Abstract: This invention relates to a layered pharmaceutical composition comprising a combination of an antihistamine and a decongestant.

Abstract: The compositions of the present invention comprise a therapeutically effective amount of particles consisting of diphenhydramine or pharmaceutically acceptable salts thereof, optionally in combination with another drug such as pseudoephedrine, or phenylephrine and hydrocodone, in combination with rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol and/or a saccharide. These compositions are useful in treating the symptoms of one or more diseases or conditions in which diphenhydramine (alone or in combination with one or two other drugs) is a therapeutically effective, e.g. allergic rhinitis, sinusitis, upper respiratory tract infections, motion sickness, Parkinson's disease, insomnia, the common cold, and nighttime pain management, particularly for subjects or patients with dysphagia, and people ‘on the move’.

Abstract: Described is a pellet composition comprising a core element comprising morphine sulfate, a filler and a binder, wherein the morphine sulfate, calculated as the anhydrous form, comprises about 50 wt % to about 85 wt % of the total weight of the core element; and a coating disposed on at least a portion of the core element, the coating comprising an insoluble matrix polymer which is insoluble at pH 1 to 7.5; an enteric polymer which is insoluble at pH 1 to 4 and soluble at pH 6 to 7.5; and an acid soluble polymer which is soluble at a pH of 1 to 4, wherein the ratio of the acid soluble polymer to the enteric polymer is 1.45:1 to 2.5:1 on a weight basis. Also described are dosage forms comprising the disclosed pellets.

Abstract: The invention provides a composition useful for making oral dosage forms capable of dissolving in the mouth in less than 40 seconds without the need for a conventional super disintegrant and having a friability of less than 1%; wherein the composition includes liquiflash particles and an excipient mass. A preferred excipient mass according to the invention contains a directly compressible inorganic salt; a cellulose derivative or a combination of a directly compressible inorganic salt and a cellulose derivative. Preferably, the liquiflash particles and the excipient mass are combined in proportions such that the active ingredient remains substantially within the microspheres when the composition is compressed to obtain a dosage form having a hardness of 20 to 50 N. The compositions of the invention allow for the fabrication of oral dosages having improved hardness and friability.

Abstract: Coated pellets which comprise an active pharmaceutical ingredient that is poorly soluble in water, release at least 80% of the active ingredient under in vitro conditions in phosphate buffer at pH 5.0 after 30 minutes and are bioequivalent to a liquid formulation of the active ingredient under in vitro fed status test conditions and/or are coated with a composition, which includes a lipophilic component (A) and a hydrogel former (B), wherein the pure lipophilic component (A) has (i) an HLB value of ?5, and/or (ii) a melting range of ?60° C., and/or (iii) a solidification range ? of less than 35° C., and/or (iv) a density of ?0.80 g cm?3.

Abstract: Controlled release dosage forms are described herein. The controlled release formulations described herein provide prolonged delivery of high dose drugs that are highly water soluble and highly hygroscopic. In specific embodiments, controlled release dosage forms for delivery of a drug selected from GHB and pharmaceutically acceptable salts, hydrates, tautomers, solvates and complexes of GHB. The controlled release dosage forms described herein may incorporate both controlled release and immediate release formulations in a single unit dosage form.

Abstract: The present invention is directed to anti-hypertensive compositions comprising a nanoparticulate temocapril, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate temocapril particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of hypertension and related diseases.

Abstract: A method of treatment for epilepsy and other disease states is described, which comprises delivery of gabapentin in a gastric retained dosage form.

Abstract: Stabilized substituted benzimidazole modified release pharmaceutical formulations with at least two drug-containing fractions, wherein the release from a first fraction precedes the release from a second fraction, pharmaceutical excipients, processes for preparing the stable formulations, packaging therefor, and their use in treatment of erosive esophagitis and heartburn associated with non-erosive gastroesophageal reflux disease.

