68 results about "Nitrendipine" patented technology

A transdermal formulation of dihydropyridine calcium antagonists and specifically nifedipine, nimodipine and nitrendipine. The calcium antagonists are dispersed in a mixed liquid. The mixed liquid comprises varying mole fractions of cis-oleic acid and dimethylisosorbide dispersed in a polypropylene glycol base.

The invention provides a pharmaceutical composition which comprises calcium channel blockers of a medicinal dose, angiotensin II receptor antagonists of a medicinal dose, one or more of B vitamins of a medicinal dose and pharmaceutically acceptable carriers, wherein the calcium channel blockers are selected from amlodipine, felodipine, israbipine, nicardipine, nifedipine, nisoldipine, nitrendipine, lacidipine, diltiazem or verapamil; the angiotensin II receptor antagonists are selected from candesartan, telmisartan, losartan, valsartan, irbesartan, eprosartan, tasosartan or olmesartan; and the B vitamins are selected from one or more of vitamin B6, vitamin B12, folic acid and calcium leucovorin. The pharmaceutical composition of the invention can improve the curative effect of the hypotensor, enhance the target organ protecting action of the hypotensor, and reduce the morbidity of complications of angina, myocardial infarction and the like.

A self-microemulsified softcapsule of nimodipine or nitrendipine is prepared from nimodipine or nitrendipine, coemulsifier, self emulsifier, oil and antioxidizing agent through proportionally mixing nimodipine or nitrendipine, coemulsifier and self emulsifier, constant-temp oscillating, adding oil and antioxidizing agent, stirring, cooling, and shaping.

The invention relates to a pharmaceutical composition containing a calcium channel blocker (CCB) or the mixture thereof, an angiotonin 3II receptor blocker (ARB) or the mixture thereof, statins or the mixture thereof and a pharmaceutically acceptable carrier, wherein the CCB is selected from l-amlodipine, amlodipine, lacidipine, nitrendipine or the mixture thereof; the angiotonin II receptor blocker is selected from telmisartan, losartan, irbesartan, candesartan or the mixture thereof; and the statins are selected from atorvastatin, simvastatin, ruishufatadine, fluvastatin or the mixture thereof. The pharmaceutical composition is used for treating various high blood pressures and preventing or treating cardiovascular and cerebrovascular diseases relevant to the hypertension, reduces the disease rate and / or mortality rate of the cardiovascular and cerebrovascular diseases and also improves the adaptability for a sufferer taking medicine.

The present invention provides one new kind of compound blood pressure reducing preparation containing angiotonin converzyme inhibitor, calcium ion agonist, Estazolam and pharmaceutically acceptable carrier. The angiotonin converzyme inhibitor is selected from Enalapril, Ramipril, Benalapril, Lisinopril, Acertil, etc. as well as their mixture; and the calcium ion agonist is selected from Nitrendpine, Amlodipine Besylate, Nifedipine, Felodipine, etc. as well as their mixture. The present invention utilizes the synergistic effect between different medicines to raise the blood pressure lowering effect, reduce side effect and improve the compliance of patient.

An oral disintegrating tablet for nisoldipine for treating coronary heart disease, hypertension, ischemic heart disease and congestive heart failure is prepared from nisoldipine, souring agnet, excipient and disintegrant.

The invention relates to a double layer slow release preparation for containing Nitrendipine, wherein the Nitrendipine double layer tablet can be prepared by double layer tablet compressing machine, or in the form of tablet using slow release medicament as core, or quick release medicament as outer layer clothing sheet, or in the form of capsule comprising quick release and slow release microcapsule and micro-balloons, or other preparation formed comprising the two portions of quick release and slow release medicament, wherein the weight ratio of the quick release medicament and slow release medicament is from 1:1 to 1:10, the advantages of the preparation are quick effect, long maintaining time, ideal hypertension effect and low price.

