Abstract: A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056 M?1-13051 M?1), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 ?m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

Abstract: Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.

Abstract: The present invention provides a compound of which active |form| is represented by a formula (A). and which can be injected into a joint cavity which is an affected part of disorders and can be accumulated in the joint cavity to exert the pharmacological effect thereof in a sustained manner, for the purpose of ameliorating cartilage disorders without developing any side effect. A compound according to the present invention, which is represented by a formula (I): (wherein all of symbols are as defined in the description), is a compound that can achieve the above-mentioned purpose. This compound does not exhibit any side effect on the cardiovascular system even when the compound is administered in an effective amount for exhibiting a cartilage regeneration activity, and is therefore extremely useful as a safe and effective preventive and/or therapeutic agent for cartilage disorders.

Abstract: The invention provides a liposome composition for delivering high pay-load of a therapeutic agent to neovascularization sites of the eyes in a patient in need thereof. The liposome composition for entrapping the therapeutic agent comprises a particle forming component composed of a variety of vesicle-forming lipids, and an agent-carrying component able to form a complex with the therapeutic agent via electrostatic charge-charge interaction or hydrophobic-hydrophobic interaction; wherein the liposome composition comprising the therapeutic agent has a mean particle diameter of about 30 to 200 nm and may accumulate at the neovascularization sites of the eyes 24 hours after the intravenous administration of the liposome composition comprising the therapeutic agent to the patient. A method for delivering the therapeutic agent to the eyes in a patient with this liposome composition is also provided.

Abstract: An oral osmotic pharmaceutical delivery system comprises a highly water-soluble drug exhibiting an erratic or an incomplete release profile when formulated in a elementary osmotic pump delivery system and at least one release enhancing agent.

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: This invention provides antimicrobial compositions containing methylglyoxal and material with methylglyoxal contained (such as manuka honey). The antimicrobial activity of methylglyoxal, or of material with a methylglyoxal presence, is maintained and/or enhanced by mixing methylglyoxal or material with a methyglyoxal presence with cyclodextrin. Methods of preparing such compositions, including powder composition, and methods of using such compositions are also provided.

Abstract: The present invention relates to a new use of a known medicament. Specifically, the invention relates to methods and compositions for enhancing the therapeutic efficacy of a therapeutic agent by increasing the uptake of the therapeutic agent by target cells, and in particular relates to a pharmaceutical composition comprising a regulating agent of lipid raft/caveolae-dependent endocytic pathway and some therapeutic agents, such as anti-tumor agents. The invention also relates to a method for screening a regulating agent of lipid raft/caveolae-dependent endocytic pathway capable of enhancing the therapeutic efficacy of anti-tumor agents.

Abstract: A direct compression formulation suitable for preparing buccal and/or sublingual and dosage forms incorporates a combination of a non-ionic polymeric solubility enhancer, a mucoadhesive polymer, a filler, a disintegrant, and a pharmaceutically active agent. Cannabinoid-cyclodextrin complexes exhibiting an improved property selected from improved stability, higher product yield and improved product uniformity may be obtained by complexing the cannabinoid with the cyclodextrin in a liquid medium containing an antioxidant. To enhance stability, product yield and/or product uniformity, complexing may be done while the liquid medium is in contact with an atmosphere having a very low oxygen content.

Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.

Abstract: A stable complex of tomoxiprole with 2-hydroxypropyl-beta-cyclodextrin with fast dissolution rate and rapid absorption wherein amorphous tomoxiprole forms a complex with 2-hydroxypropyl-beta-cyclodextrin in about equimolecular ratio. The complex shows a remarkably faster dissolution rate and absorption with respect to crystalline tomoxiprole and is particularly suitable for the production of pharmaceutical oral dosage forms, such as tablets and capsules, where rapid onset of therapeutical action is required. A method of manufacture of the complex is also described and claimed.

Abstract: A method for preparing molecular complexes between Adapalene and cyclodextrins using the technology of dense fluids under pressure, especially that of CO2 is described.

Abstract: An oral pharmaceutical liquid formulation comprising deferiprone and a taste masking composition, said taste masking composition comprising an effective amount of a sweetener (such as sucralose) per liter of liquid composition, an effective amount of a thickening and suspension aid, (for example hydroxyethylcellulose), per liter of liquid composition, an effective amount of a humectant (such as glycerin) per liter of liquid composition, and an effective amount of at least one flavoring agent, wherein a final form of said taste-masked pharmaceutical has a substantially non-bitter and palatable taste.

Abstract: Provided are methods relating to compositions that include a CDP-topoisomerase inhibitor, e.g., a CDP-camptothecin or camptothecin derivative conjugate, e.g., CRLX101.

