Patent classifications
C08B37/0012
Controlled-release and stratified cyclodextrin inclusion complex vehicles
The invention provides cyclodextrin inclusion complex delivery vehicles formulated for oral delivery, in which the cyclodextrin inclusion complex comprising N-acetylcysteine and acetaminophen as stacked guest molecules within the cyclodextrin cavity is provided together with an enzyme having a cyclodextrin-degrading activity capable of digesting the cyclodextrin, so that upon delivery of the vehicle to a target the enzyme is activated and releases N-acetylcysteine and acetaminophen from the cyclodextrin cavity. In alternative aspects, these cyclodextrin inclusion complex delivery vehicles are for example provided in the form of medicaments, food ingredients, medical food ingredients, nutritional supplement ingredients, dietary supplement ingredients, herbicides, insecticides, fungicides, animal repellents, pheromones, plant growth regulators, fragrances, fabrics or packaging materials.
Processes for the preparation of sugammadex
The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-γ-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-γ-cyclodextrin and disodium 3 -mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-γ-cyclod extrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-y-cyclodextrin from γ-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-γ-cyclodextrin comprising, inter alia, reacting γ-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent. ##STR00001##
EXCIPIENTS PROVIDING STABILIZATION AND ENHANCED WATER SOLUBILIZATION AND THEIR USES
Four major polymeric architectures, namely: (a) linear, (b) branched, (c) hyperbranched/dendritic and (d) cross-linked polymers, when formed by reaction of multifunctional alcohols, such as sugar-based alpha-, beta- or gamma-cyclodextrins, with multi-carboxylic acids form unique polyester copolymers. These copolymers have been demonstrated to substantially enhance the water-solubility and bioavailability of water insoluble compounds for a wide variety of uses.
COMPOSITIONS AND METHODS FOR DIFFERENTIAL RELEASE OF 1-METHYLCYCLOPROPENE
A clathrate of 1-methylcyclopropene with α-cyclodextrin, obtained as a solid particulate product, is modified by comminuting, classifying, or both to obtain a modified particulate. When subjected to identical atmospheric disgorgement conditions of humidity and temperature, identical masses of the modified and unmodified particulates exhibit different rates of 1-methylcyclopropene disgorgement. Specifically, we have found that a smaller mean particle size is inversely related to a greater rate of 1-methylcyclopropene release.
OXYBATE POLYETHYLENE GLYCOL PRODRUGS
Oxybate-PEG ester prodrugs are provided herein in which the polyethylene glycol is bound to oxybate via an ester linkage. These oxybate-PEG esters may be further bound to a cyclodextrin or an anion exchange resin, via an ester linkage between the oxybate and the cyclodextrin or via ionic bonding between oxybate the anion exchange resin. Compounds and compositions containing these compounds are useful in immediate release and modified release compositions for treating narcolepsy and other disorders.
DRUG DELIVERY CARRIER INCLUDING PLGA AND BETA-CYCLODEXTRIN CONTAINING DRUG
Provided is a drug delivery carrier including PLGA and β-cyclodextrin containing a drug. According to the drug delivery carrier, the time during which a drug stays in the living body may be prolonged, and due to the biodegradation thereof, few side effects occur.
Pharmaceutical compositions comprising meloxicam
Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a T.sub.max of meloxicam of 3 hours or less.
CYCLODEXTRIN-DERIVED POLYMER NANOPARTICLES FOR ADSORPTION AND SYNTHESIS THEREOF
Cross-linked polymer nanoparticles were designed and synthesized with cyclodextrins as the starting monomer. These nanoparticles display exemplary adsorption properties in terms of capacity and selectivity, which comes from the synthetic design. The nanoparticles are also highly robust for various practical adsorption applications. The new synthetic method of these nanoparticle materials involves the reaction of cyclodextrin monomers through an emulsion polymerization approach. The size of the nanoparticles can be tuned easily.
Purification of sulfobutylated cyclodextrins with specific ion exchange resins
Present invention relates to a process to reduce butane sultone hydrolysis products (4-hydroxybutane-1-sulfonic acid, and bis(4-sulfobutyl) ether disodium) in sulfobutylether cyclodextrin reaction mixtures achieved with the combined use of a strong anion exchange resin having dialkyl 2-hydroxyethyl ammonium hydroxide functionality and a cation exchange resin.
CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY
Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of a disease or disorder, e.g., autoimmune disease, inflammatory disease, central nervous system disorder, cardiovascular disease, or metabolic disorder. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.