Abstract: The invention relates to a novel pharmaceutical modified release formulation of guaifenesin and dextromethorphan. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions further comprises dextromethorphan.

Abstract: The present invention relates generally to pharmaceutical dosage forms comprising: an absorption window active agent; a controlled release component comprising enteric-coated controlled release beads, wherein the enteric-coated release beads comprise at least two pH-sensitive polymer layers. The controlled-release dosage forms provide good bioavailability of absorption window active agents.

Abstract: A cyclodextrin polymer-based injectable composition comprising cyclodextrin, a polymer which is capable of forming a hydrogel with the cyclodextrin, and a pharmacologically effective amount of at least one drug. The polymer is selected from poly(ethylene glycol), derivatives thereon or a copolymer with a poly(ethylene glycol) segment. The copolymer with a poly(ethylene glycol) segment may include a polymer selected from the group consisting of polyesters, polyurethanes, polyamides, polyethers, polysaccharides, poly(amino acid)s, polypeptides, and proteins. The composition may be injected subcutaneously, intramuscularly, intradermally, or intracranially.

Abstract: An orally administered antihyperlipidemia composition according to the present invention includes from about 250 to about 3000 parts by weight of nicotinic acid, and from about 5 to about 50 parts by weight of hydroxypropyl methylcellulose. Also, a method of treating hyperlipidemia in a hyperlipidemic having a substantially periodic physiological loss of consciousness, includes the steps of forming a composition having an effective antihyperlipidemic amount of nicotinic acid and a time release sustaining amount of a swelling agent. The method also includes the step of orally administering the composition to the hyperlipidemic once per day “nocturnally,” that is in the evening or at night.

Abstract: An improved weight and growth stimulant for domesticated animals such as cattle, pigs and sheep is comprised of an anabolic agent that is subcutaneously administered in the form of a dual release implant formulation. Increased gains are particularly improved when zeranol is administered in an immediate-release and controlled-release formulation which allows for a one-time dosage injection.

Abstract: A process for producing solid oral dosage forms with controlled active ingredient release, comprising a mixture of a) at least one active ingredient, and b) a preformulated mixture of polyvinyl acetate and polyvinylpyrrolidone, wherein the mixture is obtained by joint processing of components a) and b) in an extruder at temperatures between 50° and 200° C.

Abstract: The present invention is directed to seamless capsules and methods for making seamless capsules having a high oil content as described herein. More specifically, the present invention is directed to seamless capsules, and methods for making seamless capsules, made from a process involving the steps of: (a) preparing an emulsion comprising oil, water, an emulsifier, and at least one of a water-soluble monovalent metal salt, polyvalent metal salt, and an acid, wherein said oil is present in an amount of at least 50% by weight of said emulsion; with the proviso that said emulsion does not contain marmelo mucilage; and (b) adding portions of said emulsion to an aqueous gelling bath comprised of at least one ionic polysaccharide thereby encapsulating said portions of said emulsion in a polysaccharide gel membrane, and optionally (c) drying the resulting capsules by removing water.

Abstract: The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and at least one additional drug ingredient. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions has at least one additional drug ingredient.

Abstract: The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and pseudoephedrine. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions further comprises pseudoephedrine.

Abstract: A stabilized pharmaceutical composition of benzimidazole compounds preferably amorphous form of esomeprazole and a process for preparing the same. The pharmaceutical compositions formulated into solid dosage forms preferably multiple unit tablet dosage forms and capsules and a method for preparing the same.

Abstract: The present invention is directed to seamless capsules and methods for making seamless capsules having a high oil content. More specifically, the present invention is directed to seamless capsules, and methods for making seamless capsules, made from a process involving the steps of: (a) preparing an emulsion comprising oil, water, an emulsifier, and at least one of a water-soluble monovalent metal salt, polyvalent metal salt, and an acid, wherein said oil is present in an amount of at least 50% by weight of said emulsion; with the proviso that said emulsion does not contain marmelo mucilage; and (b) adding portions of said emulsion to an aqueous gelling bath comprised of at least one ionic polysaccharide, thereby encapsulating said portions of said emulsion in a polysaccharide gel membrane, and optionally (c) drying the resulting capsules by removing water. The capsule is, for example, an alignate gel. The capsules of the invention are suitable for a variety of applications, e.g.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (G1) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.

