Abstract: A controlled-release pharmaceutical preparation comprising diamorphine, or a pharmaceutically acceptable salt thereof.

Abstract: Process for the preparation of shaped, compressed controlled-release unit-dosage forms from a therapeutic active substance exhibiting a self-retarding release that depends on the magnitude of the force used for the compression. The process gives unit-dosage forms for which the release of the active substance is highly uniform, reproducibly identical and largely linear. To achieve this, the active substance and an additive charge that inhibits or compensates for the self-retardation of its release are processed into particles in the first stage of production, so that the preliminary compressed objects made from these particles without any further additives exhibit a rapid release (in comparison with the required controlled release) over the range of the force of compression envisaged for the production of the unit-dosage form in question, after which the particles are compressed in the second stage of production with a release-retarding agent to obtain the unit-dosage forms.

Abstract: Shearform compositions made without added glycerine are disclosed. The compositions are self-binding and exhibit excellent cohesivity when used in tableting compositions. Typically, xylitol is incorporated into a feedstock which is flash-flow processed to form a self-binding shearform matrix.

Abstract: A two-phase hydrophilic drug-containing matrix for use in transdermal drug delivery patches in which one phase is a continuous hydrophobic polymer phase which optionally includes a hydrophobic solvent that acts as a skin permeation enhancer and the other phase is a dispersed particulate hydrated inorganic silicate in whose absorbed aqueous phase the drug is dissolved.

Abstract: A pulsatile drug delivery system comprising of a plurality of particles is able to deliver drug in any desired patterns. A plurality of particles with multi-layer core capable of short-pulse release interlaced with long-duration release is designed for delivery of multi-agents simultaneously or sequentially, or single agent, according to a pre-programmed profile.

Abstract: A new pharmaceutical multiple unit tableted dosage form containing omeprazole or one of its single enantiomers or an alkaline salt of omeprazole or one of its single enantiomers, a method for the manufacture of such a formulation, and the use of such a formulation in medicine.

Abstract: Systemic delivery of parathyroid hormone to a mammalian host is accomplished by inhalation through the mouth of a dispersion of an N-terminal fragment of PTH. It has been found that such respiratory delivery of the PTH fragment provides a pulsatile concentration profile of the PTH in the host's serum. PTH fragment compositions include dry powder formulations having the PTH present in a dry bulking powder, liquid solutions or suspensions suitable for nebulization, and aerosol propellants suitable for use in a metered dose inhaler.

Abstract: A pharmaceutical tablet composition for oral administration containing pseudoephedrine pellets admixed with a tablet mixture containing a second active drug substance, either alone or in combination with pseudoephedrine or a pharmaceutically acceptable salt thereof, is disclosed. The pellets provide an extended release of pseudoephedrine, whereas the tablet mixture provides an immediate release of the second active drug and any pseudoephedrine.

Abstract: Active agents comprising coated pellets which self seal if they are damaged are described. More specifically, an active agent, or bead coated with an active agent, is coated with a rate-release controlling polymer and a hydrophilic gel-forming material which forms a gel upon hydration. If the bead is compressed into a solid compact which damages the polymer coating, the hydrophilic substance gels upon exposure to an aqueous environment. The gel provides sufficient sealing of the damaged area in the polymer so that a useful control of drug release is retained in spite of the damage to the polymer. The pellets of the invention exhibit improved flow and compactability. The compacts can be formulated to disintegrate in the gastrointestinal tract, and also may result in either controlled release or immediate release of the active agent.

Abstract: A bioceramic system for delivery of a bioactive compound, which comprises a combination of bioactive glass, bioactive glass ceramic or bioactive ceramic, hydroxyapatite, optionally one or more other calcium phosphate compound and optionally a matrix, and which may incorporate into the bioceramic system a bioactive compound. The timing of the release of the bioactive compound can be regulated as desired and depends on the conditions of the surrounding, the composition of the bioceramic system and its method preparation.

Abstract: Hydrolyzed gelatin has been found to provide an improvement in taste and mouthfeel when incorporated in small amounts into chewable tablets containing ingredients requiring taste masking. Medicinals and nutritional supplements may now be prepared as chewables for those who find tablets difficult to swallow, for example children and older adults, or for those who prefer the convenience. There is a particularly large improvement in the taste and mouthfeel of chewables incorporating magaldrate and/or calcium carbonate.

