Abstract: A unit dosage form, such as a capsule or the like, for delivering drugs into the body in a circadian release fashion comprising one or more populations of drug-containing particles (beads, pellets, granules, etc.) is disclosed. Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need at different times during the dosing period, i.e., mimicking the circadian rhythm and severity/manifestation of gastric acid secretion (and/or midnight gerd), predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro/in vivo correlations.

Abstract: A duloxetine pellet formulation comprises: (i) a core including a desired amount of duloxetine; (ii) an enteric coating comprising hydroxypropylmethylcellulose phthalate (HPMCP) as an enteric polymer; and, optionally, (iii) a separating layer located between the core and the enteric coating, the separating layer including polyvinyl alcohol and a low molecular weight hydroxypropylmethylcellulose (HPMC).

Abstract: A formulation of octreotide or pharmaceutically acceptable salts thereof, which provides controlled release of a therapeutically effective amount of octreotide for a period of at least about two months. Methods of treating acromegaly, decreasing growth hormone, decreasing IGF-1, and treating conditions associated with carcinoid tumors and VIPomas by administering a controlled release formulation of octreotide are provided herein.

Abstract: The present invention relates to solid oral pharmaceutical compositions of duloxetine, process for preparing such compositions and method of using such compositions. Preferably, the invention relates to a delayed release composition of duloxetine comprising a core comprising duloxetine, optional separating coat and an enteric coat.

Abstract: The invention relates to the use of mixture of 2 to 60 wt. % of one or more polymers (I) with 40 to 98 wt. % of one or more polymers (II), whereby the polymer (I) is a (meth)acrylate copolymer, containing 90 to 100 wt. % radically polymerised of 40 to 95 wt. % of C1 to C4 alkyl esters of acrylic or methacrylic acid and 5 to 60 wt. % of units of (meth)acrylate monomers with an anionic group with 0 to 10 wt. % of further vinylic polymerisable monomers and polymer(ll) is a vinyl polymer different from polymer (I) or a polysaccharide or a derivative of a polysaccharide, containing 88 to 100 % neutral monomer units and up to 12 wt. % polymerisable monomer units with ionic groups, for production of a coated pharmaceutical formulation, containing an active agent core and a polymeric coating made from the mixture of polymers (I) and (II), characterised in that the glass temperature of polymer (I) is not more than 70° C.

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: A nifedipine controlled release composition is provided comprising a drug-layer and a push-layer at a ratio of 1:0.5˜3 by weight. The drug-layer contains nifedipine and 40˜99 percent by weight of the drug-layer of hydrophilic polyvinylpyrrolidone homopolymer and/or copolymer carrier. The push-layer comprises about 10 to 80 percent by weight of the push-layer of osmopolymers, about 10 to 80 percent by weight of the push-layer of water-insoluble polymers, and about 5 to 50 percent by weight of the push-layer of osmagents. The composition is used in osmotic pump tablets for controlled release of nifedipine useful for administration once a day.

Abstract: The present invention relates to a new hydrophobe biomolecular structure, which is compacted due to the passing of the structure over its point of collapse, a method for the preparation of the structure and use of the new structure for the manufacture of a medicament.

Abstract: Compositions and methods for maintaining healthy mobile joints and cartilage in humans and animals are disclosed. The composition comprises glucosamine and chondroitin dispersed in a controlled-release matrix system capable of releasing the glucosamine and chondroitin over a designated time period. In another aspect, the invention provides compositions and methods for maintaining health mobile joints and cartilage in humans and animals without adversely affecting glucose regulation.

