71results about How to "Pharmacologically active" patented technology

The invention provides a kit for detecting anti-psychosis drugs in a serum and plasma by a liquid chromatography tandem mass spectrometry method. The kit comprises drug standards: amsulpiride, aripiprazole, dehydroaripiprazole, chlorpromazine, clozapine, n-desmethylclozapine, risperidone, 9-hydroxyrisperidone, quetiapine, olanzapine, ziprasidone; drug internal standard compounds: amplepiride-d5, aripiprazole-d8, chlorpromazine-d3, clozapine-d8, risperidone-d4, 9-hydroxyrisperidone-d4, quetiapine-d8, olanzapine-d8, ziprasidone-d8; drug extraction compounds: methanol solution 60% (volume ratio),acetonitrile solution 20%, isopropanol solution 10%, purified water 10%; negative plasma; and a diluent: 50% aqueous methanol solution. The kit can be used to simultaneously detect anti-psychosis drugs and active metabolites thereof, the detection time is short and the flux is large.

The invention discloses a method for separating and preparing a gelsemium alkaloid monomer from gelsemium by adopting high-speed counter current chromatography, which pertains to the separation method of medicinal plant monomers. The invention takes total alkaloids of gelsemium as a raw material and a high-speed counter current chromatograph as a separating device and the method comprises that a solvent system which is composed of stationary phase and mobile phase is prepared; the high-speed counter current chromatograph is filled with the stationary phase and then the mobile phase is pumped in and balanced; and then sampling is conducted by a sample valve; target components are collected according to the map of a detector or in combination of the detection methods of high efficiency liquid chromatography and thin layer chromatography, and distilled under reduced pressure and then recrystallized to obtain the gelsemium alkaloid monomer with high purity. By adjusting the specific proportional parameters of the solvent system, single or multiple target gelsemium alkaloid monomers can be separated by one step or step by step. The method is convenient and efficient, large in preparation amount, less in sample loss, good in separation effect and high in controllability and applicable to automatic production and the obtained gelsemium alkaloid monomer from separation has diverse pharmacological activities and application prospect to be prepared into medicines.

The invention discloses a method for separating and preparing a gelsemium alkaloid monomer from gelsemium by adopting high-speed counter current chromatography, which pertains to the separation method of medicinal plant monomers. The invention takes total alkaloids of gelsemium as a raw material and a high-speed counter current chromatograph as a separating device and the method comprises that a solvent system which is composed of stationary phase and mobile phase is prepared; the high-speed counter current chromatograph is filled with the stationary phase and then the mobile phase is pumped in and balanced; and then sampling is conducted by a sample valve; target components are collected according to the map of a detector or in combination of the detection methods of high efficiency liquid chromatography and thin layer chromatography, and distilled under reduced pressure and then recrystallized to obtain the gelsemium alkaloid monomer with high purity. By adjusting the specific proportional parameters of the solvent system, single or multiple target gelsemium alkaloid monomers can be separated by one step or step by step. The method is convenient and efficient, large in preparation amount, less in sample loss, good in separation effect and high in controllability and applicable to automatic production and the obtained gelsemium alkaloid monomer from separation has diverse pharmacological activities and application prospect to be prepared into medicines.

The invention relates to the application of gentian in antiviral drug, while its gentian content is more than 50%, wherein the test has proved that gentian has activity resistant to CVB3 and HFRS. Therefore, the gentian can treat viral myocarditis and nephrotic syndrome. And it can be made into tablet, capsule, etc.

The invention provides a tegafur derivative containing a 1,3,4-thiadiazole heterocyclic ring and an amide group. The structural formula of the tegafur derivative is as shown in the specification. A preparation method of the tegafur derivative comprises the steps of (1) dissolving a 3-(methoxycarbonylmethyl)tegafur in methanol, dropwise adding a sodium hydroxide solution, extracting by using ethyl acetate and distilled water and separating out an organic layer and a water layer, next, extracting by using ethyl acetate and blending the organic layers, and adding anhydrous sodium sulfate to obtain 1-(tetrahydro-2-furyl)-3-carbethoxy-5-fluoro-2,4-pyrimidinedione; (2) blending 1-(tetrahydro-2-furyl)-3-carbethoxy-5-fluoro-2,4-pyrimidinedione with dioxane, then adding sulfoxide chloride to obtain a 1-(tetrahydro-2-furyl)-3-chloracetyl-5-fluoro-2,4-pyrimidinedione solution, and then adding dioxane, evenly mixing and then sealing for later use; (3) taking 2-amino-5-p-nitrophenyl-1,3,4-thiadiazole, dioxane and triethylamine, and dropwise adding the 1-(tetrahydro-2-furyl)-3-chloracetyl-5-fluoro-2,4-pyrimidinedione solution obtained in the step (2) to obtain a pure product 1-(tetrahydro-2-furyl)-3-acetamido-[5-p-nitrophenyl-(1,3,4-thiadiazole-2-yl)]-5-fluoro-2,4-pyrimidinedione. The tegafur derivative has anti-tumor effect and no obvious toxicity, and is used for clinically treating malignant tumors.

