Abstract: A process is provided by which a polyrotaxane including cyclic molecules having a relatively long graft chain is easily obtained. Also provided is a polyrotaxane which includes cyclic molecules having a radical polymerization initiation site and is for use as a raw material in the process. The polyrotaxane comprises: a pseudo-polyrotaxane comprising cyclic molecules clathrated with a linear molecule, the cavities of the cyclic molecules having been pierced by the linear molecule; and blocking groups disposed respectively at both ends of the pseudo-polyrotaxane so as not to release the cyclic molecules. The cyclic molecules in the polyrotaxane have a radical polymerization initiation site.

Abstract: A method of preparing a salt product comprises the steps of: (i) providing a mixture which comprises salt dissolved in a solvent, said mixture further containing an organic material that is solid under ambient temperature conditions; and (ii) atomising said mixture and evaporating said solvent to produce a salt product comprised of particles of salt incorporating said organic material. The organic material may be a polymer such as a carbohydrate (e.g. maltodextrin or Gum Arabic). Novel salt products are disclosed which comprise hollow particles having a shell formed for individual crystallites of salt. The salt product is useful as a seasoning for food and may be used in lower amounts than conventional salt to provide the same taste. Particular advantages are obtained in the baking of bread.

Abstract: The invention concerns a fiber-enriched anti-inflammatory and/or analgesic composition for the intestine, characterized in that it comprises branched maltodextrins having between 15 and 35% of glucoside bonds, 1 to 6, a reducing sugar content less than 20%, a polymolecularity index less than 5 and a number molecular weight Mn not more than 4500 g/mole.

Abstract: Preparation of AT1 receptors antagonists formulations using the cyclodextrins, their derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular disease and their complications. Until now, no applications using the AT11 receptor antagonists and cyclodextrins or derivatives and/or biodegradable polymers for the treatment of arterial hypertension, other cardiovascular diseases and their complications, was found in the technical state of art. The present invention is characterized by the combination of two different technologies: one is the molecular encapsulation of AT11 receptor antagonists in cyclodextrins and the other is the microencapsulation in biodegradable polymers. It also comprises the increase of the effectiveness of the AT11 receptor antagonists as well as an increase in their bio-availability.

Abstract: The invention provides compositions comprising xanthohumol/cyclodextrin complexes that are water soluble and that have increased stability relative to xanthohumol alone.

Abstract: The invention provides a new class of antibiotics to which pathogenic bacteria have not been exposed, and thus should not have developed resistance. This new class of antibiotics are derivatives of ?-cyclodextrin (?-CD), which is a cyclic molecule comprising seven D-glucose units.

Abstract: Chemical compounds, being the alkyl sulfate of sulfated saccharides, particularly, dextrin, dextran, and cyclodextrin, and pharmaceutical compositions containing these compounds. The compounds of the invention provide antiviral activity, particularly in the treatment and prevention of sexually-transmitted diseases. Methods of treating viral infection and preventing viral transmission include administration include administration of the compounds of the invention orally, topically, subcutaneously, by muscular injection, by intraperitoneal injection and by intravenous injection.

Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.

Abstract: Solubility-enhanced forms of aprepitant and processes for preparing such forms. The invention also provides solubility-enhanced forms of aprepitant that also possess stability against solid state conversions. Certain solubility-enhanced forms of aprepitant comprise a cyclodextrin or any of its derivatives. Other solubility-enhanced forms of aprepitant comprise fine particle preparations of aprepitant. The invention further provides non-nanoparticulate pharmaceutical formulations prepared using solubility-enhanced forms of aprepitant. The invention also provides taste-masked and orally disintegrating pharmaceutical formulations comprising aprepitant. Further, pharmaceutical formulations comprising solubilityenhanced forms of aprepitant and processes of preparation of such formulations, as well as methods of using them are provided.

