Anal, Rectal (e.g., Suppositories, Etc.) Patents (Class 424/436)
  • Patent number: 5587175
    Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.
    Type: Grant
    Filed: December 28, 1993
    Date of Patent: December 24, 1996
    Assignee: MDV Technologies, Inc.
    Inventors: Tacey X. Viegas, Lorraine E. Reeve, Raymond L. Henry
  • Patent number: 5578310
    Abstract: A topical bioadhesive ointment composition comprising an aqueous mineral oil emulsion which is readily spread able and film-forming, and, upon application to moist skin or a mucosal surface, forms a stable, coherent layer thereon which resists removal therefrom by water or a body fluid associated with the mucosal surface to which the ointment composition is applied is disclosed. Also disclosed are pharmaceutical compositions containing the ointment compositions and a pharmaceutically active agent, e.g. , TGF.alpha.; and methods of using and methods of preparing the compositions.
    Type: Grant
    Filed: June 3, 1994
    Date of Patent: November 26, 1996
    Assignee: Berlex Laboratories Inc.
    Inventors: Thabiso M'Timkulu, Ze'ev Shaked, Richard Hsu
  • Patent number: 5562913
    Abstract: Preparation of a formulation for mitigating ill effects of smoking, wherein one or more of the n-6 EFAs selected from GLA, DGLA and AA, and one or more of the n-3 EFAs selected from SA, 20:4n-3, EPA, DPA or DHA are used, preferably so that the daily dose of each fatty acid is within the range 1 mg to 100g/day. The formulation may in many other purposes be used in the treatment or prevention of ageing of the skin of smokers.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: October 8, 1996
    Assignee: Scotia Holdings PLC
    Inventor: David F. Horrobin
  • Patent number: 5554388
    Abstract: A composition for administration to the mucosa comprises a pharmacologically active compound and a polycationic substance. The polycationic substance is preferably DEAE-dextran or chitosan and the pharmacologically active compound is preferably insulin or calcitonin. The composition may be a solution, dispersion, powder or microspheres. Other enhancers, such as lysophosphatidylcholine, can be included if desired.
    Type: Grant
    Filed: December 14, 1993
    Date of Patent: September 10, 1996
    Assignee: Danbiosyst UK Limited
    Inventor: Lisbeth Illum
  • Patent number: 5552150
    Abstract: A natural or synthetic glycerol oil which comprises at least 20% by weight, preferably at least 25% of di-linoleoyl-mono-gamma-linolenyl-glycerol (DLMG), is used to supplement foods, nutritional compositions and in skin and hair care compositions.
    Type: Grant
    Filed: November 30, 1993
    Date of Patent: September 3, 1996
    Assignee: Efamol Holdings PLC
    Inventors: David F. Horrobin, Yung-Sheng Huang
  • Patent number: 5540931
    Abstract: The present invention provides methods and formulations for site-specific immune suppression of immune/inflammatory responses with localized or topical application of immunosuppressants including cyclosporines, rapamycins (RPM), or combinations of immunosuppressants and anti-inflammatory compounds. Methods for the use of said formulations to effect site-specific immune suppression of local inflammatory/immune responses in mammalian tissue and for treatment of autoimmune, T-cell mediated immune disease, inflammatory conditions, inhibition of contact hypersensitivity, and for producing prolonged skin allograft survival, and wound healing are presented. In addition, methods for use of said formulations--in tandem with systemic applications of immunosuppressant such as cyclosporine or without same--are presented. The present invention also relates to alternative formulations and delivery systems for the efficacious treatment of the aforementioned conditions.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: July 30, 1996
    Assignees: Charles W. Hewitt, Kirby S. Black
    Inventors: Charles W. Hewitt, Kirby S. Black
  • Patent number: 5538734
    Abstract: The present invention refers to the use of 5-methyltetrahydrofolic acid, of 5-formyltetrahydrofolic acid and of their pharmaceutically acceptable salts for the preparation of controlled release pharmaceutical compositions suitable for the use in the therapy of depressive disturbances, in particular major depression, dysthymia or depressive neurosis and not otherwise specified depressive disturbances, independently from folate plasmatic levels, and to the pharmaceutical composition thus prepared.
