Abstract: Oral dosage forms are provided for the administration of a bisphosphonic acid compound in the prevention and treatment of conditions involving calcium or phosphate metabolism, i.e., conditions associated with bone resorption such as osteoporosis, Paget's disease, periprosthetic bone loss, osteolysis, malignant hypercalcemia, metastatic bone disease, multiple myeloma, and periodontal disease. The dosage forms are either enterically coated capsules housing the drug in a liquid or semi-solid carrier, or enterically coated osmotically activated drug delivery devices.

Abstract: It has been discovered that certain phosphoinositides demonstrate antibacterial activity. Particularly, these phosphoinositides have been discovered to prevent the adhesion of H. influenzae onto the nasopharyngeal cells of mammals, and, in particular, humans. Phosphoinositides useful with the present invention have the following formula: wherein R1 and R2 are selected from the group consisting of hydrogen and monounsaturated and saturated fatty acids having a carbon chain length of C6 to C20 and R1 and R2 can be the same or different; and R3 to R7 are selected from the group consisting of hydrogen or a phosphate moiety with at least two of R3 to R7 being a phosphate moiety; and hydrates and pharmaceutically acceptable salts thereof.

Abstract: A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt.

Abstract: A tablet coating comprising gellan gum is disclosed along with a process which comprises admixing gellan gum and water under effective shear conditions to prepare an aqueous gellan gum coating composition thereof whereby the aqueous gellan gum coating composition is applied in an adherent fashion to a placebo or a tablet containing a pharmaceutical to form a gellan gum coated placebo or gellan gum coated active drug.

Abstract: Cosmetic or pharmaceutical formulations such as (a) anhydrous cosmetic stick formulations and (b) anhydrous aerosol spray formulations, comprising an organic dispersion medium having particles dispersed therein, which particles are preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, modified starch, and optionally a hydrocolloid gum such as maltodextrin.

Abstract: Adhesive material from the fimbriae (esp. Type 1) of bacteria or synthetic analogues or fragments thereof is combined with a drug to provide for attachment to the gut of a mammal, thereby prolonging the transit time of the drug through the gut. The 28 kDa polypeptide from E. coli Type 1 fimbriae is the preferred adhesive material (“adhesin”). The drug is presented in a carrier such as albumin, a polylactide/glycolide copolymer or alginate microcapsules. The adhesin may be incorporated in the carrier during preparation thereof, adsorbed onto the carrier after preparation, or covalently linked thereto, for example with carbodiimide.

Abstract: A composition and method of fabrication are presented with which nanoparticles may be used as a tool to deliver drugs to a specific target within or on a mammalian body Specifically, by using stabilizers other than Dextran 70.000 during the polymerization process, according to the present invention, surfactants, which were deemed necessary coating material in the prior art, are no longer required. This is a significant simplification of the fabrication procedure. Many substances are useful as stabilizers, but the preferred stabilizers comprise Dextran 12.000 or polysorbate 85. In the present invention a drug is either incorporated into or adsorbed onto the stabilized nanoparticles. This drug/nanoparticle complex is then administered to the organism on any route such as by oral application, injection or inhalation, whereupon the drug exerts its effect at the desired site of pharmacological action.

Abstract: The present invention is directed to the encapsulation of long chain alcohols, C20-C36, in various materials including polymers and waxes. Through the proper selection of the polymer the encapsulated long chain alcohol can be advantageously added to foods such as margarines, salad dressings and the like.

Abstract: Topical gelled compositions comprising an optional drug dispersed within a polymer matrix, methods of producing the same and treatments with the complex.

Abstract: The present invention is concerned with novel pharmaceutical compositions of lipid lowering agents which can be administered to a mammal suffering from hyperlipidemia, obesitas or atherosclerosis, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising a lipid lowering agent and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.

Abstract: Topical gelled compositions comprising an optional drug dispersed within a polymer matrix, methods of producing the same and treatments with the complex.

Abstract: A rapidly dispersible powder having use as a laxative and fiber supplement, comprising psyllium particles coated with gum arabic. The present invention also includes a method for making the powder that includes providing an effective quantity of gum arabic to a fluidized bed having the psyllium particles to make the rapidly dispersible powder. The present invention further includes a method for making a constipation treatment and a treatment for fiber supplementation.

