Abstract: The present invention provides novel pharmaceutical compositions for azole antimicrobial drugs such as itraconazole, saperconazole, ketoconazole, and fluconazole. The pharmaceutical compositions are in the form of pellets which comprise a core and a drug emulsion layer, and optionally, a protective layer. The drug emulsion layer contains the azole antimicrobial drug, an emulsifier, a binder, and an absorbent aid. The preferred emulsifier is vitamin E polyethylene glycol succinate. The preferred binder is hydroxypropyl methylcellulose. The preferred absorbent aid is DL malic acid. The drug is dissolved in organic solvents. The preferred organic solvents are ethanol and methylene chloride. The protective layer contains polyethylene glycol (PEG) 20,000, which is coated on the drug emulsion layer.

Abstract: The present invention relates to the derivatives of specially substituted azole compounds which have improved antifungal activity as compared to known compounds such as fluconazole and itraconazole and the processes for the preparation thereof. This invention also relates to pharmaceutical compositions containing the compounds of the present invention and their use in treating and/or preventing fungal infections in mammals, preferably humans.

Abstract: Methods and topical pharmaceutical formulations are provided for the treatment of nail fungus (onychomycosis). The invention involves a pharmacologically active antifungal agent, plus a pharmaceutically acceptable base in a formulation having a pH of 7.5 to about 13.0, preferably about 8.0 to 11.5, and most preferably about 8.5 to 10.5. These basic formulations permeate the nail and are effective in treating fungal infections of the nail and surrounding tissues.

Abstract: This invention relates to substantially anhydrous warming, non-toxic and nonirritating lubricating compositions containing polyhydric alcohols, a gelling agent and alternatively a pH adjusting agent for treating fungal and bacterial infections. The invention also relates to methods of using such compositions for warming, lubrication, administration of active ingredients and for preventing or treating dysmenorrhea.

Abstract: Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.

Abstract: A means and method for treating pulmonary fibrosis and vaginitis in animals is described. The compositions include surfactant lipids in a pharmaceutically acceptable carrier. Surfactant lipids have been found to suppress the synergistic effect of bleomycin and SP-A in enhancing proinflammatory cytokine production. Surfactant lipids are also effective in the prevention and treatment of pulmonary fibrosis resulting from exposure to inflammatory agents affecting cytokine production. Furthermore, surfactant lipids are effective in treating attenuating the effect of proinflammatory cytokine production in vaginitis.

Abstract: The present invention provides a pharmaceutical composition of a practically insoluble drug, wherein the composition may be administered with food or without food. The composition may be in the form of a solid dispersion of the practically insoluble drug and a polymer having acidic functional groups, and the composition may in vitro form a suspension.

Abstract: Alkenyldiarylmethane (ADAM) compounds have been found effective as anti-HIV agents. Novel ADAM compounds, their pharmaceutical formulations and a method of using same to treat viral infections are described.

Abstract: The present invention provides a method of inhibiting growth of lung metastases in an individual comprising the steps of administering a dose of a lipid-drug enhancer liposomal complex and, in sequence, administering a dose of a lipid-anticancer drug liposomal complex. Furthermore, the lipid-drug enhancer liposomal complex may be administered in a continuing dose with the lipid-anticancer drug liposomal complex whereby both liposomal complexes are mixed in the nebulizer. Methods of inhibiting growth of lung metastases in an individual by the sequential administration via aerosolization of a dilauroylphosphatidylcholine-cyclosporin A liposomal complex and a dilauroylphosphatidylcholine-paclitaxel liposomal complex are also provided.

Abstract: Tinea versicolor is a fungal infection of the skin and often results in a discoloration or dyspigmentation of the infected skin. The present invention provides as a combination therapy an antifungal for treating the fungal infection and a retinoid for correcting the skin pigmentation. Preferred antifungal agents are those which are also CYP-26 inhibitors, which delay the natural enzymatic breakdown of retinoids in the skin. Alternatively, a non-CYP-26 inhibiting antifungal can be used in combination with a retinoid, with a CYP-26 inhibitor (antifungal or not) optionally added.