Abstract: A multi-particulate oral dosage form, comprising a plurality of pellets, the pellets comprising a core having disposed thereon a core composition layer, the core composition layer comprising an active agent, and a sustained-release coating disposed on the core composition layer, wherein the sustained-release coating comprises a first polymer comprising a copolymer of acrylic and methacrylic esters comprising quaternary ammonium groups and having a ratio of quaternary ammonium groups to neutral meth(acrylic) esters of 1:40 and optionally a second polymer comprising a copolymer of acrylic and methacrylic esters comprising quaternary ammonium groups and having a ratio of quaternary ammonium groups to neutral meth(acrylic) esters of 1:20, wherein the ratio of the first polymer to the second polymer is about 50:50 to about 100:0, and wherein the first and second polymer comprise about 20 wt % to about 90 wt % of the total weight of the sustained-release coating; and about 10 wt % to about 50 wt % of colloidal sili

Abstract: Oral dosage form for food and food supplement as well as dietetics comprising polyunsaturated acids in a xylose-hardened gelatine capsule with a retarded release time.

Abstract: A process for the preparation of a particulate material by a controlled agglomeration method, i.e. a method that enables a controlled growth in particle size. The method is especially suitable for use in the preparation of pharmaceutical compositions containing a therapeutically and/or prophylactically active substance which has a relatively low aqueous solubility and/or which is subject to chemical decomposition. The process comprising i) spraying a first composition comprising a carrier, which has a melting point of about 5° C. or more which is present in the first composition in liquid form, on a second composition comprising a material in solid form, the second composition having a temperature of at the most a temperature corresponding to the melting point of the carrier and/or the carrier composition and ii) mixing or others means of mechanical working the second composition onto which the first composition is sprayed to obtain the particulate material.

Abstract: A high drug load spheronized beadlet is provided wherein said beadlet comprises about 80% to 100% by weight of an acid labile medicament, preferably didanosine, about 0% to about 10% by weight of a disintegrant, and about 0% to about 10% by weight of a binder selected from the group consisting of sodium carboxymethylcellulose, hydroxypropylmethylcellulose, potassium alginate, and partially pregelatinized corn starch. A high drug load pharmaceutical composition, comprising the beadlet, with an enteric coating disposed thereon, is also provided.

Abstract: An oral dosage form of morphine is formulated by powder-layering an homogeneous mixture of morphine sulfate and hydrous lactose impalpable onto inert beads to obtain a multiparticulate product. A plurality of the powder-layered beads may be administered either in immediate release form or in an extended release form by coating with a hydrophobic material. In addition, multi-particulate oral dosage forms containing therapeutically effective agents containing a plurality of pharmaceutically acceptable inert beads powder-layered with homogeneous mixture of a therapeutically effective agent and hydrous lactose impalpable are also disclosed. A method of preparing the dosage forms as well as a method preparing spheroids containing the homogeneous mixture of therapeutically effective agent and hydrous lactose impalpable are also disclosed.

Abstract: Process for encapsulation of an uncharged crystalline solid particle include treating the crystalline solid particle material with amphiphilic substances and subsequently coating the material with a layer of charged polyelectrolyte or coating the material with a multilayer comprising alternating layers of oppositely charged polyelectrolytes.

Abstract: The inventions disclosed herein relate to compositions for the sustained release of pharmacological agents comprising pectins having a combination of both a high molecular weight and a low degree of methoxylation.

Abstract: Pharmaceutical compositions and methods of using the composition are provided. The pharmaceutical composition comprises an inert core surrounded by an active coating containing one or more bisphosphonic acids or salts thereof, a seal coating surrounding the active coating and an enteric coating surrounding the seal coating. Alendronic acid and alendronate sodium trihydrate are the preferred active ingredients. The composition may be provided in the form of pellets in a capsule or Peltabs. The invention further provides methods for the treatment of disorders caused by the abnormal dissolution or deposition of calcium salts using the inventive compositions.

Abstract: The invention concerns Gelatin compositions for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard gelatin capsules wherein the gelatin used is of non-bovine and non-pig origin and preferably derived from fish, poultry or plant sources. Especially preferred are film compositions for hard gelatine capsules prepared from fish gelatin.

Abstract: This invention refers to: multiparticulate formulations of Lithium salts for oral administration constituted by either modified release granules or mixtures of modified and conventional release granules, suitable for once-a-day administration also at high strengths of Lithium salts, and to the preparation process of said formulations.