    Type: Grant
    Filed: February 9, 1995
    Date of Patent: July 23, 1996
    Assignee: Bioresearch S.p.A.
    Inventor: Christina Le Grazie
  • Patent number: 5529782
    Abstract: A dissolvable element containing an agent material is used for local administration of the agent material in an internal body area. The dissolvable element is made of dissolvable polymer material and/or complex carbohydrate material which are food grade materials and have selected dissolving properties, such that it remains in substantially solid form before use, and dissolves due to human body temperatures and moisture during use to release the agent material in a desired timed release and dosage. As a contraceptive, the dissolvable element is preferably a film made of polyvinyl alcohol, polyethylene oxide, hydroxypropyl methyl cellulose and/or carboxymethyl cellulose. The dissolvable element may be formed as a laminate of different film layers for compound release properties, or it may be ground into particles and incorporated in a tampon or suppository. The dissolvable element may be foamed as a means for increasing its dissolution rate.
    Type: Grant
    Filed: November 3, 1994
    Date of Patent: June 25, 1996
    Inventor: Robert Staab
  • Patent number: 5518735
    Abstract: D,L-, L- and D-phenyl alanine derivatives of formula (I) defined in claim 1 in which R.sub.1 is an amidino-, guanidino-, oxamidino-, aminomethyl- or amino group have been discovered which effectively prevent blood coagulation or thrombosis. The antithrombotically active compounds have low toxicity and may be administered by mouth, subcutaneously or intravenously.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: May 21, 1996
    Assignee: Pentapharm AG
    Inventors: Jorg Sturzebecher, Helmut Vieweg, Peter Wikstroem
  • Patent number: 5518729
    Abstract: In a preferred embodiment, drugs having pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as the active ingredient one or more N-substituted 2-(1H) pyridone(s). The composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
    Type: Grant
    Filed: May 16, 1994
    Date of Patent: May 21, 1996
    Inventor: Solomon B. Margolin
  • Patent number: 5518730
    Abstract: Biodegradable controlled release delivery systems using melt-spun biodegradable polymers as carriers for bio-effecting agents such as pharmaceutical actives are disclosed. Oral dosage forms as well as implants are described.
    Type: Grant
    Filed: June 3, 1992
    Date of Patent: May 21, 1996
    Assignee: Fuisz Technologies Ltd.
    Inventor: Richard C. Fuisz
  • Patent number: 5516526
    Abstract: This invention relates to a method of protection from and treatment of neurological damage in mammals by administration of dimethylsulfoxide (DMSO) in combination with fructose 1,6-diphosphate (FDP). The effects of administration of the drugs together, either as two separate compositions or in combination, results in synergistic action that greatly improves protection from morbidity in animals (including humans) who have suffered injury to the brain.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: May 14, 1996
    Inventor: Jack da la Torre
  • Patent number: 5512600
    Abstract: A novel processing technique is reported to bond non-woven fibers and, thus, prepare structural interconnecting fiber networks with different shapes for organ implants. The fibers are physically joined without any surface or bulk modification and have their initial diameter.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: April 30, 1996
    Assignee: Massachusetts Institute of Technology
    Inventors: Antonios G. Mikos, Robert S. Langer
  • Patent number: 5508037
    Abstract: Suppository formulations having long-term stability and containing readily bioavailable .DELTA..sup.9 -THC derivatives.
