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: An oral composition comprising minicapsules wherein the minicapsules comprise one or more therapeutic or prophylactic substances in a liquid, semi-liquid, or solid core. The minicapsules have release profiles to release the substance in an active form at one or more sites along the gastro-intestinal tract to maximise absorption and/or therapeutic efficiency.

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: The invention provides an immunostimulatory nucleic acid comprising CpG motifs, and methods of use thereof in stimulating immunity.

Abstract: Methods of marking pharmaceutical products for use in clinical trials and for determining the origin or authenticity of the marked products are provided that use a variety of natural materials as markers. The natural materials have unique genetically controlled micromorphological structures that can be identified using enhanced visualization techniques. For example, cellulosic plant materials, sporopollenin and diatoms can be used as the natural materials. The natural materials are added to pharmaceutical products at sufficiently low levels so as not to have any significant effect on the products other than serving as markers. Dyes and reactants can be added to the natural materials to provide secondary markers. The markers can be identified in stool samples collected during clinical trials to prove that a particular pharmaceutical product has been ingested by a test subject.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: A modified release solid dosage product comprises a plurality of minicapsules or minispheres containing nimodipine, wherein when exposed to a use environment more than 40% of the nimodipine is released within 12 hours and wherein the Tmax is reached within 6 hours. The product may be a capsule 4 having a first population of uncoated minispheres 1 containing nimodipine for immediate release and a second population of coated minispheres 2 containing nimodipine for sustained release. There may be another population of coated minicapsules 3.

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

Abstract: The present invention is directed to compositions comprising a nanoparticulate azelnidipine, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate azelnidipine 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 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: Embodiments of a controlled release minitablet comprise an extended release core and an optional pH dependent delayed release coating thereon, wherein the extended release core comprises budesonide, a carrier, an extended release polymer, and an acid. The budesonide may be embedded in the extended release polymer to facilitate extended release of the budesonide upon administration.

Abstract: Embodiments of a controlled release minitablet comprise an extended release core and an optional pH dependent delayed release coating thereon, wherein the extended release core comprises budesonide, a carrier, and an extended release polymer. The budesonide may be embedded in the extended release polymer to facilitate extended release of the budesonide upon administration.

Abstract: The invention relates to a solid oral dosage form comprising a pharmaceutically active ingredient in combination with an enhancer which enhances the bioavailability and/or the absorption of the active ingredient. Accordingly, a solid oral dosage form comprises a drug and an enhancer wherein the enhancer is a medium chain fatty acid ester, ether or salt or a derivative of a medium chain fatty acid, which is, preferably, solid at room temperature and which has a carbon chain length of from 6 to 20 carbon atoms. Preferably, the solid oral dosage form is controlled release dosage form such as a delayed release dosage form.

Abstract: An oral cyclosporin composition comprises minicapsules having a core containing a cyclosporin, especially cyclosporin A in a solubilised liquid form. The minicapsules have a release profile to release the pre-solubilised cyclosporin, at least in the colon. The composition may be used for treating a range of intestinal diseases [FIG. 10].

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

Abstract: The present invention relates to the formulation of solid dosage forms comprising a therapeutically effective amount of an HMG-CoA reductase inhibitor, and especially Atorvastatin or Fluvastatin or salts thereof, in combination with colloidal clay such as Attapulgite, and a process for the preparation thereof by direct compression.

Abstract: A solid or semisolid implant obtainable by providing a liquid composition comprising an aqueous solution of dextran with molecular weight of 1.0-100 kDa and introducing the liquid composition into the body of a mammal, whereby the implant is formed in situ in the body of the mammal. A process for preparing a composition useful for biomedical application, comprising the steps of providing a liquid composition comprising an aqueous solution of dextran having a molecular weight of 1-100 kDa; and bringing the liquid composition to solidify; whereby water is gradually eliminated from the liquid composition during the solidification. A biomedical article prepared from the composition.

Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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: A method of lowering blood glucose in a mammal includes orally administering a therapeutically effective amount of crystallized dextran microparticles and insulin to the mammal to lower blood glucose of the mammal. The composition may be a one phase or a structured multi-phase composition for controlled release of insulin.

Abstract: A dosage form is disclosed comprising a semipermeable walled container that houses a capsule, which capsule comprises a drug formulation, a piston, and an osmotic composition. The dosage form delivers the drug formulation through a passageway at a controlled rate over a sustained-release period of time up to 24 hours.

