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: The present invention relates to triglyceride-free pharmaceutical compositions for delivery of hydrophobic therapeutic agents. Compositions of the present invention include a hydrophobic therapeutic agent and a carrier, where the carrier is formed from a combination of a hydrophilic surfactant and a hydrophobic surfactant. Upon dilution with an aqueous solvent, the composition forms a clear, aqueous dispersion of the surfactants containing the therapeutic agent. The invention also provides methods of treatment with hydrophobic therapeutic agents using these compositions.

Abstract: A fragrant potpourri gel mixture is disclosed for dispensing fragrance to the air from a container, with the mixture lacking free liquids and being pourable into or out of the container. The fragrant potpourri gel mixture is prepared by providing an aqueous-based liquid, adding a bittering agent, and combining a coloring agent to form an aqueous-based mixture. An oil-based compound having a volatile fragrance oil component is added to the aqueous-based liquid. An absorbent polymer is mixed in by agitation or stirring to absorb the aqueous-based liquid within a gel mixture and to emulsify the oil-based fragrance component throughout to form a heterogeneous gel mixture having a plurality of micro-droplets of oil fragrance components and air pockets suspended therein. The heterogeneous gel mixture is prepared at room temperatures without heating. The volatile fragrance components of the micro-droplets volatilize from the surfaces of the micro-droplets when exposed to the air.

Abstract: The present invention relates to methods for the extraction of herbs and plant materials. More particularly, the present invention relates to extraction methods for Echinacea. The extraction methods of the present invention provide a higher soluble solids content and a higher level of desired marker compounds, such as alkylamides, than conventional extraction procedures. Thus, the extraction methods of the present invention result in a greater yield at a lower cost from a given amount of starting material.

Abstract: Non-replicatable viral recombinant vectors which are recognizable by muscle cell receptors, and furthermore modified by an insertion nucleic acid coding for a polypeptide sequence to be expressed in said muscle cells, are used to obtain a drug for treating muscle cell diseases or diseases which, by virtue of their location in the body, are accessible to the products of the expression of the above mentioned nucleotide sequence, as secreted by said muscle cells. A method for producing said vectors, vectors such as those described above, and their use in pharmaceutical compositions are also provided.

Abstract: A hypocholesterolemic composition containing: (a) an active ingredient selected from the group consisting of a phytostenol, a phytostenol ester, and mixtures thereof; and (b) a potentiating agent selected from the group consisting of a chitosan, a phytostenol sulfate, a (deoxy)ribonucleic acid, and mixtures thereof.

Abstract: The present invention provides a hard gelatine capsule containing a pharmaceutical composition comprising cyclosporin A in a mixture with a surfactant of HLB value at least 10, substantially free of any oil and when a hydrophilic phase is present, the hydrophilic phase being a polyethylene glycol and/or a lower alkanol provided that any lower alkanol present is present in less than 12% of the total weight of the composition absent the hard gelatine capsule.

Abstract: Essentially non-aqueous compositions suitable for oral administration comprising a biologically active oil, or a biologically active oil or an oil-soluble ingredient as a dispersion in a suitable carrier oil, dispersed in a physiologically acceptable emulsifier or emulsifier mixture having an HLB (hydrophilic/lipophilic balance) value of between 10 and 18 and encapsulated in a capsule material that is soluble in gastric juice, their production and use in the maintenance and/or promotion of health.

Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.

Abstract: The present invention relates to complexes of proanthocyanidin A2 and one or more phospholipids, pharmaceutical compositions containing the complex of proanthocyanidin A2 and one or more phospholipids, and methods of treating or preventing atherosclerosis and myocardial and cerebral infarction in a patient by administering the complex of proanthocyanidin A2 and one or more phospholipids, as well as methods of forming such complexes

Abstract: The use of vanillin as a hypolipidemic—a hypotriglyceridemic pharmaceutical agent over a wide range of concentration in the treatment of diabetes (type-2), cardiovascular disturbances, and obesity. Vanillin is also used as a food additive for preventing the development of such pathological conditions, particularly in young people.

