Abstract: In one aspect, the present invention features a process for making a tablet including a pharmaceutically active agent wherein the tablet has both an immediate release region and a modified release region. The method includes the steps of: (a) forming a tablet shape including a powder blend containing a pharmaceutically active agent and a thermally-sensitive material; and (b) applying energy in different amounts to different regions of the tablet shape to form the tablet in a manner such that: (i) a first region of the tablet shape is exposed to said energy for a sufficient period of time to melt the thermally-sensitive material within the first region to form said modified release region of said tablet; and (ii) a second region of said tablet shape is not so exposed to the energy such that said second region forms the immediate release region of said tablet.
Type:
Grant
Filed:
September 22, 2010
Date of Patent:
November 20, 2012
Assignee:
McNeil-PPC, Inc.
Inventors:
Leo B. Kriksunov, Harry S. Sowden, Joseph R. Luber, Frank J. Bunick
Abstract: Provided are methods for reducing the excipient load of pharmaceutical formulations containing 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide as the active pharmaceutical ingredient, and compositions related thereto. In particular, provided is a pharmaceutical product comprising 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide and a stabilizer admixed throughout a solid-form unilamellar matrix, wherein the ratio of 3-fluoro-7-(2,2,2-trifluoroethoxy)phenoxathiin 10,10-dioxide to stabilizer ranges from about 2:3 to about 1:10, and related methods of forming the pharmaceutical product.
Type:
Grant
Filed:
August 20, 2010
Date of Patent:
November 20, 2012
Inventors:
Andrew Chen, Hailiang Chen, James Cecil Free, Majid Keshtmand, Mohammed Abdul Rahman, Sally A. Look
Abstract: The present invention relates to pharmaceutical compositions containing at least one protein active ingredient protected from digestive enzymes. The pharmaceutical compositions contain the at least one protein active ingredient, in free form, as well as, for liquids, a system that buffers them to a pH greater than 4 and less than or equal to 8 or, for solids, a system that exerts, when they are placed in a liquid medium, a buffer effect between a pH greater than 4 and a pH less than or equal to 8.
Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
Abstract: A tablet comprising a core containing an active agent, and a coating, the core being disposed within the coating such that the coating has a thickness about a longitudinal axis (X-Y) of about 4.85 to 4.95 mm. The position of the core within the coating dictating that the active agent is released rapidly after a lag time during which time no active agent is released.
Type:
Grant
Filed:
March 19, 2012
Date of Patent:
November 13, 2012
Assignee:
Jagotec AG
Inventors:
Guy Vergnault, Pascal Grenier, Christophe Dragan
Abstract: The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.
Type:
Grant
Filed:
February 28, 2007
Date of Patent:
November 13, 2012
Assignee:
Endo Pharmaceuticals Inc.
Inventors:
Huai-Hung Kao, Anand R. Baichwal, Troy McCall, David Lee
Abstract: The present invention is directed to nanoparticulate quinazoline derivative compositions having improved pharmacokinetic profiles and reduced fed/fasted variability. The nanoparticulate quinazoline derivative particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of hyperproliferative disorders, such as cancer and other neoplastic diseases. The compositions may include quinazolinamine derivatives such as erlotinib or a salt thereof.
Abstract: Pharmaceutical compositions comprising fluvastatin, HPMC and optionally other pharmaceutical excipients which are colour-stable upon prolonged periods of storage.
Abstract: An oral dosage form comprising a pharmaceutical tablet of one or more layers, one of which carries a biologically active substance; the formulation of said tablet includes different percentages of hydrophilic and lipophilic polymeric materials, and adjuvant substances. The tablets of the present invention show a release rate which is independent from the amounts of active substance present in the tablet.
Type:
Grant
Filed:
June 5, 2009
Date of Patent:
November 6, 2012
Assignee:
Jagotec AG
Inventors:
Guy Vergnault, Pascal Grenier, Lauretta Maggi, Ubaldo Conte
Abstract: Compositions comprising from about 40 weight parts to about 1000 weight parts of a botanical nitrate source; from about 20 weight parts to about 500 weight parts of a botanical source of nitrite reduction activity; and from about 4 weight parts to about 100 weight parts of a nitrite salt. Methods of reducing triglycerides or reducing C-reactive protein levels are also provided.
