Abstract: Aqueous drug coatings including at least one insoluble drug, wherein the insoluble drug accounts for about 85 wt % to about 97 wt % of the drug coatings are described. Such drug coatings may include only one insoluble drug, two or more insoluble drugs, or one or more insoluble drugs in combination with one or more soluble drugs.

Abstract: A pharmaceutical composition, comprising a thiazolidinedione, such as Compound (I), metformin hydrochloride and a pharmaceutically acceptable carrier, wherein the thiazolidinedione and metformin hydrochloride are each dispersed within its own pharmaceutically acceptable carrier in the pharmaceutical composition and the use of such a composition in medicine.

Abstract: The present invention is directed to aqueous drug coatings that include at least one insoluble drug, wherein the drug accounts for about 85 wt % to about 97 wt % of the drug coatings. A drug coating according to the present invention may include only one insoluble drug, two or more insoluble drugs, or one or more insoluble drugs in combination with one or more soluble drugs. The present invention also includes drug coating formulations suitable for providing drug coatings according to the present invention and dosage forms that include a drug coating according to the present invention.

Abstract: Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.

Abstract: The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine.

Abstract: The invention relates to powdered preparations containing tiotropium for inhalation, processes for preparing them as well as their use in preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.

Abstract: A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications.

Abstract: A controlled release pharmaceutical composition comprising Milnacipran or pharmaceutically acceptable salts thereof and hydrophobic release controlling agent. The composition releases 90% of the total amount of Milnacipran or pharmaceutically acceptable salts thereof between 8 to 20 hours when dissolution is carried out in 900 ml 0.1N HCl, USP apparatus Type I (Basket) at 100 rpm for 2 hrs, followed by 900 ml Phosphate buffer pH 6.8 USP apparatus Type I (Basket) at 100 rpm.

Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.

Abstract: The invention discloses nanoparticles composed of chitosan, poly-glutamic acid, and at least one bioactive agent, wherein equal moles of the positively charged chitosan and the negatively charged poly-glutamic acid substrate form an electrostatic network with zero surface charge enabling improved loading the bioactive agent.

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

Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.

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 composition comprising a cefditoren, or a salt, derivative, prodrug, or other form thereof, for example, cefditoren pivoxil, useful in the treatment and prevention of infections and related conditions. The invention provides a composition which comprises nanoparticulate particles comprising the cefditoren, or a salt, derivative, prodrug, or other form thereof and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a cefditoren, or a salt, derivative, prodrug, or other form thereof, or nanoparticles comprising the same, in a pulsatile or continuous manner.

Abstract: The present invention is providing a new sustained release drug preparation comprising such and inclusion complex of a medical compound with safe botanic drug (SBD), which sustains or retards the dissolution and release of the SBD at a controlled rate from the inclusion complex and hence from the drug preparation containing the SBD, so as to maintain the concentration of the SBD in blood at an effective level for prolonged time. SBD contains Kuguasu (KU) and saponins of Kugua (SAK). SBD is very safe and it is used for treating and preventing diabetes.

Abstract: Oral dosage forms for basic amine drugs, the dosage forms having a gastro-retentive component and a non gastro-retentive component. These dosage forms are capable of providing both IR and SR release rates for these drugs. In addition, they provide for release of the drug in the stomach and/or intestine of a mammal to which such dosage forms are administered. Such dosage forms include tablets and capsules. Such dosage forms provide improved bioavailability of otherwise poorly bioavailable basic amine drugs.

Abstract: Methods and compositions for enhancing transdermal delivery of a bioactive agent. The method contains the step of applying to a skin tissue an effective amount of a composition comprising: (a) a drug vehicle; (b) a bioactive agent encapsulated within the drug vehicle; (c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the drug vehicle; and (d) a pharmaceutically acceptable carrier, for a period of time effective to deliver the bioactive agent across the skin tissue at a desired dosage.

