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: 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 present invention provides a suppository comprising a hydrophobic hydroxypropyl methylcellulose. The present invention is useful as a suppository base which has little interaction with a drug and has an excellent retainability.

Abstract: The present invention relates to a liquid suppository composition comprising diclofenac sodium, poloxamer and at least one polymer select from the group consisting of polyethylene oxide and polyvinylpyrrolidone. The composition provides the advantages of. (1) a feel of foreign matter or discomfort does not occur when the composition is rectally administered; and (2) administration is easy and after rectal administration, the composition is neither leaked out from the anus nor shifted into the end of large intestine.

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: Biodegradable polymeric implants can provide a safe and efficient means to deliver drugs in the treatment of various diseases. Although a polymeric drug delivery system can be implanted as a solid device within a subject, it is also possible to administer such a system as an injectable liquid which solidifies in vivo. An improved formulation of a polymeric drug delivery system comprises a water insoluble copolymer that is a solid or wax at 37° C., a water soluble polymer that is a liquid at 25° C., and a hydrophobic drug. These drug delivery systems can be administered by injection, and do not require the use of a toxic curing agent or inconvenient temperature manipulations.

Abstract: The invention relates to the use of polycyclic 2-aminothiazole systems and their physiologically tolerated salts and physiologically functional derivatives for the treatment of obesity. The treatment involves administration of a compound of formula I, in which the radicals have the stated meanings, and of their physiologically tolerated salts and physiologically functional derivatives.

Abstract: The invention involves methods and compositions useful in delivering micronutrients to cells. By formulating the micronutrient in the form of an ester that is convertible to the active form of the micronutrient, one can combine it with a co-ester that inhibits esterases, so that the micronutrient can reach the targeted cells prior to degradation. Both methods and compositions are described.

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: A composition with three hormone components is administered to a mammal to cause the suppression or cessation of the menstruation cycle. Alternatively, it can be administered for treatment of tumors of the mammary gland. The composition contains at least a synthetic estrogen, a biogenetic estrogen, and a gestagen. Alternatively, the composition can include hormones which upon ingestion are metabolized to the above-mentioned hormones.

Abstract: Particles of a substantially water insoluble biologically active substance, such as Cyclosporin, are loaded with a charged glyceryl ester as an electrostatic stabilizer which imparts to the particles a zeta potential and having an active substance:stabilizer weight ratio of 1:1 to 400:1 and an average particle diameter of 1 nanometer to 10 micrometers. Compositions having such particles are found to be useful delivery systems.

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 method of treating disorders involving the urethrogentical tract by administering to pateints in need therof therapeutically effective amounts of the desethyl metabolite of oxybutynin and/or the optically active isomers thereof, which are free from said cardiac side effect of oxybutynin, while maintaining the therapeutic activities of oxybutynin or the optically active isomers thereof.

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: The present invention provides antiviral proteins, peptides and conjugates, as well as methods of obtaining these agents. The antiviral proteins, peptides and conjugates of the present invention can be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the infectivity, replication and cytopathic effects of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.

Abstract: This invention relates to an intravaginal shell or core drug delivery device suitable for administration to female humans or animals comprises testosterone or a testosterone precursor in a polymer matrix, surrounded by a sheath, and is capable of releasing the testosterone or testosterone precursor in a substantially zero-order pattern on a daily basis for at least three weeks. The device is intended to restore circulating testosterone levels to the normal physiol, range or to induce supratherapeutic testosterone levels.

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: Methods are described for treating inflammatory bowel disease in animals, including humans. Specific avian polyclonal antibodies directed to TNF are shown to have a beneficial effect in animal models predictive of human therapy for the treatment of colitis.

Abstract: A hypocholesterolemic composition, for use in reducing serum cholesterol levels in warm-blooded organisms, the composition containing: (a) a phytostanol ester and (b) a tocopherol.

Abstract: The present invention is directed to a pharmaceutical composition including a hydrophobic therapeutic agent having at least one ionizable functional group, and a carrier. The carrier includes an ionizing agent capable of ionizing the functional group, a surfactant, and optionally solubilizers, triglycerides, and neutralizing agents. The invention further relates to a method of preparing such compositions by providing a composition of an ionizable hydrophobic therapeutic agent, an ionizing agent, and a surfactant, and neutralizing a portion of the ionizing agent with a neutralizing agent. The compositions of the invention are particularly suitable for use in oral dosage forms.

