Abstract: The present invention comprises a composition, method of enhancing potency and method of delivering corticosteroids in a vehicle comprising at least two penetration enhancers, and solvents and emulsifiers. The propylene glycol and penetration enhancers are present in ratio to the total of the propylene glycol, penetration enhancers, and solvents and emulsifiers of at least about 0.70.

Abstract: The properties of biologically active compounds, for example drugs and agrochemicals, which contain in their molecular structure one or more functional groups selected from alcohol, ether, phenyl, amino, amido, thiol, carboxylic acid and carboxylic acid ester groups are modified by replacing one or more of these functional groups by a lipophilic group selected from those of the formula: RCOO—, RCONH—, RCOS—, RCH2O—, RCH2NH—, —COOCH2R, —CONHCH2R and —SCH2R, wherein R is a lipophilic moiety selected from cis-8-heptadecenyl, trans-8-heptadecenyl, cis-10-nonadecenyl and trans-10-nonadecenyl.

Abstract: The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid activity sufficient to treat narcotic withdrawal symptoms.

Abstract: This invention generally pertains to the field of psychiatry. In particular, this invention pertains to the discovery that agents capable of inhibiting the binding of cortisol to its receptors can be used in methods for preventing antipsychotic-induced weight gain. Mifepristone, a potent specific glucocorticoid receptor antagonist, can be used in these methods. The invention also provides a kit for preventing AP-induced weight gain in a human including a glucocorticoid receptor antagonist and instructional material teaching the indications, dosage and schedule of administration of the glucocorticoid receptor antagonist.

Abstract: The subject invention concerns a unit dose formulation comprising less than 2.5 mg of prednisolone or an equivalent, equipotent amount of another corticosteroid. One embodiment of a method of the invention concerns once daily administration of the unit dose formulation between midnight and 6 a.m. for the treatment of rheumatoid arthritis.

Abstract: A method for crystallizing a substance, especially an inhalable medicament, comprising the following steps: (a) dissolving said substance in a solvent, to produce a solution of said substance, (b) producing a segmented stream which consists of alternating segments of said solution of the substance and of a transport medium, (c) introducing said segmented stream into the first end of a retention stretch, which retention stretch has a first end and a second end, so that said segmented stream passes from said first end to said second end of said retention stretch, and exits from the second end of the retention stretch, (d) cooling the retention stretch, to thereby bring about crystallization of the substance in the segments of solution, in the segmented stream, as said segmented stream passes through the retention stretch, and (e) separating the crystals of material from the segmented stream as it exits from the second end of the retention stretch.

Abstract: The present invention provides compositions and methods for the solubilization of poorly soluble drugs such as triterpenes like betulinic acid and/its derivatives in pharmaceutically acceptable liquid vehicles that avoid use of potentially toxic solvents that are often used for the solubilization of poorly soluble drugs. In the compositions of this invention the drugs remain physically and chemically stable and can be administered intravascularly without undue toxicity from undissolved drug and/or from the solvent vehicles at a drug dose meant to be effective to exhibit clinically significant anticancer activity.

Abstract: Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer soluble in the liquefied hydrofluoroalkane which is selected from polymers including recurring amide containing structural units, copolymers of amide containing units and carboxylic acid ester units, polyvinylacetate and acrylic acid/methacrylic acid ester copolymers.

Abstract: The invention provides a method of using pregnadienones and pregnadienols represented by the structural formula (I): containing at least one olefinic bond in or on their D-ring for the treatment of hyperlipidemic and hyperglycemic conditions in mammals wherein X═OH or O and the olefinic bonds are at 4(5); 5(6); 16(17); or 17(20) or various combinations, and wherein the compounds contain at lest one olefinic bond in or on their D-ring. The method comprises administering an effective amount of said compounds to recipient mammals.

Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

Abstract: A method for the improved treatment of blood-borne cancers, such as lymphomas, leukemia, and myeloma. The method comprises the oral administration of an effective amount of a topically active corticosteroid to a patient who has undergone hematopoietic cell transplantation. Administration of the TAC controls a graft-versus-leukemia (GVL) reaction that is induced following a hematopoietic cell transplantation, so that a GVHD reaction does not develop, or is reduced in severity. The GVL reaction effects killing of cancerous tumor cells in the blood, mediated by the cells derived from the hematopoietic cell transplantation.

Abstract: The present invention pertains to a unit dose formulation comprising 0.25 to 2 mg of a corticosteroid. This small dose can be used to treat rheumatoid arthritis, especially if adapted to release at least 90% by weight of the corticosteroid, 2 to 8 hours after administration.

Abstract: There is provided a pharmaceutical formulation comprising an aqueous suspension of particulate compound of formula (I) 1

Abstract: Amphiphilic fluorinated block copolymers are disclosed which are useful for increasing the dispersability of particles, preferably drug particles, in a fluorine-containing propellant.

Abstract: The present invention is directed to novel lipid soluble steroid prodrugs, compositions comprising steroid prodrugs, and uses of the same.

Abstract: Described is a process for preparing beclomethsaone dipropionate Freon® clathrate comprising the use of an agent which selectively binds methanol to selectively remove methanol from a mixture of methanol and Freon® 11 containing beclomethasone dipropionate.

Abstract: The use of glucocorticosteroids in methods and formulations for prolonging and/or reactivating local anesthesia or local anesthesia previously induced by a local anesthetic agent, is disclosed.

Abstract: Methods of treating or preventing ophthalmic, otic, and nasal infections and attendant inflammation are described. The methods utilize ophthalmic, otic, and nasal compositions containing a new class of antibiotics (e.g. trovafloxacin). The compositions also contain one or more anti-inflammatory agents (e.g. dexamethasone). The compositions are utilized to treat ophthalmic, otic, and nasal conditions by topically applying the compositions to the affected tissues.

Abstract: A dry powder formulation for treatment of pulmonary conditions, via inhalation, includes an effective amount of formoterol or a salt or solvate thereof, in a dry powder form, an effective amount of fluticasone, in a dry powder form, and an excipient. A method for preparing a physically stable dry powder formulation for inhalation includes the steps of micronizing a first active polar drug, a second active non-polar drug, and a polar excipient. The second non-polar active drug is first blended with the excipient to form an intermediate mixture. The intermediate mixture is then blended with the first active polar drug. The increased separation of the polar drug and polar excipient stabilizes the formulation.

Abstract: The present invention in various embodiments provides methods of treating stroke and conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing hormones that are non-sex hormones is also provided. A method of treating stroke with ent-17&bgr;-estradiol, and a method of synthesis, and compounds produced from the synthesis are provided.

Abstract: A method and compound having betamethasone dipropionate and all-trans-retinoic is disclosed for the treatment of hair loss. The method also includes identifying any underlying conditions causing hair loss and administration of a salve of betamethasone dipropionate and all-trans-retinoic acid to the affected areas.

Abstract: The present invention provides methods of conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the delivery of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing non-sex hormones is also provided.

Abstract: The present invention provides methods of conferring protection on a population of cells associated with ischemia in a subject following an ischemic event, comprising: (a) providing an estrogen compound; and (b) administering the effective amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Novel methods are provided for the intravenous administration of an estrogen compound. Examples of ischemic events treatable according to the invention are cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma. A method of treating ischemic damage utilizing non-sex hormones is also provided.

Abstract: The invention comprises methods for conferring a cytoprotective effect on a population of cells, such as providing a polycyclic phenolic compound in a physiologically acceptable formulation, and administering the formulation in an effective dose to the population of cells.

Abstract: Methods for improving the efficiency of electroporation protocols as well as methods to enhance the permeabilized state, in order to improve the intracellular delivery of therapeutic substances, involve the use of at least one agent which is capable of prolonging the permeability of the cell membranes in the tissue exposed to an electroporation-inducing electrical field.

