33 results about "Tandospirone" patented technology

The invention relates to a preparation and refining method of exo-methylene tetrahydrophthalic anhydride and its use in preparation of tandospirone. The preparation and refining method realizes high-efficiency combination of depolymerization of dicyclopentadiene, cycloaddition of cyclopentadiene and maleic anhydride, and transformation of endo-methylene tetrahydrophthalic anhydride, is free of a single dicyclopentadiene depolymerization process, is free of a reaction intermediate product separation process, effectively solves the problem that the existing exo-methylene tetrahydrophthalic anhydride preparation method has defects of complex dicyclopentadiene depolymerization processes, low conversion rate, low yield, serious environmental pollution, high energy consumption, long production cycle and harsh storage condition requirements, and has the advantages of high yield, good quality, eco-friendly solvent, low cost and good industrial production applicability.

The invention belongs to the technical field of drug detection, and particularly relates to a method and a kit for detecting 19 kinds of drugs and their metabolites in blood by liquid chromatography tandem mass spectrometry. Substances to be tested include sulpiride, penfluridol, mianserin, buspirone, tandospirone, hydroxyzine, diazepam, venlafaxine, moclobemide, imipramine, paroxetine, rebo Cetine, amitriptyline, sertraline, digoxin, clonazepam, clopidogrel, tolbutamide, glimepiride, 1-pyrimidine piperazine, desvenlafaxine, 6- Hydroxybuspirone, norimipramine, noramitriptyline, nordiazepam, clopidogrel metabolites; detection methods include: calibrating standard solutions, processing samples to be tested, using high performance liquid chromatography‑ Mass spectrometry detects the sample to be tested. The embodiment of the present invention can quickly and accurately measure the content, the sample processing method is simple and easy, and has high sensitivity and accurate quantification.

The invention provides a tandospirone dispersible tablet, which is prepared by containing the following raw and auxiliary materials in weight percentage: tandospirone or its pharmaceutically acceptable salt 1%-8%, filler 65%-90% , Disintegrant 4% to 30%. The tandospirone dispersible tablet prepared by the invention has a faster disintegration rate and a higher dissolution rate than ordinary tablets, can be efficiently absorbed in the digestive tract, and obtains higher bioavailability. The present invention can also be dispersed in water before taking, and has a sweet taste, and is more suitable for people who have poor absorption of oral preparations, people who have difficulty in swallowing, and the elderly or children with low drug compliance.

The invention provides an L-tartaric acid tandospirone compound. The invention further provides a preparation method, a pharmaceutical composition and application of the compound. The L-tartaric acid tandospirone compound provided by the invention exists in a crystal form, and is characterized in that the compound exists in an amorphous form and has no characteristic peaks in an X-ray powder diffraction pattern. The L-tartaric acid tandospirone compound provided by the invention has very good water solubility and stability and provides the possibility of improving the bioavailability and the safety of medicines; furthermore, the compound has a simple prepapration process and high yield and is suitable for industrial production.

The invention provides a serotonin receptor agonist. Specifically, a tandospirone maleate compound is provided. The invention also provides the preparation method of the compound, as well as the pharmaceutical composition and application containing the compound. Tandospirone maleate provided by the present invention exists in the form of crystals, has stable properties, good water solubility, and significantly improved bioavailability, providing an effective solution for improving the safety and effectiveness of drugs; in addition , the preparation process of the compound of the present invention is simple, the yield is high, and it is suitable for industrial production.

Tandospirone pharmaceutical composition and preparation method and use thereof. The tandospirone pharmaceutical composition comprises a pharmaceutical active ingredient, a matrix material, a filler, a bleaching aid, a lubricant and an optional binder, and the pharmaceutical active ingredient is tandospirone, which is pharmaceutically acceptable. The salt or the solvate of tandospirenone or a pharmaceutically acceptable salt thereof, the framework material includes selected from polyethylene oxide WSR 303, polyethylene oxide WSR 1105, polyethylene oxide WSR 301, polyethylene oxide WSR 205 , the combination of one or more in polyoxyethylene N-80; Described bleaching aid is selected from the combination of one or more in sodium carbonate, sodium bicarbonate, potassium bicarbonate, magnesium carbonate, calcium carbonate. The tandospirone pharmaceutical composition of the present invention prolongs the retention time of the drug in the stomach, so that the drug can be fully released and absorbed, and its bioavailability is greatly improved.

An azaspironone drug injection and a preparation method and application thereof, characterized in that the azaspironone drug injection comprises an active component of tandospirenone and a stabilizer. Described azapirone drug injection has high stability, good anti-anxiety effect, can meet the needs of clinical patients, can effectively solve children, or have digestive system disorders, or be in coma, convulsions, convulsions and other states and patients with dysphagia ( Such as elderly patients, bedridden patients) should not take tandospirone tablets or capsules orally. The azaspipirone drug injection also has the advantages of low cost, convenient use and the like. The solution of the azaspipirone drug injection is clear, the insoluble particles meet the standard, and the stability is good; there is no visible foreign matter and no abnormal toxicity; and its concentration does not cause toxicity and obvious irritation.

