Abstract: The present invention relates to an inclusion complex of Rifampicin and cyclodextrin (CD) that can be used as an anti-tubercular drug. The present invention also relates to a process for synthesizing inclusion complexes of the anti-tubercular drug, Rifampicin, with ?-CD (?-cyclodextrin) and HP-?-CD (2-hydroxy propyl cyclodextrin) and characterization of these inclusion complexes.

Abstract: A dry hydrocolloid powder with cold-gel capabilities is produced by: dissolving a hydrocolloid comprising polysaccharide chains in an aqueous solution; heating the dissolved hydrocolloid solution to a temperature and for a time sufficient to induce a substantial alteration in the tertiary structure of the polysaccharide chains of the hydrocolloid; cooling the dissolved hydrocolloid solution to a temperature and for a time sufficient to substantially return the polysaccharide chains of the hydrocolloid to their original tertiary structure, wherein the polysaccharide chains form a gelling network; and drying the cooled hydrocolloid solution to form a dry powder. In some embodiments, the dry powder has a viscosity of between about 10 and 40 mPa-s when reconstituted in a 2% weight/weight solution at 25 degrees C. In other embodiments, the dry powder has a water absorption of greater than 20 g H2O/g powder.

Abstract: The present invention relates to a stable, aqueous odor-absorbing composition, preferably for use on inanimate surfaces. The composition comprises from about 0.1% to about 20%, by weight of the composition, of solubilized, water-soluble, uncomplexed cyclodextrin and an effective amount of at least one ingredient to improve the performance of the composition selected from the group consisting of: (1) cyclodextrin compatible surfactant; (2) cyclodextrin compatible antimicrobial active; and (3) mixtures thereof. Hydrophilic perfume improves acceptance. Optionally, the composition can contain low molecular weight polyols; metallic salts to help control odor; a humectant, etc. The composition is essentially free of any material that would soil or stain fabric. The composition is preferably applied as small particle size droplets, especially from spray containers, preferably non-manually operated sprayers.

Abstract: The invention relates to new formulations for improving the local tolerance of intravenously administered 4-(4-(2-pyrrolylcarbonyl)-1-piperazinyl)-3-trifluoromethyl-benzoylguanidine or one of the pharmacologically acceptable acid addition salts thereof.

Abstract: A composition comprising a cyclodextrin, a guanidine-based cationic compound, and sorbic acid is disclosed herein. Preservatives and methods related thereto, and experimental results suggesting certain advantages related to these compositions, preservatives, and methods are also presented herein.

Abstract: Pharmaceutical compositions comprising low doses of sensitive complexes between an estrogen and a cyclodextrin are provided with improved stability. In specific embodiments the composition comprises a complex between ethinyl estradiol and ?-cyclodextrin in a granulate preparation and in yet another embodiment the composition comprises a limited amount of polyvinylpyrrolidone since this excipient was found to degrade ethinyl estradiol. Furthermore, a method for improving the stability of an estrogen in a composition and for manufacturing such a stable composition is provided. Essentially, the granulate preparation are manufactured under careful control of the relative humidity.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, ?-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having a general formula (I, ) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6) alkylene, optionally substituted with 1-3 OH groups, or (CH2)o-phenylene-CH2)p—; o and p are independently 0-4; X is COOH, CONHR3, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl: R2 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: Solid dosage forms are produced by absorbing solutions of drug:cyclodextrin inclusion complexes on absorbing matrices and then drying. The matrices may, but need not, disintegrate in water. The resulting forms are suitable for oral or sublingual administration, and also can be used in topical administrations to mucosa covered tissues. They are particularly suitable for sublingual administration because the eluted, nondisintegrated matrix (e.g., absorbing paper) can be recovered and checked for completion of elution. This enables documentation that effective absorption occurred from the mouth cavity.

Abstract: Linear cyclodextrin copolymers and linear oxidized cyclodextrin copolymers containing an unoxidized and/or an oxidized cyclodextrin moiety integrated into the polymer backbone are described. Methods of preparing such copolymers are also described. The linear cyclodextrin copolymer and linear oxidized cyclodextrin copolymer of the invention may be used as a delivery vehicle of various therapeutic agents.

Abstract: The process entails increasing the concentration of cyclodextrin to 15% (w/w) and above to form complexes through a precipitation process in order to increase the yield of complexes, increase the amount of guest complexed, and decrease the particle size of the complex.