    Type: Grant
    Filed: February 2, 1995
    Date of Patent: April 16, 1996
    Assignee: The University of Mississippi
    Inventor: Mahmoud A. ElSohly
  • Patent number: 5500221
    Abstract: The present invention relates to a sustained-release suppository preparation characterized by comprising an acidic drug or a salt thereof which can be absorbed by rectal administration and an acidic compound or a pH buffering agent. The sustained-release suppository preparation of the present invention exhibits no rapid increase in blood concentration immediately after the administration and maintains its action for a long period of time. Thus, it is safer and exhibits a better therapeutic effect.
    Type: Grant
    Filed: March 18, 1994
    Date of Patent: March 19, 1996
    Assignee: SS Pharmaceutical Co., Ltd.
    Inventors: Masami Murata, Harumi Kishi, Takashi Narui, Shuichi Kasai, Akira Iwasa
  • Patent number: 5492937
    Abstract: A carrier composition that is a liquid at or below room temperature forms a high viscosity layer or gel at body temperature, which comprises a water-soluble, nonionic cellulose ether having a cloud point not higher than 40.degree. C., a charged surfactant and optional additives in water. The carrier composition can be used for oral or local administration of a pharmacologically active substance to the skin, mucous membrane, the eye or a body cavity.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: February 20, 1996
    Assignee: Pharmacia AB
    Inventors: Conny Bogentoft, Anders Carlsson
  • Patent number: 5490984
    Abstract: This invention discloses methods of repairing structurally defective or inadequately functioning muscles of the anal sphincter and methods of improving the competency of incompetent anal sphincters by administering an effective amount of an injectable biomaterial into the defect or into the anal sinuses, Preferred biomaterials to be used in this invention are collagen formulations.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: February 13, 1996
    Assignee: JSF Consulants Ltd.
    Inventor: Jeffrey S. Freed
  • Patent number: 5489577
    Abstract: Disclosed is a semi-solid pharmaceutical agent containing a stabilized proteinaceous bioactive substance prepared by successively mixing an oligosaccharide and an aqueous solution of a proteinaceous bioactive substance, and kneading the resultant solids with an oil or fat base. The pharmaceutical handles with ease because it is readily administered to the body through percutaneous and permucosal route which are safer and less in pain administration routes than other conventional administrations.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: February 6, 1996
    Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo
    Inventors: Masao Ikeda, Tomoki Tatefuji, Hiroshi Yamauchi
  • Patent number: 5484605
    Abstract: Chronic inflammatory intestinal diseases may be treated enterally pharmacologically active doses of said oxypurinol and or its alkali, alkaline earth, or ammonium salts.
    Type: Grant
    Filed: December 15, 1993
    Date of Patent: January 16, 1996
    Assignee: Henning Berlin GmbH Chemie-und Pharmawerk
    Inventors: Ekkehard Scheiffele, Gerhard Gerber, Werner Siems, Andreas Werner
  • Patent number: 5484598
    Abstract: Knurled surfaces such as raised ribs are provided on the shell of a soft gelatin capsule in order to enhance gripping and manipulation of the capsule. The capsule has a removable tab at one end thereof which may also be provided with a knurled surface. One embodiment of the invention is a capsule used for delivery of medicaments to an external body surface. An alternative embodiment of the capsule is disclosed for insertion into a body orifice. The composition of the capsule includes a starch or starch derivative which gives the capsule a drier feel and increases the coefficient of friction of the surface of the shell, further improving the capsule's handling characteristics.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: January 16, 1996
    Assignee: R.P. Scherer Corporation
    Inventors: Gregory A. Schurig, Frank S. S. Morton, Norman S. Stroud
  • Patent number: 5480644
    Abstract: This invention discloses methods of repairing structurally defective or inadequately functioning muscles of the anal sphincter and methods of improving the competency of incompetent anal sphincters by administering an effective amount of an injectable biomaterial into the defect or into the anal sinuses. Preferred biomaterials to be used in this invention are collagen formulations.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: January 2, 1996
    Assignee: JSF Consultants Ltd.
