Abstract: Provided herein is a copolymer that includes a soft block (A) that contains poly(ester amide) (PEA) and a hard block (B). The copolymer can be any of AB, ABA or BAB type block copolymers. By varying the relative amount of the PEA block and the hard block, one can obtain a copolymer with a Tg for mechanical integrity in drug-delivery stent applications. The copolymer can be used alone or optionally in combination with a biobeneficial material and/or a biocompatible polymer to form an implantable device or a coating on an implantable device. When the copolymer is used in combination with a biobeneficial material, the copolymer and the biobeneficial material can be co-deposited or applied in sequence during the coating process. A coating formed of the copolymer may also include a bioactive agent.
Abstract: The present invention is directed to a series of new polycationic biodegradable polyphosphoramidates. Process for making the polymers, compositions containing these polymers and bioactive ligands to enhance the cellular uptake ad intracellular trafficking, articles and methods for delivery of drugs and genes using these polymers are described. A gene delivery system based on these polymers is prepared by complex coacervation of nucleic acid (DNA or RNA) with polymers. Targeting ligands and molecules that could facilitate gene transfer can be conjugated to polymers to achieve selective and enhanced gene delivery. The current invention also provides a complex composition with buffering capacity.
Abstract: The use of a 1,3-oxathiolane nucleoside analogue and pharmaceutically acceptable derivatives thereof for the treatment of hepatitis B virus infections is disclosed. Pharmaceutical formulations are also provided.
Abstract: The invention provides elastomeric copolyester amides, elastomeric copolyester urethanes, and methods for making the same. The polymers are based on ?-amino acids and possess physical, chemical and biodegradation properties that render them suitable for use in the human body. The polymers are useful as carriers of drugs or other bioactive substances. The polymers can also be linked, intermixed, or a combination thereof, to one or more drugs. Additionally, the polymers can be used to coat stents, for example, to suppress restenosis. Furthermore, the biodegradation of the copolyester amides and copolyester urethanes allows for the delivery of essential ?-amino acids to sites in the body, for example, to facilitate wound repair of injured tissues.
Abstract: Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.
Abstract: The invention provides methods and compositions for the oral delivery of pharmaceutically active agents. In particular, the compositions generally comprise a plurality of pharmaceutically active agents embedded in a matrix that is substantially erodable when contacted with an aqueous medium. The compositions may also include an inner core comprising an inert material. The compositions may be introduced into the oral cavity of a subject by liquid beverage or food product comprising a composition of the invention.
Type:
Application
Filed:
January 29, 2008
Publication date:
July 31, 2008
Applicant:
DRUGTECH CORPORATION
Inventors:
Jonathan David Bortz, Paul Timothy Brady, Yury Lagoviyer
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.
Type:
Application
Filed:
April 2, 2008
Publication date:
July 31, 2008
Applicant:
ALZA CORPORATION
Inventors:
Liang-Chang Dong, Patrick S.L. Wong, Vincent Joseph Ferrari, Steven Espinal
Abstract: A pharmaceutical composition comprises clonidine or a pharmaceutically acceptable salt or prodrug thereof. The composition, when administered to a patient in an amount delivering a clonidine dose of about 0.1 to about 2 mg/day, exhibits clonidine release properties providing a 24-hour profile of plasma clonidine concentration that (a) does not substantially or protractedly fall below about 0.2 ng/ml and exhibits a peak concentration that is therapeutically effective and does not cause unacceptable side effects in the patient; and/or (b) exhibits a peak that substantially coincides with or closely anticipates a time of maximum plasma concentration of a catecholamine occurring in a diurnal cycle of a patient having a catecholamine-mediated disease or disorder. A method for treating a disease or disorder for which clonidine is indicated in a patient comprises administering such a composition one to three times daily in a dose of about 0.1 to about 2 mg/day to the patient.
Abstract: A capsule medication administration system includes: a first capsule for internal body marking; a second capsule for medication; a marking device which makes a marking within a living body; a drug retention section which retains a drug; a release device which releases the drug; a detection device which detects the marking; a decision device which decides whether or not a marking which has been detected by the detection device is a specified marking; and a release control device which operates the release devices if it has been decided by the decision device that it is the specified marking; wherein the first capsule comprises the marking device. The second capsule comprises the drug retention section and the release device.
