POLYOX Water-Soluble Resins NF Patents Related to Pharmaceutical Applications

Oral Drug Delivery

Osmotic Dosage Form Comprising First and Second Coats ALZA Corporation WO 9929297 1999 A dosage form comprises a drug compartment surrounded by a first coat and a second coat with an exit for administering a drug in a linear profile, especially for cardiovascular, arthritic, respiratory, cancer, analgesic and other therapies. Dosage Form and Method for Treating Incontinence ALZA Corporation US 5912268 1999 A new dosage form for the delivery of oxybutynin. A wall permeable to fluid and impermeable to oxybutynin surrounds a drug core. The wall has an exit for delivering the oxybutynin. The drug core comprises oxybutynin, PEO, and HPMC. Dosage Form Comprising Means for Changing Drug Delivery Shape ALZA Corporation WO 9912527 1999 A flexible dosage form is capable of changing its shape during the operation. This dosage form can deliver all the intended dose of therapeutic agent. It maintains its physical integrity while avoiding and/or reducing the risks associated with dose dumping. Improved HMG CoA Reductase Inhibitor Extended Release Formulation Andrx Pharmaceuticals Inc. WO 9930692 1999 A controlled-release dosage formulation compromises (a) a compressed tablet core of substituted naphthalene compound, pharmaceutically acceptable, water-swellable polymer and an osmotic agent; and (b) an outer coating layer that completely covers the osmotic core and comprises pH-sensitive coating agent and a water-insoluble polymer. Matrix for Controlled Delivery of Highly Soluble Drugs Temple University WO 9921551 1999 A monolithic tablet provides zero-order delivery of highly soluble drugs over extended periods of time. The dosage form comprises granules dispersed in a matrix of a more swellable, erodible polymer. Gastric-Retentive, Oral Drug Dosage Forms for the Controlled-Release of Sparingly Soluble Drugs and Insoluble Matter DepoMed, Inc. US 5972389 1999 A controlled release oral dosage form comprises a tablet or capsule containing a plurality of solid drug particles dispersed in a swellable/erodible polymer matrix. The particles imbibe water to cause them to swell and promote retention in fed-mode-induced patients. Sustained Release Formulation Containing Three Different Types of Polymers and Tablet Formed Therefrom Duramed Pharm, Inc. WO 9929305 1999 A Depot drug formulation includes pharmaceutical itself, and a three-component rate controlling matrix composition. The three components are a pH dependent gelling polymer, a pH independent gelling polymer, and an enteric polymer.

Monolithic System Containing One or More Drugs, Consisting of Three Layers with Different Release Mechanisms Chiesi Farmaceutici S.P.A. WO 9917745 1999 An oral controlled-release monolithic system comprises three layers consisting of a disintegrating layer, an erodible layer and a swelling layer, of which two are external and one is intermediate. Each layer contains one or more drugs. Controlled Release Pharmaceutical Compositions Containing Tiabagine Elan Corp, PLC WO 9906045 1999 A controlled-release dosage form comprises tiagabine dispersed in rate controlling polymeric matrix comprising at least one rate controlling polymer. The oral dosage can be formulated into tablets or multiparticulates. The release profile for the formulation containing POLYOX, which has a relatively low moisture content compared to the Methocels, is almost equivalent to that of the K15M grade of Methocel. Dosage Form Comprising Oxybutynin ALZA Corporation US 5840754 1998 A composition comprising oxybutynin, a controlled-release device comprising oxybutynin, and a method for administering oxybutynin are disclosed to treat incontinence. Exit Means in Dosage Form ALZA Corporation US 5718700 1998 PEO is useful as an osmopolymer that imbibes fluid, expands and pushes the drug layer from the dosage form. Once Daily Pharmaceutical Tablet having a Unitary Core Andrx Pharmaceuticals Inc. WO 9833489 1998 A controlled release tablet comprises a compressed tablet core containing a sparingly water-soluble medicament, a water-soluble osmotic compound and one or more osmotic polymers, and a completely covered membrane coating. Controlled Release Formulation for Water Insoluble Drugs in Which a Passage Is Formed in Situ Andrx Pharmaceuticals Inc. US 5736159 1998 A controlled release tablet for a calcium channel blocker treatment comprises a core containing calcium channel blocker, water soluble osmotic agent, water-soluble polymeric binder and water-swellable polymer and polymeric memb rane coating. Controlled Release Drug Delivery System Temple University US 5783212 1998 A controlled release three-layered tablet provides zero-order release. The tablet comprises two barrier layers and a drug-containing layer, each comprising swellable, erodible polymers. Gastric-Retentive Oral Drug Dosage Forms for Controlled Release of Highly Soluble Drugs DepoMed, Inc. WO 9855107 1998 A controlled-release oral drug dosage form comprises a drug dispersed in a polymer matrix that swells to at least twice its volume upon absorption of water and forms gastric retention system. Gastric-Retentive, Oral Drug Dosage Forms for the Controlled Release of Sparingly Soluble Drugs and Insoluble Matter DepoMed, Inc. WO 9811879 1998 A controlled-release oral dosage form comprises a tablet or capsule containing a plurality of solid drug particles dispersed in a swellable/erodible polymer matrix. The particles swell upon imbibing water, promoting retention in fed-mode-induced patients.