Abstract: Fungicidal compositions comprising an acceptable carrier and/or surface active agent and synergistically effective amounts of

Abstract: The topical application of an azalide antibiotic such as azithromycin to the eye is useful in treating or preventing ocular infections. In one embodiment, the azalide antibiotic is supplied to the eye in a depot for sustained release. A more convenient dosing regimen can also be provided by the use of an appropriate depot. Furthermore, a composition containing a combination of medicaments is also provided.

Abstract: 20% Zinc oxide formulations including up to 5% of at least one pharmacologically active agent and associated topical methods for improved therapeutic treatment of adverse atopic dermatological conditions.

Abstract: A method for the topical treatment of nail diseases, e.g. onychomycosis, after preparation of the infected nail with a laser beam.

Abstract: The invention relates to the therapeutic or prophylactic treatment of fungal infections. The invention provides new methods for therapeutically or prophylactically treating fungal infections using sub-lethal concentrations of an anti-invasin compound. The methods according to the invention have fewer toxicology problems than existing methods, and thus can be used prophylactically, as well as for early treatment for high risk patients without a firm diagnosis. The methods according to the invention can also be used to treat an established fungal infection. The invention further provides novel genes that regulate fungal hyphal growth.

Abstract: The invention relates to nitrofuran-containing compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making the compounds, and methods for identifying compounds with desired biological activity.

Abstract: A set of methods presented for preventing and curing axillary malodors through treating the skin, and fomites with safe, non-restricted, widely available agents.

Abstract: The present invention relates to protein tyrosine phosphatase (“PTPase”) inhibitors, and the use of PTPase inhibitors and PTPase inhibitors in combination with cytokines to treat diseases. Leishmaniasis agents have surprisingly and unexpectedly been found to be potent PTPase inhibitors. Examples of leishmaniasis agents that are also PTPase inhibitors include, but are not limited to, pentavalent antimonial compounds, imidazole compounds, and diamidine compounds. Therapeutic compositions and methods are provided that make use of these compounds to treat diseases.

Abstract: A vehicle for applying chemical compounds to wood comprises the following components in the indicated approximate percentages by weight of the total: toluene (40-70%), xylene (6-40%), benzophenone (3-18%), butyl glycol (2-9%), cetyl acetate (1-7%) and methanol (0.3-4%). The vehicle has a high wood penetration index and can be used for preparing compositions containing one or more chemical compounds useful for treating wood, for example insecticides and/or fungicides, for the purpose of treating or preventing damage caused by the attack of biological agents harmful for wood.

Abstract: The present invention concerns novel compounds of formula 1

Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.

Abstract: This invention relates to an ionic antimicrobial coating. Such a coating may contain (1) a water-insoluble polymer having a first ionized group and (2) an antimicrobial agent having a second ionized group with a charge opposite to that of the first ionized group, in which the antimicrobial agent is attached to the water-insoluble polymer via an ionic bond between the first ionized group and the second ionized group.

Abstract: The invention is directed to a biocompatible stable composition containing a hydrophobic drug, such as paclitaxel. The composition, which forms a syringeable polymeric micellar solution in aqueous or body fluids, is a freeze-dried product comprising a hydrophobic drug, i.e. paclitaxel, and an amphiphilic block copolymer wherein a hydrophobic group having affinity or attraction with the hydrophobic drug, such as paclitaxel, is incorporated on its end. The invention provides a shelf life of longer than three years in a sterilized container, stability of longer than three days in infusion fluid, has minimal side effects and shows improved bioavailability.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

Abstract: This invention relates to novel compositions, methods of use, regimens and kits for treating local fungal and bacterial infections that are susceptible to treatment administered either locally or topically and systemically. The methods of this invention relate to ways in which to relieve symptoms of such infections in an unexpectedly shorter timespan than with conventional treatment with greater predictability than those methods currently known.