Abstract: Non-crosslinked derivatives of oligo/polysaccharides of formula I, wherein: X is OH, OM, NH—R1, O—R1; M is an alkaline or alkaline-earth metal, transition metal, or cation containing a quaternary nitrogen atom; Y is H or R2; R1: the residue of an oligo/polysaccharide; R2: the residue of a C1-C4 linear chain aliphatic carboxylic acid or citric acid; provided that at least one X is NH—R1 or O—R1, while the other two X are present in acid (OH) or salified form (OM).

Abstract: A process for the preparation of cyclodextrin oligomers or polymers, whereby the cyclodextrin molecules are coupled to one another covalently via a spacer arm, based on a coupling reaction between an alkyne and an azide producing the formation of an aromatic heterocyclic bridge between the coupled units. Also described are the cyclodextrin oligomers or polymers that are obtained and their uses.

Abstract: Water-soluble iron-carbohydrate derivative complex obtainable from an aqueous iron(III) salt solution and an aqueous solution of the product of the oxidation and subsequent derivatisation of one or more maltodextrins with an aqueous hypochlorite solution at an alkaline pH value, wherein when one maltodextrin is used its dextrose equivalent is from 5 to 20 and when a mixture of a plurality of maltodextrins is used the dextrose equivalent of the mixture is from 5 to 20 and the dextrose equivalent of each individual maltodextrin in the mixture is from 2 to 40, and the subsequent derivatisation is carried out with a suitable reagent, process for the preparation thereof, and medicament for the treatment and prophylaxis of iron deficiency states.

Abstract: There is described an inclusion complex of raloxifene hydrochloride and ?-cyclodextrin in the solid phase having a specific X-ray powder diffraction spectrum. The invention also relates to a process for obtaining the raloxifene hydrochloride inclusion complex with ?-cyclodextrin of the invention. The complex of the invention is employed as a pharmaceutical ingredient in the treatment of osteoporosis, specifically postmenopausal osteoporosis.

Abstract: The invention relates to new compounds of type hexakis(6-deoxy-6-NH(CH2)n—R1)?-cyclodextrin and heptakis(6-deoxy-6-NH(CH2)n—R1)-(?-cyclodextrin, and octakis(6-deoxy-6-NH(CH2)n—R1)-?-cyclodextrin, where n=2-6 when R1=NH2 and n=0 when R1=C(?NH)NH2 and n=2-6 when R1=NH—C(?NH)NH2 and their use in the compaction of DNA and in cell permeation. The invention also relates to methods of synthesis of the above compounds.

Abstract: The present invention relates to a starch emulsifier product prepared by sufficiently solubilizing a starch and subsequently sufficiently derivatizing the sufficiently solubilized starch product, in one embodiment by reacting the sufficiently solubilized starch with an alkenyl succinic anhydride. Such starch emulsifier products are useful as emulsifying and/or encapsulating agents, particularly in systems where high load and retention of the active ingredient, low surface oil exposure, and excellent oxidation resistance is desired.

Abstract: Complexes of silanes and cyclodextrin or derivatives thereof are storage stable and allow target release of silane or decomposition products thereof.

Abstract: The invention relates to cyclodextrin derivatives of formula (I): in which: R1=—NH-E-AA-(L1)p(L2)q where E=a linear or branched C1-C15 hydrocarbon-based group with, optionally, one or more hetero atoms; AA=the residue of an amino acid; L1 and L2=a C6-C24 hydrocarbon-based group with, optionally, one or more hetero atoms; p and q=0 or 1, at least one being ?0; R2=H, —CH3, isopropyl, hydroxypropyl, sulphobutyl ether; R3=H or R2, except when R2=hydroxypropyl; all the R4=—OH or R2, except when R2=hydroxypropyl, or at least one of the R4=R1; n=5, 6 or 7. The invention also relates to a process for preparing them, and to inclusion complexes and organized surfactant systems comprising them.