The invention relates to a nitrendipine self-microemulsifying soft capsule used for treating hypertension, and a preparation method thereof. The preparation method comprises the steps of: taking gelatin, putting the gelatin in a mixed solution of glycerin, sorbic alcohol and water for swelling, adding ethylparaben, heating the mixed solution till the gelatin is dissolved, adding titanium dioxide and a pigment into the mixed solution, resting the mixed solution for defoaming after being evenly stirred and sieved, screening the mixed solution for standby; evenly mixing nitrendipine, an emulsification auxiliary agent, an oil phase and an emulsifier and heating and stirring to form a clear solution of contents of the capsule; pressing the capsule shell fluid and the contents into soft capsules by a rotational mold pill press; and after the steps of drying and surface processing, obtaining the finished products of the soft capsules. The nitrendipine self-microemulsifying soft capsule can improve the bioavailability of the nitrendipine and perform clinical effects more safely and effectively. The preparation method is relatively simple, has no special requirements for equipment, can be realized on most production lines of the soft capsules, is easy to be accepted by production departments and manufacturers and has low manufacturing cost, thus having broad prospect of clinical application.

A medicine for treating hypertension is prepared from cinnamon bark, wild jujube, and beta receptor paralyzer, or diuretic, or calcium antagon, angiotonin converzyme depressant and angiotonin II receptor antagon.

The invention relates to a medicament compound of an atenolol / nitrendipine / folacin compound, and usages thereof. The invention belongs to the technical field of pharmacy. The medicament compound contains the atenolol of theriacal dosage, the nitrendipine of theriacal dosage, the folacin compound of theriacal dosage and a vector acceptable on pharmacy. The dosage of the atenolol is 5 to 50mg; the dosage of the nitrendipine is 3 to 30mg; and the dosage of the folacin compound is 0.2 to 1.6mg. The invention has the advantages that the medicament compound enhances the curative effect of pressure reduction, prolongs the lasting time of pressure reduction and removes the side effect of quickening the cardiac rate of the reflectivity of the nitrendipine in the compound by the multi-target spot cooperative pressure reduction effect; more importantly, the medicament compound can effectively prevent, cure or ease a plurality of complicating diseases of hypertension and cardiovascular and cerebrovascular diseasesin such as stroke and the like by double target spots (Hcy, blood pressure) on the foundation of reducing the side effects. Moreover, the medicament compound can lead a sufferer to be convenient to take the medicine.

The invention relates to a medicine for treating chilblain. The medicine is prepared by taking pearl cream, Vaseline, starch, talcum powder or distilled water as a substrate and preparing following raw medicines into an ointment or liquid according to mass percentage: 0.1-5% of anisodamine and 0.1-5% of nitrendipine. With the adoption of the medicine for treating the chilblain, the anisodamine is taken as a blood vessel active medicine and has an expansion functions on arterioles, venule and blood capillaries, so that microcirculation can be improved; the nitrendipine is used as a calcium ion antagonist and has a selective expansion function on the venule of the peripheral blood vessels; and the anisodamine and nitrendipine are combined to have obvious improvement on blood supply of a chilblain part, so as to have the effect of preventing and treating the chilblain.

The invention relates to a controlled release formulation for constant speed releasing Nitrendipine, wherein the medicament is released at a constant speed, and the blood medicament concentration waves smoothly. The release sheet is a single-chamber infiltration pump comprising the two portions of a powder core containing Nitrendipine and preparation formed by semipermeable membrane with minipores and having permeability only for small molecules such as that of water (mg / part), Nitrendipine 10-50, osmoregulation agent 3-80, propelling agent 1-50, bonding agent 1-20, right amount of lubricating agent, while the semipermeable membrane comprises semi-permeable membrane material 1-50 and aperture making agent 1-50. The invention can realize constant speed release, thus achieving the goal of smooth hypertension.

The invention belongs to the field of drug synthesis, and particularly relates to a preparation method of nitrendipine. The preparation method is characterized by including following steps: (1), allowing 3-nitrobenzylidene ethyl acetoacetate intermediate and 3-aminomethyl crotonate according to a molar ratio of 1:1-1.1 to react at 70-75 DEG C in advance; (2), adding concentrated hydrochloric acidinto a reaction system of the step (1), and allowing reaction at 70-75 DEG C after adding is completed, wherein adding amount of the concentrated hydrochloric acid is 10-15% of molar weight of the 3-nitrobenzylidene ethyl acetoacetate intermediate; (3), cooling to 15-20 DEG C after reaction in the step (2) is completed, continuing reaction, and performing solid-liquid separation and recrystallization to obtain nitrendipine. Through process control, content of ester exchange impurities can be lowered effectively, and product yield can be increased.