Abstract: The present invention concerns compounds of formula the N-oxide forms, the salts, the quaternary amines and stereochemically isomeric forms thereof, wherein D represents a tetrahydrofuran or dioxolane ring substituted with aryl and azolmethyl; —A—B— represents an optionally substituted bivalent radical of formula —N═CH—, —CH═N—, —CH═CH—, —CH2—CH2; Alk represents C1-6alkanediyl; Y represents optionally substituted C1-6alkanediyl; R1 and R2 represent hydrogen, C1-6alkyl or arylC1-6alkyl; or R1 and R2 may be taken together to form an optionally substituted heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopiperidinyl, piperazinyl or phthalimid-1-yl; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydro-naphthalenyl, indenyl or indanyl; each of said aryl groups may optionally be substituted; having broad-spectrum antifungal activity; their preparation, compositions containing them an

Abstract: The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.

Abstract: There are provided granules having a good taking property wherein an active ingredient, at least one kind of soluble additive having an average particle size of smaller than 50 &mgr;m and at least one kind of disintegrator are contained.

Abstract: Compounds of general formula (I), wherein R1 selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl, and triazolyl; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo.

Abstract: This invention is directed to acyl piperazine derivatives of the following formula (Id): wherein R1b, R3, R4, R5, R6 and R10 are described herein. These derivatives are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.

Abstract: The present invention provides a polymorphic form of itraconazole.

Abstract: The present invention relates to a film-forming powder comprising at least one active substance, at least one bioadhesive agent, and optionally surfactants, wetting agents, plasticizers, binders, retardants, penetration promoters and bioerodible diluents.

Abstract: Co-precipitates of itraconazole and a water-soluble non-polymeric compound. Compositions for oral administration comprising amorphous itraconazole or a co-precipitate, and a disintegrant.

Abstract: A preparation comprising a combination of a topical and a systemic antimycotic and a physiologically acceptable lacquer base is suitable for the treatment and prophylaxis of onychomycoses. Preference is given to the use of water-insoluble lacquer preparations and a combination of at least one systemic antimycotic from the group of itraconazole, terbinafine and fluconazole or salts thereof with at least one topical antimycotic from the group of ciclopirox, 6-(2,4,4-trimethylpentyl)-1-hydroxy-4-methyl-2(1H)pyridone, amorolfine and butenafine or salts thereof.

Abstract: The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.

Abstract: An antibiofouling material, a method for making said antibiofouling material, a sensor apparatus employing said antibiofouling material, and a method of making said sensor apparatus. The disclosed antibiofouling material includes one or more biocides and one or more charge transfer compounds are embedded within a copolymer host matrix. Biocides used in the present invention may include, but are not limited to, Halobenzonitriles, Azoles, diuron; and simazine. Among its uses, the antibiofouling material of the present invention can be used in a sensor apparatus. In a preferred embodiment, one or more surfaces of said sensor apparatus are coated with an antibiofouling material comprised of one or more biocides, one or more charge transfer compounds, and a copolymer host matrix.

Abstract: The present invention pertains to methods for reducing the platelet activation state in an individual comprising administering a selective serotonin reuptake inhibitor (SSRI). The platelet activation state is reduced upon administering a SSRI, as measured by one or more platelet activation markers. The invention also relates to methods for treating or preventing an individual at risk for a vascular event, disease or disorder by administering a SSRI.

Abstract: In one embodiment, a therapeutic composition containing a pentavalent antimonial is provided. The pentavalent antimonial can be sodium stibogluconate, levamisole, ketoconazole, and pentamidine and biological equivalents of said compounds. Additionally, pentavalent antimonials that can be used in accordance with the present invention may be any such compounds which are anti-leishmaniasis agents. The therapeutic composition of this embodiment contains an effective amount of pentavalent antimonial that can be used in treating infectious diseases. The types of diseases that can be treated with the present invention include, but are not limited to, the following: diseases associated with PTPase activity, immune deficiency, cancer, infections (such as viral infections), hepatitis B, and hepatitis C. The types of cancers that the present embodiment can be used to treat include those such as lymphoma, multiple myeloma, leukemia, melanoma, prostate cancer, breast cancer, renal cancer, bladder cancer.