Abstract: The present invention relates to controlled release dosage forms composed of a naproxen layer which contains a delayed release granulate of naproxen compressed with an immediate release granulate of naproxen and an immediate release naproxen sodium layer compressed with the naproxen layer, designed to promptly exert a therapeutic effect while also maintaining the therapeutic blood concentration for a prolonged duration of 24 hours.

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: Compositions for delivery of pharmacologically active agents and methods for their administration are provided. In one embodiment, the compositions include a complex of a polycationic polymer and a pharmacologically active agent in a pharmaceutically acceptable carrier. The compositions in one embodiment permit transport of pharmacologically active compounds across mucosal membranes for systemic delivery. The polycationic polymer may be, for example, a polycationic carbohydrate such as a chitosan or a chitosan salt or derivative. The therapeutic agent a preferred embodiment is a vaccine or a nucleic acid, such as a gene or antisense oligonucleotide. The composition may be provided in different forms such as a solution, dispersion, powder or in the form of microspheres.

Abstract: A process for producing active substance compositions in the form of a solid solution of the active substance in a polymer matrix, which comprises melt extrusion of the active substance in nonionic form together with a polymer and a salt.

Abstract: The present invention relates to a saliva-soluble stimulant unit comprising an active ingredient in a gel, wherein the gel is prepared by gelling a water-binding gelling agent, and the active ingredient comprises nicotine or alkaloid having the same direction of activity, said unit having a texture profile, with parameter values of firmness, hardness, brittleness, adhesiveness, elasticity and cohesiveness within given ranges; a disintegration time within the range 5-60 minutes; and a nicotine content from 0.5 to 10 mg.

Abstract: A pharmaceutical coating for taste masking oral medications is described which includes a unique combination of triglycerides and a polymer. The triglyceride mixture melts at body temperature and the copolymer causes the coating to dissolve upon reaching the acidic environment of the stomach.

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 present invention is a saccharide-based matrix, and the products resulting therefrom, made from a maltodextrin feedstock subjected to conditions which induce flash flow of the maltodextrin so that the matrix possesses a physically or chemically altered structure from the feedstock. The present invention also includes a method of producing the matrix and of making products which take advantage of the unique properties of the matrix.

Abstract: A preparation of a pharmacologically active ionizable substance, wherein active substance is ionically complexed to an ion-exchanger resin, which is embedded in a hydrophilid eroding matrix as well as a process for the manufacture thereof.

Abstract: A preparation of a pharmacologically active ionizable substance, wherein active substance is ionically complexed to an ion-exchanger resin, which is embedded in a hydrophilic eroding matrix as well as a process for the manufacture thereof.

Abstract: Methods for treating circadian rhythm disorders and sleep disorders are described. The method involves oral administration of a sustained release composition of melatonin to produce a normal melatonin pattern when the normal pattern has been disrupted or is missing.

Abstract: Verapamil depot drug formulations include the pharmaceutical itself and a three component release rate controlling matrix composition. The three components of the matrix composition are (1) an alginate component, such as sodium alginate, (2) an enteric polymer component, such as methacrylic acid copolymer, and (3) a pH independent gelling polymer, such as hydroxypropyl methylcellulose or polyethyleneoxide. The drug release rate can be adjusted by changing the amount of one or more of these components of the composition.

Abstract: The present invention is concerned with an extended release, film coated tablet comprising as active ingredients the antihistaminic, antiallergic agent astemizole and the adrenergic, decongestant agent pseudoephedrine hydrochloride and with a process of preparing such tablets.

Abstract: This invention is directed to controlled release pharmaceutical formulations of 3'-azido-3'-deoxythymidine, also known as AZT or zidovudine and methods of use thereof. The controlled release formulations of AZT achieve and maintain a therapeutic level of AZT, while substantially reducing the side effects of AZT caused by its catabolite 3'-amino-3'-deoxythymidine (AMT) by reducing the amount of AMT produced.

