35 results about "Amlodipine" patented technology

Provided herein are stable amlodipine liquid formulations. Also provided herein are methods of using amlodipine liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).

The present invention provides a composition of nebivolol and amlodipine, comprising nebivolol, amlodipine and a pharmaceutical excipient. The nebivolol comprises one or more of nebivolol, a pharmaceutically acceptable salt thereof, and a solvate thereof. The amlodipine comprises one or more of amlodipine, a pharmaceutically acceptable salt thereof, and a solvate thereof. The pharmaceutical excipient is selected from one or more of a filler, a binder, a disintegrant, a lubricant, and a glidant. The composition does not contain a colorant and a film coating. The compound preparation of the present invention has good stability, and is beneficial to improving the antihypertensive efficacy, enhancing safety and tolerability, and reducing side effects. Compared to monotherapy, the present invention reduces the number of administered medications and improves the compliance of patients, is beneficial to improving the medication compliance of the elderly patients and individuals with dysphagia, maintains a stable plasma drug concentration, maintains long-term stable blood pressure in hypertensive patients, prevents the patients from discontinuing medication arbitrarily, and prevents disease recurrence and the progression of severe complications.

The present application provides a new application of a pharmaceutical composition containing an ARNi complex, and the new application is an application of the pharmaceutical composition containing the ARNi complex in the preparation of a medicine for treating a hypertension patient who is poorly controlled by amlodipine monotherapy.

The present invention relates to a method for producing (S)-amlodipine succinate comprising reacting (S)-amlodipine (D)-hemitartrate or a solvate thereof with a first base in the presence of a two-phase solvent system comprising a first non-polar organic solvent and water to produce (S)-amlodipine base, removing the water layer, and reacting (S)-amlodipine base with succinic acid to produce (S)-amlodipine succinate. The present invention also relates to a formulation comprising (S)-amlodipine succinate.

The utility model discloses a levamlodipine besylate tablet crusher, and particularly relates to the technical field of tablet processing, the levamlodipine besylate tablet crusher comprises a crushing cavity, the top of the crushing cavity is provided with a sealing cover in a threaded manner, the bottom of the crushing cavity is provided with a charging box in a threaded manner, the sealing cover is fixedly provided with a crushing motor, and the output end of the crushing motor is fixedly provided with a rotating shaft; a first smashing cutter and a second smashing cutter are arranged at the bottom of the rotating shaft, the second smashing cutter is located at the bottom of the first smashing cutter, a dust absorption structure is arranged on the surface of the sealing cover and located on one side of the smashing motor, the dust absorption structure comprises a treatment box, and the treatment box is located on one side of the smashing cavity. According to the levamlodipine besylate tablet crushing device, levamlodipine besylate tablets can be well crushed, generated dust can be absorbed and filtered in the crushing process, the situation that dust escapes in the environment and affects operators is avoided, and the whole levamlodipine besylate tablet crushing device is convenient to disassemble, assemble and maintain.

The invention provides a pharmaceutical composition. The pharmaceutical composition is prepared from amlodipine, empagliflozin, folic acid substances and a pharmaceutically acceptable carrier, wherein the amlodipine, the empagliflozin and the folic acid substances are in medicinal effective dose. The invention also provides application of the pharmaceutical composition in preparation of medicines for treating lower limb artery occlusion diseases.

The invention belongs to the technical field of pharmaceutical preparations, and relates to a levoamlodipine folic acid compound tablet and a preparation process thereof, and the preparation process comprises the following steps: mixing microcrystalline cellulose with vitamin C, and enabling nitrite in the microcrystalline cellulose to be in full contact with the vitamin C to obtain a first mixture; mixing folic acid with part of the first mixture to obtain a second mixture; mixing levamlodipine besylate with the remaining first mixture to obtain a third mixture; and uniformly mixing the second mixture, the third mixture and other auxiliary materials, and tabletting to obtain the tablet. The method comprises the following steps: reacting microcrystalline cellulose with vitamin C to consume nitrite in the microcrystalline cellulose so as to prevent the nitrite from reacting with secondary amino in levamlodipine to generate nitrosamine impurities with genetic toxicity;

A pharmaceutical composition comprising azilsartan medoxomil potassium and a calcium channel blocker, a method for preparing same, and use thereof are provided. Azilsartan medoxomil potassium and the calcium channel blocker are formulated into a compound formulation, thus improving the blood pressure lowering efficacy, improving safety and tolerability, and reducing adverse effects. Azilsartan medoxomil potassium can ameliorate peripheral edema caused by amlodipine by means of expanding peripheral venous vessels, while amlodipine can ameliorate adverse effects such as vasogenic edema, dry cough, and the like caused by azilsartan medoxomil potassium.

