Abstract: The proliferation of uterine fibroid leiomyoma cells is inhibited by certain Fibroid Cell Growth Inhibitor (FGI) agents. The pharmacological doses of these FGI agents in the milieu of uterine fibroid cells can be made high enough to not only inhibit proliferation, but to also causes cell death. Non-invasive or minimally invasive, non-systemic delivery methods are used to deliver the FGI agent to the milieu of the target fibroid leiomyoma cell population, thereby avoiding the disadvantages and side effects of surgical and systemic hormonal therapy interventions in the treatment of uterine fibroids. The FGI agents are substrates that are normally present or are well tolerated in the human body. The efficacy of the FGI agents appears to be related to their ability to moderate the Protein Kinase C and Mitogen Activated Protein Kinase pathways. Specific FGI agents shown to be useful to inhibit growth or proliferation of uterine fibroid cells include: &agr;-tocopherol, &agr;-tocopherol succinate, and troglitazone.

Abstract: Cytokine antagonists for use in localized clinical disorders are provided for the treatment and prevention of damage to the optic nerve, other cranial nerves, spinal cord, nerve roots, peripheral nerves or muscles caused by any one of the following: a herniated nucleus pulposus, osteoarthritis, other forms of arthritis, disorders of bone, disease, or trauma. The cytokine antagonists are used to treat these disorders by local administration. These cytokine antagonists include antagonists to tumor necrosis factor.

Abstract: The present invention provides a non-invasive method for administering polypeptides across epithelial membranes. The formulations in the present invention comprise solid polypeptide particles mixed with a permeation enhancer and excipients which are dispersed in a media for oral or intranasal administration. Also provided in the present invention is a process to prepare the formulations.

Abstract: The application is directed to the treatment of neoplastic diseases or conditions by administering R(−) desmethylselegiline, S(+) desmethylselegiline, or a combination of the two. Neoplastic diseases and conditions responsive to R(−) desmethylselegiline and/or S(+) desmethylselegiline include both malignant and benign neoplasms.

Abstract: The spray liquid of a nasal spray is formed by a hyperosmotically adjusted water saline solution with a common salt content of 1 to 4% by weight. It furthermore contains various essential oils.

Abstract: Buccal aerosol sprays or capsule 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 comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.

Abstract: A gelled composition was provided by adding a gelling component to a carrier for adsorption. Not only was the taste of the carrier for adsorption significantly reduced in this composition, but the dosage was also decreased so that the composition could be easily taken by a patient.

Abstract: A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible, biodegradable, controlled release material prolonging the release of the local anesthetic from the substrate to obtain a reversible local anesthesia when inplanted or injected in a patient, and a pharmaceutically acceptable, i.e., non-toxic, non-glucocorticoid augmenting agent effective to prolong the duration of the local anesthesia for a time period longer than that obtainable from the substrate without the augmenting agent.

Abstract: The invention encompasses compositions for increased bioavailability through mucosal delivery comprising, preferably in powder form, an intimate mixture of an effective amount of a bioactive agent and a hydrophobically derivatized carbohydrate. The compositions can also contain a surface active agent preferably for delivery to gastrointestinal mucosa and ocular delivery.

Abstract: Compositions useful for long-lasting pain relief from mucosal damage, such as mucosal inflamation, abrasions, ulcerations, lesions, trauma and incisions, without significant systemic absorption. The compositions of the invention are particularly suitable for application to the mucous membrane of the nasal cavity and buccal cavity. To relieve pain, the compositions or the invention are topically applied directly to the affected area.

Abstract: The present invention relates to fast dispersing solid dosage forms that preferably dissolve in the oral cavity within sixty (60), more preferably within thirty (30), most preferably within ten (10) seconds. A novel feature of the solid dosage forms according to the invention reside in the fact that the composition is essentially free or absolutely free of mammalian gelatin. It has been discovered that the use of certain modified starches at concentrations from 20 to 90% by weight of the solid dosage form prepares dosage forms that are mechanically and chemically stable and are able to deliver higher concentrations of an active ingredient than the heretofore utilized gelatin based fast dispersing solid dosage forms. Further, the solid dosage forms according to the invention are obtainable by removing a solvent, such as water, from a mixture comprising an active ingredient, a modified starch and a matrix forming agent via freeze drying.