Pharmaceutical Compositions for Sustained Release of HMG-CoA Reductase Inhibitor Fluvastatin Astra Aktiebolag WO 9815264 1998 A coated matrix system is especially suitable for the delivery of highly water-soluble drugs. The eroding matrix material is preferably polyethylene oxide, hydroxypropylmethylcellulose. For diffusion-controlled membrane-coated formulations, the film forming material is preferably ethylcellulose, hydroxypropylmethylcellulose or hydroxypropylcellulose. Uniform Drug Delivery Therapy ALZA Corporation WO 9737640 1997 An oral dosage form provides a constant and uniform delivery of known drugs over time. The controlled release system provides uniform drug release rate by controlling particle sizes. Composition and Dosage Form Comprising Opioid Antagonist ALZA Corporation WO 9733566 1997 A controlled release dosage form for delivery of opioids reduces potential for drug abuse. The dosage form comprises a bilayer core with first layer containing opioid and second layer including opioid antagonist, PEO and hydroxyalkylcellulose. Controlled Release Tablet Temple University WO 9748385 1997 A controlled release tablet comprises a pharmaceutical agent, a lubriuicant, and a water swellable polymer. Gastric-Retentive, Oral Controlled Drug Delivery System with Enhanced Retention Properties DepoMed, Inc. WO 9747285 1997 A gastric-retentive dosage form comprises a solid-state drug dispersed in a solid matrix of water-swellable polymer, and a chemical agent that pharmacologically induces the fed mode on the patients stomach. Pharmaceutical Formulations Pfizer WO 9718814 1997 A controlled-release formulation comprises a drug, low molecular weight polyethylene oxide, hydroxypropylmethyl cellulose, tabletting excipients, and optional enteric polymers. The use of low molecular weight polyethylene oxide enhances the erosion of the hydroxypropylmethylcellulose matrix after a predetermined period of time. Dosage Form Comprising Oxybutynin ALZA Corporation WO 9637202 1996 A composition comprising oxybutynin and a device comprising oxybutynin and polyalkylene oxide and hydroxyalkylcellulose are disclosed for oxybutynin therapy. Osmotic Device with High Drug Loading and Delayed Activation of Drug Delivery ALZA Corporation WO 9637189 1996 A device for delayed release comprises two sliding telescopic parts: the first impermeable and holding active agent and the second semipermeable and holding osmotic material and a piston. The fluid-imbibing device dispenses active agents to a fluid environment after a preset delay. Injection-Molded Dosage Form ALZA Corporation WO 9613248 1996 A dosage form comprises an injection-molded housing membrane, which permits the passage of fluid and defines the internal compartment containing a therapeutic composition and an expandable composition.

