Abstract: This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and fiber provides a lower incidence of nausea and vomiting than the conventional tablets. More particularly, the invention comprises an extended release formulation of venlafaxine hydrochloride comprising a therapeutically effective amount of venlafaxine hydrochloride in spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and, optionally, hydroxypropylmethylcellulose coated with a mixture of ethyl cellulose and hydroxypropylmethylcellulose.

Abstract: The present invention describes the use of a combination of an agrochemically active compound and a solid carrier material which surrounds the active compound, to suppress antagonistic interactions in a mixture comprising the active compound surrounded by the carrier material, and at least one further agrochemically active compound. Preferred formulations comprising such a combination include herbicides combined with a carrier material together with a safener and/or a growth regulator. Using the formulations according to the present invention, it is possible to suppress antagonistic interactions between different active compounds.

Abstract: Film-forming compositions are disclosed that can comprise, on a dry solids basis, 25 to 75 percent by weight of certain starch derivatives having a DE less than about 1, 25 to 75% plasticizer, and 0.1 to 15% hydrocolloid gum. The starch derviatives can be chemically modified starches which range in molecular weight from 100,000 to 2,000,000. These starch-based systems can completely replace gelatin in edible film-forming applications such as soft and hard gel capsules.

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 invention pertains to compositions and therapeutic and prophylatic methods for treating/preventing infections in an animal or human by administering a soluble &bgr;-glucan composition comprising &bgr;-glucan molecules having an average molecular weight of at least 1,000,000 daltons, as determined by multi-angle laser light scattering (VHMW-glucan).

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: Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2) Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. This quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.

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 unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.

Abstract: Compositions and methods of using conjugated linoleic acid preparations enriched for the t10,c12 and c9,t11 isomers are disclosed. It is found that preparations of conjugated linoleic acid containing a ratio of t10,c12 to c9,t11 of about greater than 1.2:1 are desirable for a wide variety of nutritional, therapeutic and pharmacologic uses.

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: The present invention is to provide sustained-release microcapsules which contains high amount of a drug, suppresses initial release and shows stable release, and the production method of which comprises adding a physiologically active substance to biodegradable polymer in an organic solvent containing a fat and oil (in particular, vitamin E) and dispersing and emulsifying the mixture.

Abstract: The present invention relates to a chewable soft gelatin capsule and a soft gelatin capsule of the torsional opening type, the capsule having a shell which includes: (A) gelatin (B) one or more plasticizers selected from among (b1)-(b3) below, in a total amount of 100-600 parts by weight based on 100 parts by weight of gelatin; (b1) glycerin (b2) a sugar selected from among D-sorbitol, sucrose, mannitol, fructose, sugar alcohol, and isomerized sugar (b3) a glycol selected from propylene glycol and ethylene glycol, and (C) a water-insoluble cellulose.

Abstract: This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provides a lower incidence of nausea and vomiting than the conventional tablets. More particularly, the invention comprises an extended release formulation of venlafaxine hydrochloride comprising a therapeutically effective amount of venlafaxine hydrochloride in spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and, optionally, hydroxypropylmethylcellulose coated with a mixture of ethyl cellulose and hydroxypropylmethylcellulose.

Abstract: Pharmaceutical compositions comprising a cyclosporin in a novel galenic formulations for oral administration. The compositions typically comprise a cyclosporin, 1,2-propylene glycol, a mixed mono-,di- and tri-glyceride and a hydrophilic surfactant. Further a refined glycerol-transesterified corn oil is provided representing a mixed mono-, di- and tri-glyceride suitable for the novel formulation. Dosage forms include in particular oral dosage forms.

Abstract: Improved oral cyclosporin formulations which have high bioavailability and are capable of admiration in hard capsules are provided. In the subject formations, cyclosporin is delivered in an orally acceptable vehicle comprising at least one alkanol solvent of from 2 to 3 carbon atoms in combination with at least one non-ionic surfactant. The subject formalations may further comprise at least one cosolvent, where cosolvents of interest include fatty acids and diols. The subject formulations find use in immuno-suppressive therapy.

Abstract: The present invention generally relates to safe and stable sunscreen compositions comprising of at least one sunscreen active ingredient in the form of an inert sol-gel microcapsules encapsulating ultraviolet absorbing compounds in any acceptable cosmetic vehicle. The composition according to the present invention can comprise several ultraviolet absorbers that may be encapsulated in the same sol-gel microcapsule or in different capsules. The encapsulation of the ultraviolet absorbers reduces or even prevents the contact between the sunscreen compounds and the human tissue, thus reducing various adverse effects that are associated with the use of sunscreens, such as photoallergy and phototoxicity, and makes the composition safer for use. The encapsulation also reduces or even prevents cross reactivity between the sunscreen compounds and the packaging material and between the sunscreen compounds and any other component present in the composition, thus enhance the compositions stability.

Abstract: Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2). Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. This quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.

Abstract: A softgel-compatible composition containing retinol comprises retinol-impregnated microparticles. The composition may include an optionally thickened silicone oil, or may include an emulsion comprising a silicone oil. Ascorbic acid may be present as ascorbic acid-impregnated microparticles and/or within the emulsion. Such compositions are compatible with softgels, and may also be used in other dispensing containers, such as sachets, tubes, and airless pumps.