Abstract: A targeting conjugate is provided comprising an active agent, one or more residues of a cyclodextrin (CD)-containing polymer and a biorecognition molecule. The polymer is preferably a peptide or a polypeptide comprising at least one amino acid residue containing a functional side group to which at least one of the CD residues is linked covalently; the biorecognition molecule is covalently bonded directly or via a spacer to the polymer backbone of the CD-containing polymer; and the active agent is noncovalently encapsulated within the cavity of the cyclodextrin residues and/or entrapped within the polymer matrix of the CD-containing polymer.

Abstract: Soluble amphiphilic macrocycle analogues having lipophilic groups attached to one side of the units making up the macrocycle and hydrophilic groups attached to the other side. These amphiphilic macrocyclic derivatives have the ability to self-assemble in aqueous solvent forming micelles or vesicles and can be used as hosts for the solubilization and/or stabilization of various compounds. Embodiments of the present invention utilize macrocyclic oligosaccharides and preferably cyclodextrin as the macrocyclic derivatives to be modified.

Abstract: The invention relates to a compound according to the following general formula (I), in which: m represents an integer equal to 5, 6 or 7; n and n1 represent an integer from 1 to 5; the A groups represent, in particular, a hydrogenated atom; X represents O or S; Y represents, in particular, a group NR1, R1, representing, in particular, a hydrogenated atom; W represents CH or N; and Z represents, in particular, a hydrogenated atom.

Abstract: Disclosed is a cyclodextrin compound comprising glucopyranoses constituting cyclodextrin, the glucopyranoses having substituents each having folic acid substituted for two or more primary hydroxy groups at position-6 of the glucopyranoses.

Abstract: The present invention provides products having resveratrol with high water solubility and nutraceutical and/or phytotherapic compositions having said substances. The processes for obtaining them include the solubility increase of the polyphenol corresponding to a resveratrol compound, preferably trans-resveratrol in water, by its complexation with cyclodextrin under specific conditions that favor thermodynamic equilibrium. The products of the invention present high solubility and purity in aqueous medium, being, therefore, useful to prepare nutraceutical compositions (pharmaceutical and/or alimentary) with antioxidant, anti-inflammatory, antiviral, antidiabetics, cardioprotective, neuroprotective, chemoprotective activities; besides protecting against infections and ischemia, reducing obesity, and preventing aging.

Abstract: Hyperbranched, water-soluble polymers, obtainable by Michael polyaddition of ?-, ?-, or ?-cyclodextrins and amines to bisacrylamides.

Abstract: Provided are inclusion complexes comprising a sildenafil salt (e.g., sildenafil citrate) and alpha-cyclodextrin. The complexes may be useful treating various conditions, such as male erectile dysfunction and pulmonary hypertension. In some instances the inclusion complexes increase the solubility of sildenafil. Also provided are methods of producing the inclusion complexes, as well as methods of treatment, kits and unit dosages.

Abstract: Curcumin has shown anti-inflammatory and anti-angiogenic properties that could be useful in treating various diseases such as those of rheumatology and oncology. However, curcumin is very poorly absorbed and has a very low bioavailability. This patent describes a method of increasing the delivery of curcumin by complexing it with cyclodextrins. Cyclodextrins are well known in the food industry and have been used to carry other drugs to increase bioavailability. The new combination of cyclodextrins and curcumin has been tested in pre-clinical inflammation models where it has demonstrated efficacy superior to both the positive control and curcumin.

Abstract: The invention relates to a process for the preparation of reactive cyclodextrins, in which process the cyclodextrins CD are reacted with a bifunctional alkyl compound X—(CH2)n—Y, wherein X is a group which reacts with CD, n is an integer from 2 to 20 and Y is a group which reacts with a group Z or is a group-Reactive which is capable of reaction with cellulosic or proteinic materials and, optionally, in a further step, insofar as Y is a group which reacts with a group Z, the resulting product is reacted with a reactive anchor compound Z-Reactive to form the reactive cyclodextrin, and also to reactive cyclodextrins prepared in accordance therewith, to materials dressed therewith and to the use thereof.

Abstract: Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed.

