18 results about "Paroxetine" patented technology

The present disclosure relates to a pharmaceutical composition comprising a therapeutically effective amount of latrepirdine or a pharmaceutically acceptable salt thereof and an effective amount of a PK stabilizer. The PK stabilizer may be selected from the group consisting of paroxetine, fluoxetine, and quinidine or a pharmaceutically acceptable salt thereof. The PK stabilizer in the composition results in improved pharmacokinetic profile and enhanced therapeutic effect of latrepirdine. The disclosure further relates to treatment of disorders associated with noradrenergic hyperarousal using the pharmaceutical composition.

The invention discloses a synthesis method of a 2-amino-3-trifluoromethyl naphthoquinone compound, which comprises the following steps: by taking a 1, 4-naphthoquinone compound, a Togni reagent and alkylamine as substrates, stirring in the dark at room temperature under the promotion of a proper amount of alkali to realize the construction of the 2-amino-3-trifluoromethyl naphthoquinone compound. The synthesis method has the prominent advantages that the substrate is cheap and easy to obtain, the reaction condition is mild, the operation is simple, the product is diversified and the like, and the synthesis method can be applied to derivative modification of drug molecules such as doxazosin (Doxazosin), levocetirizine (Levocetirizine), risperidone (Risperidone), desloratadine (Desloratadine) and paroxetine (Paroxetine).

Disclosed herein is an anti-tumor pharmaceutical composition based on immune checkpoint blockade and use thereof. The anti-tumor pharmaceutical composition comprises: paroxetine hydrochloride, and a T-cell enhancer, wherein the T-cell enhancer is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, cannabidiol and paroxetine hydrochloride were first found to be capable of effectively reducing the expression of PD-L1 on the tumor cell membrane, thereby blocking the PD-1 / PD-L1 signaling pathway and enhancing the ability of T cells to kill tumor cells. The T-cell enhancer added on this basis can further increase the quantity and activity of T cells, significantly increase the killing ability of T cells after immunosuppression is relieved, and greatly improve the anti-tumor effect of the drug. The components of the pharmaceutical composition used in the present invention, namely, cannabidiol, paroxetine hydrochloride, and vitamin E+thymosin, can exert a synergistic effect and improve the anti-tumor effect.

The utility model belongs to the technical field of paroxetine hydrochloride tablet manufacturing, and particularly relates to a structure capable of improving paroxetine hydrochloride tablet wet granulation efficiency, which comprises a granulator body, a control panel is mounted at the top end of the granulator body, a granulation box is connected to the top end of the granulator body and is positioned on one side of the control panel, and the control panel is mounted on the granulation box. The top end of the granulating box is correspondingly connected with a first feeding port and a second feeding port, the bottom end of the outer side wall of the granulating box is connected with a discharging port, the electric push rod is matched with the arc-shaped scraping plate, and the arc-shaped scraping plate can move up and down in the granulating box, so that materials attached to the inner wall of the interior of the granulating box are cleaned; the conditions that the stirring and mixing speed needs to be reduced during manual cleaning, meanwhile, the mixing effect is affected due to the fact that materials are attached to the inner wall of the interior of the granulation box, and stirring and mixing need to be conducted for a longer time are avoided, and then the paroxetine hydrochloride tablet wet granulation efficiency is improved by cleaning the materials attached to the inner wall of the interior of the granulation box.

The present invention relates to an orally disintegrating tablet manufactured by a direct compression method comprising paroxetine or pharmaceutically acceptable salts thereof, at least one disintegrant, at least one diluent, at least one lubricant, and one or more pharmaceutically acceptable excipients. The orally disintegrating tablet prepared using these excipients exhibits desirable properties such as facilitating disintegration, and dissolution of the drug for oral administration. The present invention also relates to the process for preparing the said solid pharmaceutical composition.