Abstract: The present invention relates to an oral particle including pseudoephedrine hydrochloride and cetirizine dihydrochloride, which primarily includes a nucleus having a diameter ranging 25˜40 mesh, a pseudoephedrine-hydrochloride layer coated outside the nucleus with a coating solution composed of pseudoephedrine hydrochloride, a binder, a lubricant and pure water/alcohol, a release-control layer coated outside the pseudoephedrine-hydrochloride layer, and a cetirizine-dihydrochloride layer coated outside the release-control layer with a coating solution composed of cetirizine dihydrochloride, a binder, a lubricant and pure water/alcohol. Accordingly, by distributing pseudoephedrine hydrochloride and cetirizine dihydrochloride into hundreds of the particles and controlling the dissolution rate with the release-control layer, the particles can perform good absorption efficiency, and quick, stable and long-term edicinal effect.

Abstract: A method for effecting weight loss by administering a combination of topiramate and phentermine is provided. The phentermine is generally administered in immediate release form, in a daily dose in the range of 2 mg to 8 mg, in combination with a daily dose of topiramate selected to prevent the loss of effectiveness of phentermine alone. Methods for treating obesity, conditions associated with obesity, and other indications are also provided, as are compositions and dosage forms containing low doses of phentermine and topiramate, e.g., 3.75 mg phentermine and 23 mg topiramate.

Abstract: There is provided a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

Abstract: Disclosed is a pharmaceutical composition for release control comprising a plurality of particles for release control. The plurality of particles for release control comprise a core material containing methylphenidate and a polymer coating layer for release control formed on the core material. The plurality of particles for release control are divided into two or more groups based on the average thickness of the polymer coating layer for release control. The particle groups are identical in terms of the composition of the polymer in the polymer coating layer, but are different in terms of the average thickness of the coated layer. The pharmaceutical composition for release control according to the present invention may control the release pattern of methylphenidate contained in the core material as desired, and can be used as an oral formulation in a variety of forms such as orally disintegrating tablets, etc.

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: Methods of nighttime administration of amantadine to reduce sleep disturbances in patient undergoing treatment with amantadine are described, as well as compositions of extended release amantadine that are suitable for nighttime administration.

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

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 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: The present invention is directed to compositions comprising a nanoparticulate vitamin K2 having improved bioavailability. The nanoparticulate vitamin K2 particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the prevention and treatment of osteoporosis. The invention also relates to a controlled release composition comprising a vitamin K2 or a nanoparticulate vitamin K2 that in operation delivers the drug in a pulsed or multi-modal manner for the prevention and treatment of osteoporosis.

Abstract: The present invention provides novel methods and compositions for the treatment and prevention of CNS-related conditions. One of the CNS-related conditions treated by the methods and compositions of the invention is Alzheimer's disease.

Abstract: An oral Tramadol-containing pharmaceutical composition suitable for once daily administration, which contains an amount of Tramadol or a pharmaceutically acceptable salt thereof, providing in vivo, a time of Tramadol peak plasma concentration (Tmax) of greater than 10 hours, and peak Tramadol plasma concentration (Cmax) which are less than three times the plasma concentration obtained 24 hours after administration (C24h) of a single dose of the composition.

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: Compositions of the present invention, comprising at least one digestive enzyme (e.g., pancrelipase) are useful for treating or preventing disorders associated with digestive enzyme deficiencies. The compositions of the present invention can comprise a plurality of coated particles, each of which is comprised of a core coated with an enteric coating comprising at least one enteric polymer and 4-10% of at least one alkalinizing agent, or have moisture contents of about 3% or less, water activities of about 0.6 or less, or exhibit a loss of activity of no more than about 15% after six months of accelerated stability testing.

Abstract: Disclosed herein is a pharmaceutical composition for treating hepatitis C virus infection comprising an HMG-CoA reductase inhibitor and bile acid. More specifically, disclosed are a pharmaceutical composition for treating hepatitis C vims infection comprising fluvastatin or a pharmaceutically acceptable salt thereof along with ursodeoxycholic acid and a preparation method thereof.

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

Abstract: A film coating composition suitable for use in coating pharmaceutical formulations to provide modified release comprising a dispersion which includes: a) an acrylic polymer, b) a vinyl acetate polymer, and c) a water-containing liquid. The film coat is useful for the achievement of modified release from pharmaceutical formulations such as tablets, pellets, etc.