Abstract: This invention relates to the field of chemical pharmaceutical industry, namely, to pharmaceutical formulations for preparation of prolonged release tablets, in particular, tablets for sublingual application, and to methods of preparation of such formulations. Pharmaceutical formulation comprises 96.0 to 99.8% wt. of the pharmaceutical drug microcapsules, 0.1 to 1% wt. of lubricant, and 0.1 to 3% wt. of water, each microcapsule comprising 96.0 to 99.2% wt. of the pharmaceutical drug and 0.8 to 4% wt. of film-forming substance. Dispersant is also introduced into formulation in the amount of 0.1 to 10% wt. of the total mixture obtained. Method of preparation of the pharmaceutical formulation comprises preparation of microcapsules by deposition of coating of film-forming substance on non-agglomerated particles of pharmaceutical drug, and addition of lubricant and dispersant.

Abstract: The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol, whereby the ethanol resistance conferring coating layer comprises at least 70% by weight of a mixture of a polymeric portion a) and an excipients portion b), with the polymeric portion a) is consisting of a water insoluble essentially neutral vinyl polymer or vinyl copolymer and the excipients portion b) is consisting of the excipients b1) 100 to 250% by weight of a non-porous inert lubricant, b2) 1 to 35% by weight of a cellulosic compound, b3) 0.1 to 25% by weight of an emulsifier and additionally or alternatively to b3), b4) 0.

Abstract: Pharmaceutical compositions of metabotropic glutamate 5 receptor (mGlu5) antagonists or a pharmacologically acceptable salt thereof are disclosed. The compositions contain the therapeutic active compound with non-ionic polymer and ionic polymer, binder and fillers in either matrix pellet, matrix tablet or coated pellets. The compositions provide a pH-independent in vitro release profile with NMT 70% in one hour, NMT 85% in 4 hour, and NLT 80% in 8 hours. The compositions are useful for the treatment of CNS disorders, such as Treatment-Resistant Depression (TRD) and Fragile X Syndrome.

Abstract: Novel methods for making dosages form comprising a cushioning component. The methods of the present invention provides dosage forms which can be compressed to form compressed dosage forms that are substantially uniform in composition and robust and exhibit reduced friability. The invention also relates to methods for making fast-disintegrating dosage forms.

Abstract: A pharmaceutical product containing an active pharmaceutical ingredient and having a controllable release of the active pharmaceutical ingredient. The pharmaceutical product comprises yeast that is capable of fermentation. The carbon dioxide production of the fermentation releases the active pharmaceutical ingredient from the pharmaceutical product.

Abstract: The invention relates generally to methods of making formulations for delivering biological agents to a patient. In one aspect, proliposomal drug-delivery systems for medicaments are provided. In another aspect, coated proliposomal formulations for poorly water soluble drugs, and methods for making the same, are provided. Certain embodiments of the present invention provide enhanced stability and bioavailability for pharmaceutical formulations.

Abstract: By coating the surface of a powder comprising a silicone resin and/or an organic powder with a specific hydrophilizing agent, such powder is hydrophilized. Such coated (treated) powder has extremely great dispersibility (ease of dispersion) and very good dispersion stability (long-term dispersion stability with lapse of time) in aqueous dispersion media, particularly under acidic and alkaline conditions, specifically at pH 3 through 13. Using the surface-treated powder, additionally, a dispersion with good dispersibility (ease of dispersion) and great dispersion stability, preferably for cosmetics can be provided. The use of the surface-treated powder, or the use of the dispersion can provide further a cosmetic excellent in dispersibility and dispersion stability and further in re-dispersibility and dispersion stability with lapse of time and smooth feeling as compared to the related art when selecting aqueous cosmetic as an agent form.

Abstract: The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 ?m) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5.

Abstract: The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.

Abstract: Pharmaceutical presentations of phenoxathiin-based MAO-A inhibitors are disclosed whereby the MAO receptors are protected from binding to active ingredient in the stomach. Particular phenoxathiin-based MAO-A inhibitors include those of the following formula: (I) wherein n is 0, 1 or 2; R1 is a branched or straight chain C1-5 alkyl or C3-6 cycloalkyl optionally substituted with hydroxyl, or one or more halogens; and X1, X2, X3, X4, and X5 are either all hydrogens or one or two of X1, X2, X3, X4, and X5 are halogen and the remainder are hydrogens, with the proviso that when n is 0 or 1 and each X is hydrogen, R1 is not methyl. A wide variety of enteric mechanisms may be utilized so as to provide release of the active ingredient essentially out of the environment of the stomach after ingestion as a pharmaceutical presentation, such as a tablet or capsule. Presentations include enteric coated tablets, enteric coated capsules, capsules containing enteric coated beads.