The invention provides the usage of tandospirone and derivatives thereof in the preparation of drugs for improving memory capability and recognition function. The invention also provides a drug combination for improving memory capability and recognition function. The tandospirone and the derivatives thereof can improve memory capability and recognition function and in particular has evident medical treatment effect on poor memory due to neurasthenia or senile dementia. The medicine of the invention can also treat neurasthenia and senile dementia; proved by clinical experiments, the medical effect is remarkable.

The invention provides a tandospirone hydrochloride crystal form II. The characteristic absorption peaks exist at the diffraction angle 2*theta within 2.127-2.527 degrees, 16.078-16.478 degrees, 19.157-19.557 degrees, 19.321-19.721 degrees, 19.499-19.899 degrees, 22.561-22.961 degrees, 29.437-29.837 degrees and 35.530-35.930 degrees in the X-ray powder diffraction diagram of the crystal form II. The invention further provides a preparation method of the crystal form II. Compared with the conventional tandospirone hydrochloride product, the tandospirone hydrochloride crystal form II provided by the invention is more excellent in water solubility and stability, and provides the possibility of improving bioavailability and safety of drugs; in addition, the preparation technology of the crystal form II is simple, the yield of the crystal form II is high, and the preparation method is suitable for industrial production.

The invention relates to a preparation method of exomethylenetetrahydrophthalic anhydride, a refining method thereof and an application thereof in a method for preparing tandospirone. The present invention combines the depolymerization of dicyclopentadiene, the cycloaddition of cyclopentadiene and maleic anhydride, and the transformation of endomethylene tetrahydrophthalic anhydride in series to complete the three-step reaction efficiently in one step, and the method does not need to carry out dicyclopentadiene separately. The depolymerization of dienes without separation of intermediate products generated by the reaction effectively solves the complicated depolymerization of dicyclopentadiene, low conversion rate and low yield in the existing preparation method of exomethylenetetrahydrophthalic anhydride , serious environmental pollution, high energy consumption, long production cycle, harsh storage conditions and other defects, and has the advantages of high yield, good quality, environmentally friendly use of solvents, low cost, and is suitable for industrialized large-scale production.

The invention provides a tandospirone enteric-coated pellet and a preparation method thereof. The enteric-coated pellet is prepared by adding tandospirone or a pharmaceutically acceptable salt thereof as an active ingredient and adding pharmaceutically acceptable auxiliary materials . The present invention also provides the use of the tandospirone enteric-coated pellets in the preparation of an anti-anxiety drug for enteral administration. The tandospirone enteric-coated pellets prepared by the invention have stable quality, no disintegration in the stomach, large distribution area in the intestinal tract, good disintegration and dissolution properties, high bioavailability, less irritation to the digestive tract mucosa, and less side effects , The patient's medication compliance is high. It can be used to treat patients with the following diseases: anxiety state caused by various neurosis, anxiety state accompanied by physical diseases such as essential hypertension and peptic ulcer, mild and moderate depression; especially suitable for digestive system diseases Patients who cause anxiety, patients with gastric mucosal injury or easy bleeding, and elderly patients who need long-term medication.

The invention provides a hydrochloric tandospirone crystal form I. The hydrochloric tandospirone crystal form I is characterized in that an X-ray powder diffraction pattern of the crystal form I shows that characteristic absorption peaks appear at 2 theta diffraction angles of 6.597+ / -0.2, 10.352+ / -0.2, 12.676+ / -0.2, 15.362+ / -0.2, 15.922+ / -0.2, 17.122+ / -0.2, 18.752+ / -0.2, and 25.522+ / -0.2 degrees. The invention also provides a preparation method of the crystal form I. Compared with the existing hydrochloric tandospirone product, the hydrochloric tandospirone crystal form I, provided by the invention, has the advantages that the water solubility and the stability are improved, and the bioavailability and the safety of a drug can be improved; in addition, the crystal form is simple in preparation process, high in yield, and suitable for industrial production.

The invention provides a tandospirone micropore osmotic pump preparation. The osmotic pump preparation can reach zero-level release, reaches 24-hour drug release, can effectively prolong the time of drug action, makes patients reduce the number of times of taking medicine daily, and improves compliance.

The invention belongs to the technical field of medical detection, and discloses a method for measuring the concentration of tandospirone in human plasma, using high performance liquid phase tandem mass spectrometry technology to detect tandospirone in pretreated human plasma samples, and using high performance liquid chromatography to detect tandospirone Tandospirone is separated from impurities, and then quantified by the isotope internal standard method. The concentration ratio of the standard in the standard solution and the internal standard in the internal standard working solution is the X axis, and the internal standard in the standard solution and the internal standard in the working solution are The peak area ratio of the standard substance is the Y axis, and the standard curve regression equation is established, and the linear least squares method is used to calculate the theoretical concentration ratio of the standard substance and the internal standard substance in the standard curve regression equation based on the peak area ratio of the analyte and the internal standard substance. , the measured concentration of tandospirone in human plasma samples was calculated by the obtained standard curve regression equation. The invention overcomes the defect of precise quantitative detection at a lower concentration level, and can meet the content determination requirement in a living body when a small dosage is administered.