Abstract: The present invention provides a pharmaceutical formulation comprising an immediate-release compartment containing an angiotensin-2 receptor blocker (ARB) as a pharmacologically active ingredient and an extended-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. Since the disclosed formulation enables the release of the two ingredients at a different time, it reduces side effects and increases the effects of the drug more than the case of separately administering the ingredients each at the same time. In addition, the formulation maximizes the effects of drug at the time of day when the complication risk of cardiovascular system diseases is highest.

Abstract: A gastroretentive drug formulation for the sustained release of an active agent in the gastrointestinal tract comprises an internal layer or compartment comprising an active agent and one or more pharmaceutical excipients, of which at least one is a polymer and two membranes forming together an envelope around the inner membrane, each membrane comprising at least one polymeric combination of an enteric polymer which is not soluble in gastric juice, and an hydrophilic swelling polymer, and at least one plasticizer.

Abstract: Disclosed in certain embodiments is a pharmaceutical composition comprising from 10 to 40 mg of oxycodone or a pharmaceutically acceptable salt thereof and 0.65 to 0.90 mg naloxone or a pharmaceutically acceptable salt thereof.

Abstract: By suitable retardation oral pharmaceutical compositions containing propiverine or one or several pharmaceutically acceptable salts thereof in an amount of 4 mg to 60 mg propiverine and having a prolonged release of the active agent are produced. Preferably a blend of active agent and optionally one or more acidic substances having a pKa value of less than 6.65 are provided with a retarding coating or are embedded in a matrix which is then optionally coated with further retarding layers.

Abstract: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.

Abstract: The present invention provides a pharmaceutical formulation comprising a compartment containing a rennin inhibitor as a pharmacologically active ingredient, and a compartment having an angiotensin-II-receptor blocker as a pharmacologically active ingredient. One of the compartments is an immediate-release compartment and the other one is an extended-release compartment. Since the disclosed formulation delivers the rennin inhibitor and angiotensin-II-receptor blocker at a specific delivery rate at a different time. It has an advantage in reducing the concern about side effects, improving drug effects, and simplifying the instructions for use of the drug. In addition, the formulation can pharmacologically, clinically, scientifically, and economically achieve more useful effects than the complex prescription case of taking the ingredients separately or each at once, in preventing and treating metabolic syndrome, cardiovascular disease and renal disease.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: A pharmaceutical composition having improved solubility comprising a hydrophobic drug or pharmaceutically acceptable salt thereof and a compound having at least one carboxylic acid moiety, wherein the molar ratio of the compound having at least one carboxylic acid moiety to the hydrophobic drug or pharmaceutically acceptable salt thereof is from about 0.1:1 to about 25:1. The pharmaceutical composition exhibits rapid dissolution upon contact with physiological solvents, such as water, saliva or gastrointestinal fluids.

Abstract: Rapidly dispersing solid dry therapeutic dosage form comprised of a water insoluble compound existing as a nanometer or micrometer particulate solid which is surface stabilized by the presence of at least one phospholipid, the particulate solid being dispersed throughout a bulking matrix. When the dosage form is introduced into an aqueous environment the bulking matrix is substantially completely dissolves within less than 2 minutes thereby releasing the water insoluble particulate solid in an unaggregated and/or unagglomerated state. The matrix is composed of a water insoluble substance or therapeutically useful water insoluble or poorly water soluble compound, a phospholipid and optionally also at least one non-ionic, anionic, cationic, or amphipathic surfactant, together with a matrix or bulking agent and if needed a release agent. The volume weighted mean particle size of the water insoluble particle is 5 micrometers or less.