Type:
Grant
Filed:
August 16, 2010
Date of Patent:
November 6, 2012
Assignees:
Board of Regents, The University of Texas System, Neogenis Laboratories, Inc.
Abstract: A pharmaceutical composition used to treat Parkinson's disease contains levodopa, carbidopa and entacapone or pharmaceutically acceptable salt thereof, and at least one kind of pharmaceutically acceptable excipients. Entacapone is not mixed with levodopa or carbidopa in the pharmaceutical composition. The preparation method of the pharmaceutical composition includes making the first particles with levodopa and carbidopa, making the second particles with entacapone, and then pressing the two kinds of particles into tablets.
Abstract: Opiate containing dosage forms and methods using same are described. These dosage forms include substantially less opiates by weight than known oral formulations. These dosage forms are intended for oral administration across the oral mucosa.
Abstract: A therapeutic device to release a therapeutic agent comprises a porous structure coupled to a container comprising a reservoir. The reservoir comprises a volume sized to release therapeutic amounts of the therapeutic agent for an extended time when coupled to the porous structure and implanted in the patient. The porous structure may comprise a first side coupled to the reservoir and a second side to couple to the patient to release the therapeutic agent. A plurality of interconnecting channels can extend from the first side to the second side so as to connect a first a plurality of openings on the first side with a second plurality of openings on the second side.
Type:
Grant
Filed:
October 4, 2011
Date of Patent:
October 30, 2012
Assignee:
Forsight Vision4, Inc.
Inventors:
Eugene de Juan, Jr., Yair Alster, Kathleen Cogan Farinas, Hanson S. Gifford, III, K. Angela MacFarlane, Cary J. Reich, Michael Barrett, Randolph E. Campbell, Douglas Sutton
Abstract: It is an object of the present invention to provide a fine core particle, which comprises a coating layer having a uniform thickness, and which can be used to produce, at a high yield, a small granule causing no sandy feeling in the oral cavity when the fine core particle is applied to a fine granule or an orally-disintegrating tablet. According to the present invention, there is provided a core particle, which comprises 50% by mass or more of microcrystalline cellulose, and which has a mean particle diameter of less than 100 ?m, a relative flow index of 7.0 to 30.0, a specific surface area of less than 0.15 m2/g, and a tapped bulk density of 0.80 g/mL or more.
Abstract: A test solution agent, a test system and a method for evaluating the compatibility of biologically active substances with N-vinylpyrdolidone are disclosed.
Abstract: In a solid pharmaceutical preparation containing water-soluble salts of levothyroxine and/or liothyronine as active ingredients, the water activity of said pharmaceutical preparation is adjusted to values of below 0.4 and, preferably, 0.1 to 0.3, measured at room temperature.
Abstract: Provided are methods of treating pain, including neuropathic pain, in human and veterinary individuals. These methods employ locally administrable pharmaceutical gallium compositions, including pharmaceutical gallium compositions suitable for administration to the skin and mucous membranes. The compositions comprise pharmaceutically acceptable gallium compounds, such as gallium maltolate or gallium nitrate, together with pharmaceutically acceptable carriers suitable for local administration, including those suitable for topical administration. The administration of such compositions provides relief from pain, itching, allodynia, hyperalgesia, and related symptoms.
Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.
Type:
Grant
Filed:
June 22, 1999
Date of Patent:
October 23, 2012
Assignee:
Alkermes Pharma Ireland Limited
Inventors:
Jon Swanson, Rajeev A. Jain, Robert Hontz, John G. Devane, Kenneth Iain Cumming, Maurice Joseph Anthony Clancy, Janet Elizabeth Codd, Gary Liversidge
Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.
Type:
Grant
Filed:
May 2, 2012
Date of Patent:
October 23, 2012
Assignee:
Cosmo Technologies Limited
Inventors:
Roberto Villa, Massimo Pedrani, Mauro Ajani, Lorenzo Fossati
Abstract: The present invention is for compositions and methods for managing the body weight of a subject using said compositions. Weight management, particularly weight gain and loss, is effectuated by producing a sensation of satiety in said subjects. The method of managing body weight includes administering the composition prior to food consumption, concurrent with food consumption, as replacement for food consumption and combinations thereof.