Abstract: This invention provides vehicles capable of delivering high concentrations of poorly hydrophilic/poorly lipophilic compounds to animals, by combining compounds having biocompatible hydrophobic domains with conjugates having both hydrophobic and hydrophilic regions. Such formulations are suitable for a number of uses in animals, particularly the administration thereto of high concentrations of therapeutically useful compound, without an undue level of side effects.

Abstract: The invention pertains to cooling agents comprising N-substituted p-menthane-3-carboxamides, menthyl acetate and solubilizer, and methods for making the cooling agents. The invention also concerns pharmaceutical compositions comprising the cooling agents, including tablets, suspensions and liquid solutions having active pharmaceutical agents for treating upper gastrointestinal tract distress, and methods for treating upper gastrointestinal tract distress in humans.

Abstract: A method is provided for delaying the onset of ejaculation in an individual. The method involves systemic and on demand administration to an individual of a pharmaceutical formulation containing an amount of an active agent selected from the group consisting of clomipramine and pharmacologically acceptable acid addition salts thereof. Drug delivery may be accomplished via any route designed to provide systemic levels of the active agent effective to delay the onset of ejaculation. Pharmaceutical formulations and dosage forms are provided as well.

Abstract: The aim of the invention is to use at least one lipid extract obtained from the fruit seeds of the mirabelle tree as an agent for preparing a cosmetic product for locally active (topical) use for skin and hair, lips, mucous membranes and/or appendages of the skin.

Abstract: Methods, kits, apparatus, and compositions for inhibiting a cerebral neurovascular disorder or a muscular headache in a human patient are provided. The methods comprise intranasally administering to the patient a pharmaceutical composition comprising a local anesthetic, and preferably a long-acting local anesthetic ingredient. A composition useful for practicing the methods of the invention is described which comprises at least one local anesthetic in a pharmaceutically acceptable carrier, wherein the composition is formulated for intranasal delivery. Cerebral neurovascular disorders include migraine and cluster headache. Muscular headaches include tension headaches and muscle contraction headaches. A kit comprising the composition and an intranasal applicator and a method of systemically delivering a pharmaceutically active agent to an animal are also included in the invention.

Abstract: The invention provides stable pharmaceutical preparations for topical and nasal uses, comprising Mupirocin calcium amorphous as an anti-microbial active agent therein, dissolved in a pharmaceutically acceptable solvent providing stability therefore.

Abstract: An autoadhesive oral transmucosal delivery device contains a pharmaceutically active agent which is delivered via mucosal tissues in the mouth. The device comprises a dry hydrogel polymer which autoadheres to the moist mucosal surface for a time sufficient for release of active agent to occur before becoming detached.

Abstract: A chemo-physiological structure and method for forming the chemo-physiological structure. In a first embodiment, a cell of an animal is provided. The cell has a membrane surface and a viral receptor coupled to the membrane surface. A linker molecule having a covalently attached polymer is covalently bonded to the membrane surface, the viral receptor, or both. The polymer prevents an extracellular virus from bonding to the viral receptor. In a second embodiment, a linker molecule having a covalently attached polymer is covalently bonded to a capsid of a virus, which prevents the virus from bonding to a viral receptor of an adjacent or nearby animal cell.

Abstract: A patient's upper airway condition such as snoring and sleep apnea is treated by selecting a particulate material selected for limited migration within tissue and for encouraging a fibrotic response of tissue to the material. A bolus of the particulate material is injected into the tissue area to structurally stiffen the tissue.

Abstract: The present invention concerns compositions and methods for preventing miscarriage and premature labor, and for treating and preventing Bacterial Vaginosis using a pH-buffering polymer. The present invention further concerns formulating such a composition or method in such a way as to provide therapeutically sufficient levels of the composition to a patient in need thereof.