Abstract: Volatile organic compound or other materials are produced in the thermoplastic manufacture of thermoplastic polyester beverage containers. Such materials can be eluted into beverages such as carbonated beverages, sparkling or still water from the polyester. Such thermoplastic polyester resins can be manufactured with a substituted cyclodextrin material that can prevent the formation of, or react with, and absorb volatile by-products during the formation of thermoplastic preforms or containers from the thermoplastic pellet or chip. Further, as the preform is blown into a polyester container, the active materials of the invention prevent the generation of additional undesirable volatile materials. Lastly, the scavenger material can act as a barrier that prevents transport of materials from the exterior of the container into the container contents.

Abstract: A method to stabilize acylglycerols comprising ?-3 polyunsaturated fatty acids against oxidative degradation characterized in that ?-cyclodextrin is mixed either batchwise or continuously with the acylglycerol comprising ?-3 polyunsaturated fatty acids, thus forming a ?-CD/acylglycerol complex.

Abstract: Disclosed are novel polymers derivatized with at least one —NOx group per 1200 atomic mass unit of the polymer. X is one or two. In one embodiment, the polymer is an S-nitrosylated polymer and is prepared by reacting a polythiolated polymer with a nitrosylating agent under conditions suitable for nitrosylating free thiol groups. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: One embodiment of the invention comprises an ion exchange composition formed by reacting unsaturated carbon to carbon moieties pendant from derivatized ion binding cryptands with a support substrate under free radical activation conditions to form a covalent bond therebetween. In another embodiment, a cryptand ion exchange composition is made by covalently bonding unsaturated carbon to carbon moieties pendant from a derivatized ion binding cryptands with unsaturated carbon to carbon moieties pendant from a support substrate under free radical activation conditions to form covalent bond.

Abstract: A process for chemically bonding an odor-encapsulating agent to textiles includes reacting a cyclodextrin with a cross-linking agent capable of forming ether bonds with the cyclodextrin and with the textile material, and curing the textile material treated with a mixture of the cyclodextrin and cross-linking agent. Preferably, the cross-linking agent is imidazolidone, which forms an ether bond with a hydroxyl group on the cyclodextrin and with a hydroxyl group. In textile materials containing cellulose, imidazolidone forms an ether bond with a hydroxyl group on the cellulose. An active agent can be complexed with the cyclodextrin for release. Textiles formed by such a process can comprise an article of clothing adapted to trap odors emanating from a wearer.

Abstract: The invention relates to soluble highly branched glucose polymers having a reducing sugar content of less than 1%, characterized in that they have a level of ?-1,6 glucoside bonds greater than 10%, preferably of between 12 and 30%, a Mw value of between 0.35×105 and 2×105 daltons, and an osmolality having a value of between 1 and 15 mOsm/kg. The invention also relates to their method of production and their applications in the Paper-Carton, Textiles, Cosmetics, and particularly Pharmaceutical and Food industries, and still more particularly in the fields of enteral and parenteral nutrition, peritoneal dialysis as a glycemia inhibiting and/or regulating agent, as an energy source during physical activities and as a digestion regulating agent.

Abstract: The invention provides cyclodextrin derivatives that may be used to transport hydrophobic molecules for pharmaceutical or cosmetic applications, by forming organised systems in an aqueous medium, alone or with phospholipids. The cyclodextrin derivatives of the present invention have the formula: in which, R1 represents a steroid, R2 represents an alkyl or aryl group, substituted if applicable, R3 represents H or R2, all the R4 represent OR2, or one of the R4 represents —NHCO(CH2)mCONHR1, m is an integer ranging from 1 to 8, and n is equal to 5, 6 or 7.

Abstract: Methods of reducing the risk of transmission of a sexually transmitted pathogen by contacting the pathogen or cells susceptible to infection by the pathogen with a &bgr;-cyclodextrin are provided. Methods for reducing the risk of transmission of a sexually transmitted pathogen to or from a subject by contacting the pathogen or cells susceptible to the pathogen in the subject with a pharmaceutical composition containing a &bgr;-cyclodextrin also are provided. Accordingly, pharmaceutical compositions, which include 1) a &bgr;-cyclodextrin, which is in an amount that blocks passage of the pathogen through lipid rafts in the membrane of a cell susceptible to the pathogen, and 2) a contraceptive, an agent for treating a sexually transmitted disease, a lubricant, or a combination thereof, are provided, as are composition formulated from a solid substrate that contains an amount of &bgr;-cyclodextrin useful for reducing the risk of transmission of a sexually transmitted pathogen.

