Abstract: Aqueous hydrocortisone sodium phosphate and monothioglycerol formulations are disclosed.

Abstract: A ras-farnesyltransferase inhibitor complex formed from a ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, a substituted cyclodextrin, and ethanol is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor, improved dissolution, enhanced stability and is essentially free of particulate matter.

Abstract: A method of treating plant and animal systems and inanimate surfaces for the purposes of controlling plant pests, introducing pesticides and nutrients into plants, mitigating frost damage to plants, increasing crop yields, controlling certain plant diseases, controlling arthropod, bacterial, fungal, mycoplasma, rickettsia, and viral pests of animals and humans, and disinfecting inanimate surfaces. The method utilizes the unique multi-directional dispersion property of the tannate complex of picro ammonium formate and the tannate complex of picro cupric ammonium formate, in aqueous solution, combined with a minor amount of a surfactant sufficient to prevent formation of ammonium picrate, to penetrate plant and animal systems and inanimate surfaces and travelling multidirectionally therein. The method is carried out by introducing a small but effective amount of the tannate complex to the plant or animal system or inanimate surface.

Abstract: A method of modifying protein solubility employs polyionic polymers. These facilitate the solubilization, formulation, purification and refolding of proteins especially incorrectly folded proteins and aggregated proteins. Compositions are described that are suitable for formulating TFPI. The compositions allow preparation of pharmaceutically acceptable compositions of TFPI at concentrations above 0.2 mg/mL and above 10 mg/mL.

Abstract: Provided is a method of formulating hydrophobic pesticides comprising emulsifying an aqueous phase and a water-immiscible phase to form a formulation; wherein the aqueous phase is comprised of water and optionally a freeze/thaw agent, one or more emulsifiers, or combinations thereof, and the water-immiscible phase comprises the hydrophobic pesticide and one or more emulsifiers.

Abstract: The present invention relates to new silver-ion super-complex compositions. More particularly, the present invention describes silver-ion super-complex compositions comprising a silver-thiosulfate ion complex further complex with a primary, secondary or tertiary amine. These silver-ion super-complex compositions are stable in a saline environment and have improved solvent miscibility.

Abstract: The selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A response to serotonin (5-HT) is achieved using analogs of oleamide. Selective potentiation and/or inhibition of the 5-HT2A and/or 5-HT1A leads to a modulation of serotonergic signal transduction of cells having various receptor subtypes. A subset of analogs is identified that inhibits rather than potentiates the 5-HT2A, but not the 5-HT1A, receptor response. These analogs enable the selective modulation of serotonin receptor subtypes and even have opposing effects on the different subtypes. An analysis of the activity of the oleamide analogs discloses that the structural features required for activity are highly selective. In particular, the presence, position, and stereochemistry of the 9-cis double bond is required and even subtle structural variations reduce or eliminate activity.

Abstract: Disclosed is both a method and composition for controlling deleterious organisms, such as insects, nematodes and weeds while maintaining beneficial soil organisms, by applying a compound comprised of a liquid medium and comprising an azide and an amino acid polymer. The azide can be selected from the group consisting of sodium azide and potassium azide or a combination of the two. The composition provides an effective pesticide, without causing significant harm to the environment. The composition may be applied to soil to control a population of a deleterious organism.

Abstract: An acidic aqueous hydrogen peroxide solution is provided with improved disinfectant activity. Concentrated solutions preferably contain up to about 8 wt./wt. % H2O2 and as-used concentrations contain about 0.5% wt./wt. % H2O2. The solution also contains from 0.05 to 8.0 wt./wt. % of at least one phosphorous-based acid, e.g. phosphoric acid and/or a phosphonic acid with from 1 to 5 phosphonic acid groups, and from 0.02 to 5 wt./wt. % of at least one anionic surfactant. The surfactant is selected from C8 to C16 alkyl aryl sulfonic acids, sulfonated C12 to C22 carboxylic acids, C8 to C22 alkyl diphenyl oxide sulfonic acids, naphthalene sulfonic acids, C8 to C22 alkyl sulfonic acids, and alkali metal and ammonium salts thereof, and alkali metal C8 to C18 alkyl sulfates, and mixtures thereof. Most preferably the solution has an emulsifier and/or hydrotrope, e.g. an alkylated sulfonated diphenyl oxide salt, an alkyl aryl polyoxyethylene surfactant, and/or a polyoxyethylene surfactant.

