Abstract: The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features pharmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.

Abstract: A pharmaceutical composition is disclosed which comprises multiparticulates wherein said multiparticulates further comprise an azithromycin core and an enteric coating disposed upon said azithromycin core.

Abstract: The present invention relates to a process for producing solid oral dosage forms with sustained release of active ingredient, comprising at least one active ingredient, a preformulated mixture of polyvinyl acetate and polyvinylpyrrolidone, where appropriate, water-soluble polymers or lipophilic additives and, where appropriate, other conventional excipients, wherein this mixture or parts of this mixture are granulated by heating to from 40° C. to 130° C., and the granules are, after admixture with conventional excipients, subsequently tabletted.

Abstract: This invention provides novel methods for the formation of biocompatible membranes around biological materials using photopolymerization of water soluble molecules. The membranes can be used as a covering to encapsulate biological materials or biomedical devices, as a “glue” to cause more than one biological substance to adhere together, or as carriers for biologically active species. Several methods for forming these membranes are provided. Each of these methods utilizes a polymerization system containing water-soluble macromers, species, which are at once polymers and macromolecules capable of further polymerization. The macromers are polymerized using a photoinitiator (such as a dye), optionally a cocatalyst, optionally an accelerator, and radiation in the form of visible or long wavelength UV light. The reaction occurs either by suspension polymerization or by interfacial polymerization.

Abstract: A composition for delivery of osteogenic proteins is disclosed. The composition comprises an osteogenic protein, a calcium phosphate material as a carrier, and an effective amount of an effervescent agent. Methods of making the compositions and methods of using the osteogenic compositions to treat osteoporotic and/or osteopenic bone are also disclosed.

Abstract: Provided are pharmaceutical formulations comprising sustained release particles each having an inner core bead comprising an active pharmaceutical ingredient an intermediate coating substantially surrounding the inner core bead, and an outer coating substantially surrounding the intermediate coating comprising a pH independent polymer. Also provided is a pharmaceutical formulation comprising two bead populations wherein each of the first and second bead populations have a different drug release profile. Also provided is a method of preparing an extended release dosage composition comprising one or more bead populations.

Abstract: The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 ?n substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect.

Abstract: The present invention is directed to pharmaceutical nanoparticulate compositions of an immunosuppressive agent. The pharmaceutical compositions comprise solid particles of an immunosuppressive agent having an effective average particle size of less than about 2000 nm and one or more surface stabilizers associated with the surface of the immunosuppressive agent particles.

Abstract: Compressible solid tablets comprising from 20 to 38 wt % of an oily or viscous liquid, from 50 to 70 wt % of a cellulose polymer and from 2 to 15 wt % of an hydrophobic coating compound, wherein said particles size is 180 microns or less. For example, the oily or viscous liquid may consist of plant oils or surfactants such as cocamide DEA, cocoamide propyl betaine and or mixtures thereof. The cellulose polymer may be carboxy methyl cellulose, microcrystalline cellulose or mixtures thereof. The coating hydrophobic composition may be silicon dioxide, calcium orthophosphate, magnesium carbonate, aluminum oxide. Compressible solid particles are also disclosed which comprise from 50 to 70 wt % of a crystalline alcohol, from 25 to 45% of a cellulose polymer and from 5 to 18 wt % of a coating hydrophobic compound. For example, the crystalline alcohol may be a polyol such as xylitol, isomaltose, sorbitol, maltitol, starch hydrolysate; a terpene such as thymol, carvacrol or menthol.

Abstract: Microencapsulated delivery vehicles comprising an active agent are disclosed. The microencapsulated delivery vehicles may be introduced into products such that, upon activation, the product provides a functional benefit to a substrate, such as a user's skin.

Abstract: The present invention relates to coated particles and pharmaceutical dosage forms comprising the active substances sensitive to environmental influences. The coating of the present invention provides stability and protection of the active substance to environmental influences and in particular from oxidation and/or environmental humidity by coating.

Abstract: A highly porous, fast-disintegrating binder suitable for pharmaceutical applications and methods of making the same are disclosed, the binder comprising microporous particles of an aqueous-soluble cellulosic polymer and a wicking agent. Pharmaceutical compositions and fast-disintegrating dosage forms containing the binder are also disclosed.

Abstract: The present invention relates to compositions and methods of treating human subjects with a beta-adrenergic receptor blocking agent (“beta-blocker”) provided in a time-sustained-release delivery system. The time-sustained-release drug delivery systems includes at least three populations of beads, where each population of beads includes a beta-blocker. The beads may be selected from immediate-release beads, enteric-release beads, sustained-release beads, and time-sustained-release beads. The beta-blocker may be selected from acebutolol, atenolol, betaxolol, bisoprolol, esmolol, metoprolol, nebivolol, butoxamine, carteolol, carvedilol, labetalol, nadolol, oxprenolol, penbutolol, propranolol, pindolol, sotalol, and timolol. According to presently preferred embodiments, the beta-blocker is propranolol.

