55 results about "Azelnidipine" patented technology

The invention relates to a preparation method of alpha crystalline azelnidipine, which comprises the following steps that: converting an azelnidipine crude product into azelnidipine methylate; then uniformly dispersing the azelnidipine methylate in normal heptane solvent; heating, decompressing, distilling and removing the solvent; and obtaining the medicinal alpha crystalline azelnidipine by cooling, filtering, drying and the like through common methods. The method for preparing the medicinal alpha crystalline azelnidipine has the advantages of simple operation, high yield, high purity and low cost, and the yield of the alpha crystalline azelnidipine prepared by the method is about 95 percent (by the azelnidipine methylate) and the purity HPLC content thereof is more than 99.5 percent.

The invention discloses a preparation method of Azelnidipine of alpha crystal form, wherein, Azelnidipine of non-alpha crystal forms is completely dissolved in a two-phase organic solvent. Water-bath is heated to certain temperature and alkane and seed crystal are added into the solution under a stirring condition. A crystal is separated out by cooling and a separated crystal product is collected, namely the Azelnidipine of alpha crystal form. The two-phase organic solvent comprises two components: low boiling point esters and benzene or derivatives of benzene, with a volume ratio of 1 to 3:15. The preparation method has one-time yield up to 85 percent to 90 percent, purity of more than 99.5 percent as well as good appearance and quality. The preparation method has easily recycled organic solvent, is beneficial to environmental protection, reduces loss in Azelnidipine and/or waste in the organic solvent, greatly reduces the production costs of products and has prospect of large-scale industrialized production.

A pharmaceutical composition is an organic salt formed by an organic acid rosuvastatin and an organic base azelnidipine with a molar ratio of 1:1. The pharmaceutical composition can be made into any dosage forms together with a pharmaceutically-acceptable carrier for reducing blood pressure and blood lipid, reducing myocardial infarction and treating cerebral apoplexy. The inventive pharmaceutical composition has the advantages of stable physiochemical indexes, controllable product quality, and convenient administration.

The invention which discloses an antihypertensive medicinal composition and concretely relates to a medicinal composition containing azelnidipine or a pharmaceutically acceptable salt thereof and fimasartan belongs to the medicinal field. In the antihypertensive medicinal composition, the weight ratio of azelnidipine or the pharmaceutically acceptable salt thereof to fimasartan is 1:0.1-500, and preferably 1:1-50. The azelnidipine fimasartan medicinal composition of the invention, which has the advantages of obvious synergism, low treatment cost, small side effect and realization of stationary blood pressure reduction when the composition is used to treat hypertension, has a good clinical application prospect.

The present invention relates to a kind of pharmaceutical composition, it comprises telmisartan salt and calcium ion antagonist or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier; Described telmisartan salt is selected from telmisartan Sodium salt, potassium salt, calcium salt, magnesium salt or amine salt of sartan, described calcium ion antagonist is selected from amlodipine, lacidipine, cilnidipine, lercanidipine, nisoldipine, nica Dipine, azedipine, barnidipine, manidipine, benidipine, verapamil, diltiazem, or a pharmaceutically acceptable salt thereof. The composition is used for preventing, delaying progress or treating patients with hypertension, angina pectoris, atherosclerosis, stroke, cardiac insufficiency, dyslipidemia, diabetes, renal function damage or hypertension accompanied by Alzheimer's disease, reducing Reduce the morbidity and/or mortality of cardiovascular and cerebrovascular diseases, reduce adverse drug reactions, and improve patients' compliance with medication.

The invention discloses an Azelnidipine composition, which consist of Azelnidipine and beta-cyclodextrin, wherein the dosage by weight of the beta-cyclodextrin is 3 to 15 times of that of the Azelnidipine, and the Azelnidipine is enveloped in a hydrophobic cavity of the cyclodextrin. The bioavailability of the Azelnidipine composition is obviously improved compared with a common preparation of the Azelnidipine, which lays a foundation for further development of a new oral preparation of the Azelnidipine.

The invention relates to a medicinal composition containing azelnidipine and atorvastatin calcium, which is used for reducing blood pressure and blood fat and reducing risks of myocardial infarction and cerebral apoplexy.

