241 results about "Glucuronide" patented technology

A composition for controlled release of an opioid from a pharmaceutical composition, the method comprises controlling the release of at least one opioid into an aqueous medium by erosion of at least one surface of a pharmaceutical composition comprising I) a matrix composition comprising a) polymer or a mixture of polymers, b) an opioid and, optionally, c) one or more pharmaceutically acceptable excipients, and (i) a coating. The matrix composition has a conus-like shape so the surface area exposed to the aqueous medium increases at least during initial erosion of the matrix composition, and the dissolution of the opioid-when tested in a Dissolution Test as described herein with or without application of sinkers-results in a zero order release of at least 80% of the opioid contained in the composition. Such compositions are especially suitable for controlled release of an opioid to obtain a delayed pead concentration and a prolonged therapeutically effective plasma concentration upon oral administration. Once or twice daily administration is possible. The matrix typically comprises PEO and the active substance is typically an opioid such as morphine or a glucuronide thereof.

The present invention provides a topical formulation and method of use where the formulation comprises macqui berry or a macqui berry extract containing anthocyanins having a very high oxygen radical absorbance capacity (ORAC). The formulation provides the macqui berry in a stabilized form which includes a glucuronide or glycuronide, a photostabilizing agent, encapsulation, or light -and/or air-blocking packaging.

A multi portion intra-oral dosage form has at least one pharmaceutically active agent or health promoting agent with at least one portion comprises a component for creating a noticeable organoleptic sensation. The sensory markers or signals are conceptual aids for a subject using the dosage form where the organoleptic sensation is such that it facilitates the subject to identify a portion and differentiate between different portions. Also contemplated are a dosage form, a method and a system for delivering active agents, such as nicotine and/or metabolites thereof, such as cotinine, nicotine N′-oxide, nomicotine, (S)-nicotine-N-β-glucuronide and mixtures, isomers, salts and complexes thereof as well as use and production of said dosage forms.

Novel estrogenic compounds of Formula I are provided.

wherein the bond represented by the wavy line may be a single or double bond such that when the wavy line is a single bond, R₁ is selected from the group consisting of hydrogen, sulfate and glucoronate or other esters, and when the wavy line is a double bond, R₁ does not exist; R₂ is lower alkyl; R₃ may be selected from the group consisting of hydrogen, sulfate, or glucuronide or other esters; and R₄ through R₁₃ may independently be selected from the group consisting of hydrogen, hydroxy, ketone, lower alkyl, lower alkoxy, halogen, and carbonyl groups and R₁₄ is selected from the group consisting of hydrogen, sulfate and glucoronide and other esters. When R₁ is hydroxy, the hydroxy or ester substituent may have either an α or a β orientation. Compositions of matter including compounds of the present invention are also provided as are methods of treating mammals in need of treatment using compounds of the present invention.

Ligand Drug conjugate compounds comprising a β-glucuronide-based linker and methods of using such compounds are provided.

The present invention relates to a multi portion intra-oral dosage form where at least one portion is rapidly disintegrating and at least one portion is slowly disintegrating, whereby the disintegration time for the slowest disintegrating portion is at least two times longer than for the most rapidly disintegrating portion. Of certain interest is use of sensory markers/signals as conceptual aids for the subject.

Also contemplated are a method and a system for delivering active agents, such as nicotine and/or metabolites thereof, such as cotinine, nicotine N′-oxide, nornicotine, (S)-nicotine-N-β-glucuronide and mixtures, isomers, salts and complexes thereof as well as use and production of said formulations.

The invention belongs to the field of marine medicines, and relates to a fucosan sulphate, a preparation method thereof and application of the fucosan sulphate in preparing an anti-influenza virus medicine. Polysaccharide with a main chain taking alpha-1,2-D-mannose and beta-1,4-D-glucuronic acid as repetitive units, and with a branched chain of alpha-1,3-L-fucosan sulphate is obtained by virtue of hot-water extraction, calcium chloride precipitation and DEAE-Cellulose chromatographic column purification. The fucosan sulphate prepared by the invention is high in inhibition effect on the influenza virus neuraminidase activities of A H1N1, H5N1 and H3N2, and obvious in protection effect on the dog kidney epithelial cells infected by A H1N1. The fucosan sulphate provided by the invention has the advantages of being rich in raw material source, simple in preparation process, easy to industrialize, high in product water solubility, high in stability, free from toxic and side effects, and the like, and has the prospect of being developed to the anti-influenza virus medicine.