Abstract: The present invention provides an oral dosage form comprising a first composition and a second composition. The first composition comprises an effective amount of a therapeutic agent and the second composition comprises an effective amount of an adverse-effect agent. The adverse-effect agent is covered with a coating that is substantially insoluble in the gastrointestinal tract. In one embodiment, the adverse-effect agent is coated with an outer base-soluble layer and an inner acid-soluble layer. The therapeutic agent can be uncoated or can be coated with a coating having an outer acid-soluble layer and an inner base-soluble layer. The dosage form discourages administration of the therapeutic agent by other than oral administration.
Type:
Grant
Filed:
September 23, 2004
Date of Patent:
June 10, 2008
Assignee:
Purdue Pharma L.P.
Inventors:
Curtis Wright, IV, Anthony E. Carpanzano
Abstract: A capsule medication administration system includes: a first capsule for internal body marking; a second capsule for medication; a marking device which makes a marking within a living body; a drug retention section which retains a drug; a release device which releases the drug; a detection device which detects the marking; a decision device which decides whether or not a marking which has been detected by the detection device is a specified marking; and a release control device which operates the release device, if it has been decided by the decision device that it is the specified marking; wherein the first capsule comprises the marking device. The second capsule comprises the drug retention section and the release device.
Abstract: The present invention pertains to pharmaceutical formulations and systems for delivery of active agents, wherein a first fraction of an active agent is suspended in a vehicle and a second fraction of active agent is solubilized in the vehicle, with the suspended fraction representing about 5 wt. % to about 80 wt. % of the active agent and the second fraction representing about 20 wt. % to about 95 wt. % of the active agent. One or more additional active agents, which may be fully solubilized, partially solubilized, or suspended, may also be present. The first and second fractions of the active agent may or may not have different release profiles. Generally, a significant fraction of the solubilized drug will release rapidly, providing for rapid onset, while the suspended drug may be formulated for delayed and/or sustained release.
Type:
Grant
Filed:
February 11, 2002
Date of Patent:
May 20, 2008
Assignee:
Lipocine, Inc.
Inventors:
Feng-Jing Chen, Srinivasan Venkateshwaran, Steven L. Krill, Mahesh V. Patel
Abstract: A sustained release formulation as a unit dose contains 100 mg-1000 mg of Acetaminophen and 15 mg-150 mg of tramadol hydrochloride, which comprises of 1) an immediate release portion comprising of 25%-75% of the total effective amount of drug in the dosage form and 2) a sustained release portion comprising of a) 25%-75% of the total effective amount of drugs in the dosage form; b) 6%-50% of gelling polymers of the total formulation, and c) optionally an enteric coating at a level of 5%-40% of the total formulation. The set forth formulation dissolves 25%-60% of the total drug in the first hour, 50%-90% of the total drug in the first four hours and not less than 80% of the total drug in the first 12 hours using USP dissolution method II at 50 rpm.
Abstract: A multiple-unit oral sustained release preparation is provided which allows controlled release of imidafenacin [4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide]. The preparation serves to ensure a prolonged effect of imidafenacin and prevent rapid elevation in the blood levels of imidafenacin. Specifically, granules or powders comprising imidafenacin dispersed in a water-insoluble polymer or a higher alcohol are used in the preparation. These preparations achieve sustained release of imidafenacin since the molecular network structure that the water-insoluble polymer or the higher alcohol forms during the preparation of the granules or powders serves to control the rate of diffusion of imidafenacin in water. Granules comprising a core granule having two layers of an inner imidafenacin coating and an outer water-insoluble polymer coating are used in the preparation. The water-insoluble polymer coating serves to control the rate of diffusion of imidafenacin in water and ensure sustained release of imidafenacin.
Abstract: It is an object of the present invention, in the case of a controlled-release pharmaceutical composition, particularly a pulsed-release pharmaceutical composition, containing an acid-unstable physiologically active substance, to provide a pharmaceutical composition having little variation in dissolution lag time and high reliability of dissolution characteristics. The present invention discloses a controlled-release pharmaceutical composition comprising: 1) a core containing an acid-unstable physiologically active substance and a disintegrant; and 2) a release-controlling coating which covers the core, and which contains a water-insoluble polymer, an enteric polymer and a hydrophobic wax.