Abstract: Once daily pharmaceutical compositions containing lithium carbonate in the form of coated granules.

Abstract: The invention relates to pellets and a production process therefor. Pellets comprise at least one oily component, which is either an active component alone or comprises such an active component. The aim of the invention is to ensure that such active components can be provided at elevated concentration in a long-term stable form for subsequent administration or further processing using such inventive pellets. The at least one oily oxidation-sensitive or else readily volatile active component is distributed homogeneously and discretely in a matrix and encapsulated without a core with at least one water-soluble polysaccharide as filmforming agent. The individual pellets have a respective particle size of at least 100 ?m, preferably of at least 300 ?m.

Abstract: A system whereby a substance which is orally taken and to be delivered into the lower digestive tract is selectively delivered into the lower digestive tract. More particularly, a system which makes it possible to surely and quickly deliver the aimed substance to the lower digestive tract without being affected by pH change in the digestive tract due to change in bacterial flora. Compositions disintegrating in the lower digestive tract characterized by containing a compound <A>, which has a molecular weight of 1000 or less and has a disulfide bond, and a polymer <B>, which has a molecular weight exceeding 1000 and is digested by enteric bacteria and/or undergoes softening, swelling or dissolution due to a decrease in pH; molded products with the use of these compositions; and preparations with the use of these molded products.

Abstract: A modified release preparation having one or more coated core elements, each core element including an active ingredient and having a modified release coating, wherein a stabilising coat is provided between each core element and its modified release coating so that, upon in vitro dissolution testing, the amount of active ingredient released at any time on a post-storage dissolution profile is within 40 percentage points of the amount of active ingredient released at any time on a pre-storage dissolution profile.

Abstract: The present invention provides low-residual-solvent containing excipients with residual solvent less than <3000 ppm. Most of the excipients are required to first be modified to become more water absorbing such as by attaching a water absorbing radical, e.g., (—CH2COONa) to the carbinol groups (—CH2OH) of the excipients to form a —CH2—O—CH2COONa linkage. The linkage of the water-absorbing groups to e excipients improves the water absorbing property of the excipients, which facilitates the replacing residual solvent with water. The residual solvent can be extracted from the excipient by way of mixing with a solvent/water solution containing (1) about 75-95% (v/v) isopropanol and about 5-25% water (v/v); (2) about 65-95% acetone and about 5-35% water; and (3) about 60-85% methanol and about 15-40% water.

Abstract: The present invention relates to a new hydrophobe biomolecular structure, which is compacted due to the passing of the structure over its point of collapse, a method for the preparation of the structure and use of the new structure for the manufacture of a medicament.

Abstract: The present invention relates to a pharmaceutical formulation for oral administration through a soft gelatin capsule drug delivery device, wherein the pharmaceutical formulation has Pseudoephedrine HCl as the active pharmaceutical ingredient. The active pharmaceutical ingredient is embedded into an oily matrix, also the formulation comprises viscosity imparting agents, a surfactant; a suspending agent; and a suspension medium. The viscosity-imparting agents are partially hydrogenated vegetable oil and colloidal silicon dioxide, the surfactant is lecithin, the suspending agent is yellow beeswax, and the suspension medium is soybean oil. In one preferred embodiment, the formulation consists essentially of about 60 mg by weight of Pseudoephedrine HCl, about 15-25 mg by weight of partially hydrogenated vegetable oil, about 10-20 mg by weight of yellow beeswax, about 2-8 mg by weight of lecithin, about 2-8 mg by weight of silicon dioxide; and about 150-250 mg by weight of soybean oil.

Abstract: The present invention provides a process for preparing hardshell gelatin capsule reducing the static electricity and enhancing the lubrication of film having good film distribution in capsule comprising the steps of: i) preparing an emulsion containing 0.4˜0.8 part by weight of diacetylated monoglycerides, 0.05˜0.1 part by weight of sodium lauryl sulfate, and 0.005˜0.01 part by weight of colloidal silicon dioxide; ii) adding the emulsion to gelatin solution containing 100 part by weight of gelatin; iii) mixing and homogenizing the resulting solution; iv) adjusting viscosity of mixture; v) allowing the obtained product to stand; and vi) forming a hardshell gelatin capsule therefrom.