The invention discloses a method for preparing a 2-triazole-quinoline-4-carboxylic acid compound. The method comprises the steps of using benzyl halide, sodium azide, a 1-3-dicarbonyl compound and isatin as raw materials, and performing one-pot synthesis under the catalysis of diethylamine and strong alkali to obtain a 1,2,3-triazole substituted quinoline-4-carboxylic acid compound. The method is easily-available in raw material, simple in operation and high in yield, and has good application prospects.

The invention discloses an alpha, beta-unsaturated cyclohexanone derivatives and application thereof as medicaments for preventing, treating or dignozing Alzheimer's disease. The alpha, beta-unsaturated cyclohexanone derivatives comprise 2,6-bis(2-chloro-3- methoxybenzylidene)cyclohexnone, 2,6-bis(2-chloro-3,4-dimethoxybenzylidene)cyclohexnone, 2,6-bis(2-bromo-3,4,5-trimethoxybenzylidene)cyclohexnone, 2,6-bis(2-chloro-3-methoxybenzylidene)-4-methylcyclohexnone, 2,6-bis(2-chloro-3,4-dimethoxybenzylidene)-4-methylcyclohexnone and the like. Through bioactivity determination, the alpha, beta-unsaturated cyclohexanone derivatives are proved to possess pharmacological activity related to resistance to Alzheimer's disease, is applicable as medicaments to prevent, treat and diagnose Alzheimer's disease, and possesses relatively good potential application prospect.

The invention relates to a natural medicament with the cancer prevention effect and a preparation method and application thereof. The natural medicament with the cancer prevention effect is prepared from the following raw materials (by weight): 30-70 parts of turmeric, 5-20 parts of broccoli, 10-50 parts of Trametes versicolor, 5-20 parts of yeast beta-glucan and 5-20 parts of pepper. According tothe natural medicament, by reducing formation of cancerogenic substances in body, cancerogenic mutation induced by harmful compounds is prevented, thus forming primary prevention of cancers; by activating immune cells such as lymphocyte, macrophage, etc., tumor inflammation of patients with cancer at an early stage is reduced, and clinical symptoms of cancer patients are improved, thus forming secondary prevention of cancers; and through synergism with other chemotherapeutic drugs, drug resistance of tumor is inhibited, thus forming tertiary prevention of cancers. Then, incidence rate and mortality of cancers are finally reduced, thus achieving the purpose of cancer prevention.

The invention relates to a traditional Chinese medicine composition capable of treating gout. The traditional Chinese medicine composition is prepared from the following traditional Chinese herbal medicines by mass: 12-20 parts of herba taxilli, 12-18 parts of ramulus mori, 25-35 parts of honeysuckle stem, 8-13 parts of radix angelicae pubescentis, 8-13 parts of angelica sinensis, 10-20 parts of radix achyranthis bidentatae, 10-20 parts of radix salviae miltiorrhizae, 8-12 parts of rhizoma corydalis, 12-18 parts of siegsbeckia orientalis, 12-18 parts of radix cynanchi paniculati and 25-35 parts of rhizoma polygonati odorati. The traditional Chinese medicine composition can tonify kidney and activate blood, unblock meridians to relieve pains, and has a significant curative effect and low toxic and side effect.

This invention belongs to pharmacy field, it relates optical pure mei pu ta fen and its preparation method and application. Racemation mei pu ta fen is splited by optical pure tartaric acid evolving object to get optical pure monomer, enantiomeric excess testing is done through capillary electrophoresis method, their e.e.valude are both excess 99 percent. Laevorotation and dextrorotation mei put a fen absolute configuration is decided by single crystal X-diffraction method as S and R. the R(+)mei pu ta fen has srong activity in analgesia activity testing, but S(-)mei pu ta fen has more stronger activity in acetylcholine esterase restrain activity testing, analgesic medicine and senile dementia medicine can be further prepared.