Abstract: The present invention relates to an orally administrable galenic form allowing improved absorption by the transmembrane or paracellular route in the gastrointestinal tract of active ingredients which are hydrophilic or ionizable in physiol. media, comprising at least one such active ingredient, an absorption-promoting agent having an HLB>8, the the absorption-promoting agent consisting of one or more lipid substances chosen from: polysorbates; polyoxyethylene ethers; esters of polyoxyethylene and fatty acids; fatty acids; fatty alcs.; bile acids and their salts with pharmaceutically acceptable cations; esters of C1-C6 alkanol with fatty acids; esters of polyol with fatty acids, the polyol comprising from 2 to 6 hydroxyl functional groups; and polyglycolyzed glycerides; in combination with one or more pharmaceutically acceptable excipients, the pharmaceutical forms comprising captopril being excluded. A controlled-release tablet contained (1) cores contg.

Abstract: The present invention provides a multi-layered soft capsule for effectively eliminating bad breath, and a method for producing the same. The multi-layered soft capsule (10) for eliminating bad breath of the present invention comprises a first soft capsule composed of a first soft capsule layer (1) and a first soft capsule content (3), and a second soft capsule composed of a second soft capsule layer (2) and a second soft capsule content (4), which is contained in the first soft capsule. Both the contents (3) and (4) contain a component having an effect of eliminating bad breath. The multi-layered soft capsule (10) of the present invention is characterized in that the second soft capsule (2) is solved in a stomach.

Abstract: Pharmaceutical compositions of modafinil compounds, and pharmaceutical, non-aqueous compositions of modafinil compounds in organic solvents are disclosed, along with their use in the treatment of diseases.

Abstract: A method of producing a free flowing and compressible liquid/power admixture of an active drug substance, by converting the active substance into a liquisolid system. This is accomplished by introducing by the drug into a non-volatile liquid or a mixture of non-volatile and volatile liquids to from a mixture, selecting at least one solid carrier material and admixing these components to produce a non-adherent, free-flowing and compressible liquid/power mass admixture, the amounts of drug and carrier being selected to optimize flow and compressibility.

Abstract: Particulate composition comprising one or more physiologically active substances and a fish gelatinous protective colloid containing at least 50% by weight of fish gelatin, wherein the fish gelatin is at least partly composed of fish gelatin having a bloom strength of above 100, and wherein the composition is obtainable by a particle forming spraying or double emulsifying method.

Abstract: This invention relates to novel multibinding compounds (agents) that are H1 histamine receptor antagonists and pharmaceutical compositions comprising such compounds. Accordingly, the multibinding compounds and pharmaceutical compositions of this invention are useful in the treatment and prevention of allergic diseases such as rhinitis, urticaria, asthma, and anaphylaxis, and the like.

Abstract: Pharmaceutical composition comprising micro particles having an average diameter ranging from 40 to 150 nm, consisting of one or more lipids, a drug and, optionally, a steric stabilizer, suitable to the transmucosal passage and to the overcoming of the blood-brain barrier and the blood-cerebrospinal fluid barrier, said micro particles being obtained dispersing in an aqueous medium cooled to 2-4° C. an oil/water or a water/oil/water micro emulsion comprising said constituents.

Abstract: A dosage form comprising a gelatin capsule formed with a composite wall and containing a liquid, active agent formulation where the wall comprises a barrier layer formed over the external surface of the gelatin capsule, an expandable layer formed over the barrier layer and a semipermeable layer formed over the expandable layer is described. The dosage forms and methods provide for the conversion of standard gelatin, liquid formulation capsules into controlled, release dosage forms that permit the controlled release of the active agent into the environment of use over time.

Abstract: The present invention provides a cellulose capsule comprising the steps of: i) preparing a mixed solution of pectin and glycerin, ii) adding said mixed solution to solubilized cellulose aqueous solution, iii) adding a small amount of glacial acetic acid, calcium gluconate, sucrose fatty acid ester to said mixture, and iv) standing by adjusting viscosity and forming a capsule.