Abstract: A cylindrical delayed release tablet with a convex or flat upper side and lower side is provided, along with a method for its production and a gelatin capsule containing 3-200 tablets of the same having identical or different release rates, wherein the tablet if made of .beta.-phenylpropiophenone derivatives of the formula I as active ingredient ##STR1## where R is n-propyl or 1,1-dimethylpropyl, and their pharmacologically acceptable salts, wherein the tablet has a height and diameter that are both, independently of one another, 1-3 mm, the active ingredient content is in the range from 81-99.

Abstract: A method of preparing a device of a selected material to have pores and pore interconnections of predetermined sizes and shapes includes the steps of forming a selectively removable open-celled porous mold form of particles which adhere to one another, with the particles corresponding to the predetermined pore sizes and shapes, and interconnections between the particles which bind them together in the form in which the connections correspond to the predetermined sizes and shapes of the pore connections. Also included are the steps of filling the vacancies between the particles and connections of the form with the selected material, and then removing the form to leave the selected material. The resulting device is at least partly porous, the pores and pore interconnections corresponding in size and shape to the particles and connections respectively.

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: A composition is provided for use as a matrix for controlled-release compositions. Such compositions utilize an active ingredient dispersed in a matrix. Active ingredients include, for example, pharmaceuticals and agricultural agents. The matrix is a blend of a poly(hydroxyethyl) methacrylate, polyethylene glycol and a time-release extending agent which is a low molecular weight polymer having hydrophilic and hydrophobic side groups, such as diblock or triblock poly(ethylene oxide propyleneoxide).

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: Hydrolyzed gelatin has been found to provide an improvement in taste and mouthfeel when incorporated in small amounts into chewable tablets containing ingredients requiring taste masking. Medicinals and nutritional supplements may now be prepared as chewables for those who find tablets difficult to swallow, for example children and older adults, or for those who prefer the convenience. There is a particularly large improvement in the taste and mouthfeel of chewables incorporating magaldrate and/or calcium carbonate.

Abstract: An improved process for preparing controlled release pharmaceutical forms comprises exposing a mixture comprising one or more excipients and one or more active ingredients compatible with each other and with said excipients to mechanical or electromechanical actions for a well established time and within a wide range of frequencies to give tablets, matrices or mono or multilayered films. Said forms can be optionally crushed to give a granulate or powder. Depending on the employed excipient, a delayed or rapid but always controllable release of the active ingredient can be attained.

Abstract: The present invention relates to a release-controlled implantable composition comprising somatotropin, a bio-compatible wax and a water-soluble polymer. The present composition exhibits superior sustained effect with little side effects, which renders it suitable for long-term administration.

Abstract: A water-dispersible tablet comprises acyclovir and a dispersing agent. The dispersing agent is a swellable clay such as a smectite, e.g. Veegum F or bentonite, and is generally present within the granules of the tablet to provide a tablet which is capable of dispersing in water within 3 minutes to provide a dispersion which will pass through a 710 .mu.m sieve. The tablet can be optionally film-coated in which case the dispersion time is less than 5 minutes.

Abstract: An immunobooster capable of delivering an immunogen to an individual or animal in a controlled release manner is described. The immunobooster contains an immunogen/hydrophobic polymer matrix with a swelling agent such that the swelling agent can swell in an aqueous environment and burst the matrix. The immunogen is released in a pulsed release manner after a desired time interval has elapsed subsequent to administration of the immunobooster. The immunobooster eliminates the need for multiple administrations of immunogen in order to build lasting immunity. Also described are methods of preparing and using the immunobooster, and kits containing the immunobooster.

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: The present invention is a process for making edible units from compression and the products resulting therefrom. The method of the present invention includes compression of shearform matrix mass sufficiently to form a comestible compression unit such as a compression tablet.

Abstract: The present invention relates to administration forms having an extended gastric residence time, in the preparation of which mixtures of polymers containing lactam groups and polymers containing carboxyl groups are used, and which are distinguished both by marked swelling properties and by high dimensional stability in the swollen state.

Abstract: Disclosed is a soft, chewable dosage form, including a matrix of hydrogenated starch hydrolysate, a water soluble bulking agent, and a water insoluble bulking agent. The present invention also includes a method of preparing a soft, chewable dosage form, including the steps of mixing under high shear force, a hydrogenated starch hydrolysate, a water soluble bulking agent, and a water insoluble bulking agent until a uniformly blended matrix is obtained. Active ingredients may optionally be incorporated in the matrix.