The application relates to application of a dihydropyridine compound or a salt thereof in preparation of a medicine for preventing and / or treating HPV infection, and belongs to the technical field of medicines and pharmaceutical preparations. The application provides application of the dihydropyridine compound or the salt thereof in preparation of the medicine for preventing and / or treating HPV infection, wherein the dihydropyridine compound is selected from one or more of nifedipine, amlodipine, lercanidipine, nimodipine, nitrendipine, nisoldipine, felodipine, benidipine, lacidipine and azelnidipine. The application scheme first reports the application of the dihydropyridine compound or the salt thereof in prevention and / or treatment of HPV, and in-vitro cell experiments are carried out through azelnidipine in the dihydropyridine compound, and further, the inhibiting effect of the dihydropyridine compound on HPV virus is verified through medicine administration of a mouse intradermal virus inoculation model and medicine administration of a mouse vaginal virus inoculation model.

This invention discloses an extracellular vesicle derived from Gastrodia elata, its preparation method, and its use in preparing drugs for treating glaucoma, belonging to the field of biomedical technology. This invention claims protection for an extracellular vesicle prepared from dried Gastrodia elata. The extracellular vesicles provided by this invention have no significant cytotoxicity and good biocompatibility. Studies have shown that these extracellular vesicles can significantly inhibit apoptosis of R28 cells and loss of Brn3a⁺ cells in the mouse retina in a glutamate excitotoxicity model. In a glaucoma model, these extracellular vesicles can effectively protect the survival of retinal ganglion cells (RGCs) and retinal function, and can significantly reduce retinal neuroinflammatory responses in the glaucoma model. Therefore, the extracellular vesicles provided by this invention have a clear anti-glaucoma-related retinal damage effect and possess great potential for development into drugs for treating glaucoma.

Disclosed herein is a liquid pharmaceutical formulation substantially free of water, comprising: (i) amlodipine or a pharmaceutically acceptable salt thereof, (ii) at least one pharmaceutically acceptable excipient, and (iii) a sufficient amount of a vehicle comprising glycerin. Also disclosed herein is a liquid pharmaceutical formulation substantially free of water and ethanol, comprising: (i) amlodipine or a pharmaceutically acceptable salt thereof, (ii) at least one pharmaceutically acceptable excipient, and (iii) a sufficient amount of a vehicle comprising glycerin.

An orally disintegrating tablet of amlodipine for oral administration comprising: a) amlodipine or pharmaceutically acceptable salts thereof, is present in an amount ranging from 2 to 10% w / w; b) at least one diluent; c) at least one disintegrant is present in the range from 1 to 10% w / w; d) at least one lubricant is present in the range from 0.2 to 7% w / w; e) at least one non-nutritive sweetener is present in the range from 0.1 to 7% w / w; f) at least one or more pharmaceutically acceptable excipients; wherein the ratio of combination of diluents to disintegrant is in the range from 15:1 to 40:1; and wherein orally disintegrating tablet is stable for at least three months under storage conditions of 25°C / 60% RH and 40°C / 75% RH.

This invention relates to a bisoprolol amlodipine tablet and its preparation method, belonging to the field of pharmaceutical formulation technology. The bisoprolol amlodipine tablet of this invention comprises bisoprolol fumarate, amlodipine besylate, chitosan, guanidinoacetic acid, maltodextrin, and pharmaceutically acceptable excipients. This invention utilizes the synergistic effect of chitosan, guanidinoacetic acid, and maltodextrin to form a stable physical barrier layer between the two active ingredients, effectively inhibiting the formation of the addition impurity AML-2, significantly improving the stability of the formulation, and the process is simple and suitable for industrial production.

The invention provides a nebivolol and amlodipine composition. The nebivolol and amlodipine composition is prepared from nebivolol, amlodipine and medicine auxiliary materials, the nebivolol comprises one or more of nebivolol, a pharmaceutically acceptable salt of nebivolol and a solvate of nebivolol; the amlodipine comprises one or more of amlodipine, pharmaceutically acceptable salts and solvates of amlodipine; the medicine auxiliary material is selected from one or more of a filling agent, an adhesive, a disintegrating agent, a lubricating agent and a flow aid; the composition is free of colorants and coating films. The compound preparation disclosed by the invention is good in stability, and beneficial to improving the antihypertensive effect, improving the safety tolerance and reducing the side effect. Compared with a single medicine, the medicine taking quantity is reduced, and the compliance of a patient is improved; for old people or people with dysphagia, the medicine taking compliance can be improved; the blood pressure of a hypertensive patient is maintained to be stable for a long time, the patient is prevented from randomly interrupting medication, and disease recurrence and malignant complication development are prevented.

This invention belongs to the field of compound synthesis technology, specifically relating to a diarylguanidine derivative with anti-lymphoma function, its preparation method, and its application. The chemical name of this diarylguanidine derivative is 3-ethyl-5-methyl-(E)-4-(2-chlorophenyl)-6-methyl-2-((2-(2-(3-phenoxyphenyl)-3-phenylguanidinyl)ethoxy)methyl)-1,4-dihydropyridine-3,5-dicarboxylic acid ester. The preparation method includes step 1: reacting phenol and 4-bromonitrobenzene in DMF solution to obtain 4-nitrodiphenyl ether compounds; step 2: placing the 4-nitrodiphenyl ether compounds in an iron-containing ethanol solution to obtain 4-aminodiphenyl ether compounds; step 3: placing the 4-aminodiphenyl ether compounds and phenyl thioisocyanate in tetrahydrofuran solution to react and obtain 1-(4-phenoxyphenyl)-3-phenylurea compounds; and step 4: reacting the 1-(4-phenoxyphenyl)-3-phenylurea compounds with amlodipine under light irradiation to obtain the target compound. The product of this invention is intended for use in the preparation of anti-lymphoma drugs.

The present disclosure provides a novel lyophilized amlodipine composition that forms an oral solution almost immediately upon mixing with an aqueous diluent when in use. The disclosed lyophilized amlodipine compositions can be stable at room temperature for at least 12-24 months and do not require refrigeration during its transportation, storage, use and its shelf life. Furthermore, the disclosed lyophilized amlodipine compositions are free of any alcohol and / or sodium benzoate that is detrimental to young children (e.g., children less than 6 years old, including infants and neonates) and other vulnerable patient populations. In addition, an oral solution redissolved by the disclosed freeze-dried amlodipine composition does not have the risk of potential dose non-uniformity caused by amlodipine suspension drug sedimentation.

The invention discloses a pharmaceutical composition for treating cardiovascular diseases as well as a preparation method and application thereof, and the composition comprises perindopril or pharmaceutically acceptable salt thereof, amlodipine or pharmaceutically acceptable salt thereof and amino-modified silicon dioxide, the amino modified silicon dioxide is prepared by modifying the surface of silicon dioxide by using 3-aminopropyltriethoxysilane as a coupling agent. The composition provided by the invention can keep stable storage under the condition of not adding an antioxidant, especially can avoid or reduce impurities generated by oxidative degradation of perindopril and amlodipine, and improves the safety of the medicine.

A biodegradable bio-scaffold patch for topical application, consisting of a porous chitosan alginate layer and a poly(lactic acid) carrier layer, wherein the porous layer encapsulates an active ingredient selected from amlodipine, nifedipine or prazosin, and the patch is configured to allow controlled release onto the skin over varicose veins.

Disclosed are an amlodipine drug targeted delivery system and a preparation method therefor. The targeted delivery system can improve the targeting property of amlodipine in preventing hepatic ischemia-reperfusion injury and is simple to prepare, highly feasible, and highly practical. The amlodipine drug targeted delivery system (Am@EXOs) prepared in the present invention enables a targeted distribution of amlodipine in the livers of hepatic ischemia-reperfusion injury model mice and precise inhibition of calcium ion overload within hepatocytes by means of a minimum dose of amlodipine, thereby reducing cell injury, improving the targeting property of amlodipine in preventing hepatic ischemia-reperfusion injury, and reducing the cost of using amlodipine.

1. The name of the design product: medicine packaging box (Beihuida). 2. The use of the design product: for packaging and storing medicines. 3. The design points of the design product: the combination of shape and pattern. 4. The picture or photo that best indicates the design points: Design 1 perspective view 1. 5. Design 1 is designated as the basic design. 6. Other circumstances that need to be explained: Design 1 is the packaging box of amlodipine besylate bisoprolol fumarate tablets (I) 14 tablets, design 2 is the packaging box of amlodipine besylate bisoprolol fumarate tablets (I) 7 tablets, design 3 is the packaging box of amlodipine besylate bisoprolol fumarate tablets (II) 14 tablets, and design 4 is the packaging box of amlodipine besylate bisoprolol fumarate tablets (II) 7 tablets.

Provided is a nebivolol and amlodipine composition, which comprises nebivolol and amlodipine. The nebivolol comprises one or more of nebivolol, a pharmaceutically acceptable salt thereof, and a solvate thereof. The amlodipine comprises one or more of amlodipine, a pharmaceutically acceptable salt thereof, and a solvate thereof. A nebivolol and amlodipine compound preparation is beneficial to improving the blood pressure reduction effect, improving the safety and tolerance, and reducing side effects. Compared with single medicines of nebivolol and amlodipine, the combination of nebivolol and amlodipine has the advantages that: the number of medicines taken is reduced, and the compliance of a patient is improved; the medicine-taking compliance of old people or people with dysphagia can be facilitated; a plasma concentration in vivo is maintained to be stable, the blood pressure of a hypertension patient is maintained to be stable for a long time, and the side effects of the single medicines are reduced; and it is avoided that a patient stops taking medicine at will, and disease recurrence and progression of malignant complications are prevented.

The invention discloses a method for detecting N-nitroso bisoprolol impurities in bisoprolol amlodipine tablets, and belongs to the field of drug impurity detection. The method comprises the following steps: preparing a reference substance solution and a test sample aqueous solution (ultrasonic dispersion and constant volume centrifugation), and then detecting by adopting HPLC-MS / MS: a chromatographic column is a C18 column (the particle size is 2-3 microns, the inner diameter is 2.1-4.6 mm, and the length is 100-250 mm), a mobile phase contains 0.1-0.5% of formic acid, 5-20 mM of an ammonium acetate aqueous solution and methanol / acetonitrile, and gradient elution is carried out; the mass spectrum is in an ESI positive ion mode, MRM scanning is carried out, and characteristic ion pairs (parent ions 372 + / -1amu, daughter ions 145 + / -1amu and the like) are monitored. The method is simple and convenient in pretreatment, environment-friendly in solvent, high in sensitivity and good in durability, trace impurities can be accurately detected, and reliable support is provided for quality control of bisoprolol amlodipine tablets.

According to the tablet containing the arginine perindopril and the levamlodipine besylate and the preparation method of the tablet, the pregelatinized starch and microcrystalline cellulose colloidal silicon dioxide co-treated substance is used as a filling agent, and the proportion of the pregelatinized starch and the microcrystalline cellulose colloidal silicon dioxide co-treated substance is controlled, so that the tablet containing the arginine perindopril and the levamlodipine besylate is prepared. The problem that the fluidity of the tablet is poor in preparation is solved, the stability is remarkably improved, the tablet has the advantages of being simple in preparation method, low in cost, good in fluidity, good in compressibility and the like, meanwhile, the tablet shows rapid disintegration, dissolution and stability, and the tablet is suitable for large-scale industrial production.

The invention discloses an arginine perindopril solid dispersion and a compound preparation thereof, and belongs to the technical field of pharmaceutical preparations. The arginine perindopril solid dispersion provided by the invention is prepared from the following components in parts by mass: 1 part of arginine perindopril, 0.1 to 0.3 part of calcium acetate and 5.2 to 5.4 parts of microcrystalline cellulose. The arginine perindopril solid dispersion and the compound perindopril amlodipine tablet prepared from the arginine perindopril solid dispersion have excellent stability, the preparation methods of the arginine perindopril solid dispersion and the compound perindopril amlodipine tablet are simple to operate, actual production is facilitated, and a drying agent can be prevented from being used during preparation packaging.

The invention discloses a method for instantly detecting the concentration of an antihypertensive drug in plasma based on a miniature mass spectrometer, the antihypertensive drug is an amlodipine and benazepril compound drug, and the detection method comprises the following steps: S1, adding a standard substance into a blank sample to obtain a standard plasma sample with a series of concentrations, processing and analyzing the standard plasma sample according to the steps S2 and S3 to obtain a standard curve; s2, adding an acetonitrile-water solution into a to-be-detected plasma sample, extracting with diethyl ether, and centrifuging to take an upper-layer organic phase; drying the upper-layer organic phase by blowing nitrogen, and dissolving residues by using an acetonitrile-water solution to obtain a blood sample; s3, the blood sample is injected in a paper capillary spraying mode, and scanning is performed in two sequences in a positive ion scanning mode; and S4, substituting the detection result of the blood sample into the standard curve to obtain the content of amlodipine and benazepril antihypertensive drugs in the blood sample. The method has the characteristic that the amlodipine and the benazepril can be effectively and quickly detected at one time at the same time.

The invention discloses a preparation method of phthaloyl amlodipine, and belongs to the technical field of chemical synthesis of medicines. In order to solve the problems of more byproducts, low intermediate purity, high cost and the like in the existing process, a process route is constructed by adopting a step-by-step convergent cyclization thought, and a four-step continuous reaction route is designed; comprising the following steps: carrying out negative pressure dehydration synthesis on high-purity N-(2-ethoxyl) phthalimide, carrying out etherification reaction under low temperature, inert gas protection and an anhydrous system, carrying out condensation reaction under reflux water separation, and carrying out Michael addition-closed-loop cyclization reaction, so as to prepare the high-purity phthaloyl amlodipine with the melting point of 149-150 DEG C; by optimizing the raw material ratio and process parameters in the reaction process, the production cost is remarkably reduced, and a high-stability raw material is provided for producing amlodipine.

The invention relates to the technical field of material mixing, in particular to an amlodipine intermediate reaction device and a using method thereof.The amlodipine intermediate reaction device comprises two mounting seats with vibration reduction structures, mounting holes and an air pump, the mounting holes are formed in one sides of the two mounting seats, and a first bonding packaging plate and a second bonding packaging plate are mounted between the mounting seats; the second bonding packaging plate comprises a second plate body, a plurality of parallel airflow channels are formed in the inner side of one end of the second plate body, a plurality of vibration assemblies are installed in the airflow channels, the upper end and the lower end of the second plate body are provided with an air inlet pipe and an exhaust pipe which are used for being communicated with the airflow channels respectively, and the other end of the air inlet pipe is connected with an air supply port of an air pump; the other end of the exhaust pipe is mounted at the upper end of the liquid collecting component through a fixing piece; the liquid collecting assembly comprises a liquid collecting box. According to the invention, the interior of the liquid collection box is always in a negative pressure state, and liquid discharge is assisted, so that liquid discharge is smoother, and the solid content gt in the microreactor is effectively avoided; and therefore, the problem of channel blockage is solved.

The present application provides a new application of a compound pharmaceutical composition of an ARNi complex and amlodipine, and the new application is an application of a pharmaceutical composition containing an ARNi complex in the preparation of a medicine for treating hypertensive patients who are poorly controlled by ARNi monotherapy.

The present invention relates to a composition comprising levamlodipine besylate hydrate and its production, pharmaceutical preparations and use, especially the composition of (S)-2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylic acid-3-ethyl ester, 5-methyl ester benzenesulfonic acid hydrate and its production method and use. The composition of levamlodipine besylate crystallized in pure water and dried is easy for industrial production, has no organic solvent residue, good thermal stability and good dissolution amount in solid-form preparations.

The present invention provides aceclofenac, amlodipine or doxazosin, or a pharmaceutically acceptable salt or solvate thereof, for use in the treatment or prophylaxis of Attention Deficit / Hyperactivity Disorder (ADHD). The invention also provides kits and methods for the treatment or prophylaxis of ADHD.