Abstract: The present invention provides matrix-forming, sustained-release pharmaceutical formulations comprising four primary components: i) an effective amount of at least one drug substance; ii) at least one pharmaceutically acceptable, water-swellable, pH independent polymer; iii) at least one pharmaceutically-acceptable, anionic, pH dependent polymer; and (iv) a pharmaceutically-acceptable polymer selected from the group consisting of a) at least one pharmaceutically-acceptable cationic polymer; and b) at least one pharmaceutically acceptable hydrocolloid. The present formulations can be used with compounds having a wide range of solubilities as well as compounds characterized as having hydrophobic or hydrophilic characteristics.

Abstract: Provided herein are pharmaceutical compositions comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided. Methods for treating pain using such compositions are also demonstrated.

Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also promotes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to a size that is retained in the stomach during the postprandial or fed mode.

Abstract: We describe a medicament for the treatment of thyroid disorders that typically result from a hypoactive thyroid gland that releases thyroxine and triiodothyronine in a sustained pattern when administered to a subject.

Abstract: The present invention provides oral preparations with good disintegration containing a slightly water-soluble active ingredient, which comprise a mixture of a solid formed product (e.g. a granule) and a second disintegrant wherein said solid formed product comprises a slightly water-soluble active ingredient, a first disintegrant and a water-soluble excipient which is formed by using a water-soluble polymer binder; or comprises a solid formed product prepared from a slightly water-soluble active ingredient, a disintegrant and a sugar alcohol by using a water-soluble polymer binder. When orally administered, these oral preparations exhibit excellent dissolution characteristics of the active ingredient in the digestive tract, and further, these preparations can show equivalent dissolution profile even at different amounts of the active ingredient, and thus enable the selection of the most suitable medicament for each patient, which makes these preparations highly useful in the clinical field.

Abstract: An oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a first population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a first rate; a population of a basic substance; and a second population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a second rate. In another embodiment, the oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a population of a pharmaceutical active; a population of a basic substance; a population of enteric coated pharmaceutical active; and a population of enteric coated basic substance. The composition can provide multiple site specific delivery of a pharmaceutical active in a rapid, delayed and/or sustained release manner into the plasma.

Abstract: Provided herein is a copolymer that includes a soft block (A) and a hard block (B) comprising a tyrosine di-peptide. The copolymer can be any of AB, ABA or BAB type block copolymers. The soft block can include a PEA polymer. A coating formed of the copolymer may also include a bioactive agent. The implantable device can be implanted in a patient to treat, prevent, or ameliorate a disorder such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, and/or tumor obstruction.

Abstract: A composition for providing relief from acidity. The composition comprises sodium bicarbonate for use in neutralizing acids. There is one of a capsule and a tablet for enclosing the sodium bicarbonate therein, such one of such capsule and such tablet being a delayed release and a timed release system so as to delay the dissolution of the sodium bicarbonate until the sodium bicarbonate is in one of a small intestine and a large intestine.

Abstract: The present invention provides pharmaceutical formulations of dipyridamole and acetylsalicylic acid, methods of making thereof, and methods of using 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: Described embodiments include a final dosage form for administering a medicament to an animal, an article of manufacture, and method. A described final dosage form includes a medicament. The final dosage form also includes a release-control substance carrying the medicament in a first medicament-release state wherein the medicament has a first bioavailability to the animal if the final dosage form is administered to the animal. The release-control substance is modifiable ex vivo by an exposure to a first stimulus to carry the medicament in a second medicament-release state wherein the medicament has a second bioavailability to the animal if the final dosage form is administered to the animal. The release-control substance is modifiable ex vivo by an exposure to second stimulus to carry the medicament in a third medicament-release state wherein the medicament has a third bioavailability to the animal if the final dosage form is administered to the animal.

Abstract: Provided embodiments include a final dosage form, an article of manufacture, and method. A final dosage form for delivering a medicament to an animal is provided. The final dosage form includes an outer layer. The final dosage form also includes a release element configured in a first medicament-release state and modifiable to a second medicament-release state upon an ex vivo exposure to a stimulus. The final dosage form further includes a chamber at least substantially within the outer layer and configured to carry the medicament. The final dosage form includes the medicament. The final dosage form may include an indicator element configured to indicate an exposure of the release element to the stimulus.

Abstract: The invention provides compositions containing polypeptides, including therapeutic polypeptides such as interleukin-11, that are suitable for oral administration.

Abstract: The present invention includes compositions and methods of making a modified release pharmaceutical formulation and a method of preparation for the embedding of modified release multi-particulates into a polymeric or wax-like matrix. The modified release multi-particulates comprise an effective amount of a therapeutic compound having a known or desired drug-release profile. Modified release multi-particulates may include a polymeric coat or may be incorporated into particle or core material. The polymer matrix comprises a thermoplastic polymer or lipophilic carrier or a mixture thereof that softens or melts at elevated temperature and allows the distribution of the modified release multi-particulates in the polymer matrix during thermal processing. Formulation compounds and processing conditions are selected in a manner to preserve the controlled release characteristics and/or drug-protective properties of the original modified release multi-particulates.