    Inventor: Jeffrey S. Freed
  • Patent number: 5472713
    Abstract: Emu oil is therapeutically used in methods for lowering cholesterol, triglycerides and low density lipoproteins and increasing high density lipoproteins; preventing and treating allergies; preventing scarring; treating headaches; preventing nose bleeds; treating and preventing cold and flu symptoms; and relieving discomfort associated with menstruation. Additionally, emu oil acts as an effective chemical buffer in combination with glycolic acid.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: December 5, 1995
    Assignee: Elf Resources, Inc.
    Inventors: Elaine Fein, John Caputo, Ann K. Nagal, Karrey-Lynn Nagal
  • Patent number: 5466461
    Abstract: New polysaccharide esters are disclosed, and more precisely esters of acidic polysaccharides chosen from the group formed by carboxymethylcellulose, carboxymethyl starch and carboxymethylchitin. These new esters and some esters of the type already known are useful as medicaments, for the manufacture of pharmaceutical and cosmetic preparations, in the field of biodegradable plastic materials and, therefore, for the manufacture of medical, surgical and sanitary articles, as well as numerous other industrial sectors in the place of acidic polysaccharides now in common use.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: November 14, 1995
    Assignee: Fidia, S.p.A.
    Inventors: Francesco della Valle, Aurelio Romeo
  • Patent number: 5462740
    Abstract: This invention provides a rectally administered composition for inhibiting epileptic seizure and to its methods of use. The composition contains, in a suitable solvent, an anti-epileptic agent for inhibiting epileptic seizure, a buffer for maintaining pH, and a thickener for imparting a viscosity to the composition effective for rectal administration by injection to a patient in epileptic seizure.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: October 31, 1995
    Assignee: Athena Neurosciences, Inc.
    Inventors: Kenneth L. Evenstad, Victoria A. O'Neill, Thomas R. Gorham
  • Patent number: 5449520
    Abstract: The invention provides a pharmaceutical composition for the rectal administration of active principles which exhibit a prevalently topical medication action at the colon level, characterized in that said active principles are formulated in a fluid vehicle able to generate a foam on rectal administration.
    Type: Grant
    Filed: October 1, 1993
    Date of Patent: September 12, 1995
    Assignee: Giuliani S.p.A.
    Inventors: Giuliano Frigerio, Enzo Giorgetti, Emilia Chiodini
  • Patent number: 5436006
    Abstract: Diclosed is a lanolin-like synthetic oil produced by esterification of glycerol with a branched fatty acid having 6 to 14 carbon atoms, a linear fatty acid having 15 to 28 carbon atoms and a dibasic acid having 4 to 10 carbon atoms while all the following conditions (a) to (c) are satisfied:(a) molar ratio of the branched fatty acid to the linear fatty acid ranges from 1.7 to 2.3,(b) 0.7 to 0.8 mol of the dibasic acid is used per mol of glycerol, and(c) the number of remaining hydroxyl group ranges from 0.4 to 0.6 for three hydroxyl groups of glycerol.The synthetic ester oil has a color, smell and stability superior to those of lanolin and an adherability, spreadability, gloss and touch very similar to those of lanolin. Such an oil can be suitably incorporated into cosmetics, toiletries and external preparations to overcome the defects of lanolin and also to exhibit the characteristic features of the oil.
    Type: Grant
    Filed: July 23, 1993
    Date of Patent: July 25, 1995
    Assignee: The Nisshin Oil Mills, Ltd.
    Inventors: Tadashiro Hirose, Yoshihiro Ueda, Takashi Murata
  • Patent number: 5436009
    Abstract: A sustained release suppository comprising in a usual suppository basea) a water-soluble therapeutically active substance, the average particle size of which is smaller than 20 .mu.m,b) a physiologically acceptable organic substance which is swellable in contact with water, andc) hydrophobic silicium dioxide.The suppository base is usually a fat having a melting range of from 29.degree. to 38.degree. C. As ingredient b) cellulose derivatives such as hydroxypropylmethylcellulose may be used, in a quantity of from 5 to 40% by weight, preferably 9 to 15% by weight. Ingredient c) is preferably used in a quantity of from 3 to 6% by weight. Also a process for manufacturing the suppositories is described.
