70 results about "Galantamine" patented technology

Galantamine formulations, including sustained-release and fast dissolve formulations, are described.

Methods and compositions of the invention employ acetylcholinesterase (ACE) inhibitors to prevent and treat diseases and other disorders of the central nervous system (CNS), including Alzheimer's disease. ACE inhibitors are administered for targeted delivery to the CNS, for example by intranasal delivery. The methods and compositions of the present invention yield therapeutic concentrations of ACE inhibitors in a CNS tissue or compartment without the attendant disadvantages, risks and side effects of oral or injection delivery. Exemplary ACE inhibitors for use within the invention include galantamine and various salts and derivatives of galantamine. Carboxylate salts of galantamine (e.g., galantamine gluconate, galantamine lactate, galantamine citrate and galantamine glucarate) described herein exhibit a significant increase in solubility compared to other forms of galantamine, such as galantamine hydrobromide.

The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.

The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and / or acting as cholinesterase inhibitors and / or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.

A composition and a method for using the composition to delay the onset of the symptoms of Alzheimer's disease in humans, comprising curcumin, piperine, oleic acid, oleanolic acid, ursolic acid, galantamine, and huperzine A, among other compounds. Curcumin is an antioxidant, while galantamine and huperzine A inhibit the activity of acetylcholinesterase in the brain. Piperine and oleic acid increase the bioavailability and gastrointestinal absorption of curcumin, galantamine, huperzine A, and other nutrients.

The invention relates to a pharmaceutical composition based on an active ingredient that is enclosed in liposomes for topical, transdermal application. The interior of said liposomes comprises an acidic, aqueous medium containing at least one cholinesterase inhibitor, preferably from the group containing donepezil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phenserine, tolserine, cymserine, thiatolserine, thiacymserine, neostigmine, huperzine, tacrine, metrifonate and dichlorvos, or an enantiomer or derivative of at least one of said compounds. In addition, the invention relates to a method for producing said composition, optionally in a sterile form and also to the use of the liposomes charged with the active ingredient in various galenic formulations for topical, transdermal application with a depot effect in the epidermis, for the prophylaxis and / or treatment of cutaneous neuropathic pain or the loss of cutaneous sensory function as a result of neuropathy.

Controlled-release galantamine formulations, including controlled-release particles, pellets, granules, and spheres are described. Controlled-release particles, pellets, granules, and spheres with immediate release top-coat are also described. Method of preparing such formulations and method of treating a variety of disorders are also disclosed.

A pharmaceutical composition containing the therapeutically active ingredients of azelastine or a pharmaceutically acceptable salt of azelastine and donepezil or rivastigmine or galantamine or a pharmaceutically acceptable salt of thereof is disclosed. A method of using the pharmaceutical composition for treating patients suffering from mental, behavioral, cognitive disorders is also disclosed.

Galantamine formulations substantially free of microcrystalline cellulose, lactose, and / or starch are described.

Haplotypes in the CDK5 gene associated with cognitive response to galantamine treatment are disclosed. Compositions and methods for detecting and using these CDK5 haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising galantamine or derivatives thereof that are approved for treating patients having one of these CDK5 haplotypes, methods and kits for predicting the response of an individual to galantamine based upon his / her haplotype profile, and methods for treating Alzheimer's patients based upon their haplotype profile.

The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and / or acting as cholinesterase inhibitors and / or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.

The present invention relates to a direct compression tablet formulation comprising, as the active ingredient, galantamine, and more specifically, galantamine hydrobromide along with a process of making the same. The tablet formulation is a direct compression tablet and has excellent content uniformity and dissolution properties.

The invention discloses application of puerarin or a medicinal composition containing the puerarin in preparation of a medicament with an effect of preventing or treating senile dementia. The puerarin can be singly used as a medicament or can be used together with other senile dementia medicaments with different mechanisms of action when used for treating or preventing the senile dementia of people or mammals, wherein the puerarin not only can reduce side or toxic effects of medicaments but also can achieve an effective of collaborative treatment when used for treating the senile dementia together with a medicinal composition consisting of triptolide, galantamine and borneol. The puerarin can significantly inhibit the deposition of beta-amyloid, and has a definite curative effect and small side effects when used for preventing and treating the senile dementia, so that the puerarin has a wide medical application prospect.

Haplotypes in the CDK5 gene associated with cognitive response to galantamine treatment are disclosed. Compositions and methods for detecting and using these CDK5 haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising galantamine or derivatives thereof that are approved for treating patients having one of these CDK5 haplotypes, methods and kits for predicting the response of an individual to galantamine based upon his / her haplotype profile, and methods for treating Alzheimer's patients based upon their haplotype profile.

Haplotypes in the CHRNA2 gene associated with cognitive response to galantamine treatment are disclosed. Compositions and methods for detecting and using these CHRNA2 haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising galantamine or derivatives thereof that are approved for treating patients having one of these CHRNA2 haplotypes, methods and kits for predicting the response of an individual to galantamine based upon his / her haplotype profile, and methods for treating Alzheimer's patients based upon their haplotype profile.

Haplotypes in the EPHX2 gene associated with cognitive response to galantamine treatment are disclosed. Compositions and methods for detecting and using these EPHX2 haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising galantamine or derivatives thereof that are approved for treating patients having one of these EPHX2 haplotypes, methods and kits for predicting the response of an individual to galantamine based upon his / her haplotype profile, and methods for treating Alzheimer's patients based upon their haplotype profile.