Abstract: An oral drug delivery composition includes a sustained release component which includes a corticosteroid drug and which is contained within a capsule that has been treated so that the sustained release component is predominately released from the capsule in the intestine following oral administration. A drug delivery composition for delivering a corticosteroid drug to the intestine also includes: (a) a sustained release component comprising a corticosteroid drug, an alkali-containing ethylcellulose material and an acid; and (b) a delayed release component which substantially prevents release of the sustained release component until the composition reaches the intestine following oral administration. The compositions of the invention are useful for treating inflammatory diseases of the gastrointestinal tract, such as Crohn's disease and ulcerative colitis, and for treating glomerulonephritis.

Abstract: A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.

Abstract: Preparation of AT1 receptors antagonists formulations using the cyclodextrins, their derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular disease and their complications. Until now, no applications using the AT11 receptor antagonists and cyclodextrins or derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular diseases and their complications, was found in the technical state of art. The present invention is characterized by the combination of two different technologies: one is the molecular encapsulation of AT11 receptor antagonists in cyclodextrins and the other is the microencapsulation in biodegradable polymers. It also comprises the increase of the effectiveness of the AT11 receptor antagonists as well as an increase in their bio-availability.

Abstract: A biodegradable, multi-layered controlled release gastroretentive baclofen or R-baclofen dosage form which is optionally divided into a first dosage of baclofen or R-baclofen for immediate release and a second dosage of baclofen or R-baclofen for controlled release in the stomach and gastrointestinal tract of a patient, folded into a capsule which disintegrates upon contact with gastric juice and the dosage form unfolds rapidly upon contact with gastric juice. The biodegradable, multi-layered gastroretentive dosage forms of the invention provide fast onset of baclofen or R-baclofen activity with prolonged absorption and minimal undesirable side effects.

Abstract: A combination of active agents is disclosed which are particularly useful for treating fluid overload conditions. Methods for using the combination of active agent are also disclosed. The combination can include a highly absorbent polyelectrolyte polymer along with an agent that increases the amount of fluid in the intestine.

Abstract: A method for treatment of acne with tetracyclines is provided. A lower sustained dose and no loading dose is employed, with an optional once-a-day dosing regimen.

Abstract: A sustained-release, oral pharmaceutical formulation of tramadol comprising a compound formed in situ of tramadol or its salt and a pharmaceutically acceptable acidic substance. The compound formed in situ has a desired water solubility. Also provided are methods of treatment using the pharmaceutical formulations. Method for preparing such formulations are also provided. The preparation method comprises repeatedly mixing tramadol or its salt with the acidic substance, and moistening the mixture and formulating the mixture under an energy input, such as heat or pressure. Optionally, drying, repeated granulating, extrudation and pelleting may also be included.

Abstract: The invention provides methods and compositions for administering an NMDA receptor antagonist (e.g., memantine) to a subject.

Abstract: The present invention provides a pharmaceutical preparation comprising a prior-release compartment containing a hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor as a pharmacologically active ingredient, and a delayed-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. The preparation of the present invention provides synergistic effects through combined administration of the non-dihydropyridine calcium channel blocker and the HMG-CoA reductase inhibitor, and induces the time-dependent absorption, metabolism and action mechanism of individual drugs through the controlled release thereof to avoid competitive antagonism between drugs, thus maximizing the effects of each pharmacologically active ingredient while minimizing side effects, for example, the risk of myopathy, and substantially increasing the compliance of patients by taking one tablet once a day.

Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.

Abstract: Modified release pharmaceutical compositions comprising mycophenolate as the active agent or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof, wherein the said composition exhibits a biphasic release profile when subjected to in-vitro dissolution and/or upon administration in-vivo are provided. The composition provides a drug release in a manner such that the drug levels are maintained above the therapeutically effective concentration (EC) constantly for an extended duration of time. Further, the difference between the maximum plasma concentration of the drug (Cmax) and the minimum plasma concentration of the drug (Cmjn), and in turn the flux defined as ((Cmax?Cmjn)/Cavg) is minimal. The present invention also provides process of preparing such dosage form compositions and prophylactic and/or therapeutic methods of using such compositions.