Type:
Grant
Filed:
May 3, 2005
Date of Patent:
October 16, 2012
Assignee:
The Procter & Gamble Company
Inventors:
Ronald James Jandacek, Gary Robert Kelm, Satinder Singh Bharaj, Jorge Villanueva Penafiel
Abstract: The present invention is directed to methods of treating vasomotor symptoms in castrated prostatic cancer patients in need of treatment, comprising administering about 15 mg or less of cyproterone acetate per day to the patients. The present invention is further directed to dosage forms comprising about 1 mg to about 15 mg of cyproterone acetate and a package comprising a plurality of dosage forms comprising about 1 mg to about 15 mg of cyproterone acetate.
Type:
Grant
Filed:
October 12, 2009
Date of Patent:
October 16, 2012
Assignee:
Teva Women's Health, Inc.
Inventors:
Salah U. Ahmed, Sundeep Sethia, Kathleen Reape, Howard Hait, Carole S. Ben-Maimon
Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
Abstract: A probiotic composition including a probiotic microorganism embedded within a matrix, the matrix substantially maintaining the viability of said microorganisms. The matrix releases said microorganisms into and upon contact with a liquid carrier. The invention includes methods for manufacturing the composition, particular forms of the composition (2) and as apparatus for administration.
Type:
Application
Filed:
November 13, 2009
Publication date:
October 4, 2012
Applicant:
UNISTRAW PATENT HOLDINGS LIMITED
Inventors:
Ken Palazzi, Mark Styan, Kristel Wallis, Jenni Sofjan, Yin Li, Patricia Conway
Abstract: Drug compositions comprising the compound HT-2157 and their therapeutic uses, including the treatment of CNS disorders and cognitive impairments and the modulation of cognitive function, are disclosed. More particularly, the present invention relates to enteric-coated formulations comprising HT-2157 that reduce the appearance of clinically relevant methemoglobinemia relative to administration of non-enteric-coated formulations comprising HT-2157.
Abstract: Disclosed are quick dissolve tablets, each including Lactobacillus delbrueckii subsp bulgaricus (LBD) and N-acetyl-glucosamine (NAG), as well as excipients, for oral mucosal administration, for improving the quality of life of Hepatitis C patients. Any formulation suitable for oral mucosal administration can be employed for administering the active ingredients in a sufficient dosage for therapeutic effect, one such formulation being: 50 mg of Lactobacillus delbrueckii subsp bulgaricus lysate strain YB-I 10 mg of N-acetyl D-glucosamine. Excipients can include one or more of, maltodextrin; xanthan gum; acesulfam K; lemon powder and a flavoring, e.g., juice; Mannitol TL-32-04, Microcrystalline Cellulose and Carrageenan, Fructose, PVP-XL TL-11-04, Gellan Gum, Citrus TL 1-04, Orange TL 19-04, Sucrolose TL-13-04, and Mg ST TL-13-04.
Abstract: Finely divided binders in powder form composed of vinyllactam polymers, where the binders have an average particle size of up to 35 ?m and an apparent density of less than 0.2 g/ml.
Type:
Grant
Filed:
April 19, 2006
Date of Patent:
September 18, 2012
Assignee:
BASF SE
Inventors:
Karl Kolter, Hermann Ascherl, Bernhard Fussnegger
Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.
Abstract: With an object of providing an orally administered agent (in particular a film-shaped orally administered agent) with which the ease and safety of taking the agent are improved, to attain this object, in an orally administered agent 1b having one drug-containing layer 11 and two water-swellable gel-forming layers 12, the water-swellable gel-forming layers 12 are provided, either directly or via intermediate layers, on the both faces of the drug-containing layer 11.
Abstract: An object of the present invention is to provide an aqueous film coating solution, and the like, which has good acid resistance and sustained release properties as well as the flexibility suitable for the tablet compression force and are highly productive and cost efficient. The aqueous film coating solution of the present invention comprises an ethyl acrylate/methyl methacrylate copolymer dispersion, a methacrylic acid copolymer LD, a plasticizer, titanium oxide and water, wherein the solid mass ratio of the ethyl acrylate/methyl methacrylate copolymer dispersion, the methacrylic acid copolymer LD, the plasticizer and the titanium oxide is 100:(40 to 100):(5 to 50):(5 to 30) and the solid content thereof is 5 to 20 mass %.
Abstract: A pharmaceutical matrix film tablet with controlled release of natural mixtures of conjugated estrogens which have been obtained from the urine of pregnant mares.