Abstract: This invention relates to fat containing consumable food products comprising ?-cyclodextrin. The food products have reduced levels of bioavailable fat but have substantially the same fat, cholesterol and caloric content as a like food without ?-cyclodextrin. The invention also relates to methods for reducing the bioavailability of fats in fat containing food products without reducing caloric intake as determined by bomb calorimetry and to methods for increasing high density lipoproteins in a subject and reducing or controlling weight by administering the food products of this invention.

Abstract: The present invention is directed to drug delivery vehicles comprising one or more cyclodextrin moieties conjugated to a dendritic polyamine for the delivery of small molecule and protein therapeutic molecules and nucleic acid therapeutic molecules, and methods of making and using the delivery vehicles.

Abstract: Amino acid compositions containing a carbohydrate and any one or more kinds of alanine, proline and glycine as amino acid can suppress a rapid increase in the blood glucose level immediately after ingestion and a decrease in the blood glucose level due to prolonged exercise, and can improve exercise performance. In addition, the present invention provides inhibitors of an increase in the blood glucose level immediately after carbohydrate ingestion, an inhibitor of a decrease in the blood glucose level due to a prolonged exercise, and an exercise performance improver. Therefore, the present invention provides an energy supplement useful for those who exercise (particularly prolonged exercise).

Abstract: Processes for precipitating polymers from a polymer-containing solution are disclosed.

Abstract: Compositions, such as hydrogel compositions, that include a hyaluronic acid, a vitamin A, and a cyclodextrin may be used as medical or cosmetic fillers, implants, or creams. For example, the compositions may be used as dermal fillers.

Abstract: This invention provides antimicrobial compositions containing methylglyoxal and material with methylglyoxal contained (such as manuka honey). The antimicrobial activity of methylglyoxal, or material with a methylglyoxal presence, is maintained and/or enhanced by mixing methylglyoxal or material with a methylglyoxal presence with cyclodextrin. Methods of preparing such compositions, including powder composition, and methods of using such compositions are also provided.

Abstract: The present invention aims to provide a hydrophilic modified polyrotaxane composition having excellent storage stability. The present invention relates to a hydrophilic modified polyrotaxane composition comprising: a hydrophilic modified polyrotaxane produced by modifying, with hydrophilic modifying groups, all or part of hydroxy groups on a cyclodextrin of a polyrotaxane containing the cyclodextrin, a polyethylene glycol which is included in the cavities of the cyclodextrin molecules in a skewered manner, and a capping group that is placed at each end of the polyethylene glycol and prevents dissociation of the cyclodextrin molecules from the polyethylene glycol; and a polyphenol antioxidant.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: The present invention relates to the use of cyclic oligosaccharides as chemical complexants of lipofuscin bisretinoids (A2E) to prevent and treat eye (i.e., retinal or macular) disease. Monomeric, dimeric, multimeric, or polymeric oligosaccharide rings act as pharmacologic agents to prevent and treat ophthalmologic disorders triggered by the accumulation of lipofuscin in the retinal pigment epithelium (RPE), which occurs as a consequence of either genetic disorders, such as Stargardt Disease (SD) and Best Disease (BD), or aging, such as Age-Related Macular Degeneration (AMD), or other diseases, such as retinitis pigmentosa, and cone-rod dystrophy.

Abstract: Nutritional compositions for improving, treating and/or preventing various medical conditions and methods of using same are provided. Such medical conditions include infection, sepsis, malabsorption, allergy, inflammatory bowel disease, and diarrhea among others. The nutritional compositions include branched chain fatty acids and may include other functional ingredients such as, but not limited to probiotics, nucleotides and amino acids. Methods of administering such nutritional products to individuals in need of same are also provided.

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 disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The invention relates to novel clathrate complexes of cyclodextrin or arabinogalactan with 9-phenyl-sym-octahydroselenoxanthene, possibly in ?-crystalline form, The clathrate complex may be in crystalline form, possibly in the form of nano-particles. In the clathrate complex, cyclodextrin is selected from ?-, ?-, ?- or hydroxypropyl-?-cyclodextrin, primarily ?-cyclodextrin. The proposed clathrate complexes make it possible to increase the water-solubility of the active compound, to improve the bioavailability, to reduce the dosage of the drug and, consequently, to reduce the toxic effect of 9-phenyl-sym-octahydroselenoxanthene. The complexes exhibit cytoradioprotective activity. The invention also relates to a liquid-phase and solid-phase methods for producing clathrate complexes, as well as to pharmaceutical compositions and drugs thereof.

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: Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral and buccal administration of cladribine.

Abstract: A method for controlling intestinal function, blood sugar level, body fat or serum lipid, or maintaining and improving glucose tolerance. The method comprises giving to human body or animal foods and drinks, having health benefits, or enriched with health benefits, wherein the foods and drinks comprise as an active ingredient a hydrogenated, indigestible dextrin that is obtained by digesting pyrodextrin with an enzyme to obtain an indigestible dextrin, and then hydrogenating the indigestible dextrin.