Abstract: Acid-labile active compounds are prepared in suppository form, particularly for rectal administration.

Abstract: This invention relates to a drug composition with a controlled drug release rate. The drug composition comprises: a matrix formed of the following ingredients (a) and (b): (a) a biodegradable, biocompatible high-molecular substance and/or polyvalent metal ions or polyvalent metal ion source, and (b) hyaluronic acid or a salt thereof; and a drug incorporated as an ingredient (c) in said matrix. The drug composition has biodegradability and biocompatibility, permits easy control of a release rate of the drug, and can persistently exhibit its pharmacological effect over a long time.

Abstract: The invention relates to solutions containing acidic compositions that have a pH of less than 1, are non-caustic to human tissue and are safe for human ingestion. These compositions may be used as the sole or major component of solutions such as cleansers, pharmaceuticals, food preservatives and disinfectants. The acidic compositions may be used in medical, industrial, military and household applications. The invention also relates methods of administering and using the acidic compositions of the invention.

Abstract: The present invention includes a hot-melt extruded film and method of preparation thereof. The film is made from a precursor composition containing at least a water soluble or water swellable thermoplastic polymer, preferably HPC and/or PEO, and a bioadhesive polymer. The film can also contain a therapeutic agent, preservative, buffering agent, antioxidant, super-disintegrant or absorbent, flavorant, colorant, water insoluble polymer, organic acid, surfactant, film modifier, and/or cross-linking agent. The film does not contain a conventional plasticizer or a material which is generally recognized in the art as a plasticizer for extruded films. The film can be sized and shaped to provide a controlled delivery of a therapeutic agent to the buccal, rectal, uterine, vaginal, abdominal, cranial, ophthalmic, nasal, sinus, or otic cavities. The film can also be used for the treatment of wounds.

Abstract: Methods and compositions are provided for enhancing the bioadhesive properties of polymers used in drug delivery devices. The bioadhesive properties of a polymer are enhanced by incorporating a anhydrideoligome into the polymer to enhance the ability of the polymer to adhere to a tissue surface such as a mucosal membrane. Anhydrideoligomes which enhance the bioadhesive properties of a polymer include water-insoluble anhydrideoligomes such as water-insoluble metal oxides, including oxides of calcium, iron, copper and zinc. The anhydrideoligomes can be incorporated within a wide range of polymers including proteins, polysaccharides and synthetic biocompatible polymers. In one embodiment, metal oxides can be incorporated within polymers used to form or coat drug delivery devices, such as microspheres, which contain a drug or diagnostic agent.

Abstract: Delivery devices capable of delivering one or more active substances by diffusion through plural micropores in the membrane or by osmotic pumping through one or more preformed passageways in the membrane are provided. The device has an about centrally located expandable core completely surrounded by an active substance-containing layer, which is completely surrounded by the membrane. The device is capable of delivering insoluble, slightly soluble, sparingly soluble and very soluble active substances to an environment of use. The preferred delivery rate is zero order. The device can deliver an active substance for a period of about 12-24 hours.

Abstract: Methods and pharmaceutical compositions for using desmethylselegiline. In particular, the present invention provides novel compositions and methods for using desmethylselegiline for selegiline-responsive diseases and conditions. Diseases and conditions responsive to selegiline include those produced by neuronal degeneration or neuronal trauma and those due to immune system dysfunction. Desmethylselegiline is the R-(−) enantiomer of N-methyl-N-(prop-2-ynyl)-2-aminophenylpropane. Claimed compositions include both the R-(−) isomer and mixtures of the R-(−) and S(+) isomers. Pharmaceutically acceptable acid addition salts may also be used. Effective dosages are a daily dose of at least about 0.015 mg/kg of body weight.

Abstract: Pharmaceutical and alimentary compositions containing Acetobacter xylinum as the active ingredient for the treatment of gastroenteral dysmicrobisms, gastroenteral acute and chronic infections and impairments of the gastroenteral functionality.