    Type: Grant
    Filed: December 15, 1992
    Date of Patent: July 25, 1995
    Assignee: Dagra Pharma B.V.
    Inventors: Tjoe H. Jauw, Hendrik W. Frijlink, Frits Moolenaar, Peter Meijlink
  • Patent number: 5433958
    Abstract: A pharmaceutical dosage unit defined by a sheath composed of a bioadhesive material which surrounds one or more capsules and one or more nonliquid supports containing the active pharmaceutical ingredient. The capsules are made of a mixture of approximately 70% gelatin and 30% glycerin. The supports can be tablets. The dosage unit is useful in providing a sustained release effect of the pharmaceutical ingredient in the lower part of the rectum for a period of 24 hours.
    Type: Grant
    Filed: March 24, 1994
    Date of Patent: July 18, 1995
    Assignee: Asta Medica Aktiengesellschaft
    Inventors: Luc Grislain, Elisabeth Le Huede, Olivier Louis
  • Patent number: 5422115
    Abstract: Methods of treatment of the human or animal body are provided to combat conditions responsive to lithium and/or C.sub.18-22 polyunsaturated fatty acid therapy, including conditions associated with essential lithium deficiency, and also transfer of lipid-enveloped viruses between humans or animals or between cells within a human or animal body. The methods include administration of an effective amount of a lithium salt of a C.sub.18-22 polyunsaturated fatty acid. Devices for combatting transmission of viral diseases including lithium salts of a C.sub.18-22 polyunsaturated fatty acid are also provided.
    Type: Grant
    Filed: October 20, 1992
    Date of Patent: June 6, 1995
    Assignee: Efamol Holding PLC
    Inventor: David F. Horrobin
  • Patent number: 5422117
    Abstract: The invention provides a multiphase pharmaceutical composition for combatting skin and anorectal conditions requiring medication comprising at least one phase containing one or more medicaments for combatting said disease and at least one porous phase containing a silicone oil absorbed therein and adapted for release, preferably delayed release, of the silicone oil whereby application of said composition at a region affected by said skin or anorectal condition deposits said medicament or medicaments thereon and a layer of silicone oil is formed thereover thus protecting the medicaments from erosion by aqueous media.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: June 6, 1995
    Assignee: EDKO Trading and Representation Company Ltd.
    Inventors: Oswald Morton, Koral Embil
  • Patent number: 5419897
    Abstract: The use of ionene polymers as anthelmintics is described. A composition for the treatment of helminth infections in an animal comprising an effective amount of at least one ionene polymer and a physiologically acceptable carrier other than water is disclosed. Also disclosed is a method for the treatment of a helminth infection in an animal.
    Type: Grant
    Filed: April 9, 1993
    Date of Patent: May 30, 1995
    Assignee: Buckman Laboratories International, Inc.
    Inventors: Kevin D. Drake, Wallace E. Puckett
  • Patent number: 5415864
    Abstract: Colonic-targeted oral drug dosage forms composed of a drug confined within a crosslinked hydrogel that exhibits pH-dependent swelling and is composed of an ionizable comonomer such as acrylic acid, a nonionizable comonomer such as an acrylamide, and a crosslinking agent that contains an aromatic azobond. Selective drug release in the colon occurs by a combination of pH-dependent swelling of the hydrogel and degradation of the hydrogel by enzymatic cleavage of the azobonds by azoreductases.