Abstract: A process for the preparation of a pulverous preparation having a finely divided carotenoid, retinoid or natural colorant is provided, which process comprises the steps of: a) forming a suspension of the active ingredient in a water-immiscible organic solvent optionally containing an antioxidant and/or an oil; b) feeding the suspension of step a) to a heat exchanger; c) heating the suspension to 100-250° C., whereby the residence time in the heat exchanger is less than 5 sec to provide a solution; d) rapidly mixing the solution of step c) with an aqueous solution of a swellable colloid and optionally a stabilizer such that the resulting mixture is at a temperature in the range of 20-100° C.; e) removing the organic solvent; and f) converting the dispersion of step e) into a pulverous preparation; where steps b) to f) are carried out continuously and in sequence.

Abstract: The invention disclosed herein includes a vitamin composition encapsulated in a soft or hard shell capsule, said vitamin composition comprising water soluble vitamin particles suspended in a fill liquid, wherein said water soluble vitamin particles are coated with a material that is substantially insoluble in the fill liquid and the shell of the capsule, but soluble in the gastrointestinal tract of a mammal, and the coated water soluble vitamin particles are of a size that are suitable for encapsulating as a suspension in said capsule. The invention also includes a process for manufacturing the same. Vitamin containing capsules according to this invention are discoloration-resistant.

Abstract: This invention provides composition comprising a cyclosporin and a carrier medium.

Abstract: A dry powder layering process for preparing pharmaceutical compositions of the leukotriene antagonist zafirlukast. The process forms coated beads suitable for sprinkling on to food and drink.

Abstract: The present invention provides oral formulations of Sulodexide for the treatment of diabetic nephropathy in patients with both insulin dependent and non-insulin dependent diabetes mellitus. Oral formulations containing doses adapted for administration to obtain a reduction in albumin excretion in patients with both micro and macro albuminuria and to produce lasting improvement in albumin excretion rate are provided. Methods of treating diabetic nephropathy using these formulations are also provided.

Abstract: A palatable oral liquid pharmaceutical composition of benzoxazinone compounds useful as HIV reverse transcriptase inhibitors comprising the benzoxazinone active ingredient in a liquid vehicle comprising a vegetable oil selected from olive oil, peanut oil, soybean oil, corn oil, safflower oil, sunflower oil, canola oil or walnut oil. Other formulating agents such as sweetening agents, lecithin suspending agents, etc. may be optionally added.

Abstract: Oral pharmaceutical formulation comprising granules having an inert core coated with a layer, comprising a 2-[[(2-pyridinyl)methyl]sulfinyl]benzimidazole having anti-ulcer activity, a disintegrant and a surfactant in a matrix of a melt coating substance essentially consisting of one or more esters of glycerol and fatty acids, a separating layer and an enteric coating layer, and a process for the preparation of such formulation using a melt coating technique for the preparation of the benzimidazole containing layer.

Abstract: Medicaments in the form of soft gelatin capsules contain paroxetin anhydrate or pharmaceutically acceptable salts thereof together with lipophilic carriers, namely silicone oils.

Abstract: A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group 3 soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated dried to form the desired soya extract.

Abstract: Flavored Gelatin Capsule and Method of Manufacture A flavored gelatin capsule and the method of manufacture of the flavored capsule is provided. The capsule may comprise (a) from about 10 to about 70 parts by weight of gelatin; (b) from about 10 to about 35 parts by weight of a suitable polyol, such as glycerol; (c) from about 8 parts by weight of water; and (c) various parts by weight of particular water soluble flavorings. The contents of the capsule may also be flavored. The composition is particularly useful in improving the palatability of fish oil medicinals.

