to become available for skin contact or skin absorption when the fatty substance softens and/or melts as the composition is applied to the skin. The benzoyl peroxide may be pre-micronized to a particle distribution size of about d90 of 0.1 to 150 microns, preferably d90 of 10 to 15 microns.

Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.

Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Abstract: The present invention provides methods for improving the pharmacokinetics of protease inhibitors and protease inhibitor precursors and pharmaceutical composition comprising protease inhibitors or protease inhibitor precursors of formula I and a cytochrome P450 monooxigenase inhibitor; when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.

Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.

Abstract: An antibiotic product is comprised of at least two dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as one or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: The invention provides methods for the administration of compounds capable of prolonging a QTc interval and methods for predicting whether an individual is predisposed to such QTc prolongation.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.

Abstract: A phospholipid gel is spontaneously formed when combining a first phospholipid, a second phospholipid, and water, wherein the first phospholipid is a neutral phospholipid and the second phospholipid is a negatively charged phospholipid. The first and second phospholipids are of natural origin, semi-synthetic origin, or synthetic origin. Preferably, they are di(C8-C22 acyl) phosphatidyl choline and di(C8-C22 acyl) phosphatidyl glycerol. The total phospholipid concentration is within a range of 6-40% by weight.

Abstract: Compositions and methods for preventing and treating wasting disorders, such as cachexia and anorexia, are provided. In one aspect, the present invention provides a method for preventing and treating a wasting disorder in a mammal. In one embodiment, the method of the invention comprises administering to such mammal a macrolide and a ?2-adrenergic agonist in combination such that the macrolide and said ?2-agonist are administered in amounts effective to prevent or at least alleviate said wasting disorder.

Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.

Abstract: Use of a macrolide antibiotic for the manufacture of a medicament for the treatment or prevention of a cancer selected from colorectal cancer, Desmoid tumor, bladder cancer, gastric cancer, and breast cancer, the macrolide antibiotic being one or more of: tylosin, pharmaceutically acceptable salts thereof, and derivatives thereof; erythromycin, pharmaceutically acceptable salts thereof, and derivatives thereof; oleandomycin, pharmaceutically acceptable salts thereof, and derivatives thereof; and spiramycin, pharmaceutically acceptable salts thereof, and derivatives thereof. Also provided are pharmaceutical compositions and methods for the treatment or prevention of the above mentioned cancers and methods for treating or preventing, in a mammal, a cancer that expresses a mutated APC gene.

Abstract: Disclosed herein are 10-desmethyl, 10 substituted-macrolides, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. The 10-desmethyl macrolides are particularly useful as antibiotics.

Abstract: The invention relates to compositions and methods related to Toll-like receptor (TLR) polypeptides. In some embodiments, the invention relates to managing TLR3 related diseases. In further embodiments, the invention relates to methods of preventing and treating inflammation. In some embodiments, the invention relates to antagonists of TLR3, to amino acid sequences that act as dominant negative molecules, and to nucleic acid sequences that encode said amino acid sequences. In additional embodiments, the invention relates to the manipulation of biological materials to evaluate TLR3 activity.

Abstract: The present invention provides a compound having a superior acid secretion inhibitory action, an antiulcer activity and the like.

Abstract: Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an ?2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.

Abstract: Bioabsorbable compositions of A) blends of bioabsorbable homopolymers and/or copolymers containing glycolide and lactide and B) salts of fatty acids and/or fatty acid esters are described. Processes for making the compositions and surgical articles made totally or in part therefrom, including suture coatings, are also described.

Abstract: Compounds according to formula I wherein m is 0 or 1; X is and R1, R2, R3 R4, and R5 are as defined herein, are useful as anti-infective agents.

Abstract: The invention relates to the use of at least one leukotriene inhibitor for preparing a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants. The invention further relates to a pharmaceutical composition for the prophylaxis and/or treatment of lung diseases, more particularly of bronchopulmonary dysplasia, in prematurely born infants, the pharmaceutical composition comprising at least one leukotriene inhibitor. The invention additionally relates to a method for the treatment and/or prophylaxis of a lung disease, more particularly of a bronchopulmonary dysplasia, in a prematurely born infant, where the prematurely born infant is administered a pharmacologically active amount of at least one leukotriene inhibitor.

Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.