    Type: Grant
    Filed: August 20, 1992
    Date of Patent: May 16, 1995
    Assignee: University of Utah Research Foundation
    Inventors: Jindrich Kopecek, Sung W. Kim, Helle Brondsted, Pavla Kopeckova
  • Patent number: 5413793
    Abstract: The invention provides a multiphase pharmaceutical composition for combatting an anorectal disease comprising at least one phase containing one or more medicaments for combatting said disease and at least one phase adapted for delayed release of a silicone oil whereby application of said composition at a region affected by said disease deposits said medicament or medicaments thereon and a layer of silicone oil is formed thereover, so protecting the medicaments from erosion by aqueous media.
    Type: Grant
    Filed: August 28, 1991
    Date of Patent: May 9, 1995
    Assignee: EDKO Trading and Representation Company Limited
    Inventors: Oswald Morton, Koral Embil
  • Patent number: 5407682
    Abstract: Azo-and/or disulfide-containing polymers for use as drug delivery systems having site-specific release of the drug in the colon are obtained by polycondensation or polyaddition of an azo- and/or polysulfide disulfide containing a, w-dihydroxy or diamino reagent with a suitable a, w-difunctional dicarboxylic acid; disocyanato-, disulfide comonomer. The resulting reduction sensitive polymers are linear macromolecules containing an azo and/or a disulfide bond in their polymer backbone.
    Type: Grant
    Filed: September 9, 1992
    Date of Patent: April 18, 1995
    Assignee: Danbiosyst UK Ltd Aisha
    Inventors: Etienne Schacht, Ian Wilding
  • Patent number: 5393528
    Abstract: A dissolvable element containing an agent material is used for local administration of the agent material in an internal body area. The dissolvable element is made of dissolvable polymer material and/or complex carbohydrate material which are food grade materials and have selected dissolving properties, such that it remains in substantially solid form before use, and dissolves due to human body temperatures and moisture during use to release the agent material in a desired timed release and dosage. As a contraceptive, the dissolvable element is preferably a film made of polyvinyl alcohol, polyethylene oxide, hydroxypropyl methyl cellulose and/or carboxymethyl cellulose. The dissolvable element may be formed as a laminate of different film layers for compound release properties, or it may be ground into particles and incorporated in a tampon or suppository. The dissolvable element may be foamed as a means for increasing its dissolution rate.
    Type: Grant
    Filed: June 1, 1993
    Date of Patent: February 28, 1995
    Inventor: Robert J. Staab
  • Patent number: 5389375
    Abstract: Suppository formulations having long-term stability and containing readily bioavailable .DELTA..sup.9 -THC derivatives.
    Type: Grant
    Filed: May 21, 1993
    Date of Patent: February 14, 1995
    Assignee: University of Mississippi
    Inventor: Mahmoud A. ElSohly
  • Patent number: 5384128
    Abstract: This invention provides a method and compositions for increasing the permeability of epithelial cells to a chloride ion in a subject comprising administering a permeability enhancing amount of a composition comprising a nontoxic, nonionic surfactant having (1) a critical micelle concentration of less than about 10 mM and a hydrophile-lipophile balance number of from about 10 to 20 and (2) a suitable hydrophobic organic group joined by a linkage to a suitable hydrophilic polyol.
    Type: Grant
    Filed: March 2, 1993
    Date of Patent: January 24, 1995
    Assignee: University of Alabama Research Foundation
    Inventors: Elias Meezan, Rongxiang Wang
  • Patent number: 5384124
    Abstract: New solid, porous unitary form comprising micro-particles and/or nano-particles, made by lyophilization are useful for the administration of therapeutically active substances, nutrition agents, diagnostic agents or cosmetic agents.
    Type: Grant
    Filed: February 12, 1992
    Date of Patent: January 24, 1995
    Assignee: Farmalyoc
    Inventors: Frederic Courteille, Anne Coutel, Guy Lebreton, Michel Veillard
  • Patent number: 5378470
    Abstract: Described are dry pharmaceutical preparations or clysters designed for rectal administration, which contain an active ingredient or mixture of active ingredients plus additives, and which are only reconstituted immediately before use by the addition of water, the volume of which can be selected to suit the particular patient. Such preparations are preferably marketed in graduated clyster flasks allowing the contents to be diluted with an amount of water appropriate to a particular patient.
