Abstract: The present invention relates to the use of a solubilizer for enhancing the solubility of an active pharmaceutical ingredient in water. The present invention further relates to a composition comprising a solubilizer and at least one active pharmaceutical ingredient. In both cases the solubilizer is an alkoxylated monoalcohol or a mixture of alkoxylated monoalcohols, where the alkoxylated monoalcohol or, if a mixture of alkoxylated monoalcohols is present, at least one alkoxylated monoalcohol in the mixture comprises at least one oxypropylene unit.

Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.

Abstract: 2?-O-substituted 14- or 15-membered azalide macrolides of Formula (I) wherein R6 represents (i) —C1-8alkyl, unsubstituted or substituted at the terminal carbon atom by a group selected from hydroxy, —C1-3alkoxy and —C(O)OC1-3alkyl, or when —C1-8alkyl is branched, substitution can alternatively be by a hydroxyl group at each of two terminal carbon atoms, (ii) —CH(NH2)C1-4alkyl, wherein the —C1-4alkyl group may be optionally interrupted by a heteroatom selected from O, S and N, (iii) —CH2N(R7)(R8), wherein R7 and R8 each independently represent H or —C1-3alkyl provided that R7 and R8 cannot both simultaneously represent H, (iv) a 4-6-membered heterocyclic ring containing up to 2 heteroatoms independently selected from O, S and N, wherein the heterocyclic ring is unsubstituted or substituted by —C1-3alkyl, (v) 5-6 membered heteroaromatic ring, unsubstituted or substituted by one to three groups independently selected from halo, hydroxyl, —C1-3alkyl, —C1-3alkoxy, —CF3, —OCF3 and —NH2, (vi) —CH(NH2)CH

Abstract: A process for the use of low concentration levels of Erythromycin to eliminate or control the growth of unwanted or undesirable bacteria (contaminating bacteria) in the fermentation production of alcohols without inhibition of the growth or replication of the yeast.

Abstract: A liquid pharmaceutical composition to be applied to the skin as a foam and that has at least one solvent, at least one active pharmaceutical ingredient, and at least one foaming agent. The foam volume and the foam stability are determined according to a standardized SITA measuring method. The foaming agent, the solvent, and the active pharmaceutical ingredient are varied in regard to the chemical type and/or concentration thereof until the foam thus produced by the SITA measuring method has a foam volume of at least 400 ml and such foam stability that after a dwell time of up to ten minutes the foam still has at least 50% of the foam volume that originally existed immediately after the foam was produced.

Abstract: A high-efficacy, long-acting, slow-release formulation of the poorly soluble drug, comprising solid dispersion of the poorly soluble drug, silica nanoparticles loaded with the poorly soluble drug, matrix material, and release enhancer, wherein the mass ratio of these components is solid dispersion of the poorly soluble drug: silica nanoparticles loaded with the poorly soluble drug: matrix material: release enhancer=1: 0.5˜1.25: 0.1˜0.3: 0.1˜0.3; the said solid dispersion of the poorly soluble drug contains povidone K30, soybean lecithin, and acrylic resin IV, wherein the mass ratio of the drug and the accessory materials is poorly soluble drug: povidone K30: soybean lecithin: acrylic resin IV=1: 1-3: 0.3˜0.8: 0.2˜0.5. Compared with the existing formulations, the in vivo half life of the high-efficacy, long-acting formulation of the poorly soluble drug disclosed in this invention is 2.3˜14.8 times longer while the mean residence time (MRT) of which is 7.94˜4.

Abstract: Oligomeric acylated biosurfactants (“OABs”) having low critical micelle concentrations of from about 1.0 ppm to about 200 ppm, preferably less than about 50 ppm, in an aqueous solution of Minimal Essential Media that can lower the surface tension in the aqueous MEM environment to less than about 50 dynes/cm2 and have the ability to increase metabolic soluble proteins and/or increase synthesis of extracellular skin matrix proteins and/or increase rates of cell turnover while at the same time exhibiting comparatively low toxicity—preferably, an LD50 of greater 200 ppm in 37 year-old female fibroblast cells. Another aspect of the present invention is directed to the use of OABs in formulations that are topically-applied, by which is meant the formulation is placed in direct contact with the skin, hair and nails as well as mucosa of the eyes, ears, nose, mouth, anus and vagina.

