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.

The present invention is snuff of setron medicine includes the medicine component selected from Ondansetron, tropisetron and granisetron; and medicine carrier selected from glucose, mannitol, lactose, sorbitol, microcrystalline cellulose and beta-cyclodextrin.

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.

A method for detecting residual intermediate of tropaic alcohol in tropisetron synthesis includes preparing test solution and control solution , dropping them separately on the same silica gel G thin layer plate , using acetone ¿C ammonia water as developing agent to carry out thin layer chromatography determination, developing chromatographic cylinder, using developer of bismuth potassium iodide solution with assistance of sodium nitride solution to develop color and checking colour developed result.

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 provides a preparation method of tropisetron, which comprises the following steps: in an inert solvent, activating indolyl-3-formic acid into mixed anhydride by using C2-C4 aliphatic halogenated carboxylic acids as a catalyst and C2-C4 aliphatic halogenated carboxylic acid anhydride as an activating reagent, and dropwisely adding a tropine alcoholic solution dissolved in the inert solvent to carry out condensation reaction, thereby obtaining the tropisetron. The method provided by the invention is simple to operate, has the advantages of mild reaction conditions, high safety coefficient, fewer side reactions, high yield and high purity, lowers the production cost and operating risk, and is especially suitable for large-scale industrial production.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a hydrochloric-acid tropisetron freeze-dried powder injection for injection and a preparation method thereof. The hydrochloric-acid tropisetron freeze-dried powder injection comprises a medicinal active ingredient, excipients and pH (potential of hydrogen) stabilizers, wherein the medicinal active ingredient is hydrochloric-acid tropisetron, the excipients include mannitol and sodium chloride, and the pH stabilizers include citric acid and sodium citrate. According to the hydrochloric-acid tropisetron freeze-dried powder injection, the mannitol and the sodium chloride serve as the excipients, the pH value of a midbody solution is controlled to be stabilized within 4.6-5.2 by citric acid and sodium citrate buffer solutions, oxidation of a main drug is inhibited, and stability of the main drug is improved; in six months of an acceleration test, the injection is stable in content, changes of related substances are small, and the storage period of the injection is prolonged. The preparation method is simple in process and suitable for industrial production.

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 belongs to the technical field of medicines, and particularly relates to a tropiseiron hydrochloride compound and a preparation method thereof. The invention also relates to application of an injection containing the tropiseiron hydrochloride compound in preparation of drugs for treating nausea and vomit.

A method for detecting residual intermediate of tropaic alcohol in tropisetron synthesis includes preparing test solution and control solution , dropping them separately on the same silica gel G thin layer plate , using acetone - ammonia water as developing agent to carry out thin layer chromatography determination, developing chromatographic cylinder, using developer of bismuth potassium iodide solution with assistance of sodium nitride solution to develop color and checking colour developed result.

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 discloses a compound preparation used for treating depression and senile dementia. The compound preparation comprises the following components in part by weight: 1 part of rolipram and 0.25 to 200 parts of antiemetic medicament, wherein the antiemetic medicament is granisetron, ondansetron, tropisetron, aprepitant or metoclopramide. The compound preparation is prepared from the rolipram and the granisetron, the ondansetron, the tropisetron, the aprepitant or the metoclopramide. The compound preparation has an effective curative effect of treating the melancholia and the senile dementia, and simultaneously solves the technical problems that in the prior art, the rolipram causes adverse reactions such as vomition, sicchasia, headache and the like.

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 discloses a compound preparation used for treating depression and senile dementia. The compound preparation comprises the following components in part by weight: 1 part of rolipram and 0.25 to 200 parts of antiemetic medicament, wherein the antiemetic medicament is granisetron, ondansetron, tropisetron, aprepitant or metoclopramide. The compound preparation is prepared from the rolipram and the granisetron, the ondansetron, the tropisetron, the aprepitant or the metoclopramide. The compound preparation has an effective curative effect of treating the melancholia and the senile dementia, and simultaneously solves the technical problems that in the prior art, the rolipram causes adverse reactions such as vomition, sicchasia, headache and the like.

The invention relates to the field of medicines, in particular, it provides a combined medicine or medicine box product and application for treating gastrointestinal reactions after chemotherapy. Through repeated exploration and a large number of experiments, the inventor found through clinical application that the traditional Chinese medicine composition with woody, sandalwood, agarwood, musk, magnolia officinalis, citrus aurantium, rhubarb, croton cream, jujube and chuanxiong as main medicinal materials and tropane The combined use of setron or its pharmaceutically acceptable derivatives can improve the clinical efficacy of chemotherapy-induced nausea and vomiting, acute vomiting, and delayed vomiting. The combination of the two has a synergistic effect on gastrointestinal reactions, and can Improve the curative effect of chemotherapy-induced gastrointestinal reactions, and reduce the adverse reactions caused by the drug itself.

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 relates to a synthesis process for preparing tropisetron by using 2-chloro-1,3-dimethylimidazoline chloride as a condensing agent. Under the action of imidazoline chloride and an organic base, react indole-3-carboxylic acid and tropinol at room temperature for 12 to 24 hours in an inert solvent, and undergo cooling, filtering, washing and other processing steps to obtain the target Product tropisetron; the molar ratio that the above-mentioned indole-3-carboxylic acid, tropinol and 2-chloro-1,3-dimethylimidazoline chloride carry out condensation reaction is: 1: 1~2: 1~3; Preferably it is 1:1 to 1.5:1 to 1.5. The synthesis process of the invention is safe, pollution-free, easy to operate, high in product yield and good in purity, and can meet the requirements of pharmaceutical production.

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 provides a preparation method of tropisetron, which comprises the following steps: in an inert solvent, activating indolyl-3-formic acid into mixed anhydride by using C2-C4 aliphatic halogenated carboxylic acids as a catalyst and C2-C4 aliphatic halogenated carboxylic acid anhydride as an activating reagent, and dropwisely adding a tropine alcoholic solution dissolved in the inert solvent to carry out condensation reaction, thereby obtaining the tropisetron. The method provided by the invention is simple to operate, has the advantages of mild reaction conditions, high safety coefficient, fewer side reactions, high yield and high purity, lowers the production cost and operating risk, and is especially suitable for large-scale industrial production.

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.

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.

The invention relates to a tropisetron pharmaceutical composition, which comprises tropisetron salts, carbomer, hydroxypropyl methylcellulose, poloxamer, 1-methyl-4-isopropylcyclo-3-alcohol and other additives. The tropisetron pharmaceutical composition disclosed by the invention is in the liquid state in vitro; after being used for a mouth mucosa, the tropisetron pharmaceutical composition is in the semi-solid gel state and serves as temperature-sensitive gel; the composition gel has a certain intensity and biological adhesive and can stay in a drug application position, so that drugs are continuously released; furthermore, drugs can be promoted to be absorbed through the mouth mucosa; the pharmacological effect is taken.