Abstract: The invention relates to a pharmaceutical formulation of nanonised fenofibrate, to a method for preparing same, and to the uses thereof.

Abstract: The present invention provides compositions comprising dicyclomine, or salts, and/or solvates and methods of making and using the compositions to treat intestinal hypermotility or Irritable Bowel Syndrome (IBS). The present invention also provides once-a-day orally disintegrating dosage forms comprising compositions of the present invention.

Abstract: A taste masked dosage form of pharmaceutical acceptable salt of escitalopram comprising (a) resin complex of pharmaceutical acceptable salt of escitalopram and cationic exchange resin or adsorbing or coating non-pareil seeds or inert particles with a mixture of pharmaceutically acceptable salt of escitalopram, cationic polymer and optionally other polymer(s) or loading non-pareil seeds or inert particles with pharmaceutically salt of escitalopram followed by polymer coating with cationic polymer and optionally other polymer(s); and (b) at least one pharmaceutical excipient.

Abstract: An intrabuccally rapidly disintegrating tablet which is manufactured by a simple method, has an enough practical hardness and is rapidly disintegrated in the buccal cavity and its production method. The intrabuccally rapidly disintegrating tablet is produced by growing a powder material into a granulated material with a fixed particle diameter, the powder material including a sugar alcohol or a saccharide as main ingredient, each of which is first particle having an average particle diameter of not more than 30 ?m, by mixing thus obtained granulated material with an active ingredient and a disintegrant, and by compressing the mixture into a predetermined shape.

Abstract: The present invention relates to a granule of gamma-hydroxybutyric acid or of one of its pharmaceutically acceptable salts, characterized in that it comprises a solid core on which the gamma-hydroxybutyric acid or one of its salts is supported.

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 method for embolization treatment was developed in which microspheres with novel properties are administered in a mammal. The microspheres are made using a novel process that results in microspheres with new combined properties of high density, low fracture, high swell capacity, rapid swell, and deformability following swell. These microspheres form occlusions with high durability, withstanding over 100 mm Hg (13.3 kPa) of pressure.

Abstract: The present invention relates to a method for preparing a granulate of at least two active principles, including a step of applying said active principles to a solid particulate medium by dusting, said active principles not being plant extracts.

Abstract: The present invention relates to a pharmaceutical composition comprising Brivaracetam or Seletracetam as active ingredient, the invention relates specifically to a prolonged release formulation made of granules containing the active ingredient in their inner core.

Abstract: A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially insoluble or sparingly soluble in water, in combination with a bioadhesion and/or mucoadhesion promoting agent adhered to the surfaces of said carrier particles. The composition is primarily intended for sublingual or intranasal administration. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.

Abstract: The present invention provides pharmaceutically acceptable compositions for once-daily dosing comprising a piperazine derivative of H1-receptor antagonists, or its salt, and/or solvate and methods of making and using the compositions in the treatment of treating vertigo and other diseases. The present invention also provides once-a-day dosage forms as orally disintegrating tablets comprising compositions of the present invention.

Abstract: The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.

Abstract: The present invention relates to compositions comprising 4-(2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4H-1,2,4-triazol-3-ylthio)acetamido)-3-chlorobenzoic acid or pharmaceutically acceptable salts thereof, and to the preparation and use of such compositions, in particular for the treatment of diseases.

Abstract: The present invention relates to a pulsed-release sildenafil pharmaceutical composition comprising an immediate release fraction containing from 5 to 100 mg of sildenafil and a controlled release fraction containing from 25 to 150 mg of sildenafil, wherein the controlled release fraction is comprised of particles containing (a) a superdisintegrant agent (b) a coating comprising at least one pH-dependent solubility polymer and at least one pH-independent solubility polymer and (c) optionally, other pharmaceutical excipients. The composition of the present invention exhibits a faster dissolution profile in alkaline media than in acid media, which allows for obtaining enhanced pulsed-release formulations.

Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.

Abstract: The present invention relates to oral taste masked pharmaceutical composition comprising ciprofloxacin or salts or esters thereof. It further relates to processes of preparing it.

