36 results about "Aripiprazole" patented technology

The present application relates to aripiprazole synthesis technical field, specifically to a kind of preparation of 1-(2,3-dichlorophenyl) piperazine hydrochloride substantially without following dimer impurity compound (I), the structure of the impurity is determined to clarify the generation mechanism of the impurity, provide the train of thought for better control of the impurity and make corresponding judgment to the impurity derived subsequently, provide help to the quality research of subsequent intermediates and finished products;The present application replaces the existing multiple recrystallization process by means of filtration and salting-out, which can effectively simplify the operation and greatly reduce the use of organic solvents.

The invention relates to the technical field of medicine packing materials, in particular to a filling process of a novel aripiprazole double-cavity pre-filling syringe, and a syringe barrel of the novel double-cavity pre-filling syringe is made of COP / COC materials; comprising the following steps of sterilization, middle plug placement, sterile filling, freeze drying, plug pressing and assembling, and a complete double-cavity pre-filled syringe is obtained.The filling process combines high strength and heat conduction uniformity of COP / COC materials, in-situ freeze-drying in the syringe is achieved, the step of powder transfer after freeze-drying of a traditional penicillin bottle is avoided, and the production efficiency is improved. According to the present invention, the sterile risk and the production cost are significantly reduced, the manufacturing process is simplified, the equipment complexity and the product loss are reduced, and the high dose accuracy and the yield are ensured.

The invention discloses an aripiprazole raw material particle size detection method, and belongs to the technical field of drug detection. Technical breakthrough is realized through specific detection instrument type selection, key parameter optimization and system verification process construction: a new ParaThak laser particle analyzer equipped with an R5 measuring lens, an RODOS / M dispersion system and a VIBRI sample injector is selected, a standardized parameter system with dispersion pressure of 3.0 Bar, a sample injection rate of 70% and optical concentration of 5%-10% is determined, and the measurement accuracy of the system is improved. A complete detection process is formed through sample amount exploration, repeatability and precision verification. According to the present invention, with the core idea of determining the optical concentration control standard, optimizing the sample amount matching concentration and verifying the reliability of the method, the problem of poor optical concentration repeatability is solved, the stability and the accuracy of the detection data are significantly improved, and the reliable detection means is provided for the quality control of the aripiprazole raw material.

The disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to an aripiprazole-trimesic acid salt form and a preparation method thereof. According to the salt form, a basic unit is composed of tetramolecular aripiprazole and tetramolecular trimesic acid. The salt form obtained by the invention has relatively high solubility performance and physical stability; the obtained salt form is not easy to generate crystal transformation or degradation, and shows excellent storage stability and process adaptability. Meanwhile, the preparation method of the salt form is simple in process and mild in condition, and has a remarkable industrial application prospect.

The present invention pertains to a composition, containing aripiprazole as an active ingredient, for enhancing the anticancer effect of a RAF inhibitor. More specifically, the present invention pertains to a composition for enhancing the anticancer effect of the RAF inhibitor, wherein the composition can treat cancer by acting as an agent for enhancing the anticancer effect of the RAF inhibitor when used in combination therapy with aripiprazole. Administering an effective amount of aripiprazole according to the present invention in combination with the RAF inhibitor is highly effective in enhancing the anticancer effect of the RAF inhibitor, such as by inducing cancer cell death, and thus the composition can be advantageously used as an agent for enhancing the anticancer effect of the RAF inhibitor.

The present invention relates to a composition containing aripiprazole as an active ingredient for enhancing the anti-cancer effect of a KRAS G12C genetic mutation therapeutic agent. More specifically, the present invention concerns a composition for enhancing the anticancer effect of a KRAS G12C genetic mutation therapeutic agent, which acts as an enhancer for the anti-cancer effect of the KRAS G12C genetic mutation therapeutic agent when used in combination therapy with aripiprazole, thereby enabling the treatment of cancer. When used at an effective dose in combination with a KRAS G12C genetic mutation therapeutic agent, aripiprazole according to the present invention excellently enhances the anticancer effect of the KRAS G12C genetic mutation therapeutic agent by inducing cancer cell death, etc. Thus, it can be advantageously used as an enhancer for the anti-cancer effect of the KRAS G12C genetic mutation therapeutic agent.

The invention discloses a composition, a method and a system for predicting the applicability of antipsychotic drugs. The invention develops a composition, a detection kit, a model construction method and a system for predicting the applicability of antipsychotic drugs on the basis of selected SNP site information. Particularly, a gene marker combination related to the curative effects of the antipsychotic drugs olanzapine, risperidone, aripiprazole and quetiapine is found by adopting a large-sample high-throughput whole-genome association analysis technology, and a corresponding mathematical model for predicting the curative effects is constructed; the model can be used for predicting the PANSS subtraction rate after the schizophrenia is treated by medication based on DNA polymorphic sites and clinical basic information of a medication user in a high, medium and low classification manner, and assists in guiding the selection of the types of the medication, so that personalized treatment of the schizophrenia patient is realized.

The present invention belongs to the field of pharmaceutical formulation, and particularly relates to an aripiprazole injectable suspension formulation having prolonged shelf life, and methods of using the formulation in treating schizophrenia and related diseases. In another aspect, the present invention also relates to a method of prolonging shelf life of an aripiprazole injectable suspension formulation.

The present invention provides a novel therapeutic means for cancer cells resistant to epidermal growth factor receptor (EGFR)-targeted anticancer agents. Almost no cell death was observed when cancer cells having an exon 19 deletion mutation in the EGFR gene (EGFR Del19), cancer cells having a substitution mutation in which the 790th amino acid threonine in the EGFR protein is substituted with methionine (EGFR T790M), and cancer cells having a substitution mutation in which the 858th amino acid leucine is substituted with arginine (EGFR L858R) were treated solely with aripiprazole or solely with an EGFR-targeted anticancer agent. However, cell viability decreased and cleavage of the apoptosis marker PARP was observed when the cancer cells were treated with aripiprazole in combination with an EGFR-targeted anticancer agent. Therefore, aripiprazole is provided as an enhancer of the anticancer effect of EGFR-targeted anticancer agents.

The present disclosure is directed to the methods of treating a patient with schizophrenia or bipolar I disorder by administering to the patient an injectable preparation of aripiprazole, wherein the patient is administered the injectable preparation about once every two months.

The application discloses a method for simultaneously regulating a new crystal form and crystal habit of aripiprazole; in the technical scheme, proteins are added in the crystallization process of aripiprazole to prepare aripiprazole with different crystal habits, and new crystal forms APZ-H1 and APZ-H2 of aripiprazole are found; the application creatively applies the protein, which is harmless to human bodies, to regulate the crystal habit of drugs, so as to replace other toxic and harmful crystal habit additives and guarantee the safety of the drugs; the method has the characteristics of simplicity, high efficiency and no pollution, is harmless to human bodies, is more green and environmental protection, and is easy to realize green industrial production.

The present invention relates to a composition containing aripiprazole as an active ingredient for enhancing the anti-cancer effect of an ERK inhibitor. More specifically, the present invention concerns a composition for enhancing the anticancer effect of an ERK inhibitor, which acts as an enhancer for the anti-cancer effect of the ERK inhibitor when used in combination therapy with aripiprazole, thereby enabling the treatment of cancer. When used at an effective dose in combination with an ERK inhibitor, aripiprazole according to the present invention excellently enhances the anticancer effect of the ERK inhibitor by inducing cancer cell death, etc. Thus, it can be advantageously used as an enhancer for the anti-cancer effect of the ERK inhibitor.

The invention provides a method for catalytic synthesis of aripiprazole by using a hydrogen transfer strategy, and the preparation method comprises the following steps: taking 7-hydroxy-3, 4-dihydro-2 (1H)-quinolinone as a starting material, and carrying out nucleophilic substitution type etherification reaction on the starting material and 4-bromo-1-butanol in an alkaline medium to generate a 7-(4-hydroxybutoxy)-3, 4-dihydro-2 (1H)-quinolinone intermediate; and then, by taking a ruthenium catalyst as a catalytic system, carrying out N-alkylation reaction on the intermediate and 1-(2, 3-dichlorophenyl) piperazine hydrochloride to finish the synthesis of the target compound aripiprazole. The method has the advantages of being short in technological process, high in atom utilization rate, high in yield, low in cost, environmentally friendly and the like.

Described is a composition comprising (a) a population of particles of an aripiprazole prodrug having a volume based particle size (Dv50) of less than 1000 nm and (b) at least one surface stabilizer comprising an adsorbed component which is adsorbed on the surface of the aripiprazole prodrug particles and a free component available for solubilisation of the aripiprazole prodrug. The surface stabilizer to prodrug ratio provides the optimal quantity of free surface stabilizer for the purposes of producing a lead-in formulation. Also described are methods of treatment using the aforementioned composition.

The present invention relates to a composition for enhancing the anticancer effect of a MEK inhibitor, the composition comprising aripiprazole as an active ingredient, and more specifically, to a composition for enhancing the anticancer effect of a MEK inhibitor, the composition being capable of treating cancer by acting as an anticancer effect enhancer of the MEK inhibitor when used in combination therapy with aripiprazole. An effective amount of aripiprazole according to the present invention is highly effective in improving the anticancer effect of the MEK inhibitor, such as by inducing cancer cell death, when administered in combination with the MEK inhibitor, and thus the present invention can be effectively used as an agent for improving the anticancer effect of the MEK inhibitor.

The present disclosure relates to a dose initiation method of performing an aripiprazole treatment on a patient in need thereof, the method comprising administering two separate aripiprazole injections and a single oral aripiprazole on the first day of aripiprazole treatment wherein the first aripiprazole injection is a long acting injection (LAI) and the second aripiprazole injection is a single dose oral aripiprazole injection. And the second injection of aripiprazole is an injection once a month (AOM). Maintaining administration is performed with a maintained dose of the LAI about two months after the first day of the aripiprazole treatment. The method is suitable for application parts of deltoid muscles and gluteus muscles.

The present invention provides a medical device containing a cake composition comprising aripiprazole as an active ingredient and capable of suppressing agglomeration of aripiprazole in a suspension obtained by resuspending a freeze-dried substance; and a cake composition comprising aripiprazole as an active ingredient. The present invention relates to a medical device containing, in a storage container whose inner wall is treated with silicone, a freeze-dried cake composition comprising separately prepared aripiprazole as an active ingredient, wherein there is a space between the inner wall and the cake composition; and a cake composition comprising aripiprazole as an active ingredient and having a strength of 5 to 100 N.

The invention relates to the technical field of pre-filling syringe production, in particular to a novel aripiprazole double-cavity pre-filling syringe freeze-drying groove frame and a using method thereof.The novel aripiprazole double-cavity pre-filling syringe freeze-drying groove frame comprises a groove frame plate, the lower surface of the groove frame plate protrudes downwards to form a plurality of hollow nest barrels, and the groove frame plate is provided with containing openings matched with the nest barrels; according to the invention, the lower surface of the groove frame plate protrudes downwards to form a plurality of hollow nest cylinders, and the nest cylinders are matched with the placing ports on the groove frame plate, so that the structure creates a special and stable placing space for the aripiprazole double-cavity pre-filled injector; due to the fact that the inner hollow structure of the nest cylinder is matched with the appearance of the injector, the injector can be firmly fixed after being placed in the nest cylinder, the situation that the injector shakes or inclines is avoided, and therefore the phenomenon that in the transferring process, the injector is damaged due to collision or the adverse effect on the freeze-drying process is caused due to position deviation is effectively avoided.

The invention belongs to the field of drug synthesis, and particularly relates to a method for removing aripiprazole oxidation impurities, the structural formula of the aripiprazole oxidation impurities is as shown in the specification: 3, 4-dihydro-7-(4-chlorobutoxy)-2 (1H)-quinolinone and 1-(2, 3-dichlorophenyl) piperazine are subjected to a condensation reaction, and after the reaction is finished, the aripiprazole oxidation impurities are obtained. The method comprises the following steps: carrying out primary refining on the obtained product in an aqueous solution of alcohol and inorganic alkali, filtering after the primary refining is finished, and carrying out secondary refining on a filter cake obtained by filtering, so that the residue of an aripiprazole oxidation impurity E in the obtained aripiprazole finished product is remarkably reduced, and the quality of the aripiprazole finished product is improved.

The application relates to the pharmaceutical technical field and discloses a preparation method of aripiprazole monohydrate with low initial release degree, which comprises the following steps: firstly, adding aripiprazole raw medicine into mixed solvent A, heating, stirring, cooling, crystallizing, stirring, filtering and drying to obtain a crude product crystal; secondly, adding the crude product crystal into mixed solvent B, stirring, cooling and crystallizing; finally, filtering the crystal, rinsing the crystal with cold mixed solvent C and drying to obtain aripiprazole monohydrate with low initial release degree. The aripiprazole monohydrate raw medicine with high purity and low burst release can be obtained by the method, wherein the proportion of anhydride in the aripiprazole monohydrate crystal form is reduced from 20% to 10% or below, the proportion of sub-micron size small particles in the medicine is obviously reduced through scanning electron microscope observation, and the initial release degree (10 min) of in-vitro release is reduced from 36-46% to 12-30%.

The invention discloses an application of domperidone in preparation of a pharmaceutical preparation for treating inflammatory skin diseases. The domperidone disclosed by the invention can be used as an active ingredient for inhibiting the P2Y14 receptor and is applied to preparation of the medicine for treating the inflammatory dermatitis, a new application of the domperidone is developed, and a new choice is provided for treatment of psoriasis and atopic dermatitis. The domperidone disclosed by the invention has good P2Y14 receptor inhibition activity, and the domperidone has no obvious influence on cell activity under the dosage of 15 mu M; after domperidone intragastric administration is carried out on a mouse with psoriasis and atopic dermatitis, the skin thickness is remarkably reduced, and inflammatory cell infiltration is relieved. According to the application, the effect of domperidone on improving inflammatory skin diseases (psoriasis and atopic dermatitis) by inhibiting P2Y14 receptors is found and verified for the first time through in-vivo and in-vitro experiments, the domperidone has the potential of preparing novel anti-inflammatory drugs, and meanwhile, the domperidone is low in clinical application risk as an FDA approved marketing drug.

To suppress bitter taste of a pharmaceutically active compound while suppressing cost without requiring a complicated process and a plurality of additives.SOLUTION: The present invention provides a bitterness suppressor for a pharmaceutically active compound, comprising a cyclodextrin and / or a derivative thereof as an active ingredient, wherein the pharmaceutically active compound is any one selected from the group consisting of duloxetine hydrochloride, aripiprazole, atomoxetine hydrochloride, donepezil hydrochloride, and dorzolamide hydrochloride.SELECTED DRAWING: None

This invention relates to blends comprising carbamate compounds for the prevention, relief, or treatment of schizophrenia, the blends comprising a carbamate compound of Formula 1, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, and more specifically, to blends and pharmaceutical compositions comprising a carbamate compound of Formula 1 and aripiprazole, respectively, and their use in the treatment of schizophrenia.

The present disclosure is directed to methods of dispersing injectable preparations comprising aripiprazole or a salt thereof. Methods of enhancing slidability of long-acting injectable preparations comprising aripiprazole or a salt thereof, comprising dispersing ingredients comprised in the preparations before administration, aripiprazole injectable preparations to be administered after the dispersion, methods of administration thereof, and use thereof are provided.

The invention belongs to the technical field of medicines, and particularly relates to application of nicotine combined aripiprazole in bipolar depression and a product. According to the treatment scheme, the treatment effect is achieved through the synergistic effect of the low-dose non-addiction nicotine and the low-dose aripiprazole, a complementary mechanism is formed by the low-dose non-addiction nicotine and the low-dose aripiprazole, and the treatment response rate is effectively increased. Meanwhile, due to the adoption of a mode of combined use of low-dose medicines, the safety risk possibly faced by high-dose use of a single medicine is successfully avoided, the treatment requirements of patients with poor tolerance to the high-dose medicines and unsatisfactory treatment effect of the single medicine can be well met, the technical blank of combined use of medicines in the field of biphasic depression treatment is filled, and the application prospect is wide. And a new effective choice is provided for clinical treatment of bipolar depression.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to an aripiprazole-4-chlorobenzoic acid-hydrate crystal form and a preparation method thereof. A basic unit of the aripiprazole crystal form is composed of one molecule of aripiprazole, one molecule of 4-chlorobenzoic acid and one molecule of water. The aripiprazole crystal form obtained by the invention has relatively high stability, and the dissolving property of the aripiprazole crystal form can meet the requirements of a sustained and controlled release preparation on the drug release characteristic, so that the stable and sustained release of the drug is realized, and the curative effect and the safety of the preparation are improved. The preparation process of the crystal form is simple, conditions are mild, process control and large-scale production are easy to realize, and the crystal form has a wide industrialization prospect.

To suppress bitter taste of a pharmaceutically active compound while suppressing cost without requiring a complicated process and a plurality of additives.SOLUTION: The present invention provides a bitterness suppressor for a pharmaceutically active compound, comprising a cyclodextrin and / or a derivative thereof as an active ingredient, wherein the pharmaceutically active compound is any one selected from the group consisting of duloxetine hydrochloride, aripiprazole, atomoxetine hydrochloride, donepezil hydrochloride, and dorzolamide hydrochloride.SELECTED DRAWING: None

To suppress bitter taste of a pharmaceutically active compound while suppressing cost without requiring a complicated process and a plurality of additives.SOLUTION: The present invention provides a bitterness suppressor for a pharmaceutically active compound, comprising a cyclodextrin and / or a derivative thereof as an active ingredient, wherein the pharmaceutically active compound is any one selected from the group consisting of duloxetine hydrochloride, aripiprazole, atomoxetine hydrochloride, donepezil hydrochloride, and dorzolamide hydrochloride.SELECTED DRAWING: None

The present disclosure is directed to a method of dose initiation for an aripiprazole treatment to a patient in need thereof; the patient is administered two, separate 100 to 500 mg injections of an aripiprazole intramuscular (IM) depot formulation at separate gluteal and / or deltoid injection sites, and a single dose of oral aripiprazole. The administration occurs on a first day of the treatment.