Abstract: The present invention relates to novel tigecycline compositions with improved stability in both solid and solution states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid or buffer.

Abstract: Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.

Abstract: The present invention provides pharmaceutical compositions suitable for oral and methods of treating subjects in need thereof. The pharmaceutical compositions of the present invention enhance bioavailability of at least one compound classified as BCS Class II, BCS Class III or BCS Class IV.

Abstract: The present invention relates to compositions, pharmaceutical compositions, and methods for preparing the same, comprising a tetracycline with improved stability and solubility. Some embodiments include a tetracycline with an excess of a divalent or trivalent cation.

Abstract: Topical minocycline compositions with reduced fluorescence are provided. In some instances, the compositions include an amount of a minocycline active agent associated with porous calcium particles. Also provided are methods of using the compositions, e.g., in the treatment of acne.

Abstract: The present invention relates to compositions, pharmaceutical compositions, and methods for preparing the same, comprising a tetracycline with improved stability and solubility. Some embodiments include a tetracycline with an excess of a divalent or trivalent cation.

Abstract: The present invention provides stable aqueous doxycycline aqueous solutions suitable for pharmaceutical, especially ophthalmic, use. The doxycycline aqueous solutions have a pH ranging from 4.5-8, and contain an antioxidant and a stabilizer such as caffeine, creatine or mixtures thereof. The solutions have improved lifetimes and can be used topically.

Abstract: A topical formulation comprising a tetracycline comprises two separate parts: (i) a first part comprising a tetracyline in solid form suspended in a first vehicle; and (ii) a second part comprising a second vehicle in which the tetracycline is soluble. Preferably the tetracycline is crystalline minocycline base. Suitably, a neutral vehicle is used for the first part of the formulation. The two parts of the formulation may be packaged in separate containers and are preferably topically applied therefrom simultaneously.

Abstract: A method of selecting the constituent elements of a therapeutic composition for application to wounds having a pathogen load is disclosed.

Abstract: An aqueous solution comprising a chelating agent at a concentration of about 0.1-0.5%, and an antioxidant agent at a concentration of about 0.1-0.5%, wherein the pH of the solution is between about 4.5 and about 7.5 is disclosed. The aqueous solution may comprise a tetracycline composition wherein the tetracycline is formulated in the aqueous solution. A method for reducing the rate and/or overall extent of degradation of a tetracycline in aqueous solution, comprising admixing in a tetracycline containing solution a chelating agent at a concentration of about 0.1-0.5% and an antioxidant at a concentration of about 0.1-0.5% and, as necessary, adjusting the pH of the solution so that it is between about 4.5 and about 7.5 is also disclosed. Tetracycline compositions of the invention may be used to treat inflammatory and/or tissue degeneration conditions.

Abstract: A method of preparing an aqueous formulation of an active material and such a formulation per se are described, wherein the active material has a very low solubility in water. The method may involve contacting active material in solid form with an optionally cross-linked water soluble polymer. The water soluble polymer is preferably a polyvinyl polymer with polyvinylalcohol being preferred. The polymer is optionally cross-linked. The method and formulation may be of particular utility in delivery of anti-cancer drugs or drugs via a pulmonary route.

Abstract: The present invention relates to novel tigecycline compositions with improved stability in both solid and solution states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid or buffer.

Abstract: Compositions for topical application to the skin and/or a wound are disclosed. In some embodiments, the compositions include a suspension or dispersion of particles of at least one poorly soluble drug chelated or otherwise complexed with a metal salt. The compositions may further contain at least one stabilizer, at least one excipient, and at least one physiologically acceptable carrier. Methods for making such compositions, pharmaceutical formulations containing such compositions, and methods of treatment utilizing such compositions are also disclosed.

Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.

Abstract: Pharmaceutical formulations containing tetracycline for topical administration, as well as methods of making and administering the same, are disclosed.

Abstract: Multi-part pharmaceutical formulations containing tetracycline for topical administration, as well as methods of making and administering the same, are disclosed.

Abstract: A biodegradable bone replacement material for the treatment of bone defects and delivery of antibiotic compounds, particularly for treating bone infections, comprising calcium sulfate hemihydrate, calcium sulfate dihydrate, an antibiotic mixture comprising a tetracycline compound and an ansamycin compound. Preferably, the ratio of calcium sulfate hemihydrate to calcium sulfate dihydrate is from 1:1 to about 3:1. Methods for treating, repairing or augmenting an osseous defect using the bone replacement material are also provided.

Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.