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: A sustained release, orally administered pharmaceutical composition comprising carnitine and an acceptable pharmaceutical excipient is described for the treatment of carnitine deficiency and other carnitine responsive conditions. The sustained release formulation avoids the characteristic problems of gastrointestinal invitation, dumping in the urine and bacterial degradation attendant previously known oral formulations of carnitine.

Abstract: The present invention includes a controlled-release composition having a matrix. The matrix contains a pharmaceutically effective amount of an active agent or a pharmaceutically acceptable salt or solvate thereof, an ionic non-gelling matrix polymer, and a pH modifier. The ionic non-gelling matrix polymer is practically insoluble and unswellable at a first aqueous fluid pH and is soluble at a second aqueous fluid pH. The pH modifier is present in an amount to control the release of the active agent from the composition. The controlled-release composition is substantially free of a gelling or swellable excipient and does not contain a functional coating or a lipophilic component. The present invention also provides methods of making and using the controlled-release compositions.

Abstract: The present invention provides enantiomerically pure substituted (S)-benzoxazinone compounds and an extended release formulation of the compounds. The compounds exhibit potent renin inhibition activities and improved bioavailability.

Abstract: The present invention is drawn to novel topiramate compositions as well as methods for treating obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention also features a pharmaceutical composition that includes, e.g., topiramate alone or in combination with a sympathomimetic agent and a novel escalating dosing strategy for administering such compositions.

Abstract: A polymeric antimicrobial comprising a derivative of poly(2-propenal, 2-propenoic acid) formed by reaction between a poly(2-propenal, 2-propenoic acid) and an alcohol or phenol to form protected carbonyl groups. The invention also relates to antiseptic compositions and compositions for treating gastrointestinal disease containing the polymeric antimicrobial.

Abstract: The invention relates to a nucleic acid-lipophilic conjugates and methods for modulating an immune response using the conjugates. The lipophilic moiety associated with an immunostimulatory nucleic acid.

Abstract: The invention provides an immunostimulatory nucleic acid comprising CpG motifs, and methods of use thereof in stimulating immunity.

Abstract: An opioid-antagonist oral dosage form which does not release a therapeutically effective amount of the opioid antagonist when the oral dosage form is orally administered to a human being, but whereby a physical alteration of the oral dosage form results in a release of the therapeutically effective amount of the opioid antagonist. An embodiment of the oral dosage form includes an opioid-antagonist layer coated onto a biologically inert pellet, and a non-releasing membrane coated onto the opioid-antagonist layer. Optionally, the oral dosage form can also include an opioid agonist, such that a method of preventing the abuse of an oral dosage form of an opioid agonist is provided by forming the oral dosage form including an opioid agonist and an opioid antagonist.

Abstract: The present invention is directed to compositions for the sustained delivery of an antibiotic, for example vancomycin, to achieve desirable release profiles. This application is also directed to methods of using the compositions and processes for manufacturing the compositions.

Abstract: A pharmaceutical paste composition comprising an active ingredient such as an addictive substance, a controlled release agent, and a pharmaceutically suitable aqueous or non-aqueous carrier. The composition may comprise one or more of a clay, or an oily, waxy, or fatty substance. The composition may be filled into a capsule or other dispensing device. The composition may reduce dose dumping of an active ingredient. Methods of making and using the composition are also described.

Abstract: A device and method is described for enabling an examining device to pass through an abnormally configured body lumen. The device may pass through a body lumen while maintaining an initial dimension. Upon encounter with an abnormally configured body lumen, the device may be depleted and take on a final dimension after a predetermined time period, regardless of its current orientation with respect to the body lumen, so that the device may pass through and vacate the abnormally configured body lumen shortly after the predetermined time period may have elapsed.

Abstract: A sustained release pharmaceutical composition comprising coating comprising at least one water-insoluble permeable polymer and at least one water soluble polymer and homogenous cores containing only tolterodine or a salt thereof and microcrystalline cellulose is described.

Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.

Abstract: Disclosed herein are compositions for treating a respiratory condition, preferably by enhancing immune response in a mammal, the compositions including a therapeutic amount of a probiotic strain of bacteria and a therapeutic amount of an additional component. Also included are methods of treating a respiratory condition, preferably by enhancing immune response, in a mammal. Kits containing the compositions, and instructions for applying the methods are also included. The method includes orally administering to the mammal a therapeutic amount of a probiotic strain of bacteria and a therapeutic amount of an additional component.