Abstract: A novel pharmaceutical combination is described, together with a method of making the same and a method of treating hypertensive patients using the same, wherein (1) the pharmaceutically active antihypertensive agent and citric acid and (2) the pharmaceutically active antikaliuretic agent and a nonionic surfactant are mixed, either together or separately, to form an essentially homogenous combination composition, and only thereafter blending with excipients to form the novel combination composition in solid dosage form.

Abstract: A dietary supplement is provided that comprises creatine combined with ginseng and astragalus and, optionally, glutamine. The dietary supplement enhances the general energy boost and muscular strength increase achieved from the consumption of creatine alone.

Abstract: This invention provides a pharmaceutical composition comprising a mycophenolate salt, the composition being adapted to release mycophenolate in the upper part of the intestinal tract.

Abstract: The present invention relates to a fast-release as well as a prolonged release type of nifedipine pellets and the process for the preparation thereof. The fast-release type of nifedipine pellets comprises a particulate core which is covered by a nifedipine coating layer. The particulate core comprises water-soluble or water-insoluble excipient(s) and a pharmacologically acceptable carrier. The nifedipine coating layer comprises an effective amount of nifedipine dissolved in organic solvent(s). This nifedipine coating layer can further be mixed with a suspension which comprises an adhesive, an emulsifier, and a dispersant. The preferred composition of the fast-release type of nifedipine includes 20-70% of the particulate core, 3-15% of nifedipine, 1-20% of emulsifier, 1-20% of adhesive, and 1-30% of dispersant.

Abstract: A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Abstract: In the formation of capsules having a polyanionic polysaccharide core and a polycationic polysaccharide membrane layer, improved binding of the polycationic polysaccharide is achieved by including polyvalent ions, especially calcium ions, at the membrane forming step.

Abstract: The present invention relates to a composition, particularly adapted to oral administration, substantially free of alkaline-reacting compounds. The composition comprises (a) a core containing an acid-labile benzimidazole active principle, where the core comprises a plurality of nuclei and the active principle mixed together and then compressed together, and where the active principle is not in the form of an alkaline salt; (b) an intermediate layer; and (c) an enteric layer; provided that omeprazole is not the benzimidazole active principle. A process for preparing the composition is also disclosed.

Abstract: The invention provides a novel polyherbal composition useful for treating acute Hepatitis E virus infection including acute liver failure due to HEV infection, healthy Hepatitis B virus carriers who develop superadded hepatitis E virus infection, acute hepatitis B virus infection, and animal hepadna virus, therapeutic effects on hepatitis B virus infection and also used as a hepatoprotective agent, said composition comprising essentially extracts of plants Rheum emodi Wall., Phyllanthus amarus Linn., Eclipta alba Hassk., Andrographis paniculate Nees., and Picrorhiza kurroa Royle ex Benth., and optionally Fumaria officinalis, Tinospora cordifolia Miers., Terminalia chebula Retz., Cichorium intybus Linn., Tephrosea purpurea Linn. and Boerhaavia diffusa Linn.

Abstract: A method for treating or preventing urinary incontinence and other motility disorders involving the urethrogenital tract, by administering to a mammal an effective amount of the R-isomers of 4-diethylamino-2-butynyl cyclohexylphenylglycolate and 4-ethylamino-2-butynyl cyclohexylphenylglycolate and pharmaceutically acceptable salts thereof.

Abstract: Tablet formulations having a structure comprising compacted granulates of a mixture of a medicament and an intra-granular disintegrant, the granulates being compacted together into a tablet with an extra-granular disintegrant and optional extra-granular lubricant and excipients.

Abstract: The invention relates to a method of treating psychotic disorders comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof.

Abstract: A method and preparations for the treatment of vaginal yeast and other yeast infections is provided for the treatment of infections caused by Candida albicans and Cryptococcus neoformans. The method and preparations of the invention can also be used for other yeast and fungal infections including systemic, mucosal and cutaneous caused by Candida and Cryptococcus. The vaginal antiyeast and antifungal preparations include, in addition to suppositories and mouth washes, troches, lotions, creams, tablets and capsules containing gentian preparations as an active ingredient obtained from the plant Radix gentianae Longdancao. For systemic fungal infections gentian preparations from the plant Radix gentianae Longdancao are taken orally in the form of lozenges, tablets, capsules or in solution form for gargling or swallowing.

Abstract: A composition comprising two suspensions: A) an aqueous suspension of microcapsules containing biologically active materials and B) an adhesive suspension of adhesive microspheres. The composition is useful for adhering microencapsulated biologically active material onto an intended substrate.

Abstract: A pharmaceutical formulation comprising an amoxycillin hydrate and an effervescent couple, for example citric acid plus sodium bicarbonate or sodium glycine carbonate, or tartaric acid or malic acid plus sodium carbonate. Potassium equivalents of these sodium salts may be used. The formulations may be free flowing powders or granules, or tablets.