Abstract: The present invention provides improved chlortetracycline-containing animal feed compositions and processes and apparatuses for their preparation. In certain embodiments, raw fermentation broth comprising chlortetracycline is divided into two portions. The first portion is mixed with a compound that complexes chlortetracycline. The second portion is acidified and the solids are removed. The acidified liquid is treated with a complexing agent to produced a chlortetracycline complex. The first and second portions thus treated are then mixed and the mixture is passed on to a filter press or other means for separation of the solids to produce a wet cake comprising complexed chlortetracycline. In alternative embodiments, the second portion may be acidified and filtered and admixed with the first portion prior to the complexing step. The resulting mixture is passed on to a filter press or other means for separation of the solids.

Abstract: Compositions for improved treatment of wounds on a patient. A first composition having a safe and effective amount of lidocaine, wherein the composition is topically applied to a wound on a patient. A second composition having a safe and effective amount of lidocaine and a safe and effective amount of topical antibiotic, wherein the composition is topically applied to a wound on a patient. A method for treating a patient having a skin wound by locally administering a safe and effective amount of lidocaine and an antibiotic compound in the skin wound such that healing of the skin wound is enhanced.

Abstract: The invention relates to hardly soluble antiphlogistic salts and antiphlogistic-antibiotic pharmaceutical preparations and their use. The hardly water soluble antiphlogistic antibiotics salts have as their cationic component one of the antibiotics gentamicin, clindamycin, neomycin, streptomycin, tetracycline, doxicyline, oxytetracycline and rolitetracycline and as their anionic component one of the antiphlogistics ibuprofen, naproxen, indomethacin, dexamethasone-21-phosphate, dexamethasone-21-sulfate, triamcinolone-21-phosphate and triamcinolone-21-sulfate. The antiphlogistic antibiotics salts are used in pharmaceutical preparations as controlled-release antibiotic/antibiotics drugs.

Abstract: Chronological aging of human skin can be delayed with the topical application of an MMP inhibitor, preferably a retinoid (an indirect MMP inhbitor); retinoids also normalize procollagen biosynthesis. Chronological aging, or natural aging, is evidenced in elderly (80+ years old) skin by increased MMP levels and decreased procollagen levels when compared with younger individuals. Prophylactic treatment of not yet chronologically-aged skin with a retinoid both inhibits degradation of dermal collagen and restores procollagen synthesis. Biopsied sections from elderly skin show that a single treatment of chronologically-aged skin with a retinoid can increase epidermal thickness, improve the dermal collagen density, and promote the formation of rete pegs and dermal papillae. Such benefits are helpful in preventing bruising, tearing, and ulceration of elderly skin. Accordingly, prophylactic treatment begun much earlier in life with an MMP inhibitor and/or a retinoid delays the onset of such symptoms.

Abstract: Methods and pharmaceutical compositions for preventing and treating disease mediated by toxin-secreting bacteria. Inventive methods and compositions are suited to preventing or treating infections caused by bacterial toxins that enter host cells via receptor-mediated endocytosis (e.g., the anthrax and diphtheria toxins). Methods comprise a step of administering to an individual a pharmaceutical composition that includes an effective amount of an inhibitor of endosomal acidification. The inhibitor may be a primary amine, a carboxylic ionophore, or a selective inhibitor of the vacuolar proton pump (V-ATPase). The inhibitors of endosomal acidification may be employed in combination with other therapeutics such as antibiotics and antitoxins in order to prevent, treat or cure the disease.

Abstract: New uses of statins as novel types of immunomodulator. More specifically, the invention relates to methods for treating multiple sclerosis through the administration of one or more statins, and even more advantageously, in combination with other multiple sclerosis agents or treatments, such as &bgr;-interferons or copaxone.

Abstract: A method of treating a diabetic foot infection in a mammal includes oral, parenteral, or intravenous administration of a pharmaceutical formulation containing an orally, parenterally, or intravenously-effective amount, respectively of an oxazolidinone.

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: The present invention provides a panel of transcriptional activator fusion proteins which comprises both tetracycline controlled transactivator proteins and reverse tetracycline transactivator proteins. These transactivators have novel phenotypes such as altered basal transcriptional activity in the absence of doxycycline, altered induced transcriptional activity in the presence of doxycycline, or differential induction by tetracycline and analogs of tetracycline.