Abstract: This invention relates to compounds of the formula 1

Abstract: The present invention provides compositions containing corticosteroid compounds as active agents for the treatment of ailments and diseases of the respiratory tract, particularly the lungs, by way of nasal and pulmonary administration. The corticosteroid compounds are present in a dissolved state in the compositions. The compositions can be formulated in a concentrated, essentially non-aqueous form for storage or in a diluted, aqueous-based form for ready delivery. In a preferred embodiment, the corticosteroid composition contains an ethoxylated derivative of vitamin E and/or a polyethylene glycol fatty acid ester as the high-HLB surfactant present in the formulation. The compositions are ideally suited for inhaled delivery with a nebulizer or for nasal delivery.

Abstract: Use of betulinic acid and/or its derivatives for inhibiting and/or preventing angiogenesis is described. Compositions containing betulinic acid derivatives with or without betulinic acid can be used for these purposed.

Abstract: This invention relates to a combination product that consists of individual dosage units of a competitive progesterone antagonist and, in addition, sequentially provided individual dosage units of a compound with gestagenic action, as well as its use for the production of contraceptives based on the inhibition of implantation (receptivity inhibition).

Abstract: A method of reducing hair growth in a mammal includes applying, to an area of skin from which reduced hair growth is desired, a dermatologically acceptable composition containing a suppressor of the metabolic pathway for the conversion of glucose to acetyl-CoA.

Abstract: The invention provides compositions and methods for treatment of narcolepsy or isolated cataplexy. Such methods entail administering a therapeutically effective regime of at least one immunosuppressive agent. The methods are particularly useful for prophylactic and therapeutic treatment of narcolepsy or isolated cataplexy.

Abstract: Angiostatic agents and another IOP lowering compound are combined in ophthalmic compositions to treat glaucoma and ocular hypertension. Methods for treating glaucoma and ocular hypertension are also disclosed.

Abstract: Apoptotic cell death in a fully differentiated, non-dividing cell such as a neuron is caused by an abortive attempt of the cell to re-enter or pass through the mitotic cycle. Therefore, agents which prevent such entry or passage are effective in preventing, or at least delaying, apoptotic cell death and are therefore useful in the treatment of neurodegenerative diseases in general, including stroke, Alzheimer's disease, Parkinson's disease and motor-neuron disease in particular.

Abstract: Methods, compositions, and compounds for modulating the GABA.sub.A receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.

Abstract: A method for preventing tissue damage associated with graft-versus-host disease in a patient having undergone hematopoietic cell transplantation, and host-versus-graft disease in a patient having undergone organ allograft transplantation. The method includes orally administering to the patient a prophylactically effective amount of a topically active corticosteroid, such as beclomethasone dipropionate, for a period of time following hematopoietic cell or organ allograft transplantation, and prior to the presentation of symptoms associated with graft-versus-host disease or host-versus-graft disease. Representative tissues includes tissue of the intestine and liver, while representative tissue damage includes inflammation thereof.

Abstract: The present invention provides a composition for attracting termites containing a steroid derivative of formula I ##STR1## The present invention also provides a method for attracting or controlling termites with the composition.

Abstract: The present invention is directed to novel lipid soluble steroid prodrugs compositions comprising steroid prodrugs, and uses of the same.

Abstract: The use of glucocorticosteroids in methods and formulations for prolonging and/or reactivating local anesthesia or local anesthesia previously induced by a local anesthetic agent, is disclosed.

Abstract: The invention provides a method for the treatment and prevention of urinary incontinence in mammals, e.g., human males and females, especially nonpregnant female mammals, by administering a nitric oxide synthase substrate and/or nitric oxide donor, alone or in combination with an estrogenic agent and/or a progestational substance, with or without supplementation with an alpha-adrenergic agonist, beta-adrenergic receptor blocking agent, cholinergic-receptor blocking compound or a cholinergic-receptor-stimulating drug, as well as pharmaceutical compositions useful in practicing the methods of this invention.