Hydrocodone Compositions ALZA Corporation WO 9608253 1996 A dosage form comprises hydrocodone, poly(alkylene oxide) possessing 75,000 to 400,000 mol.wt., hydroxyalkylcellulose possessing 9,000-150,000 mol. Wt., and a lubricant. A semipermeable wall with an exit passageway encased the therapeutic core. Tacrine Pharmaceutical Compositions ALZA Corporation WO 9600065 1996 A sustained release tacrine composition comprises an osmotic caplet containing tacrine and osmotic auxiliary giving high internal osmotic pressure. Controlled Release Tablet Temple University WO 9626718 1996 A controlled release tablet consists of a single homogenous mixture of a pharmaceutical agent and an excipient mixture comprising a water-swellable polymer and a lubricant. The rate of swelling is equal to the rate of dissolution for the water-swellable polymer. Sustained Release Formulation Containing Three Different Types of Polymers Hallmark Pharmaceuticals, Inc. WO 9626717 1996 Verpamil Depot drug formulations include the drug to be released over time, an alginate component, an enteric polymer component, and a pH independent gelling polymer. Solid Compositions Containing Polyethylene Oxide and a Non-Amorphous Active Ingredient Pharma Pass WO 9632097 1996 PEO (10-35 w.t. %) is used in a composition of sustained-release formulation. Dry mixing or granulation may be used to produce the composition. Effective Dosage Form for Antiepileptic Drugs ALZA Corporation WO 9529665 1995 An improved dosage form provides extended release of an anti-epileptic drug formulation by maintaining the integrity of the dosage form and protecting the anti-epileptic drug. Pentoxifylline Dosage Form ALZA Corporation WO 9519174 1995 A slow release dosage form of pentoxifylline is disclosed. The dosage form provides a continuous delivery of pentoxifylline over an extended period of time. Slow Release Dosage Forms of Pentoxifylline - For Treating Chronic Peripheral Arterial Disease Alza Corp. WO 9,591,174 1995 Poly(ethylene oxide) is used in an osmotic drug delivery system. Note: Also see "Osmotic drug delivery: a review of the patent literature" in the Journal of Controlled Release 35, 1-21, 1995 for expanded references in this area. Controlled Release Tablet Formulation Andrx Pharmaceuticals Inc. US 5,458,887 1995 A controlled release tablet which consists of an osmotic core containing a drug and a water swellable polymer selected from hydroxypropylmethylcellulose or poly(ethylene oxide) plus a coating which consists of a water insoluble polymer and a minor amount of non-toxic, water soluble compound in an amount which dissolves in the GI to form a plurality of micropores in the coating.

Controlled-Release Dosage Forms of Azithromycin Pfizer Inc. WO 9530422 1995 A controlled release formulation of Azithromycin is described which meets specific release criteria via various design approaches. Poly(ethylene oxide) is claimed for an erodible version of the product. Oral Therapeutic System Having Systemic Action Ciba-Geigy Corporation US Re.34,990 1995 An oral therapeutic system of administering carbamiazepine uses poly(ethylene oxide) as a swellable polymer in a sustained release tablet. Sustained Antiepileptic Therapy ALZA Corporation WO 9427587 1994 An extended release dosage form comprises valproic acid or a valproic acid derivative, and osmopolymers. Direct Compression Tableting Process Using Polyethylene Oxide as Binder-Matrix to Give Controlled Release Rate, etc. Used Exp for Antihistamine Compsn. Contg. Clemastine Fumarate Sandoz LTD US 5,273,758 1993 Poly(ethylene oxide) is dry blended with pharmaceutical agent and directly compressed to form a sustained release matrix product. Sustained-Release Hydrogel Preparation Yamanouchi Pharmaceutical EP 0,661,045, A1 1993 A hydrogel delivery system is formed by combining a drug, a water soluble polymer, for example poly(ethylene oxide), a hydrophilic matrix. The hydrophilic matrix insures complete hydration of the tablet core in the upper GI which is claimed to improve drug delivery in the colon due to pre-hydration of the gel.

Therapeutic System for Sparingly Soluble Active Ciba-Geigy US 4,992,278 1991 A dosage form for peroral administration of a sparingly soluble active agent which consists of a water swellable polymer, an active agent, and an optional water-soluble compound contained within a semi-permeable membrane. Novel Drug Carrier and Pharmaceutical Preparation Comprising the Same T. Uemura et al. US 4,690,820 1987 An oral capsule which utilizes aqueous polymers, such as poly(ethylene oxide) and oil to control gastrointestinal transmit time. Carriers for Controlled-Release Pharmaceuticals Fujisawa Pharmaceutical Co. Jp Kokei 61233632 1986 Pharmaceutical carriers for oral drug delivery are prepared from high molecular weight poly(ethylene oxide) and oils. Sustained Release Pharmaceutical Composition of Solid Medical Material Yamanouchi Pharmaceutical Co. US 4,404,183 1983 A sustained released formulation of an amorphous indomethacine is presented which uses poly(ethylene oxide) as a dispersing and rate limiting polymer.