Abstract: Methods are provided for treating or preventing infections by obligate intracellular prokaryotes, including mycoplasma, rickettsia and chlamydia, and DNA viruses, including herpes viruses, papillomaviruses, adenoviruses and hepatitis B virus. The methods involve the administration of 3:1 complexes of 3-hydroxy-4-pyrones with gallium, e.g., gallium maltolate. Therapies incorporating gallium maltolate in combination with agents used against obligate intracellular prokaryote and DNA virus pathogens are also provided, as are multi-combination therapies designed to treat co-infection by an obligate intracellular prokaryote or DNA virus in an immunocompromised individual. These multi-combination therapies rely on the ability of gallium maltolate to complement antiviral medication regimes against both HIV and other pathogens such as herpesvirus infections, including Kaposi sarcoma, CMV retinitis and blindness, and lymphomas, in patients immunocompromised by HIV infection.

Abstract: The present invention is a method of administering an antibiotic of the tetracycline family or a non-antibacterial tetracycline compound in a daily dosage over an extended period of time in order to reduce the effects of aging on a patient's skin, including the appearance of wrinkles; to reduce the systemic effects of aging on the patient, including the incidence of hair loss in men, where such systemic effects appeared to be replaced by a general feeling of vigor, increased energy levels and a more youthful physique; to reduce the effects of sun damage on a patient's skin; to reduce the onset of menopause on female patients; to reduce the incidence of myocardial infarction; to reduce the physiological effects of hypertension; to reduce the incidence stroke, and to reduce the high levels of cholesterol in the patient's bloodstream.

Abstract: The present invention relates to a method for reducing symptoms related to a neurodegenerative disease and/or treating a neurodegenerative disease, this therapy comprising the administration of a therapeutically effective amount of at least two compounds selected from the group of an inhibitor of microglial activation, an antiglutominergic agent and a voltage gated calcium channer blocker to a patient suffering from a neurodegenerative disease. The present invention also relates to a composition for reducing symptoms related to a neurodegenerative disease and/or treating a neurodegenerative disease, comprising a therapeutically effective amount of at least two compounds selected from the group of an inhibitor of microglial activation, an antiglutaminergic agent and a voltage gated calcium channel blocker in association with a pharmaceutically acceptable carrier.

Abstract: A treatment for conditions in human beings associated with either or both reactive arthritis or bursitis comprising a combination of acyclovir, minocycline hydrochloride, and metronidazole. An alternate treatment comprises the combination of valacyclovir hydrochloride, minocycline hydrochloride, and metronidazole.

Abstract: The present invention is directed to methods for preventing or treating inflammatory bowel disease by administering a composition comprising a therapeutically or prophylactically effective amount of a composition comprising between about 60% to 90% iduronylglycosaminoglycan sulfate and between about 10% to 40% dermatan sulfate, or a pharmaceutically acceptable salt, solvate, hydrate, or clathrate thereof. In a particular embodiment, a therapeutically or prophylactically effective amount of a composition comprising sulodexide, or a pharmaceutically acceptable salt, solvate, hydrate, or clathrate thereof is administered. The composition to be administered may also comprise one or more additional active ingredients selected from the group consisting of steroids, aminosalicylates, short-chain fatty acids, thioguanine derivatives, antibiotics, biological agents, antidepressants, and pain-relievers.

Abstract: The invention relates to a novel pharmaceutical composition comprising an effective amount of bio-active fraction from cow urine distillate as a bioavailability facilitator and pharmaceutically acceptable additives selected from anticancer compounds, antibiotics, drugs, therapeutic and nutraceutic agents, ions and similar molecules which are targeted to the living systems.

Abstract: The invention is a method of inhibiting a sarcoma, such as Kaposi's sarcoma, in a mammal. The method employs 6-demethyl-6-deoxy-4-de(dimethylamino)tetracycline (CMT-3.

Abstract: An injectable composition is described having a higher residual effect with reduced detrimental effects such as pain at injection site, swelling, tissue irritancy or necrosis. The composition contains as active principle a tetracycline compound, either as the free base or a salt thereof with a physiologically acceptable acid, complexed with a substantially equimolar amount of a magnesium compound, and is solubilized in a water miscible solvent system comprising glycerol formal in a an amount of about 40 (v/v); with from about 1% to about 20% (v/v) polyethylene glycol and optionally containing a pH modifier in an amount sufficient to maintain a physiologically acceptable pH. In addition, the composition may further comprise a thickener, such as polyvinyl in an amount of about 10% (w/v). The balance of the composition comprises water.

Abstract: The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical use in the ocular bacterial infections, more preferably in the treatment of conjunctivitis, keratitis and blepharitis.

Abstract: The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is —H or —CH3; wherein R2 is —H or —CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).