Abstract: A once-daily naproxen formulation for oral administration having a first portion of the naproxen as a multi-particulate pellet form, each pellet having a core of naproxen or a pharmaceutically acceptable salt thereof in association with an organic acid, the core being surrounded by a multi-layer membrane and optionally a second portion of naproxen formulated to release the drug promptly following oral administration.

Abstract: In a composition for delayed release of an active substance, the active substance is incorporated in a polysaccharide matrix which consists of an essentially crystalline straight-chain glucan and contains a glucan-degrading agent. The glucan is in particular an .alpha.-glucan which has essentially a helix structure. The glucan-degrading agent is preferably .alpha.-amylase. The composition can contain high-molecular materials such as proteins, allergens, vaccine substances and microorganisms, and preferably has the form of compressed tablets.

Abstract: A water-dispersible tablet comprises acyclovir and a dispersing agent. The dispersing agent is a swellable clay such as a smectite e.g., Veegum F or bentonite, and is present within the granules of the tablet to provide a tablet which is capable of dispersing in water within 3 minutes to provide a dispersion which will pass through a 710 .mu.m sieve. The tablet also includes a cellulostic excipient. The tablet can be optionally film-coated, in which case the dispersion time is less than 5 minutes.

Abstract: Described herein is a drug delivery system useful to deliver drugs at low dosage levels to patients in a sustained fashion and at a controlled rate. The system comprises a wettable polymeric matrix in which is dispersed a multiplicity of particles containing a substantially homogeneous blend of osmotically active excipient and not more than about 10% by weight of drug. The system is particularly well suited for delivery of therapeutic macromolecules such as protein drugs. Delivery of epidermal growth factor is exemplified.

Abstract: A sustained-release multi-granule tablet is obtained by compressing sustained-release granules, which contains a basis, and a formulation adjuvant. Each of the granules has been coated in advance with a layer of the formulation adjuvant and/or a layer of a mixture of the formulation adjuvant and the basis. The tablet releases an active substance at a suitable velocity into the digestion tract, resulting in that the inbalance in the absorption of the drug in each patient and among individual patients is minimized to achieve maximum bioavailability.

Abstract: The present invention relates to an aqueous pharmaceutical suspension composition comprising: from about 0.2% to 20% of a substantially water insoluble pharmaceutical active, e.g. ibuprofen; a suspension stabilizing effective amount of xanthan gum, pregelatinized starch and polyoxyethylene sorbitan monooleate; an effective amount of taste masking composition; and water, as well as a process for producing such aqueous pharmaceutical suspensions.

Abstract: A peroral administration form for peptidic medicaments contains the peptidic medicament, in particular insulin, distributed in a gelatine or gelatine derivate matrix, besides usual pharmaceutical excipients and additives. By selecting an appropriate gelatine, the medicament is released in the small or large intestine, so that it is no longer enzymatically decomposed by peptidases.

Abstract: A pharmaceutical preparation for oral administration comprising(a) a core containing a medicinal active ingredient,(b) a press-coated layer comprising a pH-independently water-soluble polymer, said layer being provided around the core and(c) a film comprising an enteric polymer, said film being provided around the press-coated layer. In the pharmaceutical preparation of the present invention, the medicinal active ingredient is not released during residence in the stomach and, after forwarded 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: The present invention relates to controlled release dosage forms composed of a naproxen layer which contains a delayed release granulate of naproxen compressed with an immediate release granulate of naproxen and an immediate release naproxen sodium layer compressed with the naproxen layer, designed to promptly exert a therapeutic effect while also maintaining the therapeutic blood concentration for a prolonged duration of 24 hours.

Abstract: Systemic delivery of parathyroid hormone to a mammalian host is accomplished by inhalation through the mouth of a dispersion of an N-terminal fragment of PTH. It has been found that such respiratory delivery of the PTH fragment provides a pulsatile concentration profile of the PTH in the host's serum. PTH fragment compositions include dry powder formulations having the PTH present in a dry bulking powder, liquid solutions or suspensions suitable for nebulization, and aerosol propellants suitable for use in a metered dose inhaler.