Abstract: A pharmaceutical formulation comprising desvenlafaxine having an MMD of between about 5 ?m and about 100 ?m, or a pharmaceutically acceptable salt thereof, and at least one matrix rate-controlling pharmaceutically acceptable polymer, solid unit dosage form containing it, methods for preparing such a formulation and for its use to treat depression and related disorders and diseases.

Abstract: A pharmaceutical composition for the oral administration of omega polyenoic fatty acids combined with one or more active principles incompatible therewith, is described; also described is a process for preparing said pharmaceutical composition.

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: Disclosed is an oral dosage form comprising (i) an opioid agonist in releasable form and (ii) a sequestered opioid antagonist which is substantially not released when the dosage form is administered intact.

Abstract: The present invention generally relates to pharmaceutical unit dosage forms of NSAIDs and H2-receptor antagonists, in which the H2-receptor antagonist is formulated so as to be released in a sustained manner over a predetermined period of time so as to maintain gastric pH above a desired level for a duration of time. The NSAID may then be formulated for immediate release. The pharmaceutical unit dosage forms may be administered to subjects susceptible to the development of NSAID induced gastric and/or duodenal ulcers, as the sustained release H2-receptor antagonist is formulated so as to maintain the gastric environment above the pH levels where NSAID-induced ulceration typically occurs.

Abstract: The present invention relates to improved sustained release dosage forms such as tablets and capsules, and in particular to a pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of an antimuscarinic agent, such as Tolterodine or pharmaceutical acceptable salt, derivative, prodrug and metabolite thereof in combination with a wetting agent, such as Sodium Docusate to improve the release of the active ingredient and a method for the preparation thereof.

Abstract: The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin.

Abstract: A composition comprising a high molecular weight, water soluble polymer having a cloud point from about 20 to about 90° C. and at least one carrageenan is provided. The composition may be used as a component of a pharmaceutical dosage form, such as the shell of a dosage form, to provide burst release of active ingredient contained therein.

Abstract: Pharmaceutical compositions in unit dose form comprising a hard or soft capsule containing a fill consisting of one or more inert ingredients, and one or more coatings on the capsule, wherein at least one coating comprises at least one active pharmaceutical ingredient.

Abstract: Abuse resistant polyglycol-based pharmaceutical compositions are disclosed. The composition contains one or more polyglycols and one or more active substances and it is resistant to crushing, melting and/or extraction. Moreover, such compositions have the same or lower solubility in ethanolic-aqueous medium, i.e. they are not subject to ethanol-induced dose dumping effect.

Abstract: Disclosed herein is an extended release pharmaceutical composition comprising at least two populations of extended release minitablets having a core comprising carbamazepine or its pharmaceutical salts, solvates, hydrates, an extended release polymer(s), wherein the extended release polymer of each population of minitablets is unalike. The process for manufacturing said composition is also disclosed.

Abstract: The present invention discloses an anti-tumor conjugate and pharmaceutical composition or kits comprising the conjugate, as well as a method of producing the anti-tumor conjugate. The anti-tumor conjugate of the present invention is metabolically stable in vivo, and is ultimately available for the treatment of tumors and production of anti-tumor medicaments.

Abstract: A pharmaceutical composition which comprises a therapeutically effective amount of a aminopyridine dispersed in a release matrix, including, for example, a composition that can be formulated into a stable, sustained-release oral dosage formulation, such as a tablet which provides, upon administration to a patient, a therapeutically effective plasma level of the aminopyridine for a period of at least 12 hours, preferably 24 hours or more and the use of the composition to treat various neurological diseases.

Abstract: Present invention provides pharmaceutical composition comprising memantine or a pharmaceutically acceptable salt thereof as well as a method for its production. Also provided are different formulations of the composition their structure and preferred shape.