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

Abstract: The present invention relates to an extended release once daily pharmaceutical formulation comprising venlafaxine hydrochloride and pharmaceutically acceptable excipients. More particularly, the present invention relates to an extended release composition in the form of mini-tablets which are incorporated in hard gelatin capsules.

Abstract: Minocycline oral dosage forms containing a controlled release carrier are useful for the treatment of acne.

Abstract: A once a day bupropion hydrochloride formulation is disclosed.

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: The present invention provides compositions comprising carisoprodol or pharmaceutically acceptable salts, esters or derivatives thereof. In certain embodiments, the invention provides pharmaceutical compositions comprising the skeletal muscle relaxant carisoprodol and one or more additional active agents, such as one or more nonsteroidal antiinflammatory drugs (NSAIDs). The invention further provides methods of use of such compositions in preventing, alleviating and/or treating musculoskeletal pain, muscle spasms, or other non-malignant painful conditions including methods in which the circulating levels of the active pharmaceutical form of carisoprodol are controlled by use of extended- or controlled-release formulations or by strict control of dosage regimen, so as to reduce the level of somnolence observed with other muscle relaxant compositions.

Abstract: The present invention relates to a capsule comprising a core and at least one envelope comprising at least one film-forming polymer, characterized in that it exhibits a total solubilization time for its envelope of less than or equal to 85 s, according to a test A, preferably less than or equal to 80 s, more preferably less than or equal to 70 s. The invention also relates to the method of producing said capsule, and also to the products comprising said capsule, such as the food, pharmaceutical, oral hygiene or cosmetic products.

Abstract: Disclosed are once-daily formulations containing tetracyclines, especially doxycycline. Such formulations are useful, for instance, for the treatment of collagenase destructive enzyme-dependent diseases, such as periodontal disease and acne, and acute and chronic inflammatory disease states, such as rosacea and arthritis.

Abstract: A method of forming a tablet includes the steps of pre-blending an active pharmaceutical ingredient susceptible to tackiness and a blending additive with a first mixing effort to form a pre-blend mixture, wherein the first mixing effort and a second mixing effort, resulting from mixing at least one excipient with the pre-blend mixture, form a blend suitable for direct compression and compressing the blend to form the tablet. One way of achieving the first mixing effort is to pre-blend for an extended period of time. The method allows for directly compressing the blend without the need for a granulation step or roller compression. One such active pharmaceutical ingredient susceptible to tackiness is ibuprofen.

Abstract: The present invention relates to a capsule comprising a core and at least one envelope comprising at least one film-forming polymer, characterized in that it exhibits a total solubilization time for its envelope of less than or equal to 85 s, according to a test A, preferably less than or equal to 80 s, more preferably less than or equal to 70 s. The invention also relates to the method of producing said capsule, and also to the products comprising said capsule, such as the food, pharmaceutical, oral hygiene or cosmetic products.

Abstract: Solid controlled-release oral dosage forms comprising a therapeutically effective amount of an opioid analgesic or a salt thereof which provide an extended duration of pain relief of about 24 hours, have a dissolution rate in-vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm at 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. of from about 12.5% to about 42.5% (by wt) opioid released after 1 hour, from about 25% to about 65% (by wt) opioid released after 2 hours, from about 45% to about 85% (by wt) opioid released after 4 hours, and greater than about 60% (by wt) opioid released after 8 hours, the in-vitro release rate being substantially independent of pH and chosen such that the peak plasma level of said opioid analgesic obtained in-vivo occurs from about 2 to about 8 hours after administration of the dosage form.

Abstract: The present invention is directed to pharmaceutical compositions, and methods of making such compositions, comprising microparticles containing a core comprising melperone and a controlled-release coating. The present invention is also directed to pharmaceutical dosage forms comprising melperone, including orally disintegrating tablets, conventional tablets, and capsules, and methods for their preparation.

Abstract: A multiple pulsed dose drug delivery system for pharmaceutically active amphetamine salts, comprising an immediate-release component and an enteric delayed-release component wherein (1) the enteric release coating has a defined minimum thickness and/or (2) there is a protective layer between the pharmaceutically active amphetamine salt and the enteric release coating and/or (3) there is a protective layer over the enteric release coating. The product can be composed of either one of a number of beads in a dosage form, including either capsule, tablet, or sachet method for administering the beads.