Abstract: Compounds of the general formula P1-L-P2; wherein “P1” is a pyrazinoylguanidine sodium channel blocker, “L” is a linking group, and “P2” is either (i) a pyrazinoylguanidine sodium channel blocker or (ii) a P2Y2 receptor agonist, are disclosed. Pharmaceutical formulations containing the same and methods of use thereof to hydrate mucosal surfaces such as airway mucosal surfaces are also disclosed.

Abstract: Chimeric parainfluenza viruses (PIVs) are provided that incorporate a PIV vector genome or antigenome and one or more antigenic determinant(s) of a heterologous PIV or non-PIV pathogen. These chimeric viruses are infectious and attenuated in humans and other mammals and are useful in vaccine formulations for eliciting an immune responses against one or more PIVs, or against a PIV and non-PIV pathogen. Also provided are isolated polynucleotide molecules and vectors incorporating a chimeric PIV genome or antigenome which includes a partial or complete PIV vector genome or antigenome combined or integrated with one or more heterologous gene(s) or genome segment(s) encoding antigenic determinant(s) of a heterologous PIV or non-PIV pathogen.

Abstract: Varying the daily dose of either or both of the estrogen and the progestogen administered for hormone replacement therapy (HRT) is readily and inexpensively accomplished, without the necessity of the physician prescribing a new product each time the daily dose of the estrogen or progestogen is changed, by administering preferably transdermally the estrogen and the progestogen contained in separate extrudable pharmaceutical compositions from a dispenser which contains means, preferably adjustable only by the attending physician or dispensing pharmacist, for varying the volume of either or both of the respective compositions which is dispensed as a single dose from the dispenser in response to a defined digital dispensing manipulation of the dispenser thereby facilitating optimal compliance to a combination of HRT with individually adjusted dosages of the estrogen and progestogen.

Abstract: A delayed release pharmaceutical dosage form for oral administration of a hydrophilic drug, e.g., a polysaccharide drug such as low molecular weight heparin, are provided. The dosage form comprises a composition of: (a) a therapeutically effective amount of low molecular weight heparin; (b) a bile salt or bile acid; (c) at least one surfactant selected from hydrophilic surfactants, lipophilic surfactants, and mixtures thereof; and a means for delaying release of the composition from the dosage form following oral administration. Osmotic drug delivery systems for oral administration of a hydrophilic drug are also provided, wherein an osmotically activated device houses the drug, a bile salt or bile acid, and at least one surfactant selected from the group consisting of hydrophilic surfactants, lipophilic surfactants, and mixtures thereof. Methods for administering hydrophilic drugs, particularly polysaccharide drugs such as low molecular weight heparin, are also provided.

Abstract: A dressing and method of treating wounds is provided. The dressing can comprise water-soluble or swellable polymers which are capable of forming a viscous aqueous or non-aqueous solution and form a gel, particularly a foam form of the gel. The dressing can be constructed in the form of a sponge or sheet impregnated with the gel, or coated onto a non-porous, porous or micro-porous substrate. The dressing can also be provided in a form of a dehydrated powder, such as one which can be sprinkled under a flap of tissue and which will hold the flap down as a substitute for the use of stitches. Wounds treated with dressings in accordance with embodiment of the invention will tend to heal without the formation of a typical hard scab. The gel provides an excellent surface from which to apply tooth whitener to the teeth.

Abstract: An oral adhesive preparation has a substrate and a pressure-sensitive adhesive layer provided on at least one surface of the substrate, in which the pressure-sensitive adhesive layer contains a medicine, and is substantially insoluble in water or absorbs substantially no water. Further, an oral adhesive sheet comprising a separator release-treated on one or both surfaces thereof and a plurality of sections for application to oral mucous membrane mounted on at least one surface of the separator in a specified 2 to 5 by 2 to 5 arrangement with a specified proportion of a minimum inner diameter, Dp, of an incircle passing a center of gravity, W, of a section to a shortest distance, Di, of an adjacent section is 1.5 to 6. The substrate is preferably cloth such as non-woven fabric. Sections containing a local anesthetic can be used in surface anesthesia in dentistry.