Disclosed are compounds of the formula:

wherein R₁, R₂, R₃ and R₄ are independently hydrogen, C₁-C₆ alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH₂)_n; a phosphate group, and a phosphinate group; R₉ is hydrogen, halogen or alkyl; R₁₁ is selected from the group consisting of H, C₁-C₆ alkyl, halogen, a sulfate, a glucoronide, —SO₂NH₂, —COOH, —CN, —CH₂CN—, —NHCN—, —CHO, ═CHOCH₃, —COO salt, —OSO₂alkyl, —NH₂, and —NHCO(CH₂)_n; R₁₂ is selected from the group consisting of H, a C₁-C₆ alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C₁-C₁₂ alkyl, C₂-C₁₂ alkenyl, C₂-C₁₂ alkynyl, halogen, a glucoronide, —NH₂, —SO₂NH₂, —COOH, —CN, —CH₂CN, —NHCN, —CHO, —COOsalt, —OSO₂alkyl, —SH, —SCH₃, —CH[(CH₂)_nCH₂]COOCH₂, —(CH₂)_mCOOCH₃, —(CH₂)_m—O—CH₃, —(CH₂)_m—O—(CH₂)_nCH₃, (CH₂)_m—S—CH₃, —(CH₂)_m—S—(CH₂)_nCH₃, —(CH₂)_m—NH—(CH₂)_nCH₃, —C₂-C₈ alkenyl-O—(CH₂)_nCH₃, —C₂-C₈ alkenyl-S—(CH₂)_nCH₃, —C₂-C₈ alkenyl-N—(CH₂)_nCH₃, —C₂-C₈ alkynyl-O—(CH₂)_nCH₃, —C₂-C₈ alkynyl-S—(CH₂)_nCH₃, —C₂-C₈ alkynyl-N—(CH₂)_nCH₃, —(CH₂)_m—OH, —(CH₂)_m—O—NH₂, —(CH₂)_m—S—NH₂, —NH(CH₂)_mCH₃, —NH(CH₂)_mOCH₃, —NH(CH₂)_mCHOH—COOH, —N(CH₃)₂, —(CH₂)_m(NH)CH₂OH, —NHCOOH, —(CH₂)_mNHCOOH, —NO₂, —SCN, —SO₂alkyl, —B(OH)₂, —(CH₂)_m N(CH₃)—SO₂—NH₃, —(CH₂)_m—NH—SO₂—NH₂, —NHC(═S)CH₃, and —NHNH₂; and Y is selected from hydrogen, ═O, —OCO(R₆) and —OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.

The invention provides a compound for use in medicine, the compound being a compound of the formula (VI⁰) or a salt, solvate, tautomer or N-oxide thereof:

wherein the bicyclic group:

is selected from the structures C1, C5 and C6:

wherein n is 0, 1, 2 or 3; R¹ is hydrogen, hydroxy, or O—R^z; R^2a is hydroxy, methoxy or O—R^z; provided that at least one of R¹ and R^2a is O—R^z; R^z is L^p-R^p1; SO₃H; a glucuronide residue; a mono-, di- or tripeptide residue; or

L^p is a bond, C═O, (C═O)O, (C═O)NR^p1 or S(O)_xNR^p1; x is 1 or 2; R^p1 is hydrogen or a an optionally substituted C_1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R^p1 is not hydrogen when L^p is a bond, C═O or (C═O)O; and provided also that O—R^z does not contain an O—O moiety; and excluding compounds wherein R¹ is hydroxy and R^2a is methoxy; R^p2 and R^p3 are the same or different and each is a group R^p1; and R³, R^4a, R⁸ and R¹⁰ are defined in the claims.

The compounds of formula (VI⁰) are pro-drugs of parent compounds wherein R¹ and/or R^2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

The invention provides a preparation method of flavonoid glycosides in scutellaria baicalensis. The method is suitable for quickly preparing four flavonoid glycosides comprising baicalin, wogonoside, chrysin-6-C-alpha-L-Arabic glucoside-8-C-beta-D-glucoside and oroxylinA-7-O-glucuronide. The preparation method comprises the following steps of: pulverizing scutellaria baicalensis and then adding water to extract; sequentially carrying out alcohol precipitation and high-speed centrifugation; after membrane separation, loading nonpolar macroporous absorption resin and eluting by alcohol/water; collecting eluent and concentrating and drying to obtain a scutellaria baicalensis macroporous resin component; and obtaining a scutellaria baicalensis effective component through parallel preparing liquid-phase chromatographic separation by using acetonitrile water as a flow phase. The preparation method has good selectivity and high purity of the obtained compound and greatly improves the separation and purification efficiency. The preparation process has high repeatability and good maneuverability, is easy to realize standardization and industrialization and has certain guidance effects on quickly obtaining flavones active constituents in the scutellaria baicalensis.

The present invention provides practical GOTCAB saponin synthesis process. The synthesis process includes the following steps: connecting site-28 glucose chain; connecting site-3 glycosyl; connecting rest site-3 glycosyl after protecting radical operation; making site-6' hydroxy group empty via protecting radical operation; selectively oxidizing site-6' primer hydroxy group into carboxylic acid; and finally eliminating all the protecting radicals under alkali condition.

Isolated metabolites of the cyclosporine analog ISA247 are disclosed, including in vitro methods for their preparation. The metabolites comprise a chemical modification of ISA247, wherein the modification is at least one reaction selected from the group consisting of hydroxylation, N-demethylation, diol formation, epoxide formation, and intramolecular cyclization phosphorylation, sulfation, glucuronide formation and glycosylation. Methods of preparation include semi-synthetic methods, wherein metabolites of ISA247 are produced from the microsomal extracts of animal liver cells, or from cultures using microorganisms, and completely synthetic methods, such as chemically modifying the parent compound or isolated metabolites using organic synthetic methods.