Abstract: A pharmaceutical dosage form comprising non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, along with a second active ingredient having a shorter therapeutically effective plasma concentration duration, such as phenylephrine, and methods of administering the same are provided. This method provides improved therapeutic effect, in particular pain relief along with decongestant relief, over extended time periods.

Abstract: Pharmaceutical compositions of topiramate for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined release profile. Method of treating or preventing pathological disorders in mammalian subjects comprising the administration of the novel formulations disclosed herein is also provided.

Abstract: A pharmaceutical composition may include a granulate which may include at least one active pharmaceutical ingredient susceptible to abuse by an individual mixed with at least two materials, a first material that is substantially water insoluble and at least partially alcohol soluble and a second material that is substantially alcohol insoluble and at least partially water soluble, wherein the active pharmaceutical ingredient and the two materials are granulated in the presence of water and alcohol. The composition may also include a coating on the granulate exhibiting crush resistance which may have a material that is deposited on the granulate using an alcohol based solvent. The composition further comprises a second particle comprising a fat/wax. The present invention also includes a coated granulate, various dosage forms of the composition, as well as methods of production and tableting.

Abstract: The present invention provides methods of treating heart failure and improving renal function, and/or preventing the advancement of heart failure into advanced stages, and methods of counteracting ischemia due to a myocardial infarction by providing improved methods of administering a therapeutically effective amount CGRP as a controlled release formulation. The therapies can be administered on an outpatient or inpatient basis and can further be used as maintenance therapies.

Abstract: The present invention relates to a controlled release system that can be incorporated in cosmetic, personal care, and household products to effectively encapsulate wide range of active ingredients and sensory markers and release them in response to moisture or over an extended period of time. The controlled release system of the present invention consists of oil absorbing polymer nanospheres coated with water sensitive surface active polymers.

Abstract: The invention provides a process for the production of drug carrier pellets comprising spray-drying a solution of a physiologically tolerable cellulosic binder containing a physiologically tolerable inert particulate carrier having a particle size D (v, 0.5) of less than 50 ?m.

Abstract: This invention relates to orally disintegrable, lorazepam-containing dosage forms which are storage stable and disintegrable within about 90 seconds or less. In one embodiment, there is provided a storage stable, orally disintegrable dosage form comprising: protected lorazepam particles comprising lorazepam and polymeric material having a glass transition temperature of about 65° C. or above. Also disclosed is a method of producing a storage stable lorazepam containing tablet.

Abstract: A stabilized solid controlled release dosage form having a coating derived from an aqueous dispersion of ethylcellulose is obtained by overcoating a substrate including a therapeutically active with an aqueous dispersion of ethylcellulose and then curing the coated substrate at a temperature and relative humidity elevated to a suitable level above ambient conditions until the coated dosage form attains a stabilized dissolution profile substantially unaffected by exposure to storage conditions of elevated temperature and/or elevated relative humidity.

Abstract: The present invention relates to a controlled release pellet of metoprolol and its pharmaceutically acceptable salts that uses a water soluble or a water swellable inert starting seed or core.

Abstract: A method of forming particles, comprises accelerating a first stream comprising a first liquid, applying a charging voltage of at most 1.5 kV to the first stream, and vibrating the first stream, to form particles.

Abstract: Coated particles of metal (such as calcium) silicate that exhibit excellent odor neutralization and sebum absorption properties when present within certain cosmetic and/or personal care formulations and suspensions are provided. Uncoated calcium silicate exhibits a high pH level that may have a deleterious effect upon such cosmetic and/or personal care compositions, thereby rendering the overall composition ineffective for its intended purpose, particularly if the calcium silicate is present in its usual state at high loading levels. Alternatively, if certain materials present within personal care compositions exhibit a sufficiently low pH level, the effectiveness of such calcium silicates may be compromised as well.

Abstract: Coated particles of metal (such as calcium) silicate that exhibit excellent odor neutralization and sebum absorption properties when present within certain cosmetic and/or personal care formulations and suspensions are provided. Uncoated calcium silicate exhibits a high pH level that may have a deleterious effect upon such cosmetic and/or personal care compositions, thereby rendering the overall composition ineffective for its intended purpose, particularly if the calcium silicate is present in its usual state at high loading levels. Alternatively, if certain materials present within personal care compositions exhibit a sufficiently low pH level, the effectiveness of such calcium silicates may be compromised as well.