Abstract: The invention relates to a process for the preparation of a cyclodextrin/alpha-lipoic acid complex, wherein in a first step, an alpha-lipoic acid and a cyclodextrin are dissolved in an aqueous alkaline solution having a pH above pH 7, and in a second step an acid is added to lower the pH of the solution to a pH below pH 7.

Abstract: A method of preventing or reducing the incidence of post-operative adhesions in or associated with a body cavity, which comprises introducing into the body cavity a composition containing an aqueous solution or suspension or gel formulation containing the polysaccharide dextrin.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.

Abstract: The present invention relates to a process for the preparation of inclusion compounds of piroxicam with ?-cyclodextrin. More particularly, according to the process of the invention, the aqueous solution of two components is subjected, before drying, to a freezing process at very high rate. The resulting products have physico-chemical characteristics as well as technological and biopharmaceutical properties which are advantageous compared with those obtained according to the prior art processes. The resulting products are suitable for preparing pharmaceutical compositions for the oral administration.

Abstract: The present invention relates to cyclodextrins having the following formula (I): to nanostructures comprising them, to processes for preparing them, to the use thereof, and also to compositions comprising them.

Abstract: The present invention relates to the inclusion complexes of butylphthalide, which is D, L-mixed or levorotatory, with cyclodextrin or cyclodextrin derivatives, to a process for their preparation and the use thereof. In the invention, the butylphthalide is complexed with cyclodextrin or cyclodextrin derivatives, preferably with hydroxypropyl-?-cyclodextrin in order to increase the water-solubility of butylphthalide, develop clinical solid or liquid formulations and improve the therapeutic effect of butylphthalide. The inclusion complex, in which the molar ratio of butylphthalide to cyclodextrin or cyclodextrin derivatives is in the range of 1:1-10, can be used to prepare infusion, injection, injectable powder, liquids for oral administration, syrup, tablets, granules, dispersible tablets and others.

Abstract: A method of using at least one leguminous starch derivative having a predetermined molecular mass in weight and a predetermined sol/gel transition temperature for preparing a composition for laying paper or flat carton. The leguminous starch derivative and laying compositions prepared from the same, in particular with high dried materials are also disclosed.

Abstract: It has been discovered that the uptake of anionic charged species into cells can be enhanced by noncovalently associating such species with specifically modified forms of cyclodextrin. The invention modified forms of cyclodextrin form well defined stoichiometric complexes with anionic charged molecules. This discovery enables one to produce various compositions containing anionic charged molecules and facilitates methods for enhancing the cellular uptake of double-stranded or hairpin nucleic acid.

Abstract: In accordance with the present invention, it has been discovered that the uptake of charged molecules into cells can be enhanced by noncovalently associating such molecules with molecular entities comprising an amphiphilic core with oppositely charged arms. The molecular entities form well defined stoichiometric complexes with charged molecules. Various compositions and methods for stabilizing anionic charged molecules and for enhancing the cellular uptake of any anionic charged molecules, e.g. double-stranded or hairpin nucleic acid, are provided.

Abstract: A water soluble copolymer includes first and second hydrophilic block segments or graft chains. The first hydrophilic block segment or graft chain contains cyclodextrin groups in at least a majority of its repeating units, and the second hydrophilic block segment or graft chain contains repeating units other than cyclodextrin groups. The first and second block segments or graft chains are covalently linked.

Abstract: Drug carriers, methods of synthesizing, and methods of use thereof are provided.

Abstract: The present invention relates to polymeric derivatives, which can be conjugated to an amino-containing drug to improve its in vivo properties. The polymeric derivative can subsequently be released to yield the drug in its native form. Methods of preparing and using these polymeric derivatives and drug conjugates are described.

Abstract: Cosmetic or dermatological preparations are based upon vitamin F, and the vitamin F is present in the form of a complex with a cyclodextrin which includes alpha-cylodextrin, beta-cyclodextrin, and gamma-cyclodextrin.

Abstract: The invention provides an iron-carbohydrate complex compound which is characterized by a content of iron(II). The invention also provides processes for the preparation of the iron-carbohydrate complex compound and the use thereof for treatment of iron deficiency anaemias.