The present invention provides methods and kits for the detection of glucuronide metabolites of various drugs, alcohols and other compounds using a combination of High Performance Liquid Chromatography coupled with Pulsed Electrochemical Detection. Detection of a drug and its glucuronide metabolite(s) has applications in interpretive forensic and clinical toxicology. The ability to estimate metabolite/drug ratios enables the assessment of route, dose and time of exposure. In instances where the parent drug is biotransformed quickly and can only found in low levels in biological fluids, the detection of metabolites allows for the identification of parent drugs. Furthermore, metabolite determination enables the differentiation between recent and chronic drug use.

A method for mass spectrometric analysis of a saliva sample possibly containing mycophenolic acid or its metabolites mycophenolic acid phenyl glucuronide (MPAG) or mycophenolic acid acyl-glucuronide (Acyl-MPAG), including the steps: (a) providing a saliva sample containing one or more drug or metabolites; (b) deproteinating the sample; (c) separating the one or more drug or metabolites from the saliva sample; and (d) analyzing the one or more drug or metabolites using a mass spectrometer. The sample containing one or more MPA or metabolites is obtained from in an oral fluid based biological samples i.e. whole saliva or saliva obtained by chemical or mechanical stimulation or from specific salivary glands. The size of the sample contains one or more MPA or metabolites is at least about 100 microL. A kit for use in mass spectrometric analysis of a sample may contain one or more MPA or metabolites from saliva samples, comprising: (a) reagents for deproteinating of the saliva sample, including internal standards; (b) reagents for separating the one or more MPA or metabolites from the saliva sample; (c) reagents for analyzing the one or MPA or metabolites using a mass spectrometer; (d) a solution of one or more MPA or metabolites in saliva samples; and (e) instructions for analyzing the one or more MPA or saliva using a mass spectrometer. The kit includes (a) mobile phase solutions; (b) a chromatography column; and (c) a quality control specimen.

The invention relates to a detecting technique for an endocrine disrupter in a water environment and especially relates to a co-detection method for an estrogen coalition, Estrone-3-sulfate, E1-3S, Estradiol-3-sulfate, E2-3S, Estradiol-3-glucuronide, E1-3G and17beta-Estradiol-3-glucuronide, E2-3G in a water sample by adopting a liquid chromatogram-tandem mass spectrum technique. The method comprises the steps of: enriching the E1-3S, E2-3S, E1-3G and E2-3G in a collected water sample by using a HLB (Hydrophile-Lipophile Balance) solid-phase extraction column; connecting an activated NH2 column under the HLB column and washing with carbinol; and lastly, eluting with 2% of ammonia water carbinol solution and analyzing by adopting the liquid chromatogram-tandem mass spectrum technique. The method has the advantages of environmental protection, easiness in operation, high recovery rate and quick analysis for the trace amount of estrogen coalition E1-3S, E2-3S, E1-3G and E2-3G in the watersample.

The invention discloses a method for preparing scutellarin by using Aspergillus niger AS 3.795 for hydrolyzing scutellarin-7-O-glucuronide. Aspergillus niger AS 3.795 is used for hydrolyzing scutellarin-7-O-glucuronide glucuronyl to prepare the scutellarin. The method comprises the following steps of: using Aspergillus niger AS 3.795 to biologically transform a substrate scutellarin-7-O-glucuronide, using ethyl acetate to extract transformation products from fermentation liquor and using D101 macroporous adsorption resin column chromatography and recrystallization to purify the transformation products. The purity of the prepared transformation products can reach more than 99 percent according to high performance liquid chromatography. The method has the advantages that the defect that glucuronide is difficult to hydrolyze is overcome, the scutellarin can be prepared in a large scale under moderate conditions such as normal temperature and normal pressure, the environmental protection is facilitated, the production cost is reduced and the method is suitable for industrialized production.

The invention relates to a preparation method and application of a folium apocyni veneti extract, belongs to the field of medicines and aims at increasing the extraction content of quercetin-3-O-beta-D-glucosyl-beta-D-glucoside and quercetin-3-O-beta-D-glucuronide in folium apocyni veneti by 0.5-10 percent and applying the quercetin-3-O-beta-D-glucosyl-beta-D-glucoside and the quercetin-3-O-beta-D-glucuronide to a medicament for treating depression. According to the folium apocyni veneti extract, the total flavonoids content is 58-78 percent, wherein the contained flavonoids component is prepared from the following components in percentage by weight: 5.0-25 percent of the quercetin-3-O-beta-D-glucosyl-beta-D-glucoside, 0.5-10 percent of the quercetin-3-O-beta-D-glucuronide, 0.5-20 percent of rutin, 5.0-25 percent of hyperin, 5.0-20 percent of isoquercetin, 2.0-10 percent of quercetin, 2.0-10 percent of kaempferol and the balance of other flavonoids components. The preparation method and the application are convenient and efficient, are easy in operation and low in cost, can meet development and utilization of the fields of the medicines and foods and have very large application and development values.