Abstract: A solvent comprising a combination of water and organic solvent(s) capable of dissolving a therapeutically effective amount of medicament(s) not readily soluble in aqueous solvents, said organic solvents including alcohol and glycol, and said medicaments including hydrocortisone.

Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceutical excipient, to the formulation. The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceutical excipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.

Abstract: The invention is directed to therapeutic antioxidant compositions which are enhanced by the stabilized atomic hydrogen; one of the most potent antioxidants. Such products can be used for prophylactic and therapeutic purposes in treatment of cancer, diabetes, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases, skin diseases etc. The products described can be used independently or in combination with other drugs and treatment modalities. The products can also be used as dietetic products to aid in desired weigh loss. The described products can also be used to prevent oxidative and free radical damage to food and oxidation-prone industrial products. The invention also describes the methods to produce and stabilize atomic hydrogen and prepare and use such stabilized/encaged atomic hydrogen enhanced antioxidant compositions.

Abstract: A method of treating plant and animal systems and inanimate surfaces for the purposes of controlling plant pests, introducing pesticides and nutrients into plants, mitigating frost damage to plants, increasing crop yields, controlling certain plant diseases, controlling arthropod, bacterial, fungal, mycoplasma, rickettsia, and viral pests of animals and humans, and disinfecting inanimate surfaces. The method utilizes the unique multi-directional dispersion property of the tannate complex of picro ammonium formate and the tannate complex of picro cupric ammonium formate, in aqueous solution, combined with a minor amount of a surfactant sufficient to prevent formation of ammonium picrate, to penetrate plant and animal systems and inanimate surfaces and travelling multidirectionally therein. The method is carried out by introducing a small but effective amount of the tannate complex to the plant or animal system or inanimate surface.

Abstract: In producing aqueous microbiocidal solutions by oxidation of a water-soluble alkali metal bromide, an intolerable loss of active halogen species has been found to occur during a 10-day period immediately after the product solution has been formed. Surprisingly, this loss has been found to result from an alcohol impurity in the alkali metal bromide used in the process. By eliminating or at least sharply reducing the amount of alcohol impurity in the reaction mixture, products are formed which do not undergo the intolerable loss of active halogen content during the 10-day period.

Abstract: A two-part disinfecting systems, as well as disinfecting compositions and methods for making and using the same. The two-part disinfecting system contains a first part and a second part adapted to be mixed to yield an aqueous disinfecting composition, wherein the first part comprises a chlorite and the second part comprises an acid and an optional oxidizable colorant, and wherein the first part, the second part, or both the first and second parts comprise an alpha olefin sulfonate.

Abstract: The present invention provides a virucide composition and/or sporicide composition having a high virucidal effect and sporicidal effect and being excellent in safety and workability. That is, the present invention provides a virucide composition and/or sporicide composition comprising (a) an inorganic peroxide, (b) tetraacetylethylenediamine and (c) at least one selected from a salt of an alkaline metal salt with an inorganic acid and a salt of an alkaline earth metal with an inorganic acid in a specific ratio.

Abstract: Compounds having thrombin inhibiting activity of the general formula I or II where n is 0.5, 1, 2 and HX is  and HX is optionally substituted once or twice by methyl, ethyl or hydroxyl, and the tautomers and stereoisomers thereof, which compounds have greater thermal stability betaines, and salts of mineral acids or C1-C4-carboxylic acids.

Abstract: Disclosed are biocidal compositions comprising mixtures of formaldehyde-releasing imidazolidines, such as 1,3-dimethylol-5,3-dimethylhydantoin, and 3-isothiazolones stabilized with low levels of copper salts.

Abstract: A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of the formula I wherein n is 0 or 1; R1 is selected from Cl, Br, phenyl, pyridyl or cyano; R2 is aralkyl; R3 is selected from lower alkyl, aryl or substituted aryl or heterocyclo; Z1 is selected from CO, SO2, CO2, or SO2NR5, R5 is selected from hydrogen, lower alkyl or substituted alkyl; and sulfobutylether-7-&bgr;-cyclodextrin or 2-hydroxypropyl-&bgr;-cyclodextrin is provided. The complex has unexpectedly high aqueous solubility of the ras-farnesyltransferase inhibitor and is useful for its intravenous delivery to humans with cancer. Also provided is a method for forming the complex. The ras-farnesyltransferase inhibitors are useful as anti-tumor agents.