Abstract: The present invention is directed to small interfering RNA molecules targeted against a gene of interest in respiratory epithelial cells, and methods of using these RNA molecules.

Abstract: Provided are a solid preparation comprising an enteric solid dispersion that allows a drug in the preparation to be rapidly dissolved without impairing the dissolution of the solid preparation, and a method for producing the same. More specifically, provided are a solid preparation comprising a poorly soluble drug, an enteric polymer, an excipient and a disintegrator, a mixed powder comprising at least the excipient and the disintegratior is partly or entirely covered with a solid dispersion comprising the poorly soluble dug and the enteric polymer; and a method for producing a solid preparation, comprising steps of: spraying an enteric polymer solution in which a poorly soluble drug has been dispersed or dissolved, on a mixed powder comprising an excipient and a disintegrator; and granulating and drying a resultant.

Abstract: Provided are a granule or a tablet of a solid dispersion that allows a drug in a preparation to be rapidly dissolved without impairing the dissolution of the solid dispersion, and a method for producing the same.

Abstract: The invention relates to a stable medicament for oral administration which comprises (a) a core which contains an active ingredient selected from Omeprazole, Lansoprazole and Pantoprazole, together with customary pharmaceutical adjuvants, (b) an intermediate layer applied onto the core, and (c) a gastric juice-resistant outer layer. The intermediate layer in (b) is formed as a reactive layer in which a gastric juice-resistant polymer layer material partially neutralized with alkali with cation exchange capacity is present. Further, a method for the production of the stable medicament is disclosed.

Abstract: Compositions and methods for reducing inflammation and pain associated with acidosis. One embodiment of the composition comprises a plurality of carrier particles, wherein the plurality of carrier particles hold a plurality of alkaline compounds, and wherein the alkaline compounds can be delivered to, and absorbed across, lipid membranes into the blood stream in small quantities over an extended period of time.

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: Dosage forms comprising therapeutically active compounds are disclosed herein.

Abstract: A stable composition with a benzimidazole derivative, such as Omeprazole, which does not contain a separating layer between the active compound and an enteric coating layer. Instead, the enteric coating layer is applied as a solution with a pH value of at least 6.5, and more preferably in a range of from about 7 to about 10, directly to the benzimidazole derivative substrate. This solution, with the optional addition of a plasticizer, can be directly coated onto the substrate without any necessity for an intermediate layer. Furthermore, in this pH range, the enteric coating is optionally applicable in an aqueous solution, thereby obviating the need for organic solvents for dissolving the enteric coating material. The resultant formulation maintains the stability of the benzimidazole derivative during storage and at the same time protects the product during passage through the acidic environment of the stomach.

Abstract: Microparticles and a method for their production is described. The process of the present invention provides a simple, quick, and efficient one-pot process for the production of microparticles containing a hydrophilic active agent of various and uniform morphologies, including microcapsules, microspheres, and microsponges. The microparticles are preferably used for pharmaceutical applications.

Abstract: This invention relates to a controlled release encapsulated dry powder that is formed by an emulsion comprising: A) a fully hydrolyzed polymer, B) a hydrophobic silica, C) a modified corn starch, and D) at least one fragrance oil, which is emulsified in water and spray dried to evaporate the water obtaining the encapsulated dry powder. This invention also relates to a process for the preparation of a controlled release encapsulated dry powder that is formed by an emulsion, which is spray dried. The controlled release encapsulated dry powder is used in deodorant and antiperspirant applications.

Abstract: Taste masked particles and chewable tablets made therefrom are disclosed. The taste masked particles comprise a core containing an active ingredient and a polymeric coating covering said core, said coating comprising a mixture of a) an enteric polymer; and b) an insoluble film forming polymer, the surface of said particle being free of active ingredient. The chewable tablets provide immediate release of the active ingredient.

Abstract: The present invention is directed to parenterally-administrable microparticles for providing sustained-release of a therapeutic agent in the body, where the microparticles include a polymeric core containing a therapeutically effective amount of a therapeutic agent disposed therein, a first film encapsulating the core, the first film prepared from a first biodegradable polymer soluble in an appropriate solvent therefore, and a second film encapsulating the core and the first film, the second film prepared from a biodegradable polymer soluble in an appropriate solvent therefore, wherein the first film is insoluble in the solvent used to prepare the second film, and to parenterally-administrable compositions containing such microparticles dispersed in a suitable carrier therefore.