Galantamine has be used in the treatment of a number of chronic diseases. Galantamine has been found to be safe and effective in the treatment of Alzheimer's disease. Neuropsychiatric disorders are often associated with Alzheimer's disease. It is demonstrated that galantamine is also effective in reducing or stabilizing the incidence of neuropsychiatric behaviour seen in Alzheimer's patients.

Haplotypes in the LRPAP1 gene associated with cognitive response to galantamine treatment are disclosed. Compositions and methods for detecting and using these LRPAP1 haplotypes in a variety of clinical applications are disclosed. Such applications include articles of manufacture comprising galantamine or derivatives thereof that are approved for treating patients having one of these LRPAP1 haplotypes, methods and kits for predicting the response of an individual to galantamine based upon his / her haplotype profile, and methods for treating Alzheimer's patients based upon their haplotype profile.

Galantamine and its pharmaceutically acceptable salts are of use in treating persons meeting criteria for having a risk of developing Alzheimer's type dementia, before dementia occurs by reducing thedecline of A[beta] amyloid in CSF or the increase in cortical beta amyloid, in order to delay cognitive decline.

A method of treating a subject suffering from a neurodegenerative disease by modulating microglial activation with a therapeutically effective amount of a cholinergic agonist and a cholinesterase inhibitor. In one embodiment of the invention, the cholinergic agonist is nicotine and the cholinesterase is galantamine (a relatively weak acetylcholinesterase inhibitor and a potent allosteric potentiating ligand of nAChRs)

The invention discloses a reagent and kit for enriching breast cancer stem cells from breast cancer cell strains. The reagent includes galantamine and lycorine as a screening agent. The breast cancer cell strains are MCF-7 breast cancer cell strains. The kit comprises a double-antibody, galantamine and lycorine as a screening agent, a screening-agent-dissolving auxiliary agent, sodium sulfite as an anti-oxidant, a recombinant human epidermal growth factor (EFG) which is a conventional growth factor, bovine serum albumin (BSA), insulin and B27. The provided reagent can enrich breast cancer stem cells from human breast cancer MCF-7 cell strains in a convenient, fast and efficient way, the cell spheroids are short in forming period, and the content of cancer cells and SP cells marked by CD44<+>CD24<- / low> molecules in microsphere cells is high. The developed kit can improve the efficiency for enriching cancer stem cells by science researchers.

Galantamine has been used in the treatment of a number of chronic diseases. Galantamine has been found to be safe and effective in the treatment of Alzheimer's disease. Neuropsychiatric disorders are often associated with Alzheimer's disease. It is demonstrated that galantamine is also effective in reducing or stabilizing the incidence of neuropsychiatric behaviour seen in Alzheimer's patients.

A method of treating organophosphorous (OP) poisoning comprising administering to a mammal at risk for OP poisoning an OP poisoning-inhibiting amount of galantamine.

The invention provides a new method for the preparation of (-)-galanthamine. The method includes the following steps: preparing N-methyl-N-(4-hydroxyl phenethyl)-3-hydroxyl-4-methoxyl-6-bretylium (f) by condensation of N-(4-hydroxyl phenethyl)-3-hydroxyl-4-methoxyl-6-bretylium (d) as a starting material and formaldehyde, then preparing bromo-narwedine (g) by catalytic oxidation using an oxidizing agent (Oxone / CaCl2 / TEMPO) and a phase-transfer catalyst, transforming the bromo-narwedine to levo bromo-narwedine (h) by Shieh method, obtaining bromo-(-)-galantamine (i) by asymmetric reduction, and then obtaining the (-)-galanthamine by hydrogenated debromination.

The invention belongs to the technical field of medicine, and specifically relates to a compound medicinal composition with acetylcholinesterase inhibitors such as donepezil, galantamine or huperzine A and metformin as active ingredients, a preparation method thereof and a therapeutic use thereof. Pharmacodynamic tests show that the compound pharmaceutical composition of the present invention can be used for the prevention and treatment of Alzheimer's dementia, and the combined use of the compound medicine has a synergistic effect in curative effect.

The invention discloses a method for detecting galantamine in lycoris aurea, and relates to plant sample handling, preparation of a nanogold printing electrode sensor and electrochemical detection. According to the method, the nanogold-modified printing electrode sensor is adopted to fully absorb in a sample extracting solution, then the nanogold printing electrode sensor is subjected to differential pulse voltammetry scanning to measure current values at oxidation peaks, within a detectable range, the content of the galantamine in the lycoris aurea absorbed by the nanogold printing electrodesensor is in a linear relation with the current intensities at the oxidation peaks, and according to a working curve, the content of the galantamine in the detected lycoris aurea can be calculated. The method has the advantages that the nanotechnology and the silk-screen printing technology are combined by the prepared nanogold printing electrode sensor, sensitivity, in galantamine concentration detection, of the sensor can be improved remarkably, and the minimum limit of detection of the sensor can reach to 0.013 microns.

Galantamine and its pharmaceutically acceptable salts are of use in treating persons meeting criteria for having a risk of developing Alzheimer's type dementia, before dementia occurs by reducing the decline of Aβ amyloid in CSF or the increase in cortical beta amyloid, in order to delay cognitive decline.