The invention relates to the field of pharmaceutical pharmacy, and discloses a nitrendipine soft capsule. The soft capsule consists of contents and a capsule shell, wherein the contents comprise nitrendipine, polyethylene glycol, a solubilizer and glycerol in a mass ratio of 1:(10000-200000):(500-80000):(500-80000). In the nitrendipine soft capsule, polyethylene glycol is used as a solvent of nitrendipine, and the solubilizer and a water absorption resistant component glycerol are added to form the contents of the nitrendipine solution type soft capsule. Nitrendipine exists in the soft capsule in a solution mode and can be taken conveniently, after the capsule shell is disintegrated, nitrendipine can be directly absorbed without being re-emulsified in a body, has higher dissolution rate, and is more direct, quicker and more effective. Meanwhile, the defect of large difference in curative effect caused by imbalanced dissolution and large body difference can be solved effectively, and the bioavailability is improved, and the curative effect is stable.

The invention relates to a controlled release formulation for constant speed releasing Nitrendipine, which comprises Nitrendipine powder core and release control bone matrix and auxiliary materials, wherein the powder core is Nitrendipine, the release control bone matrix is macromolecular polysaccharides and their derivative, the essential constituents of the auxiliary materials are phosphate, aliphatic acid and its salt, the proportion of the Nitrendipine ingredients is, basic remedy : release control bone matrix : phosphate : aliphatic acid and its salt = 1:0.5-7.0:0.1-2.0:1-2.0, the invention can realize constant speed release, thus achieving the goal of smooth hypertension.

The invention relates to a synthetic method of nitrendipine. The synthetic method comprises the following steps that a reactant is subjected to a heating reaction in a reactive solvent to synthesize the nitrendipine; cooling is carried out after the reaction, the nitrendipine is filtered and dried, and the reactive solvent is recovered, wherein the reactive solvent is acetonitrile. The synthetic method of the nitrendipine has the advantages that the reactive solvent nitrendipine free of an esterification reaction with the product is utilized, thereby avoiding the generation of impurities in the synthetic process, and improving the product purity of the synthetic reaction; the impurities generated during the reaction are dissolved in the reactive solvent, the nitrendipine is precipitated through cooling, and the impurities cannot be precipitated, thereby playing a role of purifying the synthetic nitrendipine; the reactive solvent nitrendipine can be purified through various methods, andthe reactive solvent nitrendipine can be still used as a reactive solvent after purification, thereby reducing the synthetic cost.

The invention discloses a sustained-release drug composite containing nitrendipine, which is composed of nitrendipine with effective dose and accessories accepted physiologically; the nitrendipine sustained-release drug composite can release the nitrendipine in a sustained way, the food effect is reduced and the bioavailability is increased.

The invention provides a preparation method of high-purity nitrendipine. The preparation method is characterized by comprising the following steps that (1) ethyl 2-(m-nitrobenzylidene)-acetoacetate, methyl 3-aminocrotonate and a solvent are added into a reaction flask, and temperature increasing for a reaction is conducted; (2) the solvent is evaporated to dryness in a pressure reduction mode, andgradual temperature increasing for a reaction is conducted till reaction liquid is solidified; (3) after the reaction liquid is solidified, the temperature and the reaction time are controlled, and thus a nitrendipine crude product is obtained; and (4) a solvent is added for backflow, the temperature is decreased to be the room temperature, and staying overnight, filtering, washing and drying areconducted to obtain a nitrendipine refined product. According to the preparation method, the reactions are conducted in segments, the problem that impurities are continuously increased along with thereactions is solved, all the impurities contained in the nitrendipine meet pharmacopoeia standard requirements, and the impurity level is significantly lower than that of other factories in China.

The present invention discloses one kind of nitrendipine dripping pill and its preparation process. The nitrendipine dripping pill is compounded with nitrendipine and dripping pill matrix. The present invention has high bioavailability, high stability, convenient taking, fast disintegration and dissolving, high leaching degree, fast medicine releasing, fast acting, simple production process, low cost and other features.