Type:
Grant
Filed:
June 14, 2004
Date of Patent:
September 18, 2012
Assignee:
Abbott Products GmbH
Inventors:
Bernd Thumbeck, Klaus Budde, Gerhard Kristen, Margit Wiards
Abstract: A solid oral sensorial product includes at least one botanical material and at least one phosphate containing stain inhibitor. The botanical material is selected from the group consisting of tobacco, tea, coffee, cocoa, and combinations thereof.
Type:
Grant
Filed:
March 26, 2010
Date of Patent:
September 18, 2012
Assignee:
Philip Morris USA Inc.
Inventors:
Donald E. Miser, William R. Sweeney, Qinglin Li, Jerome A. Merski
Abstract: A novel modified release dosage form comprising of a high solubility active ingredient, which utilizes dual retard technique to effectively reduce the quantity of release controlling agents. Present invention can optionally comprise additionally another active ingredient as an immediate release form or modified release form. Present invention also relates to a process for preparing the said formulation.
Abstract: The invention relates to pharmaceutical compositions comprising rivaroxaban, suitable for immediate release, and processes of preparing such compositions, preferably by a melt-granulation process or by a specific direct-compression process.
Abstract: We provide a pharmaceutical dosage form including an opioid antagonist surrounded by a controlled release matrix and an opioid agonist in a surrounding matrix.
Type:
Application
Filed:
May 17, 2012
Publication date:
September 13, 2012
Applicant:
Endo Pharmaceuticals Inc.
Inventors:
Huai-Hung Kao, Yadi Zeng, Michelle Howard-Sparks, Fai Jim
Abstract: Disclosed are tablets comprising hydrolytically stable formulations of (6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate disodium salt (Compound 1) prepared by a wet granulation process.
Abstract: The present invention provides a solid preparation containing an insulin sensitizer and an active ingredient (except insulin sensitizers), which shows in vivo dissolution behavior of an insulin sensitizer, which is similar to the dissolution behavior of an insulin sensitizer from “a solid preparation containing an insulin sensitizer alone as an active ingredient”. The present invention provides a solid preparation containing (1) a layer containing an insulin sensitizer, and (2) a layer containing (a) an active ingredient (except insulin sensitizers), (b) microcrystalline cellulose having a mean particle size of 5-25 ?m, (c) microcrystalline cellulose having a mean particle size of 30-100 ?m and (d) polyvinylpyrrolidone K-90.
Abstract: The present invention provides a quickly disintegrating tablet which has quick disintegrability and solubility in an oral cavity, and does not have uncomfortable tastes such as bitterness, has a small variation of a tablet physical property even in storage under a humidifying condition, and has substantially no change in a medicine content in the tablet and tablet appearance and which is superior in stability; and a manufacturing method of the tablet. That is, it provides: a quickly disintegrating tablet which is prepared by blending a medicine with a saccharide and polyvinyl alcohol, which has small variations of tablet weight, tablet hardness, tablet diameter and tablet thickness, and which is superior in medicine stability in the tablet; and a manufacturing method of the tablet.
Abstract: A dosage form comprising of a high dose, high solubility active ingredient as modified release and a low dose active ingredient as immediate release where the weight ratio of immediate release active ingredient and modified release active ingredient is from 1:10 to 1:15000 and the weight of modified release active ingredient per unit is from 500 mg to 1500 mg; a process for preparing the dosage form.
Abstract: The subject invention is a method and material for removing fluid from the intestinal tract of a host and may be useful in treating animals or human patients suffering from fluid overload states. In one embodiment, the subject method involves ingesting an enterically coated non-systemic, non-toxic, non-digestible, water absorbing polymer which absorbs fluid while passing through the intestinal tract. The polymer is excreted in the feces wherein the polymer and absorbed fluid is removed from the body. Preferred polymers include super absorbent acrylic acid polymers, preferably provided in bead form. The polymers may include functional groups for selectively removing blood borne waste products, e.g. urea, from the G.I. tract.
Abstract: The present invention provides a suitable technique namely wet milling and the process for reducing the particle size of efavirenz and making a tablet or capsule formulation with desired bioavailability equivalent to the reference listed drug without loosing its characteristics.