Abstract: The present invention relates to pharmaceutical compositions containing fenofibrate in the form of an inclusion complex with cyclodextrin, having high dissolution profile and in vivo enhanced bioavailability as compared with plain micronized fenofibrate compositions. An inclusion complex has a molar ratio of fenofibrate (preferably in micronized form) to cyclodextrin of from about 1:0.5 to about 1:4, preferably from about 1:1 to about 1:2. The immediate release fenofibrate composition is preferably in the form of a tablet or in the form of granules inside a capsule.

Abstract: Active ingredient combinations of cyclodextrins and at least one quinone and/or at least one hydroquinone for use in cosmetic or dermatological formulations.

Abstract: The present invention provides a pharmaceutical composition comprising N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and sulfobutyl ether &bgr;-cyclodextrin or a salt thereof, wherein sulfobutyl ether &bgr;-cyclodextrin increases the solubility of N-(3-chloro-4-morpholin-4-yl)phenyl-N′-hydroxyimidoformamidine and improves the photostability.

Abstract: The present disclosure concerns biologically active materials, particularly materials that comprise a biodegradeable polymer linked to a biologically active agent. The disclosure further concerns materials known as polymer-drug conjugates that typically contain a therapeutic agent, for instance a bioactive cytotoxic drug linked to a polymer backbone. The linkage typically is a convalent linkage. However, in some embodiments the disclosure concerns other polymer conjugates including those where the biologically active agent is an imaging agent, such as a tyrosinamide, a diagnostic agent, or a targeting agent, such as biotin.

Abstract: A hydrogenated starch hydrolysate having the following saccharide contents (based on the solids content of the hydrogenated starch hydrolysate): A.<8 wt.-% of hydrogenated monosaccharides (DP=1); B.<41 wt.-% of hydrogenated disaccharides (DP=2); C.<15 wt.-% of hydrogenated trisaccharides (DP=3); D.<30 wt.-% of hydrogenated quat- to deca-oligosaccharides (DP=4 to 10); and E. from about 14 to about 38 wt.-% of hydrogenated undeca- or greater polysaccharides (DP≧11); and hard boiled candies which are produced from the hydrogenated starch hydrolysate.

Abstract: Disclosed are derivatized malto-oligosaccharides and methods for the preparation thereof. In accordance with the disclosed invention, a malto-oligosaccharide is hydrogenated to thereby obtain a hydrogenated malto-oligosaccharide, and the resulting hydrogenated malto-oligosaccharide is derivatized, such as via oxidation, esterification, etherification, or enzymatic modification. The derivatization of such hydrogenated malto-oligosaccharides results in a surprisingly low level of a formation of by-products and products of degradation. In a particularly preferred embodiment of the invention, a mixture of malto-oligosaccharides is catalytically hydrogenated under reaction conditions suitable to substantially preserve the degree of polymerization (DP) profile of the mixture. The resulting malto-oligosaccharide mixture then is derivatized to form a derivatized malto-oligosaccharide mixture.

Abstract: Disclosed is a 2-alkylated-cyclodextrin derivative having the general formula I wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (CH2)p-phenylene-(CH2)q, (C1-6)alkylene, or (CH2)r—S—(C1-4)alkylene, of which each alkylene group may be substituted with 1-3 OH groups; p and r are independently 1-4; q is 0-4; X is COOH, SO2OH, (CH2—CH2—O)s—H or OH; s is 1-3; or a pharmaceutically acceptable salt thereof. The 2-alkylated-cyclodextrin derivatives are suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: The subject of the invention is a fiber-enriched composition for enteral nutrition, characterized in that it comprises 0.5 to 20%, preferably 1 to 10%, and still more preferably 1 to 5% by dry weight of branched maltodextrins having between 15 and 35% of 1→6 glucoside linkages, a reducing sugar content of less than 20%, a polymolecularity index of less than 5 and a number-average molecular mass Mn at most equal to 4500 g/mol.

Abstract: A functionalized active-nucleus complex sensor that selectively associates with one or more target species. The functionalized active-nucleus complex comprises an active-nucleus and a targeting carrier. The targeting carrier comprises a first binding region having at least a minimal transient binding of the active-nucleus to form the functionalized active-nucleus complex that produces a detectable signal when the functionalized active-nucleus complex associates with the target species and a second binding region that selectively associates with the target species. Included is a method for assaying and screening for one or a plurality of target species utilizing one or a plurality of functionalized active-nucleus complexes with at least two of the functionalized active-nucleus complexes having an attraction affinity to different corresponding target species.