Abstract: The present invention pertains to a sustained release drug delivery system which comprises a core of active ingredient, an enteric coating, a second coating of active ingredient and lastly a readily gastric-soluble protective coating. In another embodiment, the sustained release drug delivery system comprises a core of active ingredient, an enteric coating; a second coating of active ingredient; a second enteric coating and a third coating of active ingredient The sustained release dosage form of this invention is useful for pharmaceutically active ingredients that have limited aqueous solubility, especially phenytoin sodium, and other pH dependent soluble drugs.

Abstract: A pharmaceutical preparation in the form of a coated capsule which can release contents of a capsule at a lower part of the digestive tract comprising (a) a hard capsule containing at least an acidic substance, (b) a polymer film soluble at low pH which is formed on a surface of said hard capsule, and (c) an enteric coating film which is formed on a surface of said polymer film soluble at low pH. According to the pharmaceutical preparation of the present invention, any kind of a medicament can be delivered to any desired site between the upper part of the small intestine and the lower part of the large intestine in the digestive tract by controlling the amount of polymer(s) used for the polymer film soluble at low pH and/or by selecting the kind of the polymer film soluble at low pH and/or the acidic substance without any complicated requirements for each medicament.

Abstract: A process for the preparation of a controlled release system, comprising forming of an aqueous two-phase system form at least two water soluble polymers which are incompatible in solution, at least one of these polymers being cross-linkable, the cross-linkable polymer phase being emulsified in the other polymer phase; adding at least one relesable compound which is soluble in the cross-linked polymer phase in the aqueous solution, allowing the releasable compound to diffuse in the cross linkable polymer phase; cross-linking the cross-linkable polymer before or after the releasable compound is added, preferably to a degree that the pores in the cross-liked structure are substantially smaller than the particle size of the releasable compound; and separating the cross-linked structures enclosing the release able compound from the other phase. Further, the invention relates to microspheres, at least 80 wt.

Abstract: This invention in general relates to novel pharmaceutical compositions for acid labile substances as well as for methods of making such. Specifically, the invention provides a pharmaceutical composition comprising about 1 to 75% by weight acid labile compound, up to about 5% by weight disintegrant, at least one protector coat layer used to separate and protect the acid labile substance from acid reacting groups and gastric juice, and at least one enteric coat layer which surrounds the protector coating layer and ensures delivery of over 80% the acid labile substance to the small intestine.

Abstract: Preparation of a stable aqueous dispersion, or a stable water-dispersible dry powder, of xanthophylls, which comprises a) preparing a molecularly dispersed solution of at least one xanthophyll, with or without an emulsifier and/or an edible oil, in a water-miscible organic solvent, or a mixture of water and a water-miscible organic solvent, at above 30° C., b) mixing this solution with an aqueous solution of a mixture of protective colloids, b1) in which the mixture comprises at least one low-molecular-weight protective colloid component and at least one high-molecular-weight protective colloid component, whose mean molecular weights differ by at least 10,000, b2) the solvent component being transferred to the aqueous phase and the hydrophobic phase of the xanthophyll being formed as a nanodispersed phase c) and if appropriate, to prepare a water-dispersible dry powder, freeing the resulting dispersion from the solvent and the water and drying it in the presence or absence of a coating material.

Abstract: A non-toxic, edible, enteric film coating, dry powder composition for use in making an aqueous enteric suspension which may be used in coating pharmaceutical tablets comprises a) an acrylic resin, said resin comprising i) from 20 to 85 percent by weight of at least one alkyl acrylate or alkyl methacrylate moiety, ii) from 80 to 15 percent by weight of at least one vinyl or vinylidene moiety having a carboxylic acid group capable of salt formation, and iii) from 0 to 30 percent by weight of at least one other vinyl or vinylidene moiety copolymerizable with i) and ii), b) an alkalizing agent capable of reacting with the acrylic resin such that, after reaction, 0.1 to 10 mole percent of the acidic groups in 1a-ii) are present in the salt form, and c) a detacktifier.

Abstract: The present invention relates to a microgranule prepared by using an alkali compound as a stabilizer for a 5-pyrrolyl-2-pyridylmethylsulfinylbenzimidazole derivative having the following formula (1), which is a very effective antiulcerative but highly unstable under acidic conditions, and by using a water-soluble polymer as a binding agent. in which X, R1, R2, R3, R4 and R5 are defined as described in the specification.