Abstract: Stable microbicidal compositions containing a 3-isothiazolone compound, organic oxidants, copper salts and water are disclosed. Also disclosed are methods of stabilizing 3-isothiazolone compositions.

Abstract: A stabilized, injectable pharmaceutical composition for human administration comprises (a) an antineoplastic compound,(b) a solubilizing/dispersing agent, and (c) a stabilizing amount of an anti-oxidant.

Abstract: The present invention pertains to a stabilized pharmaceutical composition which comprises a mixture of (a) a pharmaceutical agent unstable at a pH above about 3.5; and (b) a stabilizing amount of an acidic pharmaceutically acceptable carrier to stabilize the pharmaceutical agent. The acidic pharmaceutically acceptable carrier is a dried premixture of a pharmaceutically acceptable carrier and an aqueous solution of an acid. The stabilized pharmaceutical composition has a pH value of less than about 3.5, and when stored at a temperature of about 50.degree. C. for about 4 weeks at about 27% relative humidity, retains at least about 80% of the pharmaceutical agent. This invention also pertains to sustained-release forms of the stabilized pharmaceutical compositions as well as to novel methods for preparing and using the stabilized pharmaceutical compositions and to stabilized pharmaceutical compositions made by the novel method.

Abstract: For the oral administration of the anti-depressant mirtazapine an aqueous solution or suspension is found which is preferably stabilized by methionine, is thickened, and which has a pH of from 2.5 to 3. By the formulation according to the invention, an undesirable local anaesthetic effect of mirtazapine is avoided.

Abstract: A synegistic system based on a phosphonic acid derivative and on a metabisulphite, for stabilizing ascorbic acid. The invention also relates to compositions, in particular cosmetic and dermatological compositions, containing ascorbic acid and this stabilizing system, and to the use of these compositions in the cosmetics and/or dermatological fields.

Abstract: The long term storage stability of injectable pharmaceutical compositions comprising a taxane or taxoid is improved by incorporating an effective amount of an antioxidant.

Abstract: For the oral administration of the anti-depressant mirtazapine an aqueous solution or suspension is found which is preferably stabilized by methionine, is thickened, and which has a pH of from 2.5 to 3. By the formulation according to the invention, an undesirable local anesthetic effect of mirtazapine is avoided.

Abstract: Disclosed is a stable dilute solution composition of a 3-isothiazolone compound selected from the group consisting of 5-chloro-2-methyl-3-isothiazolone, 2-methyl-3-isothiazolone, 5-chloro-2-ethyl-3-isothiazolone, 2-ethyl-3-isothiazolone, 4,5-dichloro-2-methyl-3-isothiazolone, and mixtures thereof in water having extremely low levels of copper ion and an oxidant.

Abstract: A sprayable or solid biodegradable wax carrier for insect pheromones and a method for constant release rate of the pheromone from the biodegradable wax. A composition comprising a pheromone and paraffin wax formulated as an aqueous emulsion or a solid suitable for application to a surface of a tree or crop for mating disruption of insect pests. Pheromone is released by diffusion or by partitioning from the biodegradable wax carrier or by pheromone exposure due to the biodegradable wax carrier degradation.

Abstract: Methods are provided to prepare a variety of tissues in a pathology-stable form keyed to the use of an aqueous solution of C.sub.2-6 dialdehyde and/or dialdehyde addition products, including the group consisting of glyoxal and/or glutaraldehyde in an amount sufficient to prevent autolysis and other degradative changes in various tissues. The said solution is capable of treating a tissue so as to maintain the tissue in a condition suitable for pathology and/or other experimental observation. The stabilizing solution is also useful to prepare parts or whole animals and plants in an anatomically preserved state for a prolonged period of time, and compositions useful in that method.

Abstract: Solid and liquid pharmaceutical preparations containing cilansetron or its acid addition salts as active substance which include an amount sufficient to stabilize cilansetron against racemization, of a physiologically compatible water-soluble acid additive selected from monobasic or multibasic organic acids having 2 to 12 carbon atoms with a first p.sub.s value between 1.1 and 4.8, acid salts of the aforementioned multibasic organic acids, and acid salts of multibasic mineral acids having a first available pK.sub.s value between 1.5 and 7.5, as well as the use of such acid additives for stabilizing cilansetron against racemization in pharmaceutical preparations.

Abstract: Stable solid forms of preservative and embalming compositions are described which can be prepared by adding a sufficient amount of a chemical or chemicals containing at least one polar group capable of forming hydrogen and Van der Waal bonds with the reactive moieties of the aldehydes and antimicrobial agents in the preservative and embalming compositions. The amount of polar chemical(s) necessary to stabilize the reactive aldehydes and antimicrobial compounds/agents is based on a molar ratio of (i) polar groups in the stabilizing chemicals to (ii) reactive groups in the active preservative ingredient of at least 0.8.

Abstract: Stable microbicidal compositions containing a 3-isothiazolone compound, chlorate or perchlorate salts, copper salts and water are disclosed. Also disclosed are methods of preventing or reducing precipitate formation in 3-isothiazolone compositions.

Abstract: Concentrated aqueous liquid disinfectant compositions which exhibit a blooming effect when diluted in a larger volume of water are provided. The concentrate compositions include non-phenolic constituents to provide a disinfecting effect, and are non pine-oil containing. Working strength dilutions of the concentrated aqueous liquid disinfectant compositions are effective against gram positive type pathogenic bacteria such as Staphylococcus aureus, as well as gram negative type pathogenic bacteria such as Salmonella choleraesuis.

Abstract: An aqueous acidic disinfecting and sterilizing composition for medical instruments, which may include brass, copper, aluminum, stainless steel, plastic and ceramic components. The composition contains hydrogen peroxide, peracetic acid, a corrosion inhibitor system, a surfactant and a stabilizer. These compositions have in use stability and are effective as a disinfectant and/or sterilant either at room or when heated. For other applications, surfactants, sequestering agents and stabilizers may be optional.

Abstract: Compositions are described that are suitable for formulating TFPI. The compositions allow preparation of pharmaceutically acceptable compositions of TFPI at concentrations above 0.2 mg/mL and above 10 mg/mL.

Abstract: An oral composition, particularly a gel, is provided which includes at least 2%, preferably 6% or higher of hydrogen peroxide in a carrier stabilized by a triphenylmethane dye. Particularly useful as the dye are FD&C Blue 1 and FD&C Green 3 at levels ranging from 0.006 to 1 %. Further stability can also be achieved through use of a chelating acid, particularly phosphoric acid.

Abstract: This invention relates to clear aqueous solutions of hydrocortisone which are free of lower alcohols. When applied to the skin, either directly or by wipe, the solution is practically invisible and has a further advantage that the solution will not irritate or dry the skin or give the stinging sensation of an alcohol containing solution. Dissolution of hydrocortisone without alcohol is accomplished by using the anionic surfactant sodium dioctyl sulfosuccinate in mixtures of glycerin, propylene glycol and polyethylene glycol diluted to final volume with water.

Abstract: The present invention provides for a stabilized solution containing a halogen containing compound which is effective as a sterilizing or disinfecting agent, and a stabilizing agent which suppresses the chemical dissociation of the halogen compound such that the sterilizing capability of the solution is maintained for extended periods of time relative to the solution without the stabilizing agent. The halogen containing compound is selected from the group consisting of chlorine dioxide, bromine oxide, bromine chloride, monochloroamine, bromic acid, iodine monochloride, iodine trichloride and iodine monobromide. The stabilizing agent is a compound having at least one accessible sulphur containing group selected from the group consisting of cyclamic acid, dimethyl sulphoxide, glyoxyl sodium bisulphite, potassium sorbate, sodium cyclamate, sodium metabisulphite, sodium oxalate, sodium sulphite, sodium thiosulphate and thioacetamide.

Abstract: Injectable aqueous compositions comprising folic acid and leucovorin and their salts, optionally including benzyl alcohol, sodium chloride and agents for adjusting pH are stabilized and buffered in the range of 6 to 10 by adding a combination of tromethamine and monothioglycerol. Such compositions remain stable for prolonged periods even when exposed to sunlight.

Abstract: Pharmaceutical compositions containing pergolide or a salt thereof stabilized to oxidation by incorporation therewith of a stabilizing agent selected from methionine, cysteine, and cysteine hydrochloride.

Abstract: A method is provided for stabilizing alkylenebisdithiocarbamates, such as 1,2-ethylenebisdithiocarbamates (EBDC), by mixing the EBDC in the presence of water with a hydroxymethane sulfinate (HMS) which degrades to formaldehyde to reduce the content of ethylenethiourea (ETU) in the EBDC. The HMS and sulfate by-product from the formaldehyde formation also act as reducing agents to inhibit further ETU formation by oxidative decomposition of EBDC. The hydroxymethane sulfinate is preferably added in an amount of about 0.1 to 5 weight percent based upon the EBDC, and the aqueous reaction mixture is then preferably dried under vacuum. Co-polymerization agents, such as hydroquinone or melamine, may also be added to further reduce and inhibit ETU content and formation.

Abstract: The present invention relates to formulations containing unsaturated fatty acids for the synthesis of prostaglandins and hydroxy-fatty acids in biological systems and to the use of such formulations for the preparation of medicaments which are suitable for curing prostaglandin deficiencies in humans or animal, for example healing or preventing diseases of the gastro-intestinal tract.

Abstract: This invention relates to an anthralin composition having improved stability. The invention further relates to a method for increasing the stability of anthralin in dermatological compositions by incorporating therein a stability enhancing amount of an acid stable anionic surfactant and a water soluble antioxidant.

Abstract: An aqueous solution of 5-aminosalicylic acid (5-ASA) and a nontoxic alkali, alkali metal or alkaline earth metal salt of 5-aminosalicylic acid having a pH of 3-5 is disclosed. The sole buffer in the solution is that intrinsically formed by 5-aminosalicylic acid and its alkali, alkali metal or alkaline earth metal salt. The solutions preferably also contain an antioxidant and a metal complexing agent. In preferrred practice, the 5-ASA salt is formed in situ by addition of an alkali, alkali metal or alkaline earth metal hydroxide to a solution of 5-ASA. The solution is stable and does not significantly discolor due to 5-ASA decomposition for extended periods of time.

Abstract: Novel catecholamine solutions for physiological uses are provided at a pH in the range of 1.0-5.0, comprising catecholamine, acetylcysteine, chelating agent and buffering agents. The compositions are stabilized from oxidation without the use of sulfites and are preferably administered by inhalation.

Abstract: The invention relates to sunscreen compositions comprising an effective component at least one compound of formula I ##STR1## wherein R.sup.1 is selected from alkyl, alkenyl, alkynyl substituted alkyl, substituted alkenyl, phenyl, substituted phenyl, substituted benzyl, cycloalkyl, cycloalkenyl, substituted cycloalkyl, substituted cycloalkenyl and polymeric groups;R.sup.2 is selected from hydrogen, alkyl and alkoxy; and wherein R.sup.1 and R.sup.2 may form a carbocyclic ring which may be substituted;R.sup.3 is selected from alkyl, sustituted alkyl, alkenyl, substituted alkenyl, alkynyl, phenyl, benzoyl, substituted phenyl, substituted benzyl, substituted benzoyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, alkanyoyl, substituted alkanoyl, polymeric groups, the group OROROR.sup.9 wherein R is a bivalent hydrocarbon radical and R.sup.9 is alkyl, alkenyl, phenyl benzyl, substituted phenyl, substituted benzyl;R.sup.4 is alkyl or alkoxy; n is an integer from 0 to 4; andR.sup.

Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.

Abstract: A one step process providing timed exposure to a substantially constant concentration of hypochlorite disinfectant is described, said process being completed when the hypochlorite is destroyed in an autocatalytic reaction with thiosulfate. The hypochlorite lifetime is precisely controlled by adjusting the initial pH of an alkaline disinfection solution of thiosulfate and hypochlorite, said solution containing a molar ratio of between 0.25 and 0.75 moles of thiosulfate to 1.00 mole of hypochlorite. Subsequently, with gradual evolution of acid and decreasing pH, the acid-dependent autocatalytic oxidation of thiosulfate is accelerated. This consumes the hypochlorite in a brief time interval, terminating the disinfection process. Also included in said alkaline disinfection solution is an appropriate concentration of Na.sub.2 HPO.sub.

Abstract: A novel bisulfite adduct of menadione, the menadione choline bisulfite adduct, a process for its preparation, and its use as an antihemorrhagic agent.

Abstract: An aqueous suspension of pure 5-aminosalicylic acid adapted for rectal administration is rendered storage stable against color formation by storing the suspension in a single dose polyethylene bottle adapted for rectal administration of the suspension, in a substantially oxygen-free atmosphere and in the presence dissolved therein of up to about 0.25% of bisulfite and protecting the suspension from exposure to atmospheric oxygen during storage by sealing the plastic bottle, in a substantially oxygen-free atmosphere, in a plastic pouch having a low oxygen transmission rate.