The invention provides a method and kit for guiding medication of nitrendipine. The method comprises steps as follows: multiplex amplification primers and an extension primer are designed respectivelyaccording to two to-be-detected target SNP sites; a multiplex amplification primer reaction system and an extension primer reaction system are prepared; in the reaction systems, an amplification reaction and a single base extension reaction are performed on the two target SNP sites respectively by using multiple sets of primers; products obtained by the single base extension reaction are subjected to time-of-flight mass spectrometry analysis, according to extension primer products with different molecular weights and represented by mass spectrum peaks, genotypes of different SNPs related to drug metabolism are identified, and medication of the nitrendipine drug for reducing high blood pressure is guided. Besides, the invention also provides a detection kit using the method. The kit can detect two SNP sites related to metabolism of the nitrendipine drug for reducing high blood pressure simultaneously and has the advantages that the kit is low in cost, doesn't need synthesis probe, takes short time and is simple and convenient in result analysis and very broad in application field.

A process for synthesizing the simple optical isomer nitrendipine features that under existance of quinine-ammonium benzylbromide as chiral phase-transfer catalyst, 2-(3-nitrobenzilidene) ethyl acetylacetate and beta-methyl amino crotonate take part in stereoselective condensating reaction in absolute alcohol to obtain target product.

A dripping pill of nitrendipine for treating hypertension is proportionally prepared from nitrendipine and the matrix chosen from polyethanediol 4000, 6000 or 10000, stearic acid, sodium stearate, poloxamer, glycerin gelatin, monoglyceride stearate, shellac and polyoxyvinyl monostearate through thermally fusing said matrix, mixing it with nitrendipine, dripping in condensing agent, removing the condensing agent from their surface, drying in air and packing.

The invention relates to a fast sieving method for a dihydropyridine blood-pressure lowering compound mixed in a Chinese medicinal herb blood-pressure lowering product. The fast sieving method comprises the following steps of: (1) sampling, crushing, adding acetone-ethanol solution with volume ratio to a sample of equal to 5 : 1 and mass of 5 times to 10 times of the sample, shaking for dissolution, filtering and keeping filtering solution; (2) taking out 1ml of the filtering solution obtained from step (1), adding with 3 drops to 5 drops of potassium hydroxide-ethanol solution with mass concentration of equal to 2 percent to 3 percent, shaking evening and observing the change of color; in the case that the solution is changed into reddish-brown, which shows the dihydropyridine blood-pressure reducing compound is doped in the sample; and the dihydropyridine blood-pressure reducing compound is one or more than two of nifedipine, nitrendipine and nimodipine. The invention also disclosesa special kit for applying the method and the kit comprises the acetone-ethanol solution with volume ratio of 5 to 1 and the potassium hydroxide-ethanol solution with mass concentration of equal to 2percent to 3 percent. The sieving method is characterized by fastness, low cost, simple operation and the like.

The invention provides a detection product for judging individualized medication type of nitrendipine. A preparation method comprises steps as follows: multiplex amplification primers and an extensionprimer are designed separately according to two to-be-detected target SNP sites; a multiplex amplification primer reaction system and an extension primer reaction system are prepared; in the reactionsystems, an amplification reaction and a single base extension reaction are performed on the two target SNP sites respectively by using multiple sets of primers; products obtained by the single baseextension reaction are subjected to time-of-flight mass spectrometry, according to extension primer products with different molecular weights and represented by mass spectrum peaks, genotypes of different SNPs related to drug metabolism are identified, and individualized medication of the nitrendipine drug for reducing high blood pressure is guided. The detection product can detect two SNP sites related to metabolism of the nitrendipine simultaneously and has the advantages that the detection product is low in cost, doesn't need probe synthesis, takes short time and is simple and convenient inresult analysis and very broad in application field.