Abstract: The invention disclosed herein is a process for increasing the achievable concentration of a pharmaceutically active ingredient relative to fill composition viscosity for dosage units. The process is particularly useful in the preparation of soft gelatin capsules containing ibuprofen, naproxen, indomethacin, and acetaminophen, as the pharmaceutically active ingredient. As a result of the process, lesser quantities of composition ingredients other than the pharmaceutically active ingredient are needed to accomplish the same therapeutically effective dosage, thereby significantly increasing the concentration of the pharmaceutically active ingredient resulting in either a reduction in overall fill volume and dosage unit size or an increase in concentration of pharmaceutically active ingredient per dosage form.

Abstract: Novel forms of sustained-release microgranules (LP) containing diltiazem are disclosed. The microgranules consist of a neutral granular carrier coated with an active layer including diltiazem or a pharmaceutically acceptable salt thereof as the active principle, a surfactant and a binder, and an outer layer providing sustained release of the active principle (layer LP).

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: A pharmaceutically acceptable solution with a medicament suitable for filling a soft gelatin capsule is made from a solvent. The solvent contains a polymer, such as polyethylene glycol, and an acid salt of a compound having 3 or more carbon atoms, and a salt such as sodium propionate. The solvent may optionally contain a cosolvent, such as dimethyl isosorbide. The medicament may preferably comprise an analgesic such as aspirin or naproxen.

Abstract: Disclosed are multibinding compounds which are antibiotics effective against bacterial infections, in particular, Gram-negative bacterial infections. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a polymyxin, circulin or octapeptin antibiotic or other suitable compound which binds to the LPS present in bacteria, in particular, Gram-negative bacteria. The multibinding compounds of this invention are useful for the prophylaxis and treatment of various bacterial infections caused by bacteria.

Abstract: The present invention relates to a disposable dispensing apparatus which provides optimal therapeutic support to humans and other animals by conveniently supplying a complex dosing regimen requiring simultaneous administration of storage-incompatible or unevenly dosed components in a shelf stable user-friendly format. The present invention is particularly useful for humans with special therapeutic needs, such as pregnant, lactating and/or menopausal women.

Abstract: This invention relates to novel dosage formulations for nutritional compositions comprising fatty acids derived from both plant and animal sources and methods for minimizing unpleasant taste, regurgitation, gastroesophageal reflux, dyspepsia, nausea, or difficulty in swallowing or ingesting nutritional agents. The nutritional compositions are intended for use by pregnant or lactating women.

Abstract: The present invention is directed to a semi-solid formulation comprising a lipid-regulating agent. Said formulation is prepared by solubilizing said lipid-regulating agent in one or more liquid components to form a clear liquid solution, then solidifying said solution by adding one or more solid or semi-solid components to said solution to form a semi-solid formulation. Said formulation can melt or dissolve upon mixing with a bulk aqueous medium. The resulting formulation results in an increase in drug solubility and oral bioavailability, and an improved dissolution rate.

Abstract: The present invention is directed to a process for preparing a formulation comprising a lipid-regulating agent dissolved in a supercritical fluid, spraying the solution through a nozzle to form small particles of the lipid-regulating agent, forming a suspension of the particles of said lipid-regulating agent in a liquid, and collecting the particles.

Abstract: A thixatropic gelatin carrier composition which is used as a vehicle in the manufacture of soft or hard gelatin capsule. The composition comprises from about 84% to 95% of a vegetable oil, from about 1% to 9% of a viscosity modifier and from about 1% to 15% of a surface active agent. When the carrier composition is stirred it becomes fluid and active solids are dispersed in the carrier during stirring. When the stirring is stopped, the carrier becomes a semi-solid and maintains the active solids in a stable uniform dispersion. Up to about 50% by weight of active solids can be dispersed in the carrier composition and the active solids can include vitamins, pharmaceuticals or nutriceuticals or combinations thereof.

Abstract: The present invention relates to novel, liquid and semi-solid pharmaceutical compositions which can be administered in liquid form or can be used for preparing capsules containing such pharmaceutical compositions. Also provided are methods of using and processes for preparing the pharmaceutical compositions of the present invention.