Abstract: A pharmaceutical composition of anti-tubercular drugs for oral use comprising Rifampicin and/or Isoniazid wherein the bioavailability of Rifampicin and/or other drugs is enhanced. Preferably the bioavailability of Rifampicin is enhanced by preventing its degradation caused by presence of Isoniazid. Rifampicin and/or Isoniazid may be present in delayed release and/or extended release form such that minimal amount of the drug is dissolved between pH 1 and 4. preferably delayed release of Rifampicin and/or Isoniazid is achieved by treating the drugs with pH sensitive polymers.

Abstract: A method for making the potassium, sodium and other hygroscopic salts of (?)-hydroxycitric acid and mixtures thereof workable by initial treatment with a desiccating agent, such as fumed silicon dioxide. These may be further rendered non-hygroscopic and non-reactive in acidic media via subsequent encasement in hydrophobic and acidophobic polymers. The calcium and magnesium salts of (?)-hydroxycitric acid likewise can be rendered nonreactive in acidic media. The resulting products are suitable for tableting, encapsulation and use in other dry media for weight loss, appetite suppression, improvements in fat metabolism and postprandial lipemia and other pharmaceutical purposes. Further, the products of this invention can be made nonreactive as components of acidic liquid drink mixes and snack bars and can be used in the production of controlled release administration formats.

Abstract: Improved starch-metal derivatives are provided which have excellent dry flow characteristics and ready dispersability in hot or cold water. The preferred derivatives comprise granules of starch which have been expanded or preswelled and cross-linked, followed by reaction with a polyvalent metal salt, especially salts of Ca, Mg, Zn Cu and Al.

Abstract: The present invention provides a composition for forming a compressed solid dosage form that is a free-flowing compressible admixture of simethicone, an adsorbant, and an optional active agent, wherein the weight ratio of simethicone to adsorbent is at least 1:2.22. Also included are solid dosage forms made from a free-flowing compressible admixture of simethicone, an adsorbant, and an optional active agent, wherein the weight ratio of simethicone to adsorbent is at least 1:2.22.

Abstract: The present invention is directed to nanoparticulate compositions comprising megestrol. The megestrol particles of the composition have an effective average particle size of less than about 2000 nm.

Abstract: A quinolinone derivative pharmaceutical composition comprising a quinolinone derivative represented by the structural formula (I): wherein the quinolinone derivative is in the form of particles, which have an average particle diameter of 0.5 to 10 ?m and such a particle size distribution that particles having a particle diameter of 15 ?m or less account for 90% or more of the totality of the particles, and also have a fusion enthalpy of 30 J/g or more, and the surface of the particles are coated with a water-soluble composition containing a water-soluble polymer, can quickly dissolve an active ingredient in the digestive tract and is also superior in long-term storage stability.

Abstract: A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

Abstract: This invention provides extended release potassium chloride granules consisting essentially of potassium chloride crystals having a mesh size of about 20–60 mesh that are coated only with ethylcellulose. The granules may be compressed into tablets that disintegrate rapidly in an aqueous environment to provide uniform dissolution of the potassium chloride. Tablets containing about 10 to about 20 milliequivalents potassium may be formulated in accordance with the invention. Processes to produce extended release granules without using surfactants, processing aids or other coating aids are also provided by this invention. A method is further provided whereby a patient's supplemental potassium requirements are met by administering an appropriate combination of dosage units chosen from available dosage units containing different quantities of potassium.

Abstract: Cosmetic and dermatological preparations having an effective content of bile acids, their salts and/or their derivatives, it being possible for said active ingredients to be present either individually or as a mixture.

Abstract: A fluid bed granulation process for manufacturing non-hygroscopic, stable granulates containing a water-soluble salt of S-adenosylmethionine is described. Said process comprises: a) the simultaneous, sequential or alternate dispersion of at least a solution of a water-soluble salt of SAMe (A) and of a solution of a coating agent (B), on a fluid bed granulation carrier (C) and b) the fluid bed granulation of the mixture. Granulates obtainable by said process and solid oral pharmaceutical forms obtainable by said granulates are disclosed.

Abstract: Process for encapsulation of an uncharged crystalline solid particle include treating the crystalline solid particle material with amphiphilic substances and subsequently coating the material with a layer of charged polyelectrolyte or coating the material with a multilayer comprising alternating layers of oppositely charged polyelectrolytes.

Abstract: Pharmaceutical compositions useful for treating autoimmune diseases in a mammal comprising as an active ingredient a therapeutically effective amount of Copolymer 1, and microcrystalline cellulose are disclosed. Processes for the manufacture of such compositions are also disclosed.

Abstract: Formulations are provided herein which allow for a once daily dosing regimen for amoxicillin and clavulanic acid.