Abstract: A composition and method for the control of appetite having food grade nutrients as the active ingredients, and a pharmaceutically acceptable delivery agent, formulated so that the active ingredient is released predominantly in the ileum. The active ingredient may include sugars, fatty acids, polypeptides, and amino acids. The delivery agent may be a pH sensitive coating, a cellulosic polymer coating or a diazotized polymer. The composition may be formulated into pellets of between 1 and 3 mm with a density of around 1.0. The composition may be administered with a liquid as a slurry, or it may be administered in a tablet form. The composition may be used in conjunction with any weight loss or weight maintenance program.

Abstract: The present invention relates to a process for producing a spherical particle comprising an aggregate of particles containing at least 95% of a water-soluble single substance having a viscosity of 10 mPa.

Abstract: The invention provides a granular product useful as a pharmaceutical carrier which can be used for the preparation of pharmaceutical compositions that are capable of rapid suspension in water or aqueous media including saliva. The compositions may be used by addition to a glass of water with stirring or taken directly in the mouth. The granular product may be prepared by a process which comprises subjecting a mixture of a thickening agent and a disintegrating agent to wet granulation with an aqueous medium as wetting agent or dry granulation and preparing the pharmaceutical composition from the granular product and the pharmaceutically active ingredient. A water-soluble inert excipient, which may be a sugar, may be mixed with the granular product prior to mixing with the pharmaceutically active ingredient.

Abstract: A process for stabilizing a sensitive substance; (a) plating a sensitive substance onto a solid carrier under a controlled atmosphere to reduce loss of the sensitive substance; (b) encapsulating the plated material under controlled atmosphere and airflow to reduce volatilization during the process and stabilize the sensitive substance.

Abstract: A controlled release analgesic dosage form comprising: a core comprising an analgesic and binding agent; and a coating comprising an enteric polymer, a water insoluble second polymer and a lubricant.

Abstract: The invention provides a drug delivery composition for colonic delivery comprising a polar drug, an absorption promoter which (a) comprises a mixture of a fatty acid having 6 to 16 carbon atoms or a salt thereof and a dispersing agent, or (b) comprises a mixture of mono/diglycerides of medium chain fatty acids and a dispersing agent, and means adapted to release the polar drug and absorption promoter in the colon following oral administration. A preferred fatty acid is capric acid or a salt thereof. Colon specific delivery can be achieved by providing the composition in a capsule, tablet or pellet which is coated with a material which dissolves in the small intestine or is degraded by the conditions in the colon.

Abstract: Tissue and organ repair, healing and augmentation are enhanced by administering pharmaceutically acceptable group IIIa element-containing compounds in amounts sufficient to provide therapeutic levels of the elements. Group IIIa element-containing compounds mimic the beneficial biological effects of endogenous growth factors to induce cells responsible for repair, healing and augmentation of tissues and organs. Group IIIa element-containing compounds are suitable for a variety of applications such as wound healing, bone fracture repair, treatment of dermatologic conditions and successful bonding of implanted tissue grafts and prostheses.

Abstract: This invention relates to stabilized nanoparticles which may be filtered under sterile conditions, comprising at least one hydrophobic, water-insoluble and non-water-dispersible polymer or copolymer (and optionally an active principle) which is emulsified in an aqueous solution or suspension comprising a phospholipid and a bile salt.

Abstract: A novel method of delivering drugs and diagnostics across the blood-brain barrier or blood-nerve barrier is disclosed. Drugs or diagnostic agents are incorporated into nanoparticles which have been fabricated in conventional ways. These nanoparticles are then coated with additional surfactant and given to the body of animals or humans. This allows drugs or diagnostic agents to cross the blood-brain barrier (bbb) to achieve one or more of the following benefits: (1) reducing the dose of a therapeutic drug or diagnostic agent which, when given peripherally, maintains the biological or diagnostic potency in the nervous system, (2) allowing drugs that normally do not cross the bbb to penetrate into the nervous system, and (3) reducing the peripheral side effects by increasing the relative amount of the drug reaching the brain.