Abstract: Volatile organic compound or other materials are produced in the thermoplastic manufacture of thermoplastic polyester beverage containers. Such materials can be eluted into beverages such as carbonated beverages, sparkling or still water from the polyester. Such thermoplastic polyester resins can be manufactured with a substituted cyclodextrin material that can prevent the formation of, or react with, and absorb volatile by-products during the formation of thermoplastic preforms or containers from the thermoplastic pellet or chip. Further, as the preform is blown into a polyester container, the active materials of the invention prevent the generation of additional undesirable volatile materials. Lastly, the scavenger material can act as a barrier that prevents transport of materials from the exterior of the container into the container contents.

Abstract: This invention relates to new cyclodextrin derivatives, processes for producing these cyclodextrin derivatives, and inclusion complexes comprised of the new cyclodextrin derivatives and guest molecules, as well as methods of making such materials and related materials and methods of using the same.

Abstract: The invention relates to the use of sequestering agents for the preparation of a medicament for the treatment of hypercortisolaemia related disorders, especially for the treatment of major depression; to pharmaceutical compositions comprising a cortisol-sequestering agent, and to the cortisol-sequestering agent 6-per-deoxy-6-per-(2,3-dihydroxypropylthio)-&ggr;-cyclodextrin.

Abstract: Methods for enhancing the complexation efficiency of a drug with cyclodextrin and for enhancing the availability of a drug following administration of a cyclodextrin-drug complex.

Abstract: A method for producing a molecular compound which comprises mixing and kneading a solid host compound and a solid or liquid guest compound by using a kneader and optionally followed by extruding and granulating, wherein the method further comprises one or more of the steps of holding the product at a temperature which is 50° C. or higher and not higher than the emission temperature for the guest compound, washing the formed molecular compound with a solvent capable of dissolving the guest compound, pulverizing in advance the solid host compound, and adding a poor solvent such as water prior to mixing and kneading. The method allows the production of a molecular compound having improved stability.

Abstract: The invention relates to the inhibitory effects of dextrin sulphate on angiogenesis and in particular the treatment of diseases or disorders which would benefit from the administration of dextrin sulphate.

Abstract: Disclosed are novel polymers derivatized with at least one —SNO group per 1200 atomic mass unit of the polymer. In one embodiment, the S-nitrosylated polymer has stabilized —S-nitrosyl groups. In another embodiment the S-nitrosylated polymer prepared by polymerizing a compound represented by the following structural formula: R is an organic radical. Each X′ is an independently chosen aliphatic group or substituted aliphatic group. Preferably, each X′ is the same and is a C2-C6 alkylene group, more preferably —CH2—, —CH2CH2—, —CH2CH2CH2— or —CH2CH2CH2CH2—. p and m are independently a positive integer such that p+m is greater than two. The polymers of the present invention can be used to coat medical devices to deliver nitric oxide in vivo to treatment sites.

Abstract: Dextrins are prepared by hydrolyzing starch with an enzyme that consists essentially of a beta-amylase enzyme. The product prepared thereby will include a dextrin, such as beta-limit dextrin. Upon ultrafiltration of this product, a dextrin-rich fraction may be recovered. If desired, the dextrin-rich fraction may be further purified via diafiltration. Retrograded amylose may be separated from the product of enzymatic hydrolysis.

Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

Abstract: The present invention concerns a process for preparing copolymers of cyclodextrin(s) and/or cyclodextrin derivative(s), characterized by the following operations: (a) preparing a solid state mixture of cyclodextrin(s) and/or cyclodextrin derivative(s) and/or inclusion complex(es) of cyclodextrin(s) and/or cyclodextrin derivative(s) and a poly(carboxylic) acid and/or a poly(carboxylic) acid anhydride or a mixture of poly(carboxylic) acid(s) and/or poly(carboxylic) acid anhydride(s), and optionally, a catalyst; and (b) heating the solid mixture to a temperature in the range 100° C. to 200° C. for a period in the range 1 min to 60 min, preferably 30 min or substantially 30 min. The present invention also concerns soluble and insoluble compounds of cyclodextrin(s) and/or cyclodextrin derivative(s) or their inclusion complexes with at least one poly(carboxylic) acid.

Abstract: The present invention relates to pharmaceutical compositions containing fenofibrate in the form of an inclusion complex with cyclodextrin, having high dissolution profile and in vivo enhanced bioavailability as compared with plain micronized fenofibrate compositions. An inclusion complex has a molar ratio of fenofibrate (preferably in micronized form) to cyclodextrin of from about 1:5 to about 1:4, preferably from about 1:1 to about 1:2. The immediate release fenofibrate composition is preferably in the form of a tablet or in the form of granules inside a capsule.