Abstract: A material which contains a lipophilic component having a pungent taste or flavor such as a spicy component (e.g., a capsaicin) and a bitter component (e.g., a turmeric extract), in which the pungent taste and/or flavor of the lipophilic component can be reduced effectively, and in which the separation among components contained therein is not caused; a method for producing the material; a composition such as a food, a beverage, a cosmetic and a medicine, which contains the material; and a liquid composition having such a form that the material is dispersed in water.

Abstract: A composition is described for topical application comprising, in a physiologically acceptable medium, at least one complex composed of a naphthoic acid derivative of formula (I), salts and esters thereof: and of at least one cyclodextrin, said soluble molecular complex obtained by the technology of dense fluids under pressure.

Abstract: Provided are methods relating to compositions that include a CDP-topoisomerase inhibitor, e.g., a CDP-camptothecin or camptothecin derivative conjugate, e.g., CRLX101.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: The invention relates to a method for preparing a soluble inclusion complex comprising one or several active substances which are hardly soluble in an aqueous medium and are included in one or several host molecules, using the following successive stages: (a) bringing one or several active substances into contact with one or several host molecules; (b) initiating a molecular diffusion stage by bringing a dense pressurized fluid into contact with the mixture obtained in (a) in a static mode in the presence of one or several diffusing agents; (c) recovering the active substance-host molecule molecular complex formed; (d) adding and mixing an interaction agent with the active substance-host molecule molecular complex; (e) recovering the soluble inclusion compound thus formed. The invention also relates to the soluble inclusion compound obtained by the method, particularly a piroxicam-cyclodextrin-arginine compound.

Abstract: The invention relates to a pharmaceutical formulation that contains a complex of a propofol salt with a cyclodextrin. The invention makes it possible to provide propofol in a formulation that can be stored and that can be administered intravenously without problems.

Abstract: This invention relates to fat containing consumable food products comprising ?-cyclodextrin. The food products have reduced levels of bioavailable fat but have substantially the same fat, cholesterol and caloric content as a like food without ?-cyclodextrin. The invention also relates to methods for reducing the bioavailability of fats in fat containing food products without reducing caloric intake as determined by bomb calorimetry and to methods for increasing high density lipoproteins in a subject and reducing or controlling weight by administering the food products of this invention.

Abstract: This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: There is provided a composition comprising (a) one or more cyclopropene complex, and (b) 0-10% water by weight based on the weight of said composition, wherein the mole ratio of cyclopropene in said composition to molecular encapsulating agent in said composition is 0.92:1 or higher, or wherein the composition is in the form of a powder and, in a two-dimensional image of a representative sample of said powder, 20% or more of the area of the images of the particles of said cyclopropene complex, based on the area of all the images of all the particles of said cyclopropene complex in said image of said sample, is in the form of particles of said cyclopropene complex that have width dimension of 10 micrometers or larger. Also provided is a process for making a composition comprising cyclopropene complex.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

Abstract: The present invention provides a novel composition comprising Nabilone and randomly methylated B-cyclodextrin (RAMEB), wherein the weight ratio (dry weight to dry weight) between Nabilone and RAMEB is about 1:60-1:140. The present invention further provides methods for increasing the bioavailability of Nabilone.

Abstract: A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056 M?1-13051 M?1), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 ?m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

Abstract: A composition comprising a water-soluble and stable complex formed by an alkyl ether derivative of gamma-cyclodextrin and curcumin and optionally comprising non-complexed cyclodextrin, the molar ratio of curcumin to cyclodextrin being between 1:1 and 1:6, and a method of manufacturing such a composition. The water-soluble and stable complex of curcumin is useful in therapy, e.g. for treatment of cancer, leukemia, myocardial infarction, stroke, sepsis, acute lung injury, acute liver failure, acute tubular necrosis, acute pancreatitis, radiation injury and other life-threatening conditions in a human or animal subject, as well as for preserving human or animal organs, tissues or cells at a hypothermic temperature.

Abstract: The present invention relates to a method for enhancing the immune system and the treatment and/or prevention of immune system related disorders in a mammal, particularly newborns, said method comprising the administration of acid oligosaccharide and neutral oligosaccharide. Food compositions suitable for use in the above method are also provided.

Abstract: A stable composition for removing unwanted molecules from a surface comprises functionally-available cyclodextrin, cyclodextrin-compatible surfactant, and cyclodextrin-incompatible surfactant. The compositions are suitable for capturing unwanted molecules from inanimate surfaces, including fabrics, including carpets, and hard surfaces including countertops, dishes, floors, garbage cans, ceilings, walls, carpet padding, air filters, and the like, and from animate surfaces, including skin, hair, and the like. The compositions can further comprise other cyclodextrin-compatible and -incompatible materials and other optional ingredients.

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.