Abstract: Drug carriers, methods of synthesizing, and methods of use thereof are provided.

Abstract: It is intended to provide a crosslinked polyrotaxane formed by crosslinking polyrotaxane molecules via chemical bonds which exhibits excellent optical properties in water or in an aqueous solution of sodium chloride; a compound having this crosslinked polyrotaxane; and a process for producing the same. The above object can be achieved by a crosslinked polyrotaxane having at least two polyrotaxane molecules, wherein linear molecules are included in a skewered-like state at the opening of cyclodextrin molecules and blocking groups are provided at both ends of the linear molecules, so as to prevent the cyclodextrin molecules from leaving, and cyclodextrin molecules in at least two polyrotaxane molecules being bonded to each other via chemical bond, characterized in that hydroxyl (—OH) groups in the cyclodextrin molecules are partly substituted with non-ionic groups.

Abstract: The invention relates to a cyclodextrin derivative corresponding to general formula (I) wherein n is a whole number from 1-6, m is a whole number equal to 5, 6 or 7, R1 is an OH group, all R1s are identical, Z is a thiourea group, X is a hydrogen atom, and R is a hydrogen atom or a bioidentification element.

Abstract: The present invention is directed to the novel use of complexes of cyclodextrin. In particular the invention is directed to a complex of a cyclodextrin selected from the group consisting of ?-CD, ?-CD and ?-CD and a cannabinoid selected from the classical cannabinoid-group consisting of canabinol, tetrahydrocanabinol and canabidiol.

Abstract: A sulfoalkyl ether-alkyl ether cyclodextrin (SAE-AE-CD) derivative is provided. The SAE-AE-CD possesses advantages over known SAE-CD and AE-CD derivatives as well as over the parent cyclodextrin by being more water soluble and less membrane disturbing. The SAE-AE-CD includes at least one sulfoalkyl ether group and at least one alkyl ether group even though the degree of substitution for the functional groups can be different. The SAE functional group can be present in molar excess over the AE functional group and vice versa. The total degree of substitution of the cyclodextrin, with respect to both functional groups, can be varied such that a minority or a majority of the hydroxyl moieties of the CD are derivatized. The SAE-AE-CD derivative can be used to solubilize compounds with insufficient water solubility. In some cases, they also stabilize compounds in solution against degradation or to solubilize degradation products formed during degradation.

Abstract: The invention relates to soluble highly branched glucose polymers, having a reducing sugar content of less than 1%, a level of ?-1,6 glucoside bonds of between 13 and 17% and an Mw having a value of between 0.9×105 and 1.5×105 daltons, characterized in that their branched chain length distribution profile consists of 70 to 85% of DP of less than 15, of 10 to 16% of DP of between 15 and 25 and of 8 to 13% of DP greater than 25.

Abstract: The invention relates to a compound corresponding to general formula (I) wherein n is a whole number from 1-6, m is a whole number equal to 5, 6 or 7, R1 is an OH group, all R1 s are identical, Z is an NHX group, X is a hydrogen atom, and R is a hydrogen atom or a bioidentification element, with the proviso that the compound wherein n=1, m=6, Z=NH2 and R1=OH is excluded.

Abstract: Disclosed are a method for the reduction of an oligosaccharide mixture and an oligosaccharide mixture prepared thereby. In accordance with the disclosed invention, a mixture of oligosaccharides having a given DP profile is reduced to a DE of essentially zero by catalytically hydrogenating the mixture under reaction conditions sufficient to preserve the DP profile of the mixture, which reaction conditions typically include a reaction temperature ranging from about 50° C. to about 150° C. and a reaction pressure ranging up to about 1500 psi. Surprisingly, when the mixture is a malto-oligosaccharide mixture, the reduced mixture will have a superior color-fastness and thermal stability as compared to a similar unreduced mixture of malto-oligosaccharides, and also low reactivity towards nitrogen-containing species.