Abstract: The invention relates to a pharmaceutical immediate release tablet comprising a core comprising 70-85 weight percent of sevelamer carbonate, calculated as an anhydrous compound, 10-25 weight percent of lactose monohydrate and, optionally, a water soluble film coat surrounding the to a process of making such tablets, to their use in medicine, and to the use of polyvinyl alcohol-polyethylene glycol graft copolymer for making such coated tablets.
Abstract: The present invention broadly relates to a process for preparing products comprising active components, and in particular biological materials, wherein the active components are stabilised. The invention further relates to compositions comprising the products, and in particular compositions comprising therapeutic biological materials.
Abstract: A composition with enhanced thermogenic activity and the use thereof in the prevention and treatment of obesity Pharmaceutical compositions of a dietary supplement or medical device, useful for the treatment and prevention of overweight and obesity and metabolic syndrome comprising: a) menthol or a peppermint essential oil comprising menthol, in association with one or more components having a thermogenetic activity, selected from: b1) capsaicin or a capsacinoid derived from Capsicum genus or a Capsicum extract containing capsaicin and/or capsacinoids; b2) a sulphur containing active principle derived from the Allium genus or an Allium extract containing it; b3) a catechin active substance derived from the genus Camellia or a Camellia extract containing it. The menthol and mint essential oil have a potentiating action on the biological activities of the other aforementioned components.
Abstract: Formulations for controlled delivery of oral transmucosal medications are provided. The formulations are characterized as hydrogel-forming or eroding-types which are bioadhesive and provide for controlled and sustained release of the medication such that enhanced bioavailability and efficacy is provided.
Type:
Grant
Filed:
January 5, 2007
Date of Patent:
August 28, 2012
Assignee:
Acelrx Pharmaceuticals, Inc.
Inventors:
Stelios Tzannis, Pamela Palmer, Thomas Schreck, Larry Hamel, Andrew I. Poutiatine
Abstract: Bioadhesive drug formulations that adhere to an oral mucosal membrane of a subject are provided together with single dose applicators and devices for delivering the drug formulations to the oral mucosa, and methods for using the same.
Type:
Grant
Filed:
July 3, 2007
Date of Patent:
August 28, 2012
Assignee:
Acelrx Pharmaceuticals, Inc.
Inventors:
Stelios Tzannis, Larry Hamel, Pamela Palmer, Thomas Schreck, Andrew I. Poutiatine
Abstract: Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys Glu Tyr Cys Cys Asn Pro Ala Cys Thr Gly Cys Tyr (“linaclotide”) or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.
Type:
Application
Filed:
August 14, 2009
Publication date:
August 23, 2012
Applicants:
Forest Laboratories Holdings Limited, Ironwood Pharmaceuticals, Inc.
Inventors:
Angelika Fretzen, Steven Witowski, Alfredo Grossi, Hong Zhao, Mahendra Dedhiya, Yun Mo
Abstract: The present invention relates to novel microporous zirconium silicate compositions that are formulated to remove toxins, e.g. potassium ions, from the gastrointestinal tract at an elevated rate without causing undesirable side effects. The preferred formulations are designed avoid increase in pH of urine in patients and/or avoid potential entry of particles into the bloodstream of the patient. Also disclosed is a method for preparing high purity crystals of UZSi-9 exhibiting an enhanced level of potassium exchange capacity. These compositions are particularly useful in the therapeutic treatment of hyperkalemia.
Type:
Application
Filed:
February 10, 2012
Publication date:
August 23, 2012
Applicant:
ZS Pharma, Inc.
Inventors:
Donald Jeffrey Keyser, Alavaro F. Guillem
Abstract: Highly compactable granulations and methods for preparing highly compactable granulations are disclosed. More particularly, highly compactable calcium carbonate granulations are disclosed. The granulations comprise powdered materials such as calcium carbonate that have small median particle sizes. The disclosed granulations are useful in pharmaceutical and nutraceutical tableting and provide smaller tablet sizes upon compression than previously available.
Type:
Application
Filed:
April 20, 2012
Publication date:
August 23, 2012
Applicant:
DELAVAU L.L.C.
Inventors:
Kevin W. Lang, James W. Dibble, Raya Levin, Gregory B. Murphy
Abstract: Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.
Type:
Grant
Filed:
May 22, 2012
Date of Patent:
November 13, 2012
Assignee:
Cosmo Technologies Limited
Inventors:
Roberto Villa, Massimo Pedrani, Mauro Ajani, Lorenzo Fossati