Abstract: The invention involves methods and products related to the micronization of hydrophobic drugs. A method of micronizing hydrophobic drugs using a set of solutions including an aqueous solution is provided. The invention also relates to products of micronized hydrophobic drugs and related methods of use.

Abstract: The invention relates to methods of treating mixtures containing polymeric materials, e.g., collagen, to form a polymer that intercalates into the polymeric material. The treatment provides greater tensile strength to the mixture, among other advantages. The polymer is formed of a monomeric unit having at least one catechol group that is oxidized to a quinone upon polymerization.

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: An oral pharmaceutical dosage form including a mixture of a delay release formulation of a non-steroidal anti-inflammatory drug (NSAID) and a mixture containing a prostaqlandin and one or more excipients.

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 relates to pharmaceutical compositions and methods for improved solubilization of triglycerides and improved delivery of therapeutic agents. Compositions of the present invention include a carrier, where the carrier is formed from a combination of a triglyceride and at least two surfactants, at least one of which is hydrophilic. Upon dilution with an aqueous medium, the carrier forms a clear, aqueous dispersion of the triglyceride and surfactants.

Abstract: This invention comprises pharmaceutical compositions for administering a biologically active compound to an animal. Particularly provided are proliposomal compositions that are advantageously used to deliver biologically active compounds to the gastrointestinal tract after oral administration.

Abstract: A sustained release formulation as a unit dose contains 100 mg-1000 mg of Acetaminophen and 15 mg-150 mg of tramadol hydrochloride, which comprises of 1) an immediate release portion comprising of 25%-75% of the total effective amount of drug in the dosage form and 2) a sustained release portion comprising of a) 25%-75% of the total effective amount of drugs in the dosage form; b) 6%-50% of gelling polymers of the total formulation, and c) optionally an enteric coating at a level of 5%-40% of the total formulation. The set forth formulation dissolves 25%-60% of the total drug in the first hour, 50%-90% of the total drug in the first four hours and not less than 80% of the total drug in the first 12 hours using USP dissolution method II at 50 rpm.

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 relates to an improved controlled delivery system that can be incorporated in dry granular, or powder, fabric care products, such as laundry detergents, tumble dryer sheets, rinse added products, and other fabric care products, to enhance fragrance performance. The controlled delivery system of the present invention comprises substantially free-flowing, powder formed of solid hydrophobic, positively charged, nano-spheres of encapsulated active ingredients, such as a fragrance, that are encapsulated in a moisture sensitive micro-spheres, solid spheres. The high cationic charge density of the nano-sphere improves fragrance deposition onto the laundered fabric.

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: The invention relates to adjuvants that contain a lecithin, an oil and an amphiphilic surfactant and that are capable of forming a stable oil-in-water emulsion vaccine so as to minimize local reactions to the vaccine in the injected animal.

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

Abstract: The present invention concerns orodispersible tablets, which are able to disintegrate in the buccal cavity upon contact with saliva by formation of an easy-to-swallow suspension, in less than 60 seconds, preferably in less than 40 seconds, containing fexofenadine in the form of coated granules, and a mixture of excipients comprising at least one disintegrating agent, a soluble diluent agent, a lubricant and optionally a swelling agent, a permeabilizing agent, sweeteners, flavoring agents and colors; the process for obtaining such orodispersible tablets and the coated granules incorporated therein and the use of said orodispersible tablets in the treatment of seasonal allergic rhinitis.

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: 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: A microcapsule system is used to store active agents and release them as a function of specific environmental parameters. The active agents are contained in capsules having a capsule wall comprising an environment-induced material. To allow sequential, time-controlled release of the active agents, provision is made for a plurality of capsules to be accommodated in at least one outer capsule, thereby forming an inner encapsulation layer, wherein the outer capsules form an outer encapsulation layer. Like the capsule wall of the inner capsules, the capsule wall of the outer capsule is made of an environment-induced material.

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: 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: A controlled release nutritional food supplement tablet having inner and an outer parts, the inner part being a slow release nucleus of melatonin and hydroxypropylmethylcellulose with the outer part being an immediate release cortex or coating of melatonin.

Abstract: The present invention relates to a novel spray drying process for the preparation of pharmaceutical compositions containing small particles of phospholipid-stabilized fenofibrate. This invention also relates to spray dried powdered compositions prepared according to this process, and to dosage forms of fenofibrate (capsules, tablets, powders, granules, and dispersions) prepared from these powdered compositions. The powdered compositions and dosage forms are useful in the treatment of dyslipidemia and dyslipoproteinemia and have the advantage that they provide reduced in vivo variability in the bioavailability of fenofibrate active species among fed and fasted patients when administered orally.

Abstract: Novel emulsion compositions which improve the rate and/or extent of absorption of drugs are disclosed. The novel emulsion compositions of the present invention include drug-containing emulsions adsorbed onto solid particles which may be further formulated into solid dosage forms, methods of preparing such emulsion compositions and their uses thereof. The emulsion compositions and their dosage forms improve the drug-load and the bioavailability of a wide range of drugs including drugs that are known or suspected of having poor bioavailability by the utilization of several different mechanisms.

Abstract: New compositions are disclosed that comprise the phytochemical Diindolylmethane (DIM), as well as its precursor, Indole-3-carbinol (I3C), and cogener, 2-(Indol-3-ylmethyl)-3,3′diindolylmethane (LTR-1), acceptable carriers and/or excipients. These compositions are administered to prevent or reduce symptoms associated with mastalgia and endometriosis.

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

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

Abstract: 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 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: 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: A method and controlled release oral unit dosage form of acetylsalicylic acid (aspirin) delays the release of the drug until a predetermined time interval after ingestion. This enables the drug to reach optimal therapeutic blood levels at a time in the early morning when the events leading up to a vascular obstruction culminating in a heart attack or stroke are most commonly occurring after the drug is taken in the evening. The convenience of taking the drug every evening should enhance compliance. By arranging for the optimal blood level to coincide with the peak incidence of strokes, a much smaller total dose of the drug may be used than is normally prescribed. This may reduce the incidence of side effects that are dose related. This will make the prophylactic use of aspirin available to more of the population.

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: 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 method of administering a medication to a post operative patient with the medication being administered at the site of a surgery performed on the patient. The medication is formed into a time release capsule (10) having a core (12) of the medication which is dispensed within the body over a predetermined period of time. The capsule is covered with a coating (14) that dissolves within the body. The time release medication is not released until the covering is sufficiently dissolved to expose the medication. During surgery, the surgeon places placing a plurality of capsules (10-10n) in the patient's body at the surgery site. The respective capsules have different coating thicknesses so the medication contained therein is dispensed at different periods of time after the surgery as a function of the thickness of the coating.

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 invention provides compositions comprising micronized fenofibrate, where the compositions have a dissolution of at least 10% in 5 minutes, 20% in 10 minutes, 50% in 20 minutes and 75% in 30 minutes, as measured using the rotating blade method at 75 rpm according to the European Pharmacopoeia, in a dissolution medium constituted by water with 2% by weight polysorbate 80 or 0.025 M sodium lauryl sulfate.

Abstract: Pharmaceutical capsule dosage forms of benzimidazole proton pump inhibitors are prepared by enclosing one or several enteric coated compressed cores in a capsule shell. The inventive formulations are stable and have higher bioavailability of the active ingredient relative to pellet and granule containing formulations.

Abstract: The pharmaceutical compositions of the present invention comprise orally administerable dosage forms that use effervescence as a penetration enhancer for drugs known, or suspected, of having poor bioavailability. Effervescence can occur in the stomach, once the tablet or other dosage form is ingested. In addition to effervescence in the stomach, or as alternative technique, by the use of appropriate coatings and other techniques, the effervescence can occur in other parts of the gastrointestinal tract, including, but not limited to, the esophagus, duodenum, and colon. The site of effervescence and drug release is chosen to correspond with the segment of the gastrointestinal tract displaying maximal absorption of the formulated drug, or to gain some other therapeutic advantage.

Abstract: The present invention relates to formulations for administering a growth hormone secretagogue. More specifically, the present invention relates to sustained release formulations for administering a growth hormone secretagogue and formulations for administering a growth hormone secretagogue that provide for a part of the dose of the growth hormone secretagogue to be administered using an immediate release formulation and part of the dose of the growth hormone secretagogue to be administered using a sustained release formulation.

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: 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: Dosage forms for oral administration of a methylphenidate drug are provided. The dosage forms provide a substantially immediate dose of methylphenidate upon ingestion, followed by one or more additional doses at predetermined times. By providing such a drug release profile, the dosage forms eliminate the need for a patient to carry an additional dose for ingestion during the day. The dosage forms and methods provided are useful in administering methylphenidate and pharmaceutically acceptable salts thereof, which generally require one or more doses throughout the day.

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 invention relates to the use of a preparation containing a first group of particles and at least one other group of particles which is not identical to the first group of particles for achieving controlled release of an active ingredient present in the cores of the particles, in particular in the human and veterinary medical sectors. The preparation is administered orally, rectally, vaginally etc. The release of the active ingredient then takes place in the appropriate medium, and there is transmucosal absorption of the active ingredient.