Abstract: Pharmaceutical aerosol formulations are provided comprising substantially nonacicular particles of a bronchodilator selected from the group consisting of ipratropium and pharmacologically acceptable salts, solvates, hydrates, esters and isomers thereof. The described formulations include a propellant selected from the group consisting of a fluorocarbon propellant, a hydrogen-containing fluorocarbon propellant, and mixtures thereof. The formulations are substantially free of both surfactant and solvent. Methods of use and drug delivery devices are also provided.

Abstract: The present invention relates to a pharmaceutical composition which includes morphine gluconate or chemical equivalent thereof. In one embodiment, the present invention includes a method of making morphine gluconate or chemical equivalent thereof by mixing morphine sulfate with sodium gluconate. The present invention also includes a method for eliciting an analgesic or anesthetic response in a mammal which includes administering a therapeutically effective amount of a pharmaceutical composition including morphine gluconate or chemical equivalent thereof.

Abstract: Methods are provided for purifying peptides and proteins by incorporating the peptide or protein into a diketopiperazine or competitive complexing agent to facilitate removal one or more impurities, i.e. undesirable components, from the peptide or protein. In a preferred embodiment, a peptide, such as insulin, containing one or more impurities, e.g., zinc ions, is entrapped in diketopiperazine to form a precipitate of peptide/diketopiperazine/impurity, which is then washed with a solvent for the impurity to be removed, which is a nonsolvent for the diketopiperazine and a nonsolvent for the peptide. Formulations and methods also are provided for the improved transport of active agents across biological membranes, resulting for example in a rapid increase in blood agent concentration.

Abstract: A composition and process for suppressing pain and irritation of tissue includes an anti-irritant in an effective amount to suppress pain and irritation temporarily when applied topically to the skin or mucosa. The anti-irritant is a natural or non-nutritive sweetener. The composition can be a solid containing an edible acid such as citric acid and ascorbic acid from fresh lemon juice to form a solution having a pH of about 2.0 to 4.0 and an anti-irritant, such as sodium saccharine. The composition can be used to apply a pharmaceutical agent to the skin, mucosa or eye without irritation. The acidic composition can further be used to remove or loosen calculus deposits from the teeth without burning or irritation of the gums.

Abstract: A pharmaceutical dosage form adapted to supply a medicament to the oral cavity for buccal, sublingual or gingival absorption of the medicament which contains an orally administerable medicament in combination with an effervescent for use in promoting absorption of the medicament in the oral cavity. The use of an additional pH adjusting substance in combination with the effervescent for promoting the absorption drugs is also disclosed.

Abstract: Liquid pharmaceutical compositions for administration to a mucosal surface, comprising a therapeutic agent and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.

Abstract: A patient's upper airway condition such as snoring and sleep apnea is treated by selecting a particulate material selected for limited migration within tissue and for encouraging a fibrotic response of tissue to the material. A bolus of the particulate material is injected into the tissue area to structurally stiffen the tissue.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal lauryl sulphate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening of primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. The amount of each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation. A method for administering insulin to the buccal mucosa using a metered dose inhaler is also disclosed.

Abstract: The libido of adult human female patients is increased by the intrapulmonary delivery of testosterone. A formulation of testosterone is aerosolized and inhaled into a patient's lungs where particles of testosterone deposits on lung tissue and then enter the patient's circulatory system. The patient's testosterone level is enhanced well above baseline levels for a short period and subsides to baseline levels with normal metabolism thereby providing desired short term effects on enhanced libido without undesirable effects of long term enhanced testosterone levels. Additional formulations are provided including formulations for aerosolized delivery of sildenafil citrate which are delivered to male or female patients.

Abstract: A powdery nasal composition comprising a drug and colloidal cellulose is provided. The composition is a nasal composition providing a superior absorption activity for the drug.

