Abstract: A controlled release microcapsulate pharmaceutical formulation for burst-free, sustained, programmable release of hydrophobic bioactive agent over a duration from 24 hours to 100 days comprising: and a blend of end-capped uncapped biocompatible, biodegradable poly(lactide/glycolide).

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: A method of treating patients, particularly for pain and/or symptoms of erythromelalgia, and other neurovascular or neuropathic disorders, etc. involves administering high doses of magnesium. The magnesium is introduced through several daily administrations, totaling approximately 2-12 times the RDA for magnesium. These higher levels are achieved through increasing daily dosage amounts gradually in response to patient tolerance and until beneficial results are seen. Total magnesium intake is divided over several doses per day and taken with copious amounts of water.

Abstract: The invention relates to new biologically degradable aliphatic copolymers of the polyesteramide or polyesterurethane type. The invention further relates to a method for preparing the copolymers and to products which can be manufactured from the new copolymers.

Abstract: A sport fishing system having: a rod and reel, including fishing line; at least one fishing lure or natural bait; and a controlled released fish attractant for applying to the fishing lure or natural bait. The system may further include an applicator for applying the controlled released fish attractant to the fishing lure or natural bait. In the preferred embodiment, the controlled release fish attractant includes: an attractant and a substantially hydrophobic, film forming release agent.

Abstract: This invention relates to a composition for use in treating benign prostatic hyperplasia including a saw palmetto extract provided in an oral controlled release formulation which allows release of active ingredients in the intestinal tract and which allows the maintenance of therapeutic levels of active agents in the bloodstream for prolonged periods of time. This invention also relates to a composition for improving the efficacy of a saw palmetto extract, a method of treating benign prostatic hypertrophy, and a method of improving the efficacy of a saw palmetto extract treatment.

Abstract: Bioerodible poly(orthoesters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents contain hydrogen bonding groups and &agr;-hydroxy acid-containing groups.

Abstract: The present invention relates to orally administrable multiple-unit sustained-release dose forms having controlled agitation-independent release of active compound and processes for their production using a selected erodable hydrophilic polymer (HPC) and a limitation of the maximum size of the active compound-containing polymer particles to ≦3 mm.

Abstract: A pharmaceutical delivery system comprising a slow-release formulation of vitamin C (ascorbic acid) and a plain-release formulation of vitamin E (tocopherol) has been found to raise and maintain the concentrations of these vitamins in the blood plasma to a ratio of approximately 2.2:1. The steady-state concentration and ratio of these antioxidants has been found to be critical in the prevention and treatment of oxidative stress related disorders such as arteriosclerosis and diabetes and neural degenerative disorders such as Alzheimer's Disease.

Abstract: Anthrax bio-terrorism is a poor man's nuclear bomb with devastating effects on the freedom and economy of any nation. No nation is immune. Urgently, there is a need for life saving technology that can be readily available and deployed in real time. Polystyrene sulfonate is the answer. It is life saving and will help in the development of next generation superior vaccines.

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: The invention is directed to sustained release formulations containing oxycodone or a pharmaceutically acceptable salt thereof which provide a mean C24/Cmax oxycodone ratio of 0.6 to 1.0 or 0.7 to 1 after oral administration at steady state to patients and methods thereof.

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 invention relates to a device for delaying the pylorus passage of orally administered medicament forms. Said device comprises a component which expands upon contact with the gastric juice and a polymer coat which is permeable to liquids but not to gases. The device can contain an active substance whose release into the gastric juice is mainly controlled by the medicament form into which it is incorporated. Unlike conventional medicament forms with delayed pylorus passage, the release of the active substance does not so much depend on the kind and structure of the polymer coat but is mainly determined by the incorporated medicament form. The inventive device can be easily rolled or folded and can be filled into capsules.

Abstract: The present invention provides a method for treatment of hypothyroidism in an adult comprising the long-term administration of T3 at a dose of 0.005-0.03 &mgr;g/kg body weight/hour/day.

Abstract: Controlled-release oral pharmaceutical compositions containing as active ingredient 5-amino-salicylic acid, comprising: a) an inner lipophilic matrix consisting of substances with a melting point below 90° C. in which the active ingredient is at least partly inglobated; b) an outer hydrophilic matrix in which the lipophilic matrix is dispersed; c) optionally other excipients.