Disclosed herein is an anti-tumor pharmaceutical composition based on immune checkpoint blockade and use thereof. The anti-tumor pharmaceutical composition comprises: paroxetine hydrochloride, and a T-cell enhancer, wherein the T-cell enhancer is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, cannabidiol and paroxetine hydrochloride were first found to be capable of effectively reducing the expression of PD-L1 on the tumor cell membrane, thereby blocking the PD-1 / PD-L1 signaling pathway and enhancing the ability of T cells to kill tumor cells. The T-cell enhancer added on this basis can further increase the quantity and activity of T cells, significantly increase the killing ability of T cells after immunosuppression is relieved, and greatly improve the anti-tumor effect of the drug. The components of the pharmaceutical composition used in the present invention, namely, cannabidiol, paroxetine hydrochloride, and vitamin E+thymosin, can exert a synergistic effect and improve the anti-tumor effect.

The present invention discloses a paroxetine hapten and an artificial antigen and a preparation method and application thereof. The paroxetine hapten of chemical formula (I) and the paroxetine artificial antigen of chemical formula (II) are synthesized using 2-hydroxyparoxetine as a precursor. The obtained antigens have good immunogenicity and reactivity, and the corresponding antibodies are easily obtained when performing animal immunization, and can be used to prepare paroxetine colloidal gold detection products.

Orally rapidly disintegrating tablet (ODT) comprising paroxetine, or pharmaceutically acceptable salts thereof, at 0.5-40 %w / w, at least one diluent (e.g., dibasic calcium phosphate dihydrate, 60-90 %

The present invention relates to an orally disintegrating tablet manufactured by a direct compression method comprising paroxetine or pharmaceutically acceptable salts thereof, at least one disintegrant, at least one diluent, at least one lubricant, and one or more pharmaceutically acceptable excipients. The orally disintegrating tablet prepared using these excipients exhibits desirable properties such as facilitating disintegration, and dissolution of the drug for oral administration. The present invention also relates to the process for preparing the said solid pharmaceutical composition.

A method of treating premature ejaculation in men may include administering a therapeutically effective dosage of a formulation to a patient in need thereof. The formulation for treating male premature ejaculation may include a phosphodiesterase 5 inhibitor (PDE5i), such as Tadalafil; an alpha-1 adrenoreceptor (alpha-1a) selective antagonist, such as Silodosin; and a selective serotonin reuptake inhibitor (SSRI), such as Paroxetine.

Compositions and methods are provided for administering patusutine, or a pharmaceutically acceptable salt thereof, to a patient suffering from a liver injury.

A pharmaceutical anti-tumor composition based on immune checkpoint blockade and its use are described. The anti-tumor pharmaceutical composition comprises paroxetine hydrochloride and a T-cell enhancer, wherein the T-cell enhancer is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, it was first discovered that cannabidiol and paroxetine hydrochloride can effectively reduce the expression of PD-L1 on the cell membrane of tumors, thereby blocking the PD-1 / PD-L1 signaling pathway and enhancing the ability of T cells to kill tumor cells. The T-cell enhancer added on this basis can further increase the number and activity of T cells, significantly increasing the killing capacity of T cells after immunosuppression is lifted and significantly improving the anti-tumor effect of the drug.The components of the pharmaceutical composition used in the present invention, namely cannabidiol, paroxetine hydrochloride and vitamin E + thymosin, can achieve a synergistic effect and enhance the anti-tumor effect.

The invention discloses a paroxetine sustained release preparation as well as a preparation method and application thereof. The paroxetine sustained release preparation comprises a core material and a wall material, the core material comprises paroxetine, a diluent, a framework material and an adhesive; the wall material comprises a film control material, a pore-foaming agent, an anti-sticking agent and a plasticizer. The core material of the paroxetine sustained-release preparation disclosed by the invention can be a multi-unit sustained-release micro-tablet and is additionally provided with a sustained-release wall material, so that compared with a tablet with a single release unit, the paroxetine sustained-release preparation has a larger surface area and is more completely absorbed, and the bioavailability can be improved; the independent release microchip system ensures the independent release behavior, the administration dosage can be reduced according to actual needs, the blood concentration fluctuation and side reaction are reduced, and the treatment effect is improved.