The invention discloses an amlodipine hapten, an amlodipine artificial antigen, an amlodipine antibody as well as a preparation method and an application thereof, amlodipine hapten ANSSA is firstly prepared, the amlodipine artificial antigen and the amlodipine polyclonal antibody are obtained by applying the hapten. The antibody has high sensitivity and high specificity recognition capability on amlodipine, the half inhibition concentration is 0.31 mu g / kg, the quantitative detection range is 0.04758-2.078 mu g / kg, the detection limit is 0.085 mu g / kg, and the cross reaction rate on felodipineand nitrendipine is lower than 1%. Besides, a colloidal gold immunochromatography technology is established by utilizing the amlodipine antibody, the colloidal gold immunochromatography technology has a wide detection range and high sensitivity, detection of amlodipine can be specifically recognized, the visual detection line is 20 ng / mL, and the colloidal gold immunochromatography technology hasa great application prospect in immune rapid detection of amlodipine in health-care food.

The invention discloses a method for carrying out mass-spectrography differentiation on nitrendipine individualized medication through a detection product. The method comprises the following steps of:according to two target SNP (single nucleotide polymorphism) sites to be detected, independently designing multiplex amplification primers and an extension primer; preparing a multiplex amplificationprimer reaction system and an extension primer reaction system; in the reaction systems, adopting multiple sets of primers to simultaneously independently carry out an amplification reaction and a single base extension reaction on the two target SNP sites; carrying out time-of-flight mass spectrometry analysis on products obtained by the single base extension reaction; according to extension primer products with different molecular weights and represented by mass spectrometry peaks, identifying the genotypes of different SNPs related to medicine metabolism; and guiding the individualized medication of a hypertension-reducing medicine, i.e., nitrendipine. The method can simultaneously detect the two SNP sites related to nitrendipin metabolism, has the advantages of low cost, short time consumption and an extremely wide application field and does not need to carry out probe synthesis, and result analysis is simple and convenient.

The invention provides a nitrendipine tablet and a preparation method thereof. The nitrendipine tablet is prepared from nitrendipine, lactose, microcrystalline cellulose, sodium carboxymethyl starch,a binding agent, magnesium stearate and the like. Through control of the particle size of raw materials, selection of concentration of a binding agent povidone K30 and a solvent precipitant ethanol, control of the parameters of the drying temperature, the tabletting pressure and the like, the quality of the nitrendipine tablet is stable, but also the requirement is conformed, meanwhile, the dissolution curve in four media is consistent with a raw research product, and the situation that the nitrendipine tablet has the same efficacy with the raw research product is guaranteed.

The invention discloses a method for preparing nitrendipine impurities. The method comprises the following steps that 2-(benzyl(methyl)amino)ethanol, diketene and base are heated in a first solvent to40DEG C-70DEG C for reaction for 30 minute-2 hour, and an intermediate acetoacetate 2-(N-methyl-N-benzylamino)ethyl ester is obtained after reaction concentration; and the intermediate acetoacetate 2-(N-methyl-N-benzylamino)ethyl ester and m-nitrobenzaldehyde are added to a second solvent, ammonia water is added, a heating reflux reaction is performed for 1 hour-16 hour, cooling and then concentration are performed, and the nitrendipine impurities are obtained by a predetermined method. According to the method for preparing the nitrendipine impurities, convenience is provided for impurity analysis and research of nitrendipine bulk drugs and a preparation thereof, and a detection method and a determination basis are provided for the production and drug safety of nitrendipine.

The invention provides a detection product for mass-spectrometry identification of personalized medication of nitrendipine through a primer composition. A preparation method of the detection product includes the steps of: designing multiple-amplification primers and extension primers separately according to two to-be-detected target SNP sites, preparing a multiple amplification primer reaction system and an extension primer reaction system, performing amplification and single-base extension reactions on the two target SNP sites simultaneously through multiple sets of primers in the reaction systems, performing time-of-flight mass spectrometry analysis on products obtained after the single-base extension reactions, identifying the genotypes of different SNPs related to metabolism of the drug according to extension primer products which are represented by mass spectrum peaks and have different molecular weights, and guiding personalized medication of the antihypertensive drug nitrendipine. The two SNP sites related to metabolism of the nitrendipine drug can be detected simultaneously, and the product has the advantages of low cost, no needs for synthetic probes, short time consumption, simple and convenient result analysis and extremely wide application fields.