Abstract: The present invention is drawn to a method of treating an unstable or overactive urinary bladder by treating the patient with tolterodine or a tolterodine-related compound, or pharmaceutically acceptable salt thereof, with a controlled release formulation that maintains a substantially constant serum level of the active moiety or moieties for at least 24 hours. The present invention is further drawn to a formulation for the method.

Abstract: The invention provides a novel soft gelatin capsule comprising a fill material consisting essentially of S-adenosylmethionine (SAMe) salt disposed within an enteric coated soft gelatin film.

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: Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.

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: 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: Controlled release of hydrophobic bioactive substances in vivo over an extended time period and without “bursts” of drug release is achieved using a liquid polymeric composition including a polymer such as poly(lactide-co-glycolide) copolymer in a mixture of hydrophilic and lipophilic solvents.

Abstract: This invention relates to a composition for use in treating benign prostatic hyperplasia including a saw palmetto extract provided in an oral controlled release formulation which allows release of active ingredients in the intestinal tract and which allows the maintenance of therapeutic levels of active agents in the bloodstream for prolonged periods of time. This invention also relates to a composition for improving the efficacy of a saw palmetto extract, a method of treating benign prostatic hypertrophy, and a method of improving the efficacy of a saw palmetto extract treatment.

Abstract: Constipation and Irritable Bowel Syndrome are treated by a delayed and sustained release composition of an opioid antagonist which commences release of the opioid antagonist in the mid to distal small intestine or ascending colon and provides sustained release along any remaining part of the small intestine and along the colon. Preferred opioid antagonists are naloxone and naltrexone.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: An antibiotic product, in particular a tetracycline, such as doxycycline, 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 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 composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for delivery of an active agent to a patient comprising administering to the patient a composition comprising a polypeptide and an active agent covalently attached to the polypeptide. Also provided is a method for protecting an active agent from degradation comprising covalently attaching the active agent to a polypeptide. Also provided is a method for controlling release of an active agent from a composition comprising covalently attaching the active agent to the polypeptide.

Abstract: This invention relates to a controlled or sustained release formulation designed to deliver a PDE4 inhibitor for treating an inflammatory disease such as asthma or COPD and the like.

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: A unit dose sustained-release oral dosage form containing a plurality of melt-extruded particles, each consisting essentially of a therapeutically active agent, one or more retardants, and an optional water-insoluble binder is disclosed. The particles have a length of from about 0.1 to about 12 mm and can be of varying diameters and each unit dose provides a release of therapeutically active agents over at least about 8 hours. Methods of preparing the unit doses as well as extrusion processes and methods of treatment are also disclosed.

Abstract: Microencapsulated and/or enteric coated compositions containing a mixture of sorbents with specific adsorption affinities for uremic toxins including ammonia, urea, creatinine, phenols, indoles, and middle molecular weight molecules and a bacterial source which metabolizes urea and ammonia are provided. Also provided are methods of using these compositions to alleviate symptoms of uremia in patients.

Abstract: A composition useful for reducing serum glucose levels by an oral controlled release system and a method for treating diabetes in a human being by controlling the blood glucose level (BGL) and reducing the complications associated with diabetic hyperglycemia and also the long term management of Non-Insulin Dependent Diabetes Mellitus (NIDDM) by avoiding the problems associated with the tight control of BGL, i.e., hypoglycemia tolerance and seizures. The composition is directed to a solid, hydrophilic matrix controlled release oral dosage form where the dosage form contains a therapeutically effective amount of antidiabetic drug in the matrix ensuring complete bioavailability of the drug from the matrix of the tablet.

Abstract: Copolymers of lactide and glycolide with high glycolide content. The average glycolate block length is less then about 3, which allows the copolymer to be soluble in slightly polar solvents such as methylene chloride.

Abstract: The invention encompasses novel salts of topiramate, and pharmaceutically acceptable polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, or amorphous forms thereof, as well as pharmaceutical compositions and pharmaceutical unit dosage forms containing the same. In particular, the invention encompasses pharmaceutically acceptable salts of topiramate, including without limitation topiramate sodium, topiramate lithium, topiramate potassium, or polymorphs, solvates, hydrates, dehydrates, co-crystals, anhydrous, and amorphous forms thereof. The invention further encompasses novel co-crystals or complexes of topiramate, as well as pharmaceutical compositions comprising them. The invention also encompasses methods of treating or preventing a variety of diseases and conditions including, but not limited to, seizures, epileptic conditions, tremors, cerebral function disorders, obesity, neuropathic pain, affective disorders, tobacco cessation, migraines, and cluster headache.

Abstract: Disclosed is a sustained-release preparation comprising 1) a polymer of lactic acid having a weight-average molecular weight of about 25,000 to about 60,000 and 2) a physiologically active substance, and which releases the physiologically active substance over a period of at least about 5 months; the sustained-release preparation shows an almost continuous zero order release of the physiologically active substance over a period of as long as about 5 months.

Abstract: The present invention provides new oral dosage formulations comprising a nicotine active, optionally combined with an antidepressant, which through the controlled release of the active ingredient(s) alleviate some of the nicotine withdrawal symptoms a person may experience during attempts to quit smoking.

Abstract: The efficacy of vitamins and other nutritional agents in treating and preventing various disease states is improved by administering therapeutically effective levels of these agents on a substantially continuous, 24-hour basis. The concentration of lipid peroxides formed by the autoxidation of lipids, and the concentration of oxygen free radicals, are reduced by continuously administering antioxidant agents. The regeneration of nerve tissue is improved by continuously administering at least one pharmaceutically-acceptable B complex vitamin.

Abstract: Pharmaceutical gastroretentive drug delivery systems for the controlled release of an active agent in the gastrointestinal tract are disclosed, which comprise: (a) a single- or multi-layered matrix comprising a polymer that does not retain in the stomach more than a conventional dosage form selected from (1) degradable polymers that may be hydrophilic polymers not instantly soluble in gastric fluids, enteric polymers substantially insoluble at pH less than 5.5 and/or hydrophobic polymers and mixtures thereof; (2) non-degradable polymers; and any mixtures of (1) and (2); (b) a continuous or non-continuous membrane comprising at least one polymer having a substantial mechanical strength; and (c) a drug; wherein the matrix when affixed or attached to the membrane prevents evacuation from the stomach of the delivery system for a period of time of from about 3 to about 24 hours.

Abstract: An osmotic pump having a minimally compliant, volume efficient piston positioned within a capsule. The capsule has an interior surface, a beneficial agent, and an osmotic agent. The piston is movable with respect to an interior surface of the capsule, and defines a movable seal with the interior surface of the capsule. The movable seal separates the osmotic agent from the beneficial agent. The piston has a length to total diameter ratio of about 1.1:1 and a core diameter to total diameter ratio of about 0.9:1. The piston enables greater beneficial agent and/or osmotic agent payload without increasing the size of the capsule. The osmotic agent imbibes liquid from a surrounding environment through a semipermeable body to cause the piston to move and in turn cause delivery of the beneficial agent from the capsule.

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: A polymer having a satisfactory balance between in vivo degradability and satisfactory mechanical properties, which is an A1BA2 type polymer comprising a segment A1 and a segment A2 each having a modified amino acid and a segment B consisting of polyethylene glycol with a number-average molecular weight of 8000 or higher bonded at one end to the segment A1 and at the other end to the segment A2, and has a number-average molecular weight of 10000 to 600000; an in vivo degradable material which comprises the polymer; and a film for preventing tissue adhesion, an artificial dura mater, a suture, an implant preparation, or a sustained-release drug base each comprising the degradable material.

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: An antibiotic product, in particular a betalactam such as cephalosporin (in particular cefuroxime and/or cefpodoxime) or a penicillin (in particular axmoxicillin or dicloxacillin) 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 levofloxacin, 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 a fluroquinilone such as ciprofloxacin, 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: Block copolymers based on poly(ortho esters) containing amine groups. These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.

Abstract: Pharmaceutical dosage units containing flupirtine or a pharmaceutically acceptable salt of flupirtine with controlled release of active substance using a delayed-action or controlled-release component. There are 0.001 to 20 parts delayed-action component for each part by weight flupirtine (calculated as the base) and the release rate of flupirtine is between 5 and 300 mg per hour. In some cases, the dosage units may also contain a rapidly releasing component of flupirtine or of one of its salts. The dosage units reduce the sedative effect of flupirtine.

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.