Abstract: An injectable composition of higher residual effect with reduced detrimental effects such as pain at injection site, swelling, tissue irritancy or necrosis and containing as active principle a tetracycline compound, either as the free base or a salt thereof with a physiologically acceptable acid, complexed with a substantially equimolar amount of a magnesium compound, is solubilized in a water miscible solvent system comprising, either (i) a) glycerol formal in an amount of from about 10 to 50% v/v; with b) polyethylene glycol in an amount of from about 1 to 15% v/v; or (ii) from about 25 to about 75% v/v of N-methylpyrrolidone, the composition optionally containing a pH modifier in an amount sufficient to maintain a physiochemically acceptable pH, the balance being made up with water q.s.

Abstract: The invention is a method of inhibiting cancer growth, by inhibiting cellular proliferation, invasiveness, or metastasis, or by inducing cytotoxicity against cancer in mammals. The method employs 6-demethyl-6-deoxy-4-de(dimethylamino)tetracycline (CMT-3) and other functionally related chemically modified, preferably non-antibacterial, tetracycline compounds to inhibit cancer growth. The method is particularly effective to inhibit the establishment, growth, and metastasis of solid tumors, such as tumors derived from colon cancer cells, breast cancer cells, melanoma cells, prostatic carcinoma cells, or lung cancer cells.

Abstract: Tissue-destructive conditions related to excess proteinase activity in a biological system are treated or prevented by administering to the system a composition which combines a tetracycline and a bisphosphonate in synergistic proteinase inhibiting amounts.

Abstract: Methods for screening for compounds which potentiate the activity of antibacterial agents against bacteria resistant to the antibacterial agent alone, pharmaceutical compositions including such potentiators, and methods of treating bacterial infections using a combination of a potentiator and a potentiated antibacterial agent, which are useful for overcoming the resistance of a bacterial strain for an antibacterial agent.

Abstract: The invention is a method of inhibiting cancer growth, including cellular proliferation, invasiveness, or metastasis in mammals. The method employs 6-demethyl-6-deoxy-4-dedimethylaminotetracycline (CMT-3) and other functionally related chemically modified, preferably non-antibacterial, tetracycline compounds to inhibit cancer growth. The method is particularly effective to inhibit the establishment, growth, and metastasis of solid tumors, such as tumors derived from colon cancer cells, breast cancer cells, melanoma cells, prostatic carcinoma cells, or lung cancer cells.

Abstract: The present invention relates to leave on, oil-in-water, skin care compositions, comprising: (A) from about 0.05% to about 20% of an acidic active ingredient, preferably having a solubility parameter from about 6 to about 12; (B) from about 0.1% to about 25% of alkoxylated alcohols, alkoxylated polyols, and mixtures thereof; (C) from about 1% to about 20% of an acid stable, hydrophobic, structuring agent selected from the group consisting of saturated C.sub.16 to C.sub.30 fatty alcohols, saturated C.sub.16 to C.sub.30 fatty alcohols containing from about 1 to about 5 moles of ethylene oxide, saturated C.sub.16 to C.sub.30 diols, saturated C.sub.16 to C.sub.30 monoglycerol ethers, saturated C.sub.16 to C.sub.30 hydroxy fatty acids, and mixtures thereof, having a melting point of at least about 45.degree. C.; (D) from about 0.

Abstract: An injection solution for subcutaneous or intramuscular administration to an animal, and a method of producing same, are provided. The injection solution is substantially free of chloride ions and employs a basic amino acid as a pH-adjusting agent, characteristics that make the injection solution more physiologically tolerable upon injection. Preferably, the injection solution comprises 5 to 30 g of oxytetracycline per 100 ml of injection solution, where the oxytetracycline is provided in a magnesium complex; 0 to 25 g of polyvinylpyrrolidone per 100 ml of injection solution; a basic amino acid in an amount sufficient to adjust a pH of the injection solution to from 5.5 to 9.5; and an additive in an aqueous/organic solvent phase.

Abstract: An antibiotic formulation comprising gentamicin, and optionally tetracycline or oxytetracycline, for use in plants.

Abstract: A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated, to an effective killing level, by applying an electric field across the surface containing the biofilm.

Abstract: Novel aqueous oxytetracycline compositions comprising oxytetracycline, polyethylene glycol with a mean molecular weight of 400, and magnesium oxide. These compositions have good clarity and low viscosity.

Abstract: Oxytetracycline aqueous solutions, particularly for parenteral administration containing N-Methylpyrollidone as a solvent are disclosed.

Abstract: A novel complex of carrageenan and a member of the group consisting of emepronium, doxycycline, and propranolol, pharmaceutical preparations containing such a complex, and its use in medicine.

Abstract: This invention relates to 2-substituted aminopyridone compounds which have histamine H.sub.2 -antagonist activity.