Abstract: A composition that may take the form of a dietary supplement or of a medicament is disclosed which comprises as active ingredients propionyl L-carnitine and the isoflavone genistein for the therapeutic treatment of osteoporosis and menopause syndrome.

Abstract: To provide a transmucous absorption enhancer comprising a medium-chain fatty acid salts or a bile acid salt and a glycyrrhizic acid salts capable of sustaining the effect of the absorption enhancer and allowing an agent (especially a physiologically active peptide) to be absorbed via a mucosa (especially a large intestine mucosa).

Abstract: This invention pertains to a method that can control, treat, and prevent Diabetes Mellitus. The method includes means of administering a potent product, including mainly the active ingredient Linalool, in any one of several forms, alone or with other additives and catalysts, such as vitamin E to enable the body to handle and control, then correct the complications of Diabetes Mellitus. A modest percentage of users suffering from this disease can be cured completely while the majority of others improve remarkably and experience lower blood glucose and reduce the glycated hemoglobin HbAlc readings to what are medically acceptable and healthy levels. Others, who are vulnerable to the disease due to hereditary factors, or other reasons, can help prevent it. The method works in several ways, including activation of the pancreas and re-establishing the ability of body cells to utilize and handle better and well, the glucose in the blood, and regulate the level of natural insulin in the body.

Abstract: The present invention relates to a synergistic formulation comprising pharmaceutically effective amount of &agr;/&bgr; arteether and a neutralized refined vegetable oil suitable for administration by rectal route, method for the treatment of cerebral and comatose malaria and process for the preparation of the said formulation.

Abstract: The present invention provides a method for eliciting an onset hastened analgesic and anti-inflammatory response and combating nausea in acute migraine attacks. This method comprises administering a pharmaceutical composition comprising more than one active ingredient, wherein said more than one active ingredient consist essentially of: (i) domperidone or an analogue thereof in an amount sufficient to hasten the onset of the analgesic and anti-inflammatory response and to combat nausea in an acute migraine attack, and (ii) a NSAID, a pharmaceutically acceptable salt thereof or a pure (−) or pure (+) optical isomeric form thereof in an analgesically and anti-inflammatory effective amount, wherein said NSAID is selected from the group consisting of proprionic acid derivatives, acetic acid derivatives, fenamic acid derivatives, biphenylcarboxylic acid derivatives and oxicams.

Abstract: The S-isomer of a compound represented by the following formula: and pharmaceutically acceptable salts thereof is disclosed as being useful for treating urinary disorders, including urinary incontinence, and gastrointestinal disorders, including gastrointestinal hyperativity.

Abstract: The present invention provides a method for treating a demyelinating disease in a subject which includes administering to the subject a therapeutically effective amount of a high affinity neuromodulatory Na,K-ATPase so as to treat the demyelinating disease.

Abstract: The present invention is concerned with bioadhesive pharmaceutical compositions comprising a pharmaceutically effective amount of an active ingredient, from 80% to 98.8% (w/w/) pre-gelatinized starch, and from 1% to 10% (w/w) of a hydrophilic matrix forming polymer, characterized in that the composition further comprises from 0.2% to 5% (w/w) alkaliC16-22alkyl fumarate as a lubricant; solid dosage forms such as tablets which are suitable for oral, nasal, rectal and vaginal administration; processes of preparing the compositions and solid dosage forms.

Abstract: A method of delivering one or more therapeutic agents comprising providing a suppository comprising one or more therapeutic agents and a biocompatible carrier medium and shaped to be capable of cooperating with the periurethral musculature to retain the suppository in place in the urethra, inserting the suppository into the urethra, and retaining the suppository within the urethra by the action of the periurethral musculature for a period of time sufficient to permit the therapeutic agent to diffuse substantially into the urethra, the referred suppository comprising a shaft having a first end and a second end and shaped to be capable of cooperating with the action of the periurethral musculature to retain the suppository within the urethra and a substantially ellipsoidal knob extending from the second end of the shaft and sized to prevent insertion into the urethra.

Abstract: A dietary supplement system having a daytime component and a nighttime component is provided, wherein the daytime component comprises at least one thermogenic substance and the nighttime component comprises at least one adrenal support substance.