Abstract: A controlled release bead comprises: (i) a core unit of a substantially water-soluble or water-swellable inert material; (ii) a first layer on the core unit of a substantially water-insoluble polymer; (iii) a second layer covering the first layer and containing an active ingredient; and (iv) a third layer of polymer on the second layer effective for controlled release of the active ingredient, wherein the first layer is adapted to control water penetration into the core. A method of producing the controlled release bead is also disclosed.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

Abstract: Method of preventing parturient hypocalcemia and milk fever (parturient paresis) in lactating animals comprising administering to the animal during the dry period a compound which reduces absorption of calcium from the drinking water and/or from the ration of said animal. The method is based on the powerful, natural calcium regulating mechanisms and is applicable under commercial farming conditions.

Abstract: This invention relates to proliposomal drug-delivery systems for medicaments. In particular, it relates to enteric-coated proliposomal formulations for poorly water soluble drugs and methods for making the same. The drug delivery system comprises a pharmaceutical agent, a phospholipid and a coating material. The present invention provides enhanced stability and bioavailability for pharmaceutical formulations.

Abstract: The present invention relates to microspheres, processes for the manufacture of said microspheres, pharmaceutical compositions comprising said microspheres, and sustained release methods of administering an effective pharmaceutical amount of a bioactive compound to a subject. The microspheres of the present invention comprise a water insoluble organic matrix comprising an interior region, throughout which are homogeneously dispersed a plurality of microcapsules consisting essentially of a core of bioactive compound coated with material containing charged organic groups and a surface region substantially free of said bioactive compound.

Abstract: The present invention is an encapsulated yeast composite comprising a core comprising yeast and a coating containing an emulsifiable lipid. The yeast includes Saccharomyces cerevisiae. The invention also relates to other encapsulated bioactive substance composites. The nature of the coating provides controlled release of the bioactive substance from the encapsulate. The encapsulated composites are useful in the production of food compositions, food products, and animal feed products.

Abstract: EEM-S obtained by extracting with hot water or a lower alcohol at least one mushroom selected from among Lentinus edodes, Flammulina velutipes, Hypsizygus marmoreus, Pleurotus ostreatus, Pholiota nameko, Grifola fondosa, Volvariella speciosa ver. speciosa, Lyophllum decastes, blanc du pays, Tricholoma matsutake, Ganoderma lucidum and Phellinus yucatensis, treating the obtained extract by the molecular sieve method and thus eliminating low-molecular-weight and high-molecular-weight fractions: and preparations thereof. This EEM-S exerts physiological effects such as anticancer, immunopotentiating, antioxidative, hypotensive and hypoglycemic effects.

Abstract: The pharmaceutical formulation consists of a number of pellets that comprise an inert nucleus, a layer with the active ingredient, one or more intermediate layers that comprise at least a system of modified release, and an external layer of enteric coating. These pellets can be obtained applying the different layers by means of fluid bed coating techniques using aqueous solutions or suspensions of the components of such layers. The pharmaceutical formulations can be hard gelatin capsules or tablets and are suitable for use in the prevention and treatment of disorders related to abnormal gastric acid secretion.

Abstract: The present invention relates to encapsulated cells producing viral particles, especially retroviral particles containing the genome of a retroviral vector carrying therapeutic genes, to methods for the preparation of such encapsulated cells, as well as to the use of such encapsulated cells for the delivery of genes, especially therapeutic genes, to target organs/cells.

Abstract: The invention concerns Gelatin compositions for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard gelatin capsules wherein the gelatin used is of non-bovine and non-pig origin and preferably derived from fish, poultry or plant sources. Especially preferred are film compositions for hard gelatine capsules prepared from fish gelatin.