Abstract: The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, the compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.

Abstract: The present invention relates to a method for treating dry eye disease, comprising the steps of identifying a subject suffering from dry eye disease, and administering to the subject an effective amount of azithromycin. The present invention also relates to a method for reducing contact lens intolerance in a subject, comprising the steps of: identifying a subject suffering from contact lens intolerance due to dry eye disease; and administering to the eyes of the subject an aqueous ophthalmic solution comprising azithromycin. The present invention also relates to a method for improving post surgery visual acuity outcome in a patient, comprising the steps of: identifying a patient in need of an ophthalmic surgical procedure, administering to the patient an effective amount of azithromycin prior to the ophthalmic surgical procedure, and performing the ophthalmic surgical procedures on the patient.

Abstract: The invention provides polymorphs of a motilide having a structure represented by formula Ia

Abstract: Described herein are macrolide and ketolide antibiotics and pharmaceutical compositions, methods, and uses thereof for treating gastrointestinal diseases.

Abstract: For the purpose of treatment and/or prevention of pulmonary disorders caused by the destruction of pulmonary alveoli resulting from smoking, air pollution, noxious gas, etc., there are provided, among others, a method of administering clarithromycin or a salt thereof to a mammal and a pharmaceutical composition comprising clarithromycin or a salt thereof.

Abstract: The present invention has as its objective to provide mucoadherent compositions with enhanced properties of bioadhesivity, consistency, stability and vaginal pH regulation. It can also be the carrier of an active principle for the treatment or prophylaxis of disturbances or diseases caused in mucosa, particularly in the vaginal tract, as well as their use.

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: Granules and coated granules, characterized in that they contain the following: a core containing at least one active ingredient which is optionally associated with at least one waxlike compound and optionally at least one polymer and/or binding agent; at least three successive layers of coating from the core outwards; a functional polymer coating (1) optionally containing a waxlike compound, enabling immediate, delayed or prolonged release, which can have a structure which is different from that of the first but which has a complimentary release function and which conditions the suspension medium.

Abstract: An environmentally safe, pesticidally effective composition is provided to control insect/mite pests. In an exemplary embodiment, a composition is provided that includes a pesticidally effective, yet environmentally safe, concentration of at least one spinosyn with at least one additional contact-acting insecticide and/or miticide and at least one solvent or carrier.

Abstract: Triazole-containing macrolide and ketolide antibiotics, therapeutic compositions containing them and methods of use for treating diseases caused by one or more resistant organisms are described.

Abstract: Compositions and methods for modulating HSP70 function, particularly for the targeted killing of cancer cells, are disclosed.

Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.

Abstract: A pH-sensitive solid pharmaceutical composition for oral formulation and preparation method thereof is provided. The solid pharmaceutical composition contains a pharmaceutical active ingredient, a nano-matrix carrier and a pH-sensitive polymer material.

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.

Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.

Abstract: The present invention relates to a granular pharmaceutical composition comprising a drug having a disagreeable taste, a wax and a sugar alcohol; a method for preparing the same; and a pharmaceutical product for oral administration, comprising the granular composition. The product excellently masks a disagreeable taste possessed by a drug and provides good sensation upon oral administration, and therefore is easily ingested by even the elderly, children, and patients suffering dysphagia. Moreover, the product is suitable for administration using tube.

Abstract: The present invention relates to a pharmaceutical composition and its preparation method for the eradication of Helicobacter pylorif in the forms of effervescent tablet, suspension or powder. The pharmaceutical composition comprises an effective dose of ?-lactam antibiotic, an effective dose of macrolide antibiotic, an effective dose of antacid such as proton pump inhibitor and H2 blocker, and a pharmaceutical acceptable carrier. An effective dose of alkaline substance such as carbonate or bicarbonate can be added to increase the pH of the stomach when the PPI antacid is used, which can protect the degradation of acid-labile antibiotics or PPI to further increase the bioavailability of the pharmaceutical composition for the purpose of Helicobacter pylori eradication.