Abstract: The present invention is directed to multibinding compounds which are &bgr;2 adrenergic receptor agonists and are therefore useful in the treatment and prevention of respiratory diseases such asthma, bronchitis, and the like. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Method and apparatus for recovering non-solvent fills from a gelatin-containing material by adding the gelatin-containing material to a suitable solvent to form a mixture including a solvent phase and a phase containing said non-solvent fill and then separating the solvent phase from the phase containing said non-solvent fill, followed by recovering the non-solvent fill.

Abstract: A pharmaceutical composition has a blend of at least first and second components and a medicament in a sufficient amount to be therapeutic where the first component is hydroxypropylcellulose (HPC) and the second component is at least one other polymer selected from the group consisting of methylcellulose (MC), ethylhydroxyethylcellulose (EHEC), hydroxyethylmethylcellulose (HEMC), hydrophobically modified hydroxyethylcellulose (HMHEC), hydrophobically modified ethylhydroxyethylcellulose (HMEHEC), carboxymethylhydroxyethylcellulose (CMHEC), carboxymethyl hydrophobically modified hydroxyethylcellulose (CMHMHEC), guar, pectin, carrageenan, agar, algin, gellan gum, acacia, starch and modified starches, co-polymers of carboxyvinyl monomers, co-polymers of acrylate or methacrylate monomers, mono- and co-polymers of oxyethylene and oxypropylene and mixtures thereof and a medicament in a sufficient amount to be therapeutic, with the proviso that low-substituted hydroxypropylcellulose (L-HPC) is excluded from said firs

Abstract: A method is provided for preparing shells, concentric shells or porous, homogenous gels from alkali borate glass particles at low temperatures (i.e. room temperature or less than above 100° C.). The alkali borate glass particles contain one or more cations such as aluminum which react with an aqueous solution containing an anion such as hydroxide to form an aqueous insoluble material having a solubility limit of less than about 0.01 wt. percent. The resulting shells or gels may be used in many different applications such as a filler in resins, as filters, precursors for nano-sized powders, as thin surface films or catalyst support media. The resulting shells or gels may also have a chemotherapeutic drug added thereto, following which the resulting product is administered to a mammal and the insoluble material is dissolved form the product in vivo through administration of chelating agent.

Abstract: The present invention provides a process for encapsulating a shear sensitive fill mass which contains a pharmaceutical active agent or nutrient, characterized in that said fill mass is heated and subsequently cooled, prior to the encapsulation. The invention also provides capsules comprising shear sensitive fill material obtained by the said process which have a high and constant dissolution rate.

Abstract: This invention provides novel formulations for N-[4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)ylcarbonyl)-3-chlorophenyl]-5-fluoro-2-methyl-benzamide, or a pharmaceutically acceptable salt thereof, and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more pharmaceutically acceptable preservatives or antioxidants

Abstract: A pharmaceutical dosage form particularly suitable for the administration of active principles in multiple therapies is disclosed. The pharmaceutical dosage form is a double capsule where in an internal capsule is placed inside an external one. Each internal and external capsule includes one or more active principles. A double capsule according to the invention is preferably used in triple or quadruple therapies against the microorganisms Helicobacter Pylori. Advantages of this pharmaceutical dosage form consist in providing a simple posology for administration of two and more active principles, allowing the active principles to activate at the right intervals of time and in the preestablished quantities, and preventing interactions between active principles.

Abstract: A method of increasing glutathione levels in mammalian cells comprising administering an oral bolus of encapsulated pharmaceutically stabilized glutathione in a rapidly dissolving formulation to a mammal on an empty stomach. Pharmaceutical formulations including glutathione are also disclosed.

Abstract: A composition and method are provided for the treatment of symptoms associated with reduced estrogen production, such as occurs in perimenopausal and menopausal women, wherein the composition contains at least one phytoestrogen containing food, herb or extract thereof, and at least four herbs or extracts which are effective at treating conventional menopausal symptoms.