The invention relates to a granule for treating hypertension. The granule is characterized by comprising a calcium channel blocker, a beta receptor inhibitor, Chinese medicinal herbs and a medicinal carrier, and is prepared from the following components in percentage by weight: 0.1-60 percent of isradipine, 3-15 percent of labetalol, 10-20 percent of yellowmouth dutchmanspipe root and 7-70 percent of the medicinal carrier. The granule has the advantages of high safety, high synergistic effect among raw material components, high bioavailability, and capability of effectively reducing the side effects of separate azelnidipine on the health of a patient.

A method for separating the enantiomers of the chiral drug Azedipine by simulated moving bed chromatography, using simulated moving bed chromatography to separate, and the product with a purity of 98% R-enantiomer can be obtained at the extraction port of one of the two outlets solution, the separation process is a continuous process. After simulated moving bed chromatographic separation, under suitable operating conditions, the purity of R-enantiomer can reach more than 98%, and the yield can reach 95%. The solvent can be recovered, the cost is low, and the pollution is less. Continuous production can be realized, which is beneficial to guarantee the product stable quality.

The invention provides a preparation method of an azelnidipine intermediate, namely 1-benzhydryl-3-hydroxylazetidine hydrochloride. The preparation method comprises the following steps: 1) preparation of a reaction solution I: mixing dimethylaniline and epoxy chloropropane in proportion and adding an organic solvent to prepare the reaction solution I; 2) preparation of a reaction solution II: letting the reaction solution I react at 0-60 DEG C to prepare the reaction solution II; and 3) preparation of 1-benzhydryl-3-hydroxylazetidine hydrochloride: adding the reaction solution II into a microreactor by the use of a pump with flwo velocity of 1-200ml/min, heating to 60-250 DEG C at pressure of 0-2 MPa, completely reacting, and carrying out separation purification to obtain white crystals, namely 1-benzhydryl-3-hydroxylazetidine hydrochloride.

The invention relates to a pharmaceutical composition of azelnidipine and particularly relates to a composition of jointly applying three alkaline auxiliary materials. The medicine has good storage stability and solves the problem of poor stability of azelnidipine and short storage time.

The invention relates to an azelnidipine and isosorbide dinitrate compound composition, which consists of an azelnidipine common layer and an isosorbide dinitrate slow-release layer. Each unit preparation comprises 2-8mg of azelnidipine and 5-40mg of isosorbide dinitrate and each tablet is 0.1g theoretically. Azelnidipine and isosorbide dinitrate are organically combined to reduce the dosage of medical accessories to a maximum extent, which can not only relieve angina and reduce the blood pressure stably, but also improve the survival rate of the patients. The compound composition has high medical effective ratio and is convenient to take and beneficial for price reduction and industrialized production.

The invention relates to a preparation method of an azelnidipine alpha crystal form. According to the technical scheme, the preparation method comprises the following steps; I, adding non-alpha-crystal-form azelnidipine or crude azelnidipine of other forms into isopropanol of which the amount is not less than 5 times the mass of the non-alpha-crystal-form azelnidipine or the crude azelnidipine, heating for dissolved clarification, cooling to the temperature of 40 DEG C, observing whether crystallization occurs or not, if so, replenishing the isopropanol for dissolved clarification once again, cooling to the temperature of 40 DEG C or less for crystallization, preserving heat at the temperature of 10 DEG C below zero to 0 DEG C for 6 to 12 hours, and filtering to obtain an azelnidipine-diisopropanol compound; II, putting the azelnidipine-diisopropanol compound solid prepared by filtering in the step I into a crystal transformation kettle, adding cyclohexane in an amount which is not less than 6 times the mass of the azelnidipine-diisopropanol compound solid for crystal transformation with stirring, stirring for not less than 3 hours, finishing crystal transformation, filtering, and performing vacuum drying under a reduced pressure to obtain the azelnidipine alpha crystal form. By adopting the method, the crude azelnidipine and the non-alpha-crystal-form azelnidipine can be transformed into the azelnidipine alpha crystal form.

The invention relates to a medicine for treating hypertension, which is a compound preparation consisting of telmisartan angiotensin converting enzyme receptