Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of a therapeutically active agent incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.

Abstract: A pelletized sustained release pharmaceutical composition including a core element including approximately 0.1 to 95% by weight, based on the total weight of the core element, of an active ingredient of low aqueous solubility; approximately 0.1 to 55% by weight of a core seed; and a core coating for the core element, including approximately 30 to 97% by weight, based on the total weight of the core coating, excluding filler, of an enteric polymer; approximately 3 to 50% by weight of an insoluble polymer; and 0 to approximately 50% by weight of plasticizer, the enteric polymer comprising at least approximately 70% by weight of the total weight of the enteric polymer and insoluble polymer; the core coating being such that the active ingredient is released in a controlled fashion over an extended period in the intestine but substantially no release occurs in the acid environment of the stomach and blood levels of active ingredient are maintained within the therapeutic range over an extended period of time.

Abstract: Liquisolid systems are acceptably flowing and compressible powdered forms of liquid medications. According to the concept of liquisolid systems, liquid lipophilic drugs, or water-insoluble solid drugs dissolved in suitable non-volatile solvents, may be converted into free-flowing and readily compressible powders by a simple admixture with selected powder excipients referred to as the carrier and coating materials. Various grades of microcrystalline or amorphous cellulose may be used as carriers, whereas very fine particle size silica powders may be used as coating materials. Based on the theory that the carrier and coating materials can retain only certain amounts of liquid and at the same time maintain acceptable flow and compression properties, a new formulation-mathematical model is provided to calculate the optimum quantities of carrier and coating materials required to yield acceptably flowing and compressible liquid/powder admixtures.

Abstract: This invention relates to devices useful for the controlled delivery of one or more beneficial agents to an environment of use. More specifically, this invention concerns such devices which are powered by hydrogel. This invention also relates to the controlled delivery of one or more beneficial agents to an aqueous environment of use through the use of such hydrogel powered dispensing devices. Also disclosed are methods for the controlled delivery of one or more beneficial agents to an aqueous environment of use which comprises administering to or otherwise placing the devices of this invention in the environment of use.

Abstract: Controlled release beads containing a core around which is a drug-containing layer e.g. a layer containing furosemid and a process for their preparation and their use in a pharmaceutical preparation. The controlled release beads have excellent mechanical and release characteristics.

Abstract: The present invention provides a base for coating a solid enteric pharmaceutical preparation whose dissolution pH ranges from 3 to 4. The coating base is a cellulose acetate maleate which is prepared by substituting a water-soluble cellulose derivative with 0.25 to 0.5 acetyl group and 0.35 to 0.6 maleyl group per glucose ring of the cellulose derivative. The cellulose acetate maleate has a dissolution pH ranging from 3 to 4.

Abstract: A controlled release pharmaceutical composition in oral dosage unit form comprising a hard or a soft shell capsule containing a filling comprising a therapeutically effective number of active spherical granules comprising an effective amount of at least one carbonic anhydrase inhibitor active medicament, a pharmaceutically acceptable normally solid diluent adapted to form a diffusable matrix for the carbonic anhydrase inhibitor active medicament and an optional pharmaceutically acceptable excipient. A method for the preparation and for the administration of the above defined composition is provided as well.

Abstract: The invention relates to a delayed-release lacquer solution for pharmaceutical preparations which is characterised in that it is free from halogenated hydrocarbons.

Abstract: The present invention relates to pharmaceutical compositions containing as active ingredient micronized nebivolol of formula (I) and ways of preparing said compositions.

Abstract: A capsule shell comprising 79.6-98.7% by weight of a hydroxypropylmethyl cellulose, 0.03-0.5% by weight of carrageenan, and 0.14-3.19% by weight of a potassium ion and/or a calcium is prepared by drying an solution comprising 18-28% by weight of hydroxypropylmethyl cellulose whose 2% aqueous solution has a viscosity of 2.4-5.4 centistokes at 20.degree. C. as a base, 0.01-0.09% by weight of carrageenan as a gelling agent, and 0.05-0.6% by weight of a potassium ion and/or calcium ion as a co-gelling agent. The capsule shell exhibits disintegrating ability equivalent to gelatin shells without degrading that ability even under special conditions containing much calcium ions.

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: A solid pesticide composition is taught which includes a solid carrier, a pesticide and an amount of flour and/or starch to promote the dispersion of the pesticide into the wax. The solid carrier includes paraffin oil, paraffin wax and microcrystalline wax. A solid pesticide composition is provided without having to include a chemical surfactant.

Abstract: A cellulosic enteric base is dissolved in an organic solvent capable of being admixed with water in any rate or a mixed solvent of the organic solvent and water to give a polymer solution, followed by mixing the polymer solution with water, then removing the organic solvent to give a concentrate; adding an anionic surfactant to the concentrate and then drying to give polymer powder. The polymer powder is introduced into water to give an emulsion containing polymer particles having an average particle size of not more than 1 .mu.m and the emulsion is dispersed in water containing a plasticizer to give a coating liquid. A drug is coated with the coating liquid to give a solid enteric pharmaceutical preparation.

Abstract: Sustained release formulations include an augmented microcrystalline cellulose, an active agent, and a sustained release carrier and methods for making same are disclosed.

Abstract: Compositions of natural, especially plant, constituents in the form of spheroids in particular of the medicinal type and formulations necessary to their preparation by a technical extrusion and spheronization system. Compositions characterized by the direct use of large quantities of solutions of natural, especially plant, origin such as liquid extracts adsorbed by natural or synthetic polymer-type substances. These various components are selected so that their combination permits the obtainment of a mass of a plasticity compatible with the technical extrusion and spheronization system. According to the process, liquid extract is prepared, this extract is incorporated in a substance of a polymeric type, the correctly moistened mass is extruded by micro-extrusion techniques and the extrudates are spheronized and then dried and calibrated.

Abstract: A pharmaceutical preparation for oral administration which is controlled to release a medicinal active ingredient at a targeted site in the intestinal tract comprising (a) a core containing a medicinal active ingredient and (b) a press-coated layer comprising an enteric polymer, said layer being provided around the core. In the pharmaceutical preparation of the present invention, the medicinal active ingredient is not released during residence in the stomach and, after discharged from the stomach, until reaching a targeted site in the intestine, and thereafter is quickly released, so that the medicinal active ingredient is efficiently delivered to the targeted site in the intestinal tract.

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 an effective amount of a surfactant, which, in preferred embodiments is an anionic surfactant present in amounts ranging from about 0.1% to about 0.5%, by weight of the microcrystalline cellulose, wherein the microcrystalline cellulose and surfactant are in intimate association with each other. One preferred anionic surfactant utilized in the novel excipient is sodium lauryl sulfate.

Abstract: Provided are enteric coating compositions which utilize a low viscosity cellulose acetate phthalate polymer as a film former. The cellulose acetate phthalates have an inherent viscosity of about 0.2 to 0.6 dL/g and phthalyl values of from 30 to 40% and can be applied to solid oral medicaments with less solvent than conventional cellulose acetate phthalate polymers. Also provided is a process for preparing the low viscosity cellulose acetate phthalate polymers.

Abstract: A method for reducing the cholesterol level in mammalian blood by administering a water soluble cellulose ether thereto. The cellulose ethers have a viscosity, measured as a 2% aqueous solution at 20.degree. C., of at least about 35 cps. Oral administration is preferred, and, in one embodiment the high viscosity water soluble cellulose ether is hydroxypropyl methylcellulose, contained in a nutritious foodstuff.

Abstract: A solid oral dosage form for the treatment of gastrointestinal disorders comprising a therapeutically effective amount of a pharmaceutical suitable for the treatment of gastric disorders selected from the group consisting of cimetidine, ranitidine, famotidine, diphenoxylate, loperamide, loperamide-N-oxide, pharmaceutically acceptable salts thereof and combinations thereof; and a therapeutically effective amount of simethicone wherein the pharmaceutical and simethicone are separated by a barrier which is substantially impermeable to simethicone.

Abstract: The novel diclofenac preparation with controlled release is in the form of pellets. The active ingredient, applied to inert pellets, is coated with a membrane layer which contains, in addition to 35-65% by weight of a water-insoluble polymer, 5-20% by weight of at least one water-soluble and/or water-insoluble pore-forming agent and 20-50% by weight of adjuncts. The pore-forming agents permit a very uniform release of diclofenac such that administration twice a day is sufficient. A film coating resistant to gastric juice is applied over the membrane layer.

Abstract: A composition for oral preparations, having a complex formed by dispersing or dissolving an unpleasantly tasting basic drug and a functional polymer compound in a substance having a low melting point, 10 to 70% by weight, based on the composition, of sugar alcohol and 0.1 to 7% by weight, based on the composition, of basic oxide. The composition for oral preparation is excellent in masking unpleasantly tasting basic drugs and has excellent performance in biological use.

Abstract: This invention pertains to a dosage form for the management of epilepsies wherein the dosage form comprises administering valproic acid or a valproic acid derivative at a continuous rate over an extended time.

Abstract: It comprises: (1) preparing an aqueous phase containing surface active suspensor agents and, optionally, a chemically or biologically active chemical substance; (2) preparing an organic phase containing a biocompatible polymer or monomer and, optionally, a lipid or chemically or biologically active chemical substance; (3) mixing both phases in a continuous manner in a constant average phase-volume ratio, continuously removing a recently formed colloidal suspension; (4) continuously eliminating the solvent from the colloidal suspension; and (5) completely eliminating the organic solvent and part or all of the water in order to obtain the desired concentration of nanospheres or dry product.Application in biomedicine, pharmacy, medicine, cosmetics, chemical industry, agriculture, veterinary science, etc.

Abstract: A device for controlled release of an active substance through one or more asymmetric membranes by diffusion and/or osmotic pumping.

Abstract: The invention relates to flavour-masked pharmaceutical compositions for oral administration, their preparation and their use as medicaments.The new pharmaceutical preparations according to the invention make it possible to administer pharmaceutical active substances having very unpleasant organoleptic properties such as, for example, very bad taste, even in liquid form.

Abstract: A new oral pharmaceutical formulation containing a novel physical form of a magnesium salt of omeprazole, a method for the manufacture of such a formulation, and the use of such a formulation in medicine.

Abstract: A process for producing a pharmaceutical composition is disclosed. In the process, 1 part by weight of a physiologically inert powdery additive, 0.001-1 part by weight of a macromolecular additive per part by weight of said insert powdery additive, and at least one drug substance are used as ingredients and processed en bloc by means of a multi-screw extruder. The drug substance used in the process can be selected from the following group: subliminable drug, volatile drug, drug hydrolyzable in the presence of water, drug which develops whiskers, and hygroscopic or deliquescent drug. The process confers increased physicochemical stability to the pharmaceutical composition and the drug substance contained therein.

Abstract: An aqueous core microcapsule has a capsular wall provided with a peptide(s) of pre-determined binding specificity(ies) appended to the surface, the wall being the reaction product of an anionic polymer or salt thereof and a polyamine, salt thereof, mixtures thereof, or mixtures thereof with monoamines. The aqueous core may contain an active ingredient(s), and be targeted for delivery to specific cell tissues. The microcapsules are provided as a composition and in a kit with instructions for use in imaging, diagnosis, therapy, vaccination, and other applications.

Abstract: Formulations of chewable pharmaceutical tablets for delivery of prescription pharmaceutical actives, non-prescription pharmaceutical actives, or over-the-counter actives comprise as an excipient an aggregate of coprocessed microcrystalline cellulose and a galaotomannan. Addition of these excipients imparts improved smell, taste, texture, and mouthfeel to the finished product.

Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of a therapeutically active agent incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material comprising at least one inner coating layer and one outer coating layer;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.

Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of a therapeutically active agent incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.

Abstract: A dosage form for orally administering chemical or medicinal substances such as vitamins, trace elements, amino acids, nutritive substances, vaccines, etc., to domestic or wild animals, and a method for preparing same, are disclosed. Said dosage form includes: a porous water-soluble central core containing binders selected from polypeptides, polysaccharides, polymers and colloids, and/or diluents selected from polyols, metal oxides, carbonates, phosphates and microcrystalline cellulose, and an effective amount of at least one bioactive substance; and a palatable hydrophobic outer layer containing at least one lipid substance selected from fatty alcohols, fatty acids, glycerol esters, hydrogenated oils, waxes, paraffin, lanolin, coconut oil and fatty acid salts; a polymeric agent for modulating the disintegration and adhesion of said outer layer, and natural or synthetic palatable substances.

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: Disclosed are compositions and dosage forms containing moguisteine and having controlled release properties, methods for using such compositions and dosage forms and methods for making them.

Abstract: Multiparticulate controlled release preparations incorporating an alkalinizing potassium salt, preferably potassium bicarbonate, as an active ingredient, which are suitable for forming pharmaceutical dosage forms for oral administration. Such dosage forms are useful for potassium supplementation and for the treatment of degenerative bone or cardiovascular diseases, e.g., osteoporosis and hypertension.

Abstract: Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.

Abstract: A controlled release composition including spheroid cores of diltiazem or a pharmaceutically acceptable salt thereof and optionally a spheronizing agent, the cores being coated with a controlled release layer, and a method of manufacturing the same, is disclosed. The spheronizing agent when present is preferably microcrystalline cellulose. Ethylcellulose is a preferred release coating. The controlled release coating preferably contains a plasticizer, a surfactant and a tack-modifier.

Abstract: Disclosed is a liquid-suspension controlled-release enteric-coated pharmaceutical formulation for the administration of naproxen, comprising (a) microgranules of naproxen and an excipient; (b) four successive coats of polymeric hydrophilic and hydrophobic materials, at least the innermost of said coats imparting controlled-release properties to said naproxen according to a predetermined release profile, and at least the outermost of said coats imparting resistance to dissolution in gastric fluids; and (c) a liquid administration vehicle. This composition enables the oral administration of naproxen as a single daily dose the adjustment of the dosage to a patient's requirements, and avoids detrimental effects of prolonged contact of naproxen with the gastric mucosa thus aiding oral intake and minimizing the drug's typical side effects.

Abstract: Drug formulations comprising coated, very sparingly water-soluble drugs for inhalational pharmaceutical forms, and process for their preparation.Drug formulations comprising micronized particles of very sparingly water-soluble drugs which are coated with a natural, physiologically acceptable ampholytic surfactant soluble in water to give a micellar/colloidal solution, and a process for the preparation of these drug formulations, are described. When placed in an appropriate final container and after the addition of a chlorine-free, partially fluorinated propellant gas liquefiable under pressure, these formulations are suitable for inhalation.

Abstract: The present invention relates to a pharmaceutical composition in a unit dosage form for peroral administration in a human or lower animal, having a gastrointestinal tract comprising a small intestine and a colon with a lumen therethrough having an inlet to the colon from the small intestine, comprising:a. a safe and effective amount of rapidly dissolving bisacodyl incorporated into or coated on the surface of a dosage form selected from the group consisting of a spherical substrate, an elliptical substrate, a hard capsule, or a compressed tablet, with a maximum diameter of about 3 mm to about 10 mm; andb. an enteric polymer coating material comprising at least one inner coating layer and one outer coating layer;wherein the dosage form has a smooth surface free from edges or sharp curves; the elliptical substrate and the hard capsule have a ratio of the long to short diameters of no greater than about 1.

Abstract: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions.

Abstract: An oral pharmaceutical preparation releasable in the lower digestive tract, characterized by having a double-coated structure wherein a solid drug having a core containing an active ingredient is covered with both an inner coat made of a cationic polymer and an outer coat made of an anionic polymer.

Abstract: A solid composition for peroral therapy of cognition impairment is formulated to stabilize the acid labile drug, CI-979 HCl, by layering a mixture of thereof with a binder on mini-sugar spheres, and finally covering the structure with a protective coating.

Abstract: A method for the production of microcapsules embedded with pharmaceuticals, peptides, proteins, enzymes and vaccines, which uses biodegradable solvents, and microcapsules free of toxic residual solvents is described. The microcapsules are obtained by spraying of a solution, suspension or water-in-oil dispersion of active materials and biodegradable polymers.

Abstract: Oxalate-degrading enzymes and bacteria were encapsulated for both enteric and intraperitoneal administration. We have shown that via alginate microencapsulation of Oxalobacter formigenes, enzymatic activity was retained for several months. A new process was developed which strengthened the alginate microcapsules and their tolerance to citrate treatment. Much smaller (30-50 .mu.m) alginate microcapsules were made for injection as means of implantation. For oral administration, multi-encapsulated microspheres of cellulose acetate phthalate in poly-2-vinylpyridine (pKa=3.5) were prepared to protect the enzymes from gastric juices.

Abstract: A fibrogen-free substrate having as a hemostatic agent on a surface thereof a mixture of a clot-promoting amount of thrombin and an amount of epsilon aminocaproic acid (EACA) effective to accelerate the rate of blood clotting induced by the thrombin is useful as a hemostatic patch which is safe, inexpensive and which rapidly controls bleeding from a wound. A patch which rapidly stanches the flow of blood from a lesion on a parenchymal organ by pressing it against the surface of the organ for 3-5 minutes, is produced by applying thrombin, EACA and CaCl.sub.2 to a rigid sheet of biodegradable foam, such as an absorbable gelatin sponge, and compressing the dry sheet to produce a flexible sheet which conforms to the contour of the organ without the necessity of pre-moistening. The EACA raises the pH of the acidic fluid associated with the wound and thereby accelerates the activation of the thrombin.

Abstract: This invention is directed to a multilayered controlled release pharmaceutical dosage form. More particularly the dosage form is adapted for water soluble drugs and comprises a plurality of coated particles wherein each has multiple layers about a core containing a drug active whereby the drug containing core and at least one other layer of drug active is overcoated with a controlled release barrier layer and preferably an outer layer of additional drug is adapted for immediate release to preferably provide one immediate releasing layer and at least two controlled releasing layers of a water soluble drug from the multilayered coated particle.

Abstract: An oral pharmaceutical composition is described for targeted slow release in the treatment of inflammatory bowel diseases. Also described are pharmaceutical compositions for peroral treatment targeted to different areas of the intestinal tract afflicted by ulcerative colitis and certain aspects of Crohn's disease.

Abstract: Compositions which contain active substances and are in the form of solid particles can be obtained by intimately mixing the active substance with a water-soluble melt composed ofa) 10-90% by weight of a water-soluble polymer A with a viscosity V.sub.a of 1,000-120,000 cps andb) 10-90% by weight of a water-soluble polymer B with a viscosity V.sub.b of 1-500 cpsas carrier substance, where the viscosities V.sub.a and V.sub.b are those of a 2% by weight aqueous solution at 20.degree. C., measured by the ASTM D 2363-72 capillary method (European Pharmacopoeia, Vol. III, p. 37), and processing the melt with shaping to give the particles.