Abstract: The present invention relates to compositions of submicron-to micron-size particles of antifungal agents. More particularly the invention relates to aqueous suspensions of antifungal agents for pharmaceutical use.

Abstract: Compositions having synergistic effective amounts of one or more antibacterial agents, a nitroimidazole, and an antifungal agent effective against a Candida species. The compositions are particularly useful in the treatment of genitourinary infections.

Abstract: The inventions relates to the use of silica in the formulation of antifungal composition for the treatment of cutaneous mycoses, and method to manufacture an antifungal powder with boric acid and silica.

Abstract: The invention provides a biological dressing for treatment of a dermatological disease comprised of a gum resin, a topically acceptable volatile solvent, and a pharmacologically active agent. The gum resin is present in a suitable amount that the composition, when the solvent evaporates, will dry to form a solid coating that sticks to the skin or mucosal membrane to which the composition is applied and maintain the pharmacologically active agent over a sustained period of time in contact with sites on the skin or mucosal membranes exhibiting symptoms of the disease. Methods are provided for treating symptoms of dermatological diseases with such a pharmacological composition. Biological dressings including tincture of benzoin and clotrimazole are shown to be efficacious for the long-term amelioration of symptoms of athlete's foot.

Abstract: This invention relates to treatment or alleviation of a disease, condition or disorder selected from inflammatory bowel disease, Chron's disease, colitis ulcerosa, Coeliac disease, dermatitis herpetiformis, dermatomyositis, enteritis allergia, erytherma nodosum leprosum, ileitis regionalis, psoriasis, purpura, scleritis or scleroderma by administering to a living body certain imidazole, triazole, or 1,4-dihydropyridine derivatives.

Abstract: This invention relates to compositions and methods for treating vulvovaginitis and vaginosis. The compositions of this invention contain antifungal agents as well as a buffering system that, when administered to a patient's vagina, maintains the pH of the vagina so as to achieve a healthy environment that encourages the growth of appropriate flora. Antifungal agents that are useful in the compositions of this invention include azole antifungal agents. Buffering systems include gluconodeltalactone.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: The present invention provides a novel pharmaceutical composition based on the use of a particular oil phase which comprises a lipophilic, pharmaceutically active agent, a mixture of diglyceride and monoglyceride in a ratio of from about 9:1 to about 6:4 by weight (diglyceride:monoglyceride) wherein the diglyceride and monoglyceride are mono- or di-unsaturated fatty acid esters of glycerol having sixteen to twenty-two carbon chain length, one or more pharmaceutically acceptable solvents, and one or more pharmaceutically acceptable surfactants. The composition is in a form of self-emulsifying formulation which provides high concentration and high oral bioavailability for lipophilic compounds.

Abstract: The present inventive subject matter relates to amorphous drug beads comprising an amorphous active drug and an organic surfactant having improved solubility, absorption and wettability characteristics. The present inventive subject matter further relates to methods of preparing the amorphous drug beads, wherein molten drug beads are subject to a cooling step with or without shear.

Abstract: A formulation of a sparingly water-soluble, crystalline pharmaceutically active agent wherein the active agent is converted to and stabilized in its amorphous form as a solid solution of a normally hydrophobic vehicle is described. The amorphous state is stabilized by the composition of the formulation, providing long shelf life of the improved composition. This stabilized formulation also provides increased solubility and bioavailability of the active agent. Solutions of the active agent are stabilized by the composition, preventing recrystallization and precipitation of the less soluble, crystalline form of the active agent from aqueous solutions thereof.