The application discloses a method for simultaneously detecting the concentration of six drugs in blood, comprising the following steps: S1, taking a blood sample, centrifuging, and adding methanol to precipitate protein; S2, preparing a series of concentration calibration solution, quality control sample and internal standard working solution; S3, adding the internal standard working solution to the supernatant 1 prepared in S1, vortex mixing, centrifuging, and taking the supernatant 2; S4, using high performance liquid chromatography-tandem mass spectrometry to detect the supernatant 2 obtained in S3 for the selected drugs, and performing mass spectrometry screening analysis on the basis of the retention time of the compound, two pairs or three pairs of parent ions / daughter ions; the drugs include one, multiple or all of fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram and escitalopram; the detection method provided by the application has the characteristics of simple and convenient sample pretreatment, small required sample volume, high sensitivity, high accuracy and high throughput.

The invention relates to the technical field of neuroscience and drugs, and discloses application of parecoxib as an MEF2A transcription inhibitor in preparation of antiepileptic drugs, which is characterized in that the parecoxib is in targeted combination with N-terminal alpha1 helix and MADS box structural domain of MEF2A protein to inhibit DNA binding capacity of MEF2A, so that downstream NEK7 / CD74 gene transcription is blocked, and microglial cell mediated neuroinflammation is reduced; according to the present invention, the transcriptional activity action mechanism of parecoxib is inhibited through the MEF2A targeting DNA binding interface, specifically, the parecoxib is specifically bound with the N-terminal alpha 1 helix (residues ARG17, THR20, PHE21, LYS23 and ARG24) and MADS box structure domain of MEF2A so as to inhibit the conformational change and the DNA binding ability (the molecular docking simulation shows the high affinity binding), and the transcription of the downstream target gene (such as NEK7 and CD74) is inhibited by blocking the binding of the MEF2A and the DNA so as to inhibit the transcriptional activity of the MEF2A; therefore, the activation of NLRP3 inflammasomes is reduced; excessive activation of microglial cells is inhibited, and the steady state of the neural network is maintained.

The invention relates to a preparation method of a paroxetine main intermediate as shown in a formula I (-)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine. The preparation method comprises the following steps: by taking methyl p-fluorobenzoylacetate as a raw material, carrying out asymmetric hydrogenation to obtain an intermediate shown in a formula II; reacting the intermediate shown in the formula II with sodium methoxide and methylamine hydrochloride to obtain an intermediate shown in a formula III; generating an intermediate IV from the intermediate III under the action of reducing agents such as lithium aluminum hydride; reacting the intermediate shown in the formula IV with malonic acid monoester at room temperature to obtain an amide intermediate shown in the formula V; reacting the intermediate formula V with various chlorophosphodiesters at room temperature to obtain an intermediate formula VI; generating an intermediate formula VII from the intermediate formula VI under an alkaline condition; the intermediate formula VII generates a formula I (-)-trans-4-(4-fluorophenyl)-3-hydroxymethyl-1-methylpiperidine under the action of reducing agents such as lithium aluminum hydride. The process has the characteristics of relatively high yield, simple process, environmental friendliness and the like, and has a relatively good industrial application prospect. # imgabs0 #

The present disclosure addresses the problem of providing a prophylactic and / or therapeutic agent capable of effectively inhibiting progression of internal carotid artery stenosis.　This prophylactic and / or therapeutic agent for internal carotid artery stenosis includes an inhibitor of the P2X4 receptor as an active ingredient. The inhibitor of the P2X4 receptor is an antagonist against the P2X4 receptor. Examples of the antagonist against the P2X4 receptor include paroxetine, suramin, fluvoxamine, NP-1815-PX, NC-2600, NCP-916, BAY 2328065, 5-BDBD, BX430, and the like. The antagonist is preferably paroxetine.

The invention discloses application of an Eloralintide and paroxetine combination, a compound preparation and a preparation method, and belongs to the technical field of depression complicated with obesity treatment. Wherein the mass ratio of the Eloralintide to the paroxetine is (1: 10) to (1: 20). The Eloralintide and the paroxil provided by the invention have a synergistic effect, so that the bioavailability is improved, the side effect is reduced, and a new effective treatment choice is provided for obesity caused by depression. Animal experiment results show that after the two are combined, the effects of reducing body weight, improving depression-like behaviors and regulating metabolic functions are obviously better than those of single drug treatment, and the composition has a wide clinical application prospect.