33 results about "Tropisetron" patented technology

The invention provides compositions and methods for the treatment of mild cognitive impairment (MCI), and for inhibiting, reducing, delaying and/or preventing the progression of MCI to Alzheimer's disease. The methods entail administering an effective amount of one or more compounds selected from the group consisting of tropisetron, disulfuram, honokiol and nimetazepam. The methods also are useful for prophylactic and therapeutic treatment of amyloidogenic diseases, including Alzheimer's disease.

This invention relates to a synthesizing technology for preparing tropisetron with chloro 1, 3-dimethyl-2-chlorin imidazoline as the condensation agent, in which, indole-3-formic acid is reacted with tropaic alcohol for 12-24h under room temperature then to be cooled, filtered and cleaned to get the objective product tropisetron, and the mol ration of the indole-3-formic acid, tropaic alcohol and chloro 1, 3-dimethyl-2-chlorin imidazoline for condensation reaction, and the option is 1:1-1.5:1-1.5.

The invention relates to a citric acid tropisetron raw material medicine and a preparation technology of the citric acid tropisetron raw material medicine and an injection liquid, and belongs to the field of chemical pharmacy; in the process of tropisetron salifying, the citric acid is used as acid radical; the chemical name of the citric acid tropane tropisetron is [(1alpha H, 5alpha H)-8-methyl-azepine bicyclo-(3, 2, 1) octyl group-3alpha-]-1H- benzpyrole-3- formic ether citrate; and the molecular formula is C23H28N209. In the process of tropisetron salifying, the tropisetron is dissolved in ethanol; the mixture is added with ethanol solution of the citric acid, evenly stirred and stands till the needed solid is separated out; the crude citric acid tropisetron is filtered, heated and dissolved in distilled water, is added with the activated carbon for backflowing and decoloring, cools and stands after being filtered so as to separate out white cystal; the mixture is filtered; the filter cake is dried and then distilled water is used for the secondary recrystallization to obtain the refined citric acid tropane tropisetron. The clinical research shows that compared with the imported muriatic acid tropisetron injection solution, the citric acid tropisetron injection solution has similar curative effect and safety.

The present invention is nasal spray of setron medicine includes the medicine component selected from Ondansetron, tropisetron and granisetron, osmotic pressure regulator and water.

A medicinal preparation for preventing and/or treating psychoneurotic diseases such as integration dysfunction and Alzheimer's disease which contains tropisetron or its pharmaceutically acceptable salt as the active ingredient.

The invention relates to an oral spray for controlling nausea and vomit of chemotherapy and radiation therapy, the formula of the oral spray is composed of ingredients with the following parts by weight: 5-50 parts of drug absorption enhancer, 2-20 parts of drug active ingredient and 30-90 parts of buffer, the drug absorption enhancer can be any one or the combination of more of the following ingredients: azone, propylene glycol, polysorbate (Tween), ethylene glycol deoxycholic acid sodium salt, brij, sodium decanoate, lauric acid, stearic acid, sodium lauryl sulphate, stearyl alcohol sodium sulfate, dioctyl succinate sodium sulfonate, oleic acid, GK2, menthol and borneol; the drug active ingredient can be any one combination of the following ingredients: palonosetron hydrochloride, granisetron, ondansetron, azasetron and tropisetron; and the ingredients of the buffer are sodium citrate buffer solution and phosphate buffer solution. The oral spray provides a formulation which is safer, painless and convenient for patients with advanced tumor, elderly and weak patients, children patients and the patients who suffer from the metal illness and do not obey the oral administration or the injection drug administration.

A transdermal composition of the present invention comprises (a) a matrix containing (i) 20 to 80 % by weight of an alcohol, (ii) 1 to 50 % by weight of a skin penetration enhancer selected from the group consisting of a fatty acid and a derivative thereof, a fatty alcohol and a derivative thereof, an amide, a terpene, a surfactant and a mixture thereof, and (iii) 15 to 80 % by weight of water; and (b) 1 to 15 % by weight, based on the weight of the matrix, of an antivomiting agent selected from the group consisting of tropisetron, ondansetron, granisetron and pharmaceutically acceptable salts thereof, which is capable of delivering the antivomiting agent efficiently over a period of a day or more without skin irritation.