Abstract: The present invention provides a base for suppository comprising oily or fatty base and polyethlene. The suppository prepared by the use of the base of the present invention has superior heat resistance which should not cause quality deterioration such as deformation and cracks, and shows good release, internal absorbability, safety and like compared to those of the suppositories used thus so far in the applied region.

Abstract: The present invention relates to pharmaceutical compositions and methods for improved solubilization of triglycerides and improved delivery of therapeutic agents. Compositions of the present invention include a triglyceride and a carrier, where the carrier is formed from a combination of at least two surfactants, at least one of which is hydrophilic. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the triglyceride and surfactants. An optional therapeutic agent can be incorporated into the composition, or can be co-administered with the composition. The invention also provides methods of enhancing triglyceride solubility and methods of treatment with therapeutic agents using these compositions.

Abstract: The claimed invention pertains to methods for treating a patient who is at risk for a vascular (e.g., cardiovascular, cerebrovascular) event comprising administering to the patient an effective amount of a lipid-modifying drug. The claimed methods are particularly effective in patients having a lipid profile comprising a low Low Density Lipoprotein and a low High Density Lipoprotein.

Abstract: The invention provides a pharmaceutical composition for rectal or vaginal administration which comprises at least two parts wherein the composition comprises (i) two or more physiologically acceptable substances each in separate parts of the composition which are such that on admixture they react to produce a physiologically acceptable gas; (ii) in at least one part of the composition a polymer stabiliser which is adapted to facilitate the formation of a water-soluble collapsible foam structure; and (iii) in at least one part of the composition a pharmaceutically active substance; an its use in the treatment or prophylaxis of disorders of the intestines, rectum or vagina.

Abstract: The present invention is directed to the transmucosal, transdermal or oral administration of ketamine, either alone or in combination with other pain medications, to manage and treat pain and to reduce drug dependency in a subject.

Abstract: The present invention discloses a composition for dermatological infections by the use of a lytic enzyme in a carrier suitable for topical application to dermal tissues. The method for the treatment of dermatological infections comprises administering a composition comprising effective amount of a therapeutic agent, with the therapeutic agent comprising a lytic enzyme produced by infecting a bacteria with phage specific for that bacteria.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: The use of S(−)sodium 2-(4-isobutylphenyl)propionate (the sodium salt of S(+)-ibuprofen) in pharmaceutical compositions for the treatment of inflammation, pain and pyrexia is described. Preferred compositions comprise S(−)sodium 2-(4-isobutylphenyl)propionate dihydrate. Processes to prepare S(−)sodium 2-(4-isobutyl-phenyl)propionate and its use in a process to prepare S(+) 2-(4-isobutylphenyl)propionic acid of high enantiomeric purity are also described.

Abstract: Compositions and methods for the prophylactic and therapeutic treatment of bacterial infections are disclosed which comprise administering to an individual an effective amount of a composition comprising an effective amount of lytic enzyme and a carrier for delivering the lytic enzyme. This method and composition can be used for the treatment of upper respiratory infections, skin infections, wounds, burns, vaginal infections, eye infections, intestinal disorders and dental problems.

Abstract: A delayed and sustained release composition of an additive and/or toxic agent such as nicotine is delivered systemically in therapeutic amounts while avoiding the peak plasma levels which gives rise to addiction and/or toxic side effects. The composition is delivered for absorption predominantly from the colon.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal C8 to C22 alkyl 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.

Abstract: A first composition for topical application and a second for oral administration, make up a comprehensive program for the treatment and relief of hemorrhoids. The topical application composition contains supplements for healing of hemorrhoids including an agent for the enhancement of the formation of collagen and elastin, an antioxidant having a proanthocyanidin as the active agent in combination with vitamin C, one or more anti-inflammatory agents, and vitamin E. In the preferred embodiment, the composition is made from gotu kola extract, grape seed extract, horse chestnut extract, aloe vera, vitamin C, and vitamin E. A few drops each of Essential Oils of Chamomile and Lavender may be included. The composition may be formulated as an ointment, cream or gel for external application. The components of the composition work synergistically to relieve the pain, discomfort and swelling associated with hemorrhoids while enhancing the connective tissue sheathes surrounding and supporting the veins and capillaries.