Abstract: A microcapsule having a core, a shell and seeds fully or partially embedded in said shell. The core and seeds are active substances which preferably function as a leavening agent. The shell is composed of either a water soluble or meltable natural polymer, including vegetable waxes. When the shell is ruptured, the active substances will react with each other and the dough mixture thereby producing a leavening effect and/or dough conditioning effect in baked goods.

Abstract: A composition, comprising (a) microcrystalline cellulose; and (b) a compressibility augmenting agent which (i) physically restricts the proximity of the interface between adjacent cellulose surfaces; or (ii) inhibits interactions between adjacent cellulose surfaces; or (iii) accomplishes both (i) and (ii) above, is disclosed. The composition is in the form of agglomerated particles of microcrystalline cellulose and the compressibility augmenting agent in intimate association with each other.

Abstract: A process for the administration of a flowable solid, semisolid, or liquid medium exhibiting a controlled release of at least one active substance to plants by means of injection using needle-free, pressure-actuated devices is characterized in that the medium comprises active substance-containing microparticles of a maximum size of 100 .mu.m including the following components:a) 0.5-70%-wt. of at least one active substance,b) 10-70%-wt. of at least one biodegradable polymer,c) up to 20%-wt. of formulation adjuvants.

Abstract: A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from about 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide.

Abstract: A stable dry powder skin care powder having prolonged and controlled release properties, useful as baby powders, body talcs, deodorizing powders, OTC eczema preparations, foot powders, anti-fungal powders, etc. The dry powder is preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, starch and maltodextrin. The particle is designed so that activity of, e.g., an anti-inflammatory agent such as Dragosantol.RTM. can be specifically triggered by skin conditions, such as moisture, for optimal timing of delivery.

Abstract: Solid, fibrous bioabsorbable hemostatic compositions containing a bioabsorbable polymer and a hemostatic compound, methods for making the hemostatic compositions, and methods for using the hemostatic compositions are disclosed.

Abstract: A method of controlling the particle size and particle size distribution of an aqueous emulsion having a non-aqueous disperse phase during the production thereof, in which the production of the emulsion is carried out in the presence of a dispersion of a templating agent, such as a polymer latex, and surfactantParticle size and particle size distribution of the dispersion is controlled by selecting the templating agent and surfactant such as to cause deposition of the disperse phase on particles of the dispersed templating agent, such that the particle size distribution of the templating agent provides a template for the particle size distribution of the final emulsion.

Abstract: A composition comprising a mononucleate solid crop protection particle coated with a water-insoluble coating material has a diameter in the range of 0.5 to 50.mu.. This composition is made by a process which results in substantial non-agglomeration of the coated particles. In a particular embodiment, a crop protection composition comprises a mononucleate solid crop protection particle coated with either wood rosin, rosin derivatives, waxes, fatty derivatives, sterols, long-chain sterol esters and sulfur. Alternatively, the coating material may be a water-insoluble synthetic latex polymer. The composition may be used in a mixture which also includes a crop protection chemical partner comprising a solid particle. The partner ordinarily degrades the solid crop protection particle when stored or aged together as a solid particle mixture. However, when the composition solid particle is coated, this degradation is prevented.

Abstract: Two or more hydrophilic polymers that are not soluble in each other at a particular concentration and temperature, but which have a positive spreading coefficient in solution, are used to form multi-layered polymeric microspheres. The multi-layer microspheres produced by the method are distinguished by extremely uniform dimensioned polymer layers and actual incorporation of a substance to be delivered into the polymer layers. In the preferred embodiment of the method, two polymers are dissolved in an aqueous solvent, the substance to be incorporated is dispersed or dissolved in the polymer solution, the mixture is suspended in an organic solvent or polymer/water mixture and stirred, and the solvent is slowly evaporated, creating microspheres with an inner core formed by one polymer and an outer layer formed by the second polymer.

Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.

Abstract: A multiple unit oral pharmaceutical dosage form having a plurality of pellets in a water soluble capsule or in a tablet compressed from the pellets, wherein each pellet contains (a) a substantially inert core, (b) an active ingredient layer over the inert core, and containing (i) a pharmacologically active particulate active ingredient, (ii) a nonembedding amount of a binder for adhering the active ingredient over the inert core, and optionally (iii) a pharmaceutically acceptable, inert adjuvant, such as colloidal silica, and (c) a coating over the active ingredient layer for retarding the release of the active ingredient from the active ingredient layer into an aqueous body fluid solvent in situ, the nonembedding amount of the binder is suitably from about 1% wt. to about 10% wt.