The invention relates to a detection method for alpha-tropine as impurity in hydrochloric acid tropisetron, which is characterized by adopting the gas chromatography for detection, and particularly includes the following steps: (1) preparing sample hydrochloric acid tropisetron solution with concentration of 10mg/m1 to 30mg/ml; (2) preparing reference sample alpha-tropine solution with the concentration of 0.02mg/m1 to 0.06mg/m1; (3) performing headspace sample injection and chromatogram acquisition; and (4) calculating the result through the appearance method based on the peak area. The invention has the characteristics that the detection method is convenient, quantitative and sensitive, and can be widely applied to the control and improvement of the medicine quality.

The invention discloses a synthetic method of tropisetron oxide, namely N-hydroxy tropisetron, belonging to the field of drug synthesis. According to the invention, 2-nitrophenyl acetate is used as araw material, and six reactions are successively conducted to synthesize the tropisetron oxide, namely N-hydroxy tropisetron; optimal preparation steps and reaction conditions are screened out througha large number of experiments; and the purity of the prepared target product can reach 99% or above, and the prepared target product does not contain tropisetron serving as a crude drug, can be usedfor research on pharmacokinetics, crude drug impurity identification and the like, and has important application value in impurity identification of tropisetron, research on metabolic mechanism of tropisetron and research design of novel drugs of tropisetron.

The invention provides a tropisetron composition for injection and relates to the technical fields of medicines and medicine preparation. The tropisetron composition is characterized in that the main medicines are tropisetron and melatonin, wherein the melatonin comprises a quick release part and a slow release part included by cyclodextrin. According to the tropisetron composition provided by the invention, the treating effect of the tropisetron is improved; problems of instability and rapidness in distribution and clearing caused when MT (melatonin) is orally absorbed are avoided, and a first-pass effect of the MT is reduced; the use level of the tropisetron is lowered; a medicine administration design in which a quick release manner and a slow release manner are combined is accordant with physiological secretion characteristics of the MT, the problem of the MT that the half-life period is short is solved, and the biological availability of a product is improved; the treatment of the tropisetron to CINV (Chemotherapy Induced Nausea and Vomiting) is enhanced, after the tropisetron and the melatonin are combined, not only the CINV can be treated, the treatment effect of the tropisetron to the CINV can be improved, the treatment course can be shortened, but also the use level of the tropisetron is lowered, the side effect of the tropisetron is reduced, and the immune capability of a human body can be improved; by maintaining the melatonin with a certain concentration in the blood of the human body, a stress reaction of the body can be effectively reduced, and the treatment of the CINV is benefited.

The invention belongs to the technical field of medicines, and particularly relates to an application of tropisetron in preparation of daily chemicals or medicines for improving skin, and the tropisetron is used for improving skin. Tropisetron is used for preventing and treating nausea and vomiting caused by cancer chemotherapy. The inventor accidentally finds that the tropisetron has an excellenteffect of improving the skin, so that the skin of a human body can better exert the function of a first organism protective film.

The invention discloses a detection kit for metabolic markers of ondansetron and tropisetron, a detection method of the detection kit and application of the detection kit and the detection method. The detection kit is used for detecting gene polymorphism of the metabolic markers CYP2D6C100T, CYP2D6G1846A and CYP2D6*5 of the ondansetron and the tropisetron. According to the kit, specific amplification primers and sequencing primers are designed according to the polymorphism of the three genes CYP2D6C100T, CYP2D6G1846A and CYP2D6*5. The kit comprises the following components of an amplification reaction solution, the CYP2D6C100T sequencing primer, the CYP2D6G1846A sequencing primer, the CYP2D6*5 sequencing primer and a positive control. According to the invention, blood direct expansion, rapid amplification and optimized pyrosequencing technologies are combined to detect gene polymorphism related to prediction of drug effects and adverse reactions of the ondansetron and the tropisetron, and suggestions from the gene perspective are provided for clinical use of the ondansetron and the tropisetron.

The invention belongs to the technical field of drug synthesis, and particularly relates to a preparation method of tropisetron bisindole impurities. The preparation method of the tropisetron bisindole impurities comprises the following steps: (1) dissolving 3-indolecarboxylic acid and an acylation reagent in a solvent and reacting, and carrying aftertreatment to obtain 3-indoloformyl chloride; and (2) dissolving tropisetron in tetrahydrofuran, cooling to the temperature of minus 15-20 DEG C, adding alkali, then dropwise adding a tetrahydrofuran solution of the 3-indoloformyl chloride, reacting for 2-10 hours at a room temperature after dropwise adding is finished, and carrying out aftertreatment to obtain tropisetron bisindole impurities. The preparation method is simple to operate, gentle in reaction, high in yield and high in purity of product, is suitable for mass spectrometry on crude drugs, and has quite high commercial value.