    Type: Grant
    Filed: December 20, 1993
    Date of Patent: January 3, 1995
    Assignee: Henning Berlin GmbH
    Inventor: Wolfgang Lahr
  • Patent number: 5360612
    Abstract: This invention relates to pharmaceutical compositions for rectal administration containing semi-synthetic glycerides produced by interesterification, and, as the active ingredient, triazole derivatives of the formula ##STR1## wherein R.sup.1 is phenyl optionally sustituted with from one to three substituents independently selected from the group consisting of F, Cl, Br, I, CF.sub.3,(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, and 5-chloropyrid-2-yl; X is OH, F, Cl or Br; R.sub.2 is H.sub.2, CH.sub.3 or F; and R.sub.3 is H or F.
    Type: Grant
    Filed: October 13, 1992
    Date of Patent: November 1, 1994
    Assignee: Pfizer Inc.
    Inventors: Walter F. Fries, Gunther F. D. Pfaff, Jorg C. Pfitzner, Gerhard Simon
  • Patent number: 5352455
    Abstract: Controlled release compositions comprising a water swellable carrier and an active material having crenellated surface exhibit improved release properties. Suppositories and pessaries of generally cylindrical shape having four or five crenellations spaced equally around the perimeter and extending substantially along the length of the cylinder are preferred. Suppositories comprising four or five rounded crenellations which release morphine sulphate are especially useful.
    Type: Grant
    Filed: January 17, 1992
    Date of Patent: October 4, 1994
    Assignee: British Technology Group Ltd.
    Inventor: Steven Robertson
  • Patent number: 5346703
    Abstract: Balanced pH, thermo-irreversible gels are ideal vehicles for drug delivery to a body cavity of a mammal. The gels contain a mixture of a polyoxyalkylene block copolymer or polyether together with an ionic polysaccharide which is thermo-irreversibly gelled in the presence of a counter-ion.
    Type: Grant
    Filed: August 31, 1992
    Date of Patent: September 13, 1994
    Assignee: Mediventures, Inc.
    Inventors: Tacey X. Viegas, Lorraine E. Reeve, Raymond L. Henry
  • Patent number: 5332582
    Abstract: The invention provides methods for stabilizing amino-substituted steroid therapeutic agents in topical ophthalmic and other pharmaceutical formulations using effective stabilizing amounts of lightly cross-linked carboxy-containing polymers; Stabilized and stabilized/solubilized pharmaceutical compositions adapted for various routes of administration are also described.
    Type: Grant
    Filed: December 2, 1992
    Date of Patent: July 26, 1994
    Assignee: Insite Vision Incorporated
    Inventors: John C. Babcock, Jon R. Polansky, Lyle M. Bowman, Sheng-Wan Tsao, Erwin C. Si, Santosh K. Chandrasekaran
  • Patent number: 5328691
    Abstract: A natural or synthetic glycerol oil which comprises at least 20% by weight, preferably at least 25% of di-linoleoyl-mono-gamma-linolenyl-glycerol (DLMG), is used to supplement foods, nutritional compositions and in skin and hair care compositions.
    Type: Grant
    Filed: June 1, 1992
    Date of Patent: July 12, 1994
    Assignee: Efamol Holdings PLC
    Inventors: David F. Horrobin, Yung-Sheng Huang
  • Patent number: 5324523
    Abstract: Controlled release pharmaceutical preparations are prepared by homogenizing an organic or inorganic pharmaceutical active substance such as an opium alkaloid or its salts, an opium antagonist or its salts, an aliphatic or aromatic amine derivative or its salts, a phenolate type medicament, or Zn, Fe, Mg, K, Na salts, a fatty acid or its salt necessary to achieve a continuous phase transfer and an ethylene vinyl acetate copolymer and formulating the resulting homogeneous mixture bya) direct compressing orb) admixing with a solvent orc) using a second, auxiliary polymer.The preparations are suitable for oral or rectal administration or for tissue implantation.
