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: An antibiotic product, in particular metronidazole, is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: An antibiotic product, in particular an erythromyacin, is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: Novel forms of sustained-release microgranules (LP) containing diltiazem are disclosed. The microgranules consist of a neutral granular carrier coated with an active layer including diltiazem or a pharmaceutically acceptable salt thereof as the active principle, a surfactant and a binder, and an outer layer providing sustained release of the active principle (layer LP).

Abstract: The present invention concerns a method for the control of various diseases in bee-hives by applying to the bee-hives an effective amount of an essential oil in a slow-release formulation whereby the term oils embraces but is not limited to oils extractable from plant or the essential component thereof such as monoterpenes like menthol, geraniol, thymol, myrcene, citral, limonene, carene, camphor, eugenol, or cineol (eucalyptol); natural oils like lemon oil, eucalyptus oil, or neem oil; or organic acids like formic acid, acetic acid or oxalic acid. Most preferred are monoterpenes like thymol or menthol. Most preferred is thymol.

Abstract: Compositions for sustained delivery of a biomolecule including an anionic polymer and a cationic polymer which ironically interact with each other and, optionally, with the biomolecule. Methods for making the compositions, including the step of combining the negatively charged polymer with the positively charged polymer to form an ionic complex are also provided. The biomolecule may be complexed with one of the polymers before it is complexed with the oppositely charged polymer. The complex is exposed to conditions that cause the formation of precipitated microcarriers, such as a change in pH or the addition of a complexing molecule. The compositions are preferably formulated into microcarriers.

Abstract: Disclosed is an oral controlled release macrolide pharmaceutical formulation. In a preferred embodiment, the formulation comprises a citrate salt of a preferred macrolide, clarithromycin. Also disclosed are methods for preparing, isolating and characterizing soluble and stable citrate salt of macrolides and use thereof in all solid dosage forms of macrolides.

Abstract: The present invention provides storage stable, shaped particles of allotropic organic compounds. The particles of the present invention can be shaped according to the desired application. Preferred shapes of such particles are microspheres, particularly those having diameters of about 1 to about 1,000 microns. The stable shaped particles of the present invention are particularly well-suited to the fabrication of pharmaceutical formulations, particularly where sustained release and uniform bioavailability are desired. The storage stable particles are formed by a solid state crystallization of allotropic organic compounds. The solid state crystallization process of the present invention affords a means for achieving a storage stable crystalline form of said allotropic compound without loss or deterioration of the original particle dimensions.

Abstract: An antibiotic product for delivering at least Tetracycline or Doxycycline that is comprised of three dosage forms with different release profiles with each of Tetracycline and Doxycycline being present in at least one of the dosage forms.

Abstract: A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate.

Abstract: The present invention relates to oral dosage forms comprising a) one or more active ingredients b) a formulated mixture of polyvinyl acetate and polyvinylpyrrolidone c) where appropriate other excipients customary for producing the dosage form, wherein they float on gastric fluid and display delayed release of active ingredient, and to the use and production thereof.

Abstract: This invention relates generally to the production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals. Advantageously, the inorganic used is calcium sulfate.

Abstract: The invention relates to a pharmaceutical formulation containing tolterodine or a tolterodine-related compound, or a pharmacologically acceptable salt thereof, as active ingredient, in which the formulation exhibits a controlled in vitro release of the active ingredient in phosphate buffer at pH 6.8 of not less than about 80% after 18 hours, and after oral administration to a patient is capable of maintaining a substantially constant serum level of the active moiety or moieties for 24 hours. The invention also relates to the use of the pharmaceutical formulation for treating overactive bladder and gastrointestinal disorders.

Abstract: A pharmaceutical dosage form such as a capsule capable of delivering therapeutic agents into the body in a time-controlled or position-controlled pulsatile release fashion, is composed of a multitude of multicoated particulates (beads, pellets, granules, etc.) made of one or more populations of beads. Each of these beads except an immediate release bead has at least two coated membrane barriers. One of the membrane barriers is composed of an enteric polymer while the second membrane barrier is composed of a mixture of water insoluble polymer and an enteric polymer. The composition and the thickness of the polymeric membrane barriers determine the lag time and duration of drug release from each of the bead populations. Optionally, an organic acid containing intermediate membrane may be applied for further modifying the lag time and/or the duration of drug release.

Abstract: An antibiotic product for delivering at least Amoxicillin or dicloxacillin that is comprised of three dosage forms with different release profiles with each of Amoxicillin and dicloxacillin being present in at least one of the dosage forms.