Abstract: A consumer care composition or a food composition comprising a mesoporous microparticulate material wherein at least some of the pores of the material are loaded with at least one ingredient and the loaded mesoporous microparticulate material is encapsulated by a capping layer is described.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of at least one neutral cellulosic compound and 1 to 25% by weight of at least one emulsifier, each calculated on dry weight of the polymer mixture.

Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

Abstract: In various embodiments, the present invention is directed to a taste masked pharmaceutical composition comprising a therapeutically effective amount of taste masked sulfamate-substituted monosaccharide particles comprising a sulfamate-substituted monosaccharide or a pharmaceutically acceptable salt or derivative thereof that are coated with one or more taste-masking layers, and optionally one or more of taste-masked neltrexone, 5-HT3 receptor antagonist, phentermine, and vitamin B-12. The present invention relates to methods of making the taste masked and ODT compositions, and methods of using the compositions for treating a patient subject to an epileptic condition, migraines, dysphagia, achieving/maintaining weight loss, or alcoholism or drug addiction.

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: Stable and uniform distribution of gel beads or other particulate material, dispersed in a liquid medium can be obtained by including a density-reducing agent within the gel beads to provide the particle with a desired bulk density, for example a density close to that of the disperse liquid medium. Suitable density control can prevent migration due to gravity leading to settling in storage. Gel beads formulated with agar are suitable for use in cosmetics and for inclusion in cosmetics formulating processes which may employ modestly elevated temperatures. Attractive and novel cosmetics bead suspensions are described. Additional to cosmetics, pharmaceutical, foodstuff and other applications are disclosed. Examples of suitable density-reducing agents include very low density hollow polymeric microspheres and temperature-sensitive expandable thermoplastic microspheres.

Abstract: Methods for treating bladder cancer comprising intravesicular administration of a stabilized pharmaceutical formulation comprising 5-(1-aziridinyl)-3-(hydroxymethyl)-2-[(E)-3-hydroxyprop-1-enyl]-1-methyl-1H-indole-4,7-dione (EO9). More specifically, the stabilized pharmaceutical formulation is instilled in the bladder for a time sufficient to treat the cancer.

Abstract: The present invention provides an oral pharmaceutical formulation comprising coated spheroids of a kinase inhibitor such as neratinib, which formulation is designed to reduce or eliminate side effects associated with existing oral formulations of kinase inhibitors.

Abstract: In one embodiment a dosage form comprises at least one active ingredient and a molded matrix which comprises 10-100% of a material having a melting point of less than about 100 degrees C. selected from the stamp consisting of thermoplastic polyalkylene oxides, low melting hydrophobic materials, thermoplastic polymers, thermoplastic starches and combinations thereof, and the matrix is capable of providing modified release of the active ingredient upon contacting of the dosage form with a liquid medium. The dosage form may additionally comprise uncoated particles which may contain at least one active ingredient. In another embodiment, a dosage form comprises at least one active ingredient, a plurality of particles and a molded matrix, wherein at least a portion of the particles are coated.

Abstract: The invention provides novel pharmaceutical compositions of Elvucitabine. The invention also provides pharmaceutical compositions and oral dosage forms having unique physical-chemical properties.

Abstract: A controlled release dosage form of tacrolimus, comprising a solid dispersion of tacrolimus, wherein a controlled release base, which is selected from the group consisting of a water-soluble macromolecule, a gum base, and a membrane forming agent and does not form the solid dispersion of tacrolimus, is further contained, is disclosed. The controlled release dosage form of tacrolimus has an excellent controlled release and shows a stable blood concentration.

Abstract: The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of amoxicillin and consisting of suspensions of coated particles of amoxicillin (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of amoxicillin, in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of amoxicillin, said liquid phase being furthermore saturated with amoxicillin.

Abstract: There is provided a method for preparing a pharmaceutical composition comprising compressible coated, taste-masked and/or controlled-release coated drug-containing particles, rapidly-dispersing microgranules comprising a disintegrant and a sugar alcohol, a saccharide, or a mixture thereof, and other optional, pharmaceutically acceptable excipients wherein the orally disintegrating tablet (ODT) or rapidly dispersing tablet (RDT) composition having acceptable tableting, organoleptic, and pharmacokinetic properties.

Abstract: The invention relates to an improved process for preparing a new medicament formulation of the active substance dabigatran etexilate of formula I in the form of the methanesulphonic acid salt thereof, and this new medicament formulation as such.