    Type: Grant
    Filed: June 27, 1991
    Date of Patent: June 28, 1994
    Assignee: Alkaloida Vegyeszeti Gyar
    Inventors: Miklos Zsuga, Tibor Kelen, Jozsef Nagy, Judit Barkanyi, Magdolna Bene, Sandor Ondi, Imre Gulyas, Istvan Gyoker, Janos Repasi, Agota Repasi
  • Patent number: 5318780
    Abstract: Balanced pH, hyperosmotic, hypoosmotic, or isoosmotic gels are ideal vehicles for drug delivery. They are especially suited for topical body cavity or injection application of drugs or diagnostic agents; for drug or diagnostic agent delivery to the eye of a mammal; as protective corneal shields; or as ablatable corneal masks useful in laser reprofiling of the cornea. The compositions without the addition of a drug or diagnostic agent are useful as medical devices, for instance, in separating surgically or otherwise injured tissue as a means of preventing adhesions.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: June 7, 1994
    Assignee: Mediventures Inc.
    Inventors: Tacey X. Viegas, Lorraine E. Reeve, Raymond L. Henry
  • Patent number: 5316768
    Abstract: The present invention is directed to the use of antiviral compounds having the following generalized structure: ##STR1## wherein R is 2H or .dbd.O; R' is OH, H, or COOH (single substitution); and R" is OH, H, or alkyl; and pharmaceutically acceptable salts thereof as therapeutic substances having antiviral activity against human cytomegalovirus ("HCMV") and for treating diseases caused by HCMV. Dimeric forms of the forgoing antiviral compounds having antiviral activity against HCMV are also disclosed. Pharmaceutical compositions containing the disclosed antiviral compounds are disclosed for topical and systemic administration.
    Type: Grant
    Filed: September 11, 1992
    Date of Patent: May 31, 1994
    Assignee: Murdock International Corporation
    Inventors: Bronwyn G. Hughes, Steven G. Wood
  • Patent number: 5314689
    Abstract: Acyl-Carnitine in pharmaceutical formulations provides therapeutic and preventive antiviral action against HSV, CMV, VZV, HIV and others.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: May 24, 1994
    Assignee: Attilio Bernardini
    Inventors: Laura Scandurra, Laure Aurelian
  • Patent number: 5310562
    Abstract: In a preferred embodiment, drugs having heretofore unknown pharmacological properties which are useful in the medicinal therapy of fibrotic disease for the reparation and prevention of fibrotic lesional tissues, such drugs including as the active ingredient 5-methyl-1-phenyl-2-(1H)-pyridone. The pharmaceutical composition of this invention is novel as an anti-fibrotic drug, namely, as an agent for treating fibrosis. Any existing compounds have not been shown to be effective for the reparation and prevention of fibrotic lesions.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: May 10, 1994
    Inventor: Solomon B. Margolin
  • Patent number: 5296228
    Abstract: Sustained release pharmaceutical compound delivery compositions and methods for their production are disclosed wherein ion exchange resin particles are loaded with releasably bound pharmaceutical compounds and incorporated in an aqueous reversibly gelling polymeric solution. The pores of the ion exchange resin are sufficiently small to lock in the pharmaceutical compound without exposure to the large polymer molecules. The pharmaceutical compound remains bound within the pores of the ion exchange resin particles until after administration to a target tissue site where small ions migrate into the pores and initiate an exchange reaction.
    Type: Grant
    Filed: March 13, 1992
    Date of Patent: March 22, 1994
    Assignee: Allergan, Inc.
    Inventors: Nienyuan J. Chang, Kenneth J. Himmelstein