Abstract: The present invention describes, inter alia, novel prodrugs comprising fluorinated amphiphiles, compositions comprising the novel prodrugs, and methods of use of the prodrugs and compositions.

Abstract: Inflammatory dermatoses are controlled and cleared by topical application to the affected areas of the skin of a composition containing both a corticosteroid and a retinoid. The combined therapy is more effective than either active ingredient alone and is particularly effective for chronic dermatoses which are or have become resistant to corticosteroid treatment alone. After clearing has been obtained with once or twice daily applications of the corticosteroid-retinoid composition, usually after several weeks, clearance can be maintained by less frequent application or lower concentrations of the composition or by application of only one of the corticosteroid or retinoid, less potent corticosteroids, or other non-steroidal therapies, depending upon the particular dermatosis being treated.

Abstract: Compositions of angiostatic agents for treating GLC1A glaucoma and methods for their use are disclosed.

Abstract: One or more formulations for treating psoriasis and other skin disorders characterized by redness, itching, flaking, scaling, and plaque-type growth. The formulation includes a carrier component, one or more active ingredient components, and a surfactant component. The carrier preferably includes an alcohol in substantially equal volume with isopropyl myristate. The active ingredient component preferably includes a superpotent or high-potency corticosteroid such as clobetasol propionate, an anti-flaking ingredient such as zinc pyrithione, or a combination of the two. It may also include an anti-fungal compound. The surfactant component preferably includes an alkyl sulfate such as sodium lauryl sulfate. The formulations made by applied topically either in spray form or as a direct-contact liquid.

Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation and in particular to a pharmaceutical aerosol formulation which comprises (a) particulate medicament; (b) at least one sugar; and (c) a fluorocarbon or hydrogen-containing chlorofluorocarbon propellant. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.

Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.

Abstract: The present invention provides an external therapeutic composition for dermatitis comprising an aqueous solution including a therapeutically effective amount of an adrenal cortical steroid, a cyclodextrin, polysaccharides, and a carrier such as water, prepared by clathrating the adrenal cortical steroid in the cyclodextrin using a homomixer to form a clathrate, and adding the clathrate to an aqueous solution of polysaccharides, while being stirred uniformly, to dissolve the clathrate in the aqueous solution, as well as a method for the treatment of dermatitis in a mammalian subject, which comprises administering to said subject a therapeupically effective amount of the external therapeutic composition for dermatitis described above. The external therapeutic composition for dermatitis according to the present invention is extremely safe and can cure dermatitis such as an atopic dermatitis or the like without side effects.

Abstract: The present invention is directed to a method of conferring protection on a population of cells associated with an ischemic focus, in subject, comprising:(a) providing an estrogen compound having insubstantial sex-related activity; and(b) administering an effective cumulative amount of the compound over a course that includes at least one dose within a time that is effectively proximate to the ischemic event, so as to confer protection on the population of cells. Also directed is a method of treating a myocardial infarct in a subject and an ischemic event with the above combination.

Abstract: A pharmaceutical aerosol formulation which comprises particulate medicament, a fluorocarbon of hydrogen-containing chlorofluorocarbon propellant and a surfactant of general formula (I), wherein n is an integer of 1 to 18; m is an integer of 0 to 17; and R.sup.1, R.sup.2 and R.sup.3 are each independently a hydrogen atom or a C.sub.1-4 alkyl group.

Abstract: Apoptotic cell death in a fully differentiated, non-dividing cell such as a neuron is caused by an abortive attempt of the cell to re-enter or pass through the mitotic cycle. Therefore, agents which prevent such entry or passage are effective in preventing, or at least delaying, apoptotic cell death and are therefore useful in the treatment of neurodegenerative diseases in general, including stroke, Alzheimer's disease, Parkinson's disease and motor-neuron disease in particular.

Abstract: The present invention relates to a pharmaceutical composition or preparation which comprises hydroxyl containing steroidal hormones and organic nitrite/nitrate or other nitric oxide donating agents.