Abstract: A novel maintenance therapy regime/regimen for the treatment of acne related diseases includes administering an oral antibiotic with a topical fixed-dose combination of a retinoid, such as adapalene, and an anti-bacterial agent, such as benzoyl peroxide.

Abstract: The present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.

Abstract: The invention relates to a dermatological pharmaceutical composition for the treatment of skin inflammation diseases, such as dermatitis, atopic dermatitis, vitiligo, alopecia areata, acne, psoriasis and pruritus. The invention comprises a base anti-inflammatory agent, such as indometacin; one or more optional active ingredients selected alternatively from among at least a corticoid and an antibiotic; and a combination of topical antioxidants used to potentiate the anti-inflammatory effect, selected from among green tea, lipoic acid, curcumin, ascorbyl palmitate, Coenzyme Q10, resveratrol, Pycnogenol™, L-camosine, taurine, vitamin E, vitamin C, papaya extract, isoflavones, manganese, lycopene and quercetin. At least one of the topical antioxidants is a peroxisome proliferator-activated receptor-gamma (PPAR-?) activator. The invention also includes at least one antioxidant substance with an antiproliferative effect on keratonocytes, e.g.

Abstract: The present invention features methods and kits that utilize Ang-2 antagonists for the treatment, inhibition, and prevention of a systemic anthrax infection. The invention described herein also features methods for the diagnosis of a systemic anthrax infection by detecting elevated levels of Ang-2 in the serum of a subject.

Abstract: The invention provides for new methods for treatment and diagnosis of irritable bowel syndrome (IBS). In particular, there is disclosed the use of a Chlamydia activating agent and one or several antibiotics selected from macroildes and benzoxazinorifamycins in the preparation of combination agent for simultaneous, concomitant or sequential administration for the treatment of IBS.

Abstract: Described herein are materials and methods for the inhibition of bacterial QS. Methods of treating bacterial infections by administration of one or more ellagitannins in amount effective to inhibit bacterial QS is also provided.

Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.

Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.

Abstract: The invention provides implantable drug releasing materials comprising a calcium phosphate composition, a biodegradable polymer adsorbed onto the calcium phosphate composition, wherein the polymer comprises acidic amino acid residues, and a drug adsorbed onto or reacted with the polymer. The invention is further directed to dental and bone implants and implantable medical devices comprising the implantable drug releasing material, methods for preparing the implantable drug releasing material, and methods for delivering the implantable drug releasing material to bone or teeth.

Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.

Abstract: The present invention relates to a method of forming shape-retentive and shape-conforming aggregate wound dressings and biomaterials composed of gel nanoparticles and wound or bodily fluid in which the aggregates are held together by non-covalent bond physical forces such as, without limitation, hydrophobic-hydrophilic interactions and hydrogen bonds. The method comprises introducing a dry powder of gel nanoparticles to a wound site in which the nanoparticles absorb some of the blood or wound exudate and coalesce in situ into the claimed shape-retentive aggregate dressing. The method also comprises introducing the dry nanoparticle powder in or on a wet bodily tissue in vivo to form the claimed shape-retentive biomaterial. In addition, the method also comprises incorporating biomedical agents to produce medicated aggregate dressings or biomaterials for a variety of medical applications. This invention also relates to uses of the method of formation of the shape-retentive aggregates of gel nanoparticles.

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 lacking cladinose sugar substituted at the C-3 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-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Abstract: This application relates to methods of identifying pharmacoperone agents that can restore function to a misfolded protein, such as a misfolded protein that causes disease. Also disclosed are methods of using such pharmacoperone agents to treat a disease or disorder that results from the misfolded protein.

Abstract: A liquid composition suitable for topical use comprising is provided that includes a phospholipid foaming agent and at least one solvent; and a pharmaceutically acceptable active agent; wherein the liquid composition is capable of mechanically foaming without an additional propellant; and wherein upon mechanical foaming of 250 ml of the liquid composition results in a foam with a foam volume of at least about 400 ml and a foam stability wherein at least about 50% of the foam volume is still present after about 5 minutes at 25° C., as determined using a SITA foam measurement. Also provided herein are methods of making disclosed compositions and methods of use.

Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.

Abstract: Novel 2?-O,3?-N-bridged macrolides useful in treatment of inflammatory diseases. More particularly, the invention relates to 2?-O,3?-N-bridged 14-membered macrolides and to 2?-O,3?-N-bridged 15-membered azalide macrolides useful in treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof.

Abstract: The present invention discloses systems and methods for controlling arthropod populations. The systems include a polymeric substrate, a semiochemical that is reactive upon an adult-stage arthropod, and an insecticide that is toxic to an immature-stage arthropod. The semiochemical may be a sex pheromone that disrupts mating behavior of the adult-stage arthropod. The insecticide may be a per os insecticide that only affects the immature-stage arthropod. The arthropod to be controlled may be gypsy moths, in which case the semiochemical may be disparlure and the insecticide may be spinosad. Further disclosed are methods for preparing systems for use in controlling arthropod populations.

Abstract: Several diterpene glycosides (e.g., rubusoside, rebaudioside, steviol monoside and stevioside) were discovered to enhance the solubility of a number of pharmaceutically and medicinally important compounds, including but not limited to, paclitaxel, camptothecin, curcumin, tanshinone HA, capsaicin, cyclosporine, erythromycin, nystatin, itraconazole, and celecoxib. The use of the diterpene glycoside rubusoside increased solubility in all tested compounds. The diterpene glycosides are a naturally occurring class of water solubility-enhancing compounds that are non-toxic and that will be useful as new complexing agents or excipients in the pharmaceutical, agricultural (e.g., solubilizing pesticides), cosmetic and food industries. Aqueous solutions by using rubusoside to increase the solubility of otherwise insoluble drugs will have several new routes of administration. In addition, aqueous solutions of therapeutic compounds with rubusoside were shown to retain the known pharmacological activity of the compounds.

Abstract: The invention relates to a novel solubilized small molecule topical formulation for the transdermal delivery of small molecule agents comprising: a small molecule agent, one or more micelle forming compounds, one or more skin penetration enhancers, a surfactant, and one or more solvents, wherein the small molecule agent is solubilized in the solvent. The invention further relates to the use of the topical formulation as well as the process for making the topical formulation.

Abstract: Oral pharmaceutical dosage form containing at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another, at least one of the medicaments being selected from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, clopidogrel.

Abstract: The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.

Abstract: GABAA receptor mediated hypersomnia can be treated by administering a GABAA receptor antagonist (e.g., flumazenil; clarithromycin; picrotoxin; bicuculline; cicutoxin; and oenanthotoxin). In some embodiments, the GABAA receptor antagonist is flumazenil or clarithromycin. The GABAA receptor mediated hypersomnia includes shift work sleep disorder, obstructive sleep apnea/hypopnea syndrome, narcolepsy, excessive sleepiness, hypersomnia (e.g., idiopathic hypersomnia; recurrent hypersonmia; endozepine related recurrent stupor; and amphetamine resistant hypersonmia), and excessive sleepiness associated with shift work sleep disorder, obstructive sleep apnea/hypopnea syndrome, and hypersomnia (e.g., idiopathic hypersomnia; recurrent hypersomnia; endozepine related recurrent stupor; and amphetamine resistant hypersomnia.

Abstract: Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans.

Abstract: The invention relates to an oral compositions comprising telithromycin that have taste masking properties, a process for the preparation thereof, and methods of using the composition.

Abstract: An anti-aging composition is provided that contains high potency retinol along with anti-irritant properties. In particular, an anti-aging composition includes a base, from about 0.001% to 20.0 vol % retinol, at least one anti-irritant agent, at least one antioxidant, at least one anti-inflammatory agent, and a moisturizing complex. In one non-limiting illustration, the anti-aging composition contains about 1.0 vol % retinol, plantago lanceolata, hypericum perforatum leaf extract, phytosphingosine, leontopodium alpinum extract, glycyrriza glabra root extract, sambucus nigra flower extract, nordihydrognaiaretic acid, oleanolic acid, spiraea ulmaria flower extract, evodia rutaecarpa fruit extract, boswellia serrata extract, and additives.