Abstract: Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.
Type:
Application
Filed:
October 10, 2006
Publication date:
April 10, 2008
Applicant:
Penwest Pharmaceuticals Co.
Inventors:
Anand R. Baichwal, Kevin Fitzmaurice, Steve Labudzinski
Abstract: Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.
Type:
Application
Filed:
October 10, 2006
Publication date:
April 10, 2008
Applicant:
Penwest Pharmaceuticals Co.
Inventors:
Anand R. Baichwal, Kevin Fitzmaurice, Steve Labudzinski, Michelle Howard-Sparks, William Hein
Abstract: The invention relates to sustained release pharmaceutical compositions of venlafaxine, process for preparing such compositions and method of using such compositions. Preferably, it relates to a sustained release pharmaceutical composition of venlafaxine comprising a first sustained release portion and a second sustained release portion wherein the first and the second sustained release portions are mixed in particular proportion in the formulation.
Abstract: A resin composition is prepared by reacting components comprising dibasic acid, diamine, polyol and monoalcohol, wherein (a) at least 50 equivalent percent of the dibasic acid comprises polymerized fatty acid; (b) at least 50 equivalent percent of the diamine comprises ethylene diamine; (c) 10-60 equivalent percent of the total of the hydroxyl and amine equivalents provided by diamine, polyol and monoalcohol are provided by monoalcohol; and (d) no more than 50 equivalent percent of the total of the hydroxyl and amine equivalents provided by diamine, polyol and monoalcohol are provided by polyol. This resin composition may be formulated into, for example, personal care products, fragrance releasing products and candles.
Abstract: A composition includes 10-50 wt. % quercetin; ?3 wt. % papain; ?3 wt. % calcium salt; ?1 wt. % zinc salt; ?1 wt. % bee pollen; ?1 wt. % pumpkinseed; ?0.5 wt. % bromelain; and 0.1 to 1.5 wt. % saw palmetto; wherein the composition is a sustained release composition in tablet or capsule form suitable for oral administration to a human. Methods of making and using the composition are provided.
Abstract: A capsule for oral administration to a human subject. The capsule comprises at least two different pharmaceutical compositions in granular form. This Abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.
Type:
Application
Filed:
July 28, 2006
Publication date:
January 31, 2008
Applicant:
Sovereign Pharmaceuticals, Ltd.
Inventors:
Suresh Dixit, Ralph Brown, Juan Carlos Menendez, Kripesh Munnirpallam
Abstract: This invention relates to an oral dosage form of a pharmaceutically active ingredient comprising: (a) an outer capsule and (b) non-uniform pellets, having a non-uniform shape and/or size, contained within the capsule, wherein the pellets comprise a compressed powder comprising a pharmaceutically active ingredient. In one embodiment the active ingredient is selected from the group consisting of doxycycline, omeprazole, esomeprazole, and propafenone. Pharmaceutical formulations of the active ingredients as well as methods and tools for making the oral dosage form are also described.
Type:
Application
Filed:
July 14, 2006
Publication date:
January 17, 2008
Inventors:
Ping He, Damodar Patel, Suketu Sanghvi, Robert Femia
Abstract: The present invention is directed to the systemic administration of Fosfluridine Tidoxil, (5-fluorouridine)-5?-phosphoric acid (3-dodecylmercapto-2-decyloxy)propylester or a salt thereof, for the treatment of intraepithelial proliferative diseases such as actinic keratosis. The Fosfluridine Tidoxil can be systemically administered alone or in combination with topical treatment agents.
Type:
Application
Filed:
July 14, 2006
Publication date:
January 17, 2008
Applicant:
HEIDELBERG PHARMA GMBH
Inventors:
Erwin Boehm, Michael Kulke, Eggert Stockfleth
Abstract: The present invention relates to a controlled release pellet of metoprolol and its pharmaceutically acceptable salts that uses a water soluble or a water swellable inert starting seed or core.
Type:
Grant
Filed:
July 11, 2003
Date of Patent:
January 1, 2008
Inventors:
Mongkol Sriwongjanya, Samuel Yuk, Avinash Nangia
Abstract: The present invention is related to a solid pharmaceutical composition comprising two separate regions, a first region comprising at least one non-steroidal anti-inflammatory drug (NSAID) and an adequate pharmaceutical carrier containing a retardant material for an extended release delivery of said non-steroidal anti-inflammatory drug (NSAID), and a second region comprising a stabilized gastroprotective prostaglandin and an adequate pharmaceutical carrier for an immediate release of said stabilized gastroprotective prostaglandin.
Abstract: The present invention provides elastomeric copolyester amides, elastomeric copolyester urethanes, and methods for making the same. The polymers that are based on ?-amino acids and possess suitable physical, chemical and biodegradation properties. The polymers are useful as carriers of drugs or other bioactive substances. The polymers can be linked, intermixed, or a combination thereof, to one or more drugs.
Abstract: The invention relates to immunostimulatory nucleic acid compositions and methods of using the compositions. The T-rich nucleic acids contain poly T sequences and/or have greater than 25% T nucleotide residues. The TG nucleic acids have TG dinucleotides. The C-rich nucleic acids have at least one poly-C region and/ore greater than 50% c nucleotides. These immunostimulatory nucleic acids function in a similar manner to nucleic acids containing CpG motifs. The invention also encompasses preferred CpG nucleic acids.
Type:
Grant
Filed:
December 9, 2002
Date of Patent:
September 18, 2007
Assignees:
University of Iowa Research Foundation, Coley Pharmaceutical GmbH
Inventors:
Arthur M. Krieg, Jörg Vollmer, Christian Schetter
Abstract: Pharmaceutical compositions in unit dose form comprising capsules containing one or more first active pharmaceutical ingredient in a pharmaceutically acceptable vehicle, coated with one or more second active pharmaceutical ingredients, wherein the unit dose form is a pharmaceutical grade finished dosage form, and methods of making and using the same.
Abstract: The present invention relates to a novel controlled release dosage form that releases therapeutic amounts of a sedative or hypnotic agent rapidly after administration and maintains therapeutic levels for about eight hours after administration.
Abstract: The present invention relates to extended release pharmaceutical compositions comprising a beta-blocker drug or a pharmaceutically acceptable salt thereof, wherein said composition comprises at least two extended release portions, each portion having an in vitro dissolution profile that is different from another portion.
Abstract: A resin composition is prepared by reacting components comprising dibasic acid, diamine, polyol and monoalcohol, wherein (a) at least 50 equivalent percent of the dibasic acid comprises polymerized fatty acid; (b) at least 50 equivalent percent of the diamine comprises ethylene diamine; (c) 10-60 equivalent percent of the total of the hydroxyl and amine equivalents provided by diamine, polyol and monoalcohol are provided by monoalcohol; and (d) no more than 50 equivalent percent of the total of the hydroxyl and amine equivalents provided by diamine, polyol and monoalcohol are provided by polyol. This resin composition may be formulated into, for example, personal care products, fragrance releasing products and candles.
Abstract: A method for determining the release of a peptide from a sustained release polylactide formulation which can be carried out in a shorter time than a real-time method by accelerating the release of the peptide from the formulation. It can be used to discriminate between batches of formulations for quality control purposes and to discriminate between formulations, for example, having different drug loadings.
Type:
Grant
Filed:
October 5, 2001
Date of Patent:
July 24, 2007
Assignee:
AstraZeneca AB
Inventors:
Brian Collingwood Clark, David Michael Cross, Paul Richard Gellert, Rodney Simon Kittlety
Abstract: Once a day modified release oral dosage form comprising of granules or pellets which are either compressed into tablet or filled inside the capsule, wherein the pellet has a core of active ingredient coated on non pareil seeds with a rate controlling functional coating of co-polymer of polyvinyl acetate optionally with an intermediate separating coating between the core and the functional coating layer.
Abstract: Methods and compositions for preventing abuse of dosage forms comprising an opioid analgesic and an aversive agent (e.g., a dye) in an effective amount to deter an abuser from administering a tampered form of the dosage form intravenously, intranasally, and/or orally are revealed.
Abstract: Composite materials comprising a water-soluble compound adsorbed onto a basic inorganic material and a bio-degradable polymer which yields acidic degradation products, methods of producing same, and methods of use thereof are described, wherein the composite materials are designed so as to provide controlled release of the water soluble molecule.
Abstract: A pharmaceutical composition of anti-tubercular drugs for oral use comprising Rifampicin and/or Isoniazid wherein the bioavailability of Rifampicin and/or other drugs is enhanced. Preferably the bioavailability of Rifampicin is enhanced by preventing its degradation caused by presence of Isoniazid. Rifampicin and/or Isoniazid may be present in delayed release and/or extended release form such that minimal amount of the drug is dissolved between pH 1 and 4. preferably delayed release of Rifampicin and/or Isoniazid is achieved by treating the drugs with pH sensitive polymers.
Abstract: The invention is directed to a drug delivery device for controlled release of a drug, comprising a core that has a cylindrical plug embedded therein; and a coating that at least partially surrounds the core. The core is comprised of a drug and excipients. The coating surrounding the core is essentially impermeable to the drug. The cylindrical plug, which is embedded in the core, may be hollow or solid. The drug delivery device enables zero-order drug release profiles as well as more complicated release profiles to be obtained. The invention is also directed to a method of making the drug delivery device.
Type:
Grant
Filed:
July 10, 2002
Date of Patent:
March 27, 2007
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
Moshe Fleshner-Barak, E. Itzhak Lerner, Vered Rosenberger
Abstract: The invention provides compositions comprising an RAR antagonist for promoting chondrogenesis and methods employing such compositions for treating cartilage and associated bone abnormalities resulting from injury or disease and for ex vivo tissue engineering.
Type:
Grant
Filed:
November 19, 1999
Date of Patent:
March 6, 2007
Assignee:
University of Western Ontario
Inventors:
Tully Michael Underhill, Andrea Dawn Weston
Abstract: A stable composition of a drug comprising a carrier having a phosphatidylcholine component which entraps the drug is applied to the skin for transdermal delivery of the drug.
Abstract: The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).
Abstract: Methods and reagents for improved treatment and diagnostic imaging, particularly of cancer. The methods and reagents utilize specific targeting of treatment and imaging ligands to the targeted tumor, or specific organ or tissue, in association with extracorporeal affinity adsorption of the targeting ligand. The targeted species include antibodies as well as other peptides with specific affinity to the targeted tumor organ or tissue. Included are hybrid targeting molecules, such as hybrid F(ab?)2, with one binding site specific for the target and the other binding site specific for the targeted treatment or visualization ligand. The affinity adsorption devices may include adsorbents specific to one or more of the components of the targeting molecule-targeted ligand moiety.
Abstract: Bioerodible poly(ortho esters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents from dioxane-based di(ketene acetals). Block copolymers contain these bioerodible poly(ortho esters). These block copolymers have both hydrophilic and hydrophobic blocks. They form micelles in aqueous solution, making them suitable for encapsulation or solubilization of hydrophobic or water-insoluble materials; and they also form bioerodible matrices for the sustained release of active agents.
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of an irritant to impart an irritating sensation to an abuser upon administration of said dosage form after tampering.
Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.
Type:
Grant
Filed:
May 23, 2003
Date of Patent:
December 26, 2006
Assignee:
Sicor, Inc.
Inventors:
Dorla Mirejovsky, Peter Lindsay Macdonald
Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.
Type:
Grant
Filed:
December 20, 2002
Date of Patent:
December 12, 2006
Assignee:
Schering Aktiengesellschaft
Inventors:
Wolfgang Heil, Ulf Tistam, Ralph Lipp, Johannes-Wilhelm Tack
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic; an opioid antagonist; and a bittering agent in an effective amount to impart a bitter taste to an abuser upon administration of the dosage form after tampering.
Type:
Grant
Filed:
August 6, 2002
Date of Patent:
December 5, 2006
Assignee:
Euro-Celtique S.A.
Inventors:
Benjamin Oshlack, Robert Colucci, Curtis Wright, Christopher Breder
Abstract: Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse; and an effective amount of a bittering agent to impart a bitter taste to an abuser upon administration of said dosage form after tampering.
Type:
Grant
Filed:
August 6, 2002
Date of Patent:
November 28, 2006
Assignee:
Euro-Celtique S.A.
Inventors:
Benjamin Oshlack, Robert Colucci, Curtis Wright, Christopher Breder