Abstract: The use of complex coacervates of two or more biopolymer materials, preferably at least one of these being gelatin, as a fat-replacing ingredient. The complex coacervates may be used in foods and cosmetics and preferably are of substantially spherical or elliptical shape and have an average D.sub.3,2 particle size, of from 0.2 to 100 microns.

Abstract: The object of the present invention is to obtain a targeted and controlled release of drugs, the pharmacological action and absorption of which takes place in the intestine and in particular in the ileum and in the colon.To achieve this objective the drug is coated with two membranes, one having pH dependent solubility and the other insoluble but permeable to intestinal juices.As long as the coated drug remains in the stomach and in the upper part of the intestinal tract, that is as long as the pH is lower than 5.5, it is not released.Only when it reaches an environment with a higher pH (small intestine and/or colon), the pH dependent membrane dissolves and the release of the drug can begin.From this moment the second membrane, pH-independent but permeable to intestinal juices, carries out its action which is to slow down and control the dissolution of the drug in the small intestine-colon tract.

Abstract: Compositions comprising an immunogenic amount of an antigen encapsulated in a stabilized hydrogel microbead are disclosed. The compositions provide a delivery system for antigens such as vaccines. Also provided are methods of stimulating an immune response comprising administration of the inventive compositions.

Abstract: This invention relates to novel biopesticidal compositions comprising an active insecticidal ingredient selected from insecticidal bacteria and viruses such as B. thuringiensis crystal protein or spores or mixtures thereof and baculoviruses such as nuclear polyhedrosis viruses, granulosis viruses and non-occluded viruses; a polymer; and an inorganic light blocking agent wherein the light blocking agent protects the active ingredient from both ultraviolet light and sunlight and the polymer forms a matrix in which the active ingredient and light blocking agent are dispersed therein. Methods for producing the biopesticidal compositions and methods of controlling insects are also included within the scope of the invention.

Abstract: A dry moisture barrier film coating composition for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, and optionally a flow aid, a colorant, and/or a suspending agent. A liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprises polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent. A method of coating pharmaceutical tablets and the like with a moisture barrier film coating comprises forming a liquid coating solution or dispersion for forming a moisture barrier film coating for pharmaceutical tablets and the like comprising polyvinyl alcohol, soya lecithin, water, and optionally a flow aid, a colorant, and/or a suspending agent, applying the coating solution or dispersion onto the tablets to form a film coating on the tablets, and drying the film coating on the tablets.

Abstract: Aerial spray or discharge drift is controlled in aqueous compositions via the use of selected non-visco-elastic amounts of guar, one or more derivatives of guar, or combinations thereof.

Abstract: In vivo-soluble composite particles involving a particle of a polymeric substance such as polylactic acid and the like soluble in a living body, having coated on a surface thereof, a calcium phosphate compound having a Ca/P ratio of about 1.0 to 2.0. The in vivo-soluble composite particles have a highly increased adsorptivity with regard to medicaments, antigens and others and also the in vivo-soluble composite particles can be dissolved or decomposed in the living body without producing a remainder in the body.

Abstract: A cosmetic composition is provided comprising:A) a cosmetically acceptable carrier; andB) 0.05 to 3.0% by weight, based on the weight of the total composition, of a .beta.-1,3-glucan having a mean molecular weight of 10.sup.5 to 25.10.sup.6.

Abstract: A stable dry powder skin care powder having prolonged and controlled release properties, useful as baby powders, body talcs, deodorizing powders, OTC eczema preparations, foot powders, anti-fungal powders, etc. The dry powder is preferably prepared by a process comprising spray-drying a mixture of liposome encapsulated active agent, starch and maltodextrin. The particle is designed so that activity of, e.g., an anti-inflammatory agent such as Dragosantol.RTM. can be specifically triggered by skin conditions, such as moisture, for optimal timing of delivery.

Abstract: The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual's ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual's system.

Abstract: Aerial spray or discharge drift is controlled in aqueous compositions via the use of selected non-visco-elastic amounts of guar, one or more derivatives of guar, or combinations thereof.