Abstract: A gelatin capsule having adjusted water activity and preserved in a closed system, which contains, packed herein, an additive(s) selected from the group consisting of carboxymethyl cellulose calcium, crosscarmellose sodium, partially gelatinized starch and polyvinyl polypyrrolidone in the proportion of 50 to 150 wt. % of the total quantity of the gelatin of the said capsule.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: A method for preparing a core material containment system which prevents or controls leaching of the core material from the containment system, said method comprising the steps of: (1) providing a shell material having a softening temperature above about 70.degree. F.

Abstract: A pharmaceutical formulation comprising an amoxycillin hydrate and an effervescent couple, for example citric acid plus sodium bicarbonate or sodium glycine carbonate, or tartaric acid or malic acid plus sodium carbonate. Potassium equivalents of these sodium salts may be used. The formulations may be free flowing powders or granules, or tablets.

Abstract: The present invention relates to novel liquid oral suspensions incorporated within a soft gelatin capsule comprised of a bitter or bad-tasting pharmaceutical active (such as antihistamines, decongestants and the like) which is dispersed within an adsorbate comprised of magnesium trisilicate, silicon dioxide or mixture thereof. The adsorbate is dispersed within an aqueous or non-aqueous carrier base and combined with other flavors, sweeteners, emulsifiers and the like. The adsorbate not only taste-masks the active but also insures that is evenly dispersed through the liquid suspension so that a uniform dosage rate is readily achievable. The encapsulation of the adsorbate within a gelatin capsule makes administration easier for children andmore convenient. The capsule also affords the adsorbate suspension greater shelf life.

Abstract: Disclosed are pharmaceutical compositions which have been modified to release pharmaceutically acceptable mycophenolate salts in the upper part of the intestinal tract and methods of treatment using the pharmaceutical compositions.

Abstract: A process is described for preparing microspheres, films and coatings from protein or modified protein in which the protein product is stabilized by carrying out the preparation in the presence of an aqueous solution of at least one .alpha.-hydroxy acid. Preferred .alpha.-hydroxy acids are glycolic acid, lactic acid, .alpha.-hydroxybutyric acid or a mixture of two or more thereof. The microspheres, films and coatings so produced have improved stability in aqueous solution.

Abstract: Process for controlling myiasis in cattle and sheep livestock and compositions for carrying out this process.Composition for topical or parenteral use for controlling myiasis in cattle and sheep, with an effective larvicidal amount of a compound of formula I, in particular Fipronil.

Abstract: Stabilized compositions comprising, in combination with a gas, a fluorinated amphiphilic compound. The compositions are particularly suitable for use in diagnostic applications, including ultrasound. The compositions can take the form of vesicular compositions, such as micelles and liposomes.

Abstract: A dietary supplement comprising a reaction product of sodium bicarbonate and apple cider vinegar which is lyophilized.

Abstract: Lipophilic substances of poor oral bioavailability are mixed with at least one solid fat and phospholipid to obtain a dried solid composition suitable as an oral dosage form. The solid lipid compositions are exemplified for food additives or dietary supplements such as Coenzyme Q10 and for pharmaceuticals such as dexanabinol. The Coenzyme Q10-dry lipid mixtures shows improved drug release in vitro and enhanced oral bioavailability in vivo compared to a commercial CoQ10 formulation. The dexanabinol-dry lipid mixture similarly shows greatly enhanced oral bioavailability compared to known formulations.

Abstract: An improved method for the treatment of central nervous system disorders comprises treating patients with an enteric fluoxetine formulation.

Abstract: Soft gelatin capsules having a capsule shell comprising gelatin, plasticizers and, if desired or required, further auxiliary agents, and a capsule filling containing a solvent including a migrateable solvent such as 1,2-propyleneglycol as a solvent in the capsule filling and in the capsule shell. The manufacture of said capsules is improved, if in the process for making the soft gelatin capsules the gelatin bands are cooled with a liquid, and preferably with water.

Abstract: The present invention relates to a pharmaceutical composition containing cyclosporin. More specifically, the present invention relates to a pharmaceutical composition containing cyclosporin, an oil component, a hydrophilic cosurfactant consisting of propylene carbonate or a mixture of propylene carbonate and polyoxyethylene-polyoxypropylene block copolymer, and a surfactant. The composition of the present invention is characterized in that it can be dissolved in an external phase such as water, artificial gastric juice and intestinal juice, etc. to form a self-emulsion with mild stirring and therefore, by appropriately adjusting the constitutional ratio of each component the diameter of particles in the inner phase of the emulsion thus formed can be readily controlled to 100 nm or below. The composition of the present invention can be formulated into the oral preparations such as soft capsules, hard capsules sealed with gelatin bending at the conjugated portion, oral liquid preparations, etc.

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: This invention provides orally administerable pharmaceutical formulations comprising raloxifene, its ethers or esters, or a pharmaceutically-acceptable salt thereof, in combination with a hydrophilic carrier composition.

Abstract: A method of preventing or alleviating a migraine headache in a patient subject to migraine headaches comprises administering to the patient daily, for an effective period of time, a daily effective amount of a dietary supplementation of serotonin and norepinephrine precursors to increase the level of serotonin and norepinephrine in the patient.