Abstract: Compositions and methods of treatment for conditions in humans and animals which have an inflammatory component, are disclosed. The composition comprises a glucosamine component dispersed in a controlled-release matrix system capable of releasing the glucosamine over a designated time period. In another aspect, the invention provides compositions and methods for the treatment of arthritis in humans and animals without adversely effecting glucose regulation.

Abstract: The present invention is an encapsulated yeast composite comprising a core comprising yeast and a coating containing an emulsifiable lipid. The yeast includes Saccharomyces cerevisiae. The invention also relates to other encapsulated bioactive substance composites. The nature of the coating provides controlled release of the bioactive substance from the encapsulate. The encapsulated composites are useful in the production of food compositions, food products, and animal feed products.

Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

Abstract: The present invention relates to an oral preparation of esculetin with controlled release. The oral preparation of esculetin with controlled release of the present invention comprises a gel-forming polymer base, preferably hydroxypropylmethylcellulose. The preparation may be coated with an enteric polymer base such as hydroxypropylmethylcellulose acetate succinate to thereby enhance solubility in the intestines. When orally administered, the preparation can continuously release esculetin. Thus, the administration frequency and dose can be reduced and a therapeutic effect on arthropathy can be established.

Abstract: A stable pharmaceutical pellet formulation that employs a core containing omeprazole or a pharmaceutically acceptable salt of omeprazole and lysine or arginine. The pellet core is directly enteric coated without a separating layer being applied between the core and the enteric coating.

Abstract: The invention relates to an oral pharmaceutical composition which has excellent drug release-controlling ability in the mouth even 5 to 10 minutes after its administration and also has excellent drug releasing ability in the digestive tract without using capsules. It also relates to an oral pharmaceutical composition which comprises one or more drugs having a bitter taste, one or more solid proteins, and one or more pharmaceutically acceptable polymer bases, wherein the proteins are present in the polymer bases preferably as particles.

Abstract: The invention relates to a method for producing capsules provided with a polyelectrolyte covering, and to the capsules obtained using this method.

Abstract: Processes for manufacturing a low-substituted hydroxypropyl cellulose are described that include dipping pulp into an alkaline solution to prepare an alkali cellulose, reacting the alkali cellulose with a hydroxypropylating agent to yield a product in a complete dissolution state, dissolving completely the product in an aqueous medium to provide a product in a complete dissolution state, neutralizing with an acid to yield a precipitate, washing, drying, and pulverizing to yield a powder having a volume-average particle diameter of less than 25 microns which is determined by a dry laser diffraction method, a loose bulk density of 0.29 g/ml or more and less than 0.40 g/ml, and a tapped bulk density of 0.55 g/ml or more. Low-substituted hydroxypropyl celluloses are also described.

Abstract: Pharmaceutical compositions, processes for preparing the compositions and methods of using the composition are provided. The pharmaceutical composition comprises an inert core surrounded by an active coating containing one or more bisphosphonic acids or salts thereof, a seal coating surrounding the active coating and an enteric coating surrounding the seal coating. Alendronic acid and alendronate sodium trihydrate are the preferred active ingredients. The composition may be provided in the form of pellets in a capsule or Peltabs. The invention further provides methods for the treatment of disorders caused by the abnormal dissolution or deposition of calcium salts using the inventive compositions.

Abstract: The present invention relates to methods useful for the treatment of neoplastic diseases, tumor cells, and the treatment of cancer delivering compounds of the formula The invention provides various methods of delivering such compounds, combinations of treatments, and altering such compounds to enhance their effectiveness.

Abstract: The present invention is concerned with pellets comprising a 710-1180 &mgr;m (16-25 mesh) sugar core, a coating film of a water-soluble polymer and an antifungal agent, and a seal coating layer wherein the residual concentration of dichloromethane is below 600 ppm; pharmaceutical dosage forms comprising said pellets and a method of preparing said pellets.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: A superior enteric formulation of the antidepressant drug, fluoxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.