Abstract: An antibiotic product for delivering at least cephalosporin or Metronidazole that is comprised of three dosage forms with different release profiles with each of cephalosporin and Metronidazole being present in at least one of the dosage forms.

Abstract: Film coatings for enteric and colonic release at selected pH are provided by selecting and/or formulating a shellac of a predetermined acid number. The method includes the selection of the acid number to provide the release at the specified pH and a method of providing a shellac of a predetermined acid number by blending of shellacs of different acid numbers. In general, films that release or dissolve at or above pH 7.4 are based on the selection of shellac with an acid number below 74. Films that release or dissolve above pH 7.0 are comprised of shellac selected with an acid number below 80. Films that release or dissolve at below pH 7.0 are comprised of shellac selected to have an acid number above 80. The film coating may be modified with a water soluble resin and/or a plasticizer. Preferably the shellac will comprise 50% or more of the resin system, and is formed out of water, not alcohol.

Abstract: The invention is directed to self-assembling, polymer-based delivery systems for proteins. The delivery systems comprises an active agent and a polyol ester of the invention, having a linear polyol containing six or more hydroxyl groups as a central backbone and biodegradable hydroxy carboxylic ester groups attached to the central backbone.

Abstract: An oral pharmaceutical dosage form comprising an acid susceptible proton pump inhibitor and one or more NSAIDs in a fixed formulation, wherein the proton pump inhibitor is protected by an enteric coating layer. The fixed formulation is in the form of an enteric coating layered tablet, a capsule or a multiple unit tableted dosage form. The multiple unit dosage forms are most preferred. The new fixed formulation is especially useful in the treatment of gastrointestinal side-effects associated with NSAID treatment.

Abstract: A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed.

Abstract: An enteric coated pharmaceutical dosage form comprising an H+,K+-ATPase inhibitor is disclosed. The dosage form comprises at least two portions of the H+,K+- ATPase inhibitor to be released in at least two consecutive pulses. The dosage form has at least one fraction with a pulsed delayed release and another fraction with instant release of the H+,K+-ATPase inhibitor. The portions are released in time by from 0.5 and up to 12 hours interval, preferably by from 0.5 and up to 8 hours, and more preferably by from 0.5 and up to 4 hours interval. The dosage form is intended for once daily administration.

Abstract: An antibiotic product for delivering at least Amoxicillin or Clarithromycin that is comprised of three dosage forms with different release profiles with each of Amoxicillin and Clarithromycin being present in at least one of the dosage forms.

Abstract: Desoxypeganine and its pharmaceutically acceptable acid addition salts can be used in the treatment of drug addiction or drug dependence. Said substances are administered preferably in a continuos and controlled manner. The pharmaceutical administration form enables controlled release, e.g. for oral transdermal or another route of parenteral administration.

Abstract: An oral pharmaceutical modified release multiple-units composition for the administration of a therapeutically and/or prophylactically effective amount of a non-steroid anti-inflammatory drug substance to obtain both a relatively fast onset of the therapeutic effect and the maintenance of a therapeutically active plasma concentration for a relatively long period of time is disclosed.

Abstract: A method is provided for encapsulating sperm in a particle wherein the particle provides for the timed release of the sperm. In particular, the method uses a gel forming polymer to form the particle and a medium for maintaining most of the sperm in a non-capacitated stage while it is encapsulated. Further provided is a method for artificial insemination using the encapsulated sperm wherein the sperm is naturally or artificially capacitated after the artificial insemination. In an embodiment, capsules containing a core of sperm in a semen extender are formed as a mixture having membranes of different thicknesses to provide varying time of sperm release. In another embodiment, the sperm and extender are dispersed throughout solid beads that vary in chemical property and diameter to provide varying time of sperm release. The extender may be free of glucose, xanthine oxidase and H2O2, and contain fructose, fructose-6-phosphate, pyruvate, lactate or mixtures thereof as a carbohydrate source.

Abstract: A sustained/prolonged release pharmaceutical dosage form is disclosed. The form comprises a hard shell capsule and a formulation comprising (a) a water insoluble medicant, (b) a high melting fatty ester, (c) a low viscosity oil, (d) a cellulosic polymer, and (e) a non-ionic surfactant.

Abstract: Precursor polyhydric alcohol esters where acyl moieties originate from aliphatic homopolymer or copolymer polyesters and contain free hydroxyl at their terminal ends, are reacted to provide 2-carboxy ethenyl groups. The resulting products can be used in formation of hydrogels for drug delivery or can be reacted to attach aminoxyl radical or drug molecule residue or other biologically active agent for delivery of these, for example, from vascular stents.

Abstract: The invention provides fenofibrate compositions comprising granulates. The granulates can comprise micronized fenofibrate, inert hydrosoluble carrier particles, hydrophilic polymers, and, optionally, surfactants.

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

Abstract: The present invention is to provide a sustained-release preparation which comprises a compound having angiotensin II antagonistic activity, its pro-drug or their salt, and a biodegradable polymer, and if necessary, a polyvalent metal, and which is highly stable and active and shows angiotensin II antagonistic activity while maintaining circadian rhythm of blood pressure for a long time.

Abstract: Disclosed herein is sustained-release formulations of tramadol comprising tramadol saccharinate coated with at least one sustained-release coating. The sustained release formulations may also contain tramadol in non-sustained release form, and other pharmaceutically acceptable excipients. Also disclosed are methods of preparation of and methods of treatment using the inventive formulations.

Abstract: Sustained release formulation containing tacrolimus or its hydrate is provided. The time (T63.2%) required for 63.2% of the maximum amount of tacrolimus or its hydrate to be dissolved is 0.7 to 15 hours. The time is measured in accordance to the Japanese Pharmacopoeia, the 13-th edition, Dissolution Test, No. 2 (Puddle method, 50 rpm) using an aqueous 0.005% hydroxypropyl cellulose solution. This aqueous test solution is adjusted to pH 4.5, accordingly. The formulation further comprise a solid base which is a water-soluble polymer and/or wax. The formulation is in the form of a powder, fine powder, granule, tablet or capsule. Furthermore, the formulation is administered to a patient once a day for preventing organ or tissue rejection by transplantation or autoimmune diseases.

Abstract: There is disclosed a method for stabilizing active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, by means of anhydrous granulation of active substances and dried pharmaceutically acceptable auxiliary substances for the preparation of pellet cores or granules. All pharmaceutically acceptable auxiliary substances employed are dried before use so that their weight loss at drying is less than 1.0% of the total weight of the pharmaceutically acceptable auxiliary substance, preferably less than 0.5%. Organic solvents used in process of anhydrous granulation should contain less than 0.2% of water. A novel pharmaceutical formulation with controlled release of active substances that are unstable in acidic medium, unstable when stored for longer periods of time in the presence of water and at the same time sensitive to heating, is disclosed as well.

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 controlled release formulation of lipoic acid is disclosed. The lipoic acid is combined with excipient materials in such a way that those materials provide for gradual release of the lipoic acid in a manner which makes it possible to substantially increase the period of time over which therapeutic levels of lipoic acid are maintained relative to a quick release formulation. These features make it possible to use lipoic acid to reduce serum glucose levels and maintain those levels over time thereby obtaining a range of desired therapeutic results.

Abstract: Methods for preparing biodegradable microparticles are provided. Also provided are microparticles prepared by the method which include IGF-1 entrapped therein. The microparticles allow for controlled release of IGF-1 and other polypeptides over prolonged periods of time.

Abstract: The present invention provides solid pharmaceutical compositions for improved delivery of a wide variety of pharmaceutical active ingredients contained therein or separately administered. In one embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier including a substrate and an encapsulation coat on the substrate. The encapsulation coat can include different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides. In another embodiment, the solid pharmaceutical composition includes a solid carrier, the solid carrier being formed of different combinations of pharmaceutical active ingredients, hydrophilic surfactants, lipophilic surfactants and triglycerides. The compositions of the present invention can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients, such as drugs, nutrionals, cosmeceuticals and diagnostic agents.

Abstract: An osmotic delivery system for controlled delivery of a beneficial agent includes an implant capsule having a beneficial agent reservoir, an osmotic agent which expands on contact with fluid imbibed through a permeable membrane retained by the implant capsule, a delivery port, and a valve for opening and closing the delivery port. When the osmotic agent expands, a pressure is exerted against a separating member positioned between the beneficial agent reservoir and the osmotic agent. The separating member moves within the capsule, thereby forcing the valve to move a distance such that the beneficial agent can exit the reservoir through the delivery port.