Abstract: Methods for treating specific patient groups for sexual dysfunction are provided. The methods of the present invention comprise the utilization of pharmaceutical compositions in patients who are free of cardiac disease and/or who have not been given organic nitrates.

Abstract: Specific Cytokine Antagonists, including TNF antagonists and/or Interleukin-1 antagonists, are used as novel therapeutic agents for the treatment of hearing loss, including presbycusis and other forms of sensorineural hearing loss. The present invention provides a method for inhibiting the action of TNF and/or IL-1 antagonists for treating hearing loss in a human by administering a TNF antagonist and/or an IL-1 antagonist for reducing the inflammation affecting the auditory apparatus of said human, or for modulating the immune response affecting the auditory apparatus of said human, by administering a therapeutically effective dosage level to said human of a TNF antagonist and/or an IL-1 antagonist. Administration may be systemic, through the subcutaneous, intramuscular, oral, or intravenous routes; or by delivering an anatomically localized application in the region of the head.

Abstract: A method for inhibiting the action of TNF for treating neurological conditions in a human by administering a TNF antagonist for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human, comprising the step of: administering a therapeutically effective dosage level to said human of said TNF antagonist selected from the group consisting of etanercept, infliximab, and D2E7 (a human anti-TNF mAb from Knoll Pharmaceuticals) for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human. In addition, for the viral-associated neurological disorders, the following additional step is performed: administering a therapeutically effective dosage level to said human of an antiviral agent or anti-retroviral agents for reducing the inflammation of neuronal tissue of said human, or for modulating the immune response affecting neuronal tissue of said human.

Abstract: Cytokine antagonists for use in localized clinical disorders are provided for the treatment and prevention of damage to the optic nerve, other cranial nerves, spinal cord, nerve roots, peripheral nerves or muscles caused by any one of the following: a herniated nucleus pulposus, osteoarthritis, other forms of arthritis, disorders of bone, disease, or trauma. The cytokine antagonists are used to treat these disorders by local administration. These cytokine antagonists include antagonists to tumor necrosis factor; interleukin-1; interleukin-6; and interleukin-8.

Abstract: Devices, methods, and compositions for treating vaginal fungal, bacterial, viral and parasitic infections by intravaginal or transvaginal administration of therapeutic and/or palliative antifungal, antibacterial, antiviral or parasiticidal drugs to the vagina or to the uterus.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: A device, methods and pharmaceutical compositions are disclosed for transnasal or transocular drug delivery to the central nervous system using a combination of electrotransport or phonophoresis with chemical permeation enhancers.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of preventing prostate carcinogenesis comprising the steps of administering to a human subject having a precancerous precursor of prostate adenocarcinoma, a pharmaceutical preparation comprising a chemopreventive agent to prevent, prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: The present invention relates to complexes between (1) a target-binding moiety; (2) a cavity-forming moiety; and (3) a pharmacological compound to be delivered to a target, wherein the pharmacological compound is buried inside of the cavity-forming moiety, but not covalently bound to either the target-binding moiety or the cavity-forming moiety. The complexes of thus invention may be used as to deliver a pharmacological compound to cells, tissues, organs, viruses, microorganisms or other surfaces that are characterized by an entity that binds the target-binding moiety portion of the complex. The present invention also relates to pharmaceutical compositions comprising the non-covalent complexes of this invention. The invention also relates to methods of delivering a pharmacological compound to a target in a patient. The present invention also relates to the use of the complexes of this invention for the separation of chemical entities from their chiral forms or contaminants.

Abstract: A device, methods and pharmaceutical compositions are disclosed for transnasal or transocular drug delivery to the central nervous system using a combination of electrotransport or phonophoresis with chemical permeation enhancers.

Abstract: A method of administering transmucosally, particularly to oral or nasal mucosa, levosimendan or a pharmaceutically acceptable salt thereof to a patient. The method comprises contacting an intact mucous membrane with a source of levosimendan, and maintaining said source with said mucous membrane for a sufficient time period to deliver levosimendan to the patient. Transmucosal preparations of levosimendan are also described. Levosimendan is useful in the treatment of heart failure.