Abstract: A cyclodextrin oligomer comprising two cyclodextrins connected through a spacer at the secondary side, characterized in that said spacer comprises the unit B which is a rigid and preferably hydrophilic structural element.

Abstract: A stable form of artemisinin wherein an artelinic acid or artesunic acid is complexed with cyclodextrin analogs, preferably, &bgr;-cyclodextrin. The complexed cyclodextrin artemisinin formulation shields the peroxide portion of the artemisinin backbone from hydrolytic decomposition rendering it stable in solution. Artelinic acid and cyclodextrin are placed into contact with one another to yield a 2:1 molecular species. Artesunic acid and cyclodextrin yield a 1:1 molecular species. The complexed cyclodextrin artemisinin formulation is effective for the treatment of malaria and is stable in solution for long periods of time.

Abstract: The present invention relates to a process for the preparation of a water soluble inclusion complex of neem seed kernel extract (NSKE) containing azadirachtin-A in cyclodextrin and its use in an insecticidal formulation. The process of the present invention comprises the following steps adding neem seed kernel extract containing azadirachtin-A to cyclodextrin, the molar ratio of azadirachtin-A to the cyclodextrin ranging from 1:0.5 to 1:20, stirring the above mixture, filtering the above mixture to obtain a water soluble inclusion complex of neem seed kernel extract, if desired, freeze/spray drying the said water soluble complex of neem seed kernel extract to get a free flowing pale cream powder.

Abstract: The present invention provides a composition for preparing substances having nano-pores, said composition comprising cyclodextrin derivative, thermo-stable organic or inorganic matrix precursor, and solvent for dissolving said two solid components. There is also provided an interlayer insulating film having evenly distributed nano-pores with a diameter less than 50 Å, which is required for semiconductor devices.

Abstract: The subject matter of the invention is branched maltodextrins, characterised by the fact that they present between 22% and 35%, preferably between 27 and 34%, glucosidic linkages 1→6, a content of reducing sugars lower than 20%, a polymolecularity index lower than 5 and a number average molecular weight Mn at most equal to 4500 g/mole, and the method of obtaining these branched maltodextrins.

Abstract: A &ohgr;-cycloalkyl-prostaglandin E2 derivatives of the formula (I) 1

Abstract: Improved artificial tear compositions are described. The compositions are preferably formulated as sterile, isotonic solutions. The solutions contain a unique combination of three demulcents. The solutions preferably also contain one or more electrolytes and may also contain a nonionic surfactant. The solutions provide ocular comfort and are particularly useful in patients that are experiencing mild to moderate dryness or other irritation of the cornea. The solutions may be packaged as either an unpreserved unit dose product or as a preserved multi-dose product. The multi-dose products contain a very mild antimicrobial preservative system, and consequently can be frequently applied to the eye with little risk of ocular irritation attributable to the preservative components.

Abstract: A multivalently interactive molecular assembly having a plurality of functional groups or ligands, in which a ratio between Rh and Rg expressed as Rh/Rg is 1.0 or less. Here, Rh is a hydrodynamic radius calculated from dynamic light scattering (DLS) assay performed in aqueous solution; and Rg is a radius of gyration determined based on the Zimm plot generated using data obtained by static light scattering (SLS) assay.

Abstract: Described are inclusion complexes formed between cyclodextrin and drospirenone. In a specific embodiment of the invention, the cyclodextrin is &bgr;-cyclodextrin. The invention further relates to methods of providing such an inclusion complex, and to the use of said inclusion complex for improving the solubility of drospirenone, for providing pharmaceutical compositions, for use as a medicament in the treatment of symptoms associated with menopause and in female contraception.

Abstract: This invention relates to new cyclodextrin derivatives, processes for producing these cyclodextrin derivatives, and inclusion complexes comprised of the new cyclodextrin derivatives and guest molecules, as well as methods of making such materials and related materials and methods of using the same.

Abstract: The present invention relates generally to nutritive medium, medium supplement, media subgroup and buffer formulations that contain lipid. Specifically, the present invention provides powder nutritive medium, medium supplement and medium subgroup formulations, particularly cell culture medium supplements (including powdered sera such as powdered fetal bovine serum (FBS)), medium subgroup formulations and cell culture media comprising all of the necessary nutritive factors including lipid components that facilitate the in vitro cultivation of cells. The invention is particularly directed to methods of production of these media, media supplement, media subgroup and buffer formulations, and also provides kits and methods for cultivation of prokaryotic and eukaryotic cells, particularly bacterial cells, yeast cells, plant cells and animal cells (including human cells) using these dry powder nutritive media, media supplement, media subgroup and buffer formulations.