Abstract: Urinary incontinence is alleviated in a mammal by administering to the mammal a urinary incontinence alleviating amount of dextromethorphan, dextrorphan, their mixtures and/or pharmaceutically acceptable salts, alone or in combination with a pharmacologically active agent such as an anticholinergic, sympathomimetic, tricyclic antidepressant, antispasmodic, direct-acting smooth muscle relaxant, estrogen, compound having estrogen-like activity, or any combination of the foregoing.

Abstract: A pharmaceutical product. The pharmaceutical product includes a container constructed from a material containing one or more of polypropylene, polyethylene, and ionomeric resins. The container defines an interior space. A volume of a fluoroether-containing inhalation anesthetic is contained in the interior space defined by the container.

Abstract: Novel pharmaceutical dosage forms provide for pulsatile delivery of methylphenidate, i.e., release encapsulated drug in spaced apart “pulses.” The dosage forms are comprised of first, second and optionally third dosage units, with each dosage unit having a different drug release profile. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads or particles, or may comprise a single tablet with the first, second and optionally third dosage units each representing an integral and discrete segment thereof. Methods of treatment using the pharmaceutical dosage forms are provided as well.

Abstract: There is provided a coating composition that masks the undesirable taste of a pharmaceutically active ingredient, i.e. drug or medicine, that is consumed orally. The coating composition has polyvinyl acetate, and a dimethylaminoethyl methacrylate and neutral methacrylic acid ester. Optionally, an alkaline modifier may be included in the coating composition to enhance release of the active ingredient.

Abstract: A dosage form is disclosed comprising a semipermeable walled container that houses a capsule, which capsule comprises a drug formulation, a piston, and an osmotic composition. The dosage form delivers the drug formulation through a passageway at a controlled rate over a sustained-release period of time up to 24 hours.

Abstract: A resin composition is prepared by reacting components comprising dibasic acid, diamine, polyol and monoalcohol, wherein (a) at least 50 equivalent percent of the dibasic acid comprises polymerized fatty acid; (b) at least 50 equivalent percent of the diamine comprises ethylene diamine; (c) 10-60 equivalent percent of the total of the hydroxyl and amine equilvalents provided by diamine, polyol and monoalcohol are provided by monoalcohol; and (d) no more than 50 equivalent percent of the total of the hydroxyl and amine equivalents provided by diamine, polyol and monoalcohol are provided by polyol. This resin composition may be formulated into, for example, personal care products, fragrance releasing products and candles.

Abstract: The present invention is an improvement in the treatment of mania and depression by administering topiramate in a sustained-release formulation. The sustained-release formulation of the present invention may also be co-administered with anti-psychotics and anti-depressants.

Abstract: An insecticidal bait composition which is particularly useful against social insects, such as cockroaches and ants is disclosed. The bait composition comprises a solid or semi-solid bait matrix including a food material for an insect and one or more non-microencapsulated insecticides in an amount effective to act essentially as a primary kill agent and one or more microencapsulated insecticides, excluding pyrethroids, in an amount effective to act essentially as a secondary kill agent, the non-microencapsulated insecticide and microencapsulated insecticide being the same or different.

Abstract: An oral solid dosage form includes a therapeutically effective amount of an NSAID and a proton pump inhibitor in an amount effective to inhibit or prevent gastrointestinal side effects normally associated with the NSAID. Also disclosed is a method of treating a human patient in need of antiinflammatory, analgesic and/or antipyretic therapy, comprising orally administering to the patient an oral pharmaceutical dosage form which includes a therapeutically effective amount of an NSAID and an amount of a proton pump inhibitor effective to substantially inhibit gastrointestinal side effects of the NSAID. The invention is further related to a method of prophylactically treating a human patient who is on a therapy known to have significant gastrointestinal side effects or is about to begin such a therapy, via concurrent administration of an NSAID and a proton pump inhibitor in a combination (single) oral dosage form.

Abstract: Provided is an oral dosage form suitable to deliver a combined dosage of progesterone and which upon delivery through the gastrointestinal tract provides a blood concentration of from about 0.1 ng/ml to about 400 ng/ml progesterone; said dosage form comprising a combination that includes (a) a first solid form comprising from about 25 mg to about 500 mg micronized progesterone in a solid polyethylene glycol carrier having an average molecular weight of from about 1000 to 10,000 and constituting at least about 30% of said first solid form; and (b) a second solid form comprising an estrogen.

Abstract: An antibiotic product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as two or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.

Abstract: A stabilized insect mating disruption pheromone compositions comprising an insect pheromone and 2,2′-Methylenebis(6-t-butyl-p-cresol). Methods of use and microcapsules containing these compositions are also provided.