Mucosal Drug Delivery

Site-Specific Adhesion within the GI Tract Using Nanoparticles Stabilized by High Molecular Weight, Linear Poly(ethylene Oxide) Polymers NanoSystems LLC WO 9625153 1996 Nanoparticulate crystalline therapeutic or diagnostic agents are formulated with stabilizers and high molecular PEO to enhance contact between the active agents and the GI tract, providing site-specific, extended therapeutic or diagnostic effect. Oral Vehicle Composition Procter & Gamble Co. WO 9523591 1995 An oral muco-adhesive vehicle composition contains a water-soluble muco-adhesive polymer to improve contact of active ingredients with throat and mucous membranes. Mucosal Adhesive Device for Long-Acting Delivery of Pharmaceutical Combinations in Oral Cavity Rutgers University WO 9515137 1995 An oral cavity mucosal adhesive dosage unit releases drugs at a constant rate for at least 12 hours in the oral mucosa. The unit comprises a mucosal adhesive polymer layer having intermixed pharmaceuticals adhered to a protective backing layer or a tablet containing a mucosal adhesive polymer and intermixed pharmaceuticals. Dissolvable Device for Contraception or Delivery of Medication - Comprising at Least One Film Formed From eg., Polyvinyl Alcohol or Polyethylene Oxide, With Inert Gas Distributed Throughout R. J. Staab US 5,393,528 1995 Delivery of a contraceptive (i.e. nonoxymol-9) in a system which will dissolve and not require removal. X-Ray Contrast Compositions Containing Film-Forming Materials Sterling Winthrop Inc. US 5,405,600 1995 A mucoadhesive X-ray contrast agent is produced by mixing a mucoadhesive polymer, a divalent cation, and a X-ray contrast agent. Poly(ethylene oxide) is listed as a suitable non-ionic mucoadhesive polymer. Oral Vehicle Compositions The Proctor & Gamble Company US 5,458,879 1995 An oral liquid pharmaceutical mucoadhesive composition consisting essentially of a water soluyble mucoadhesive polymer such as poly(ethylene oxide), sodium carboxymethyl cellulose, and a pharmaceutically active agent(s). Solid Form Xerostomia Product Block Drug EP 613,684 1994 A solid product for relieving xerostomia symptoms which comprises a lubricating polymer comprising poly(ethylene oxide) and a sialologue in a pharmaceutically acceptalbe, substantially non-cariogenic carrier. Buccal Drug Usage Zetachron Inc. US 4,764,378 1988 An excipient for a pharmaceutical compound which melts at body temperature but will not spontaneously deform at higher temperatures is presented. Product uses blend of poly(ethylene glycol) and poly(ethylene oxide).

Pharmaceuticals for Oral Cavities Daiichi Seiyaku Co. Jpn. Kokei 59181218 1984 Sustained-release pharmaceuticals absorbed through the mucosal tissue contains poly(ethylene oxide) as a pharmaceutical excipient. Composition for Treating Acne Vulgaris Westwood Pharmaceuticals Inc. US 4,355,028 1982 A physically and chemically stable gel, made with poly(ethylene oxide) and containing salicylic acid and benzoyl peroxide are useful in the treatment of acne vulgaris.

Transdermal Drug Delivery

Water Soluble Pressure Sensitive Muco-adhesive-Useful in Devices which May be Placed in Mucosa-lined Body Cavities to Release Active Agents Cygnus Therapeutic Systems WO 9,505,416 1995 Water soluble pressure sensitive adhesive which includes a water soluble polymer that is rendered tacky at room temperature by the addition of a plasticizer. PEO is one of several claimed water soluble polymers. Extrudable Composition for Topical or Transdermal Drug Delivery Johnson & Johnson Consumer Prod. EP 598,606 1994 A composition for use in topical drug delivery or more specifically adhesive bandages. Consisting of a thermoplastic polymer chosen from hydroxypropyl cellulose and poly(ethylene oxide), a water-soluble polymer derived from acrylic acid, medicament, and a plasticizer. Composite Microporous Membrane Hoechts Celanese Corp. US 5,294,346 1994 A water soluble polymer is used to coat a porous membrane for use in transdermal delivery. The polymer coating is placed between the porous membrane and the adhesive to prevent plugging of the pores. PEO is one of the claimed polymers in the coating layer. Low-Melting Moldable Pharmaceutical Excipient and Dosage Forms Prepared Therewith Zetachron Inc. US 5,004,601 1991 An excipient useful for delivering pharmaceutically active compounds which melts at body temperature but does not deform at higher temperatures utilizes poly(ethylene oxide) as a component. Adhesive Polyethylene Oxide Hydrogel Sheet and Its Production Nepera Inc. US 4,686,558 1987 An adhesive sheet of hydrophilic gel is produced by subjecting a liquid film of an aqueous solution of poly(ethylene oxide) to ionizing radiation. Bioadhesive Exruded Film for Intra-Oral Drug Delivery and Process Johnson & Johnson Products US 4,713,243 1987 Extrusion processing is used to produce a single or multi-layered thin film which is useful in intraoral controlled drug delivery. The bioadhesive layer is prepared from hydroxypropyl cellulose, poly(ethylene oxide), and a glycol plasticizer.

Hydrogels for Wound Care

Hydrogel Patch Cygnus Inc. WO 9702811 1997 A disposable hydrogel patch converts the concentration of biologically important molecules such as glucose to a detectable signal such as electric current. The hydrogel patch comprises a hydrophilic polymer that forms a gel in the presence of water, an enzyme, and an electrolyte. Hydrogel Laminate Bandages and Wound Dressing Johnson & Johnson Consumer Products US 5,480,717 1996 A process is described in which an aqueous solutin of hydrophilic polymer is crosslinked while in contact with a supporting adhesive laminate. Ionizing radiation crosslinks the hydrogel and also induces copolymerization between the hydrophilic polymer and the substrate. The interfacial copolymerization is claimed to reduce delamination. Gel Forming System for Use As Wound Dressing Nepera Inc. US 5,578,66 1996 Poly(ethylene oxide) and/or polyvinylpyrrolidone is combined with an acidic containing polymer and an amino containing polymer in order to produce a gel suitable for use as a wound dressing. Injectable Polyethylene Oxide Gel Implant and Method for Production University of Miami WO 9606883 1996 A biocompatible polyethylene oxide gel implant and a method for production are claimed. The implant is prepared by dissolving a sample of polyethylene oxide in a saline solution in a sealed canister, removing free oxygen from the canister and replacing it with inert gas, and irradiating the canister to simultaneously crosslink and sterilize the polyethylene oxide. Adhesive Hydrogels Having Extended Use Lives And Process For The Preparation Of Promoter Nepera Inc. US 5,405,366 1995 A non-stringy adhesive hydrophilic gel comprising an aqueous mixture of at least one crosslinkable water-soluble polymer, a humectant and a crosslinking promoter. The humectant controls both the degree of crosslinking and the rate of water loss from the final product. Poly(ethylene oxide) can be used as the water-soluble polymer. Bilayer Wound Dressing Medipro Sci. Ltd. WO 9,204,923 1992 Self adhesive bilayer wound dressing has a permeable backing film and a tacky polymer complex adhesive layer. The adhesive layer can be produced, for example, by coprecipitation of poly(acrylic acid) and poly(ethylene oxide). Hemostatis Adhesive Bandage Johnson & Johnson Co. US 4,616,644 1986 A thin film of poly(ethylene oxide) is applied to the surface of a perforated adhesive bandage to improve the hemostatic effect of the bandage. Novel Dressing and Use Thereof Union Carbide Corp. US 3,419,006 1968 A transparent, permeable, and high water absorbing surgical dressing for wounds, burns, and infections is prepared by the cross linking of poly(ethylene oxide).

Injectable, Implant
Controlled Expansion Sphincter Augmentation Media Menlo Care, Inc. EP 811373 1997 A composition for injecting into tissues surrounding the urethra or ureter. The composition comprises physiologically acceptable solid polymer particles of a polyethylene oxide polymer or copolymer, or polyvinylpyrrolidone polymer or copolymer dispersed in a biodispersible liquid carrier. Controlled Expansion Sphincter Augmentation Media Menlo Care, Inc. EP 730847 1996 A composition for injecting into tissues surrounding the urethra or ureter. The composition comprises solid swellable polymer particles and a liquid carrier, and is used to treat urinary incontinence and vesicoureteral reflux. Dissolvable Device for Contraception or Delivery or Medication STAAB, Robert J. US 5393528 1995 A device for delivery of an active agent into body cavities has improved heat and humidity stability. The device comprises at least one dissolvable film formed from polyvinyl alcohol, polyethylene oxide, hydroxypropylmethylcellulose and mixtures thereof.

Coatings
One Step Thromboresistant Lubricious Coating Union Carbide Corporation US 5645931 1997 Articles having lubricious polymer coatings are disclosed. The coatings comprise a composite of polyethylene oxide and polyisocyanate. One Step Thromboresistant Lubricious Coating Union Carbide Corporation US 5558900 1996 A method of making articles having lubricious polymer coatings is disclosed. The coatings comprise a composite of polyethylene oxide and polyisocyanate.

Extrusion
Hot-Melt Extrudable Pharmaceutical Formulation University of Texas WO 9749384 1997 Hot-melt extrudable pharmaceutical formulation comprises a therapeutic compound and a high molecular weight polyethylene oxide. The composition can be hot-melt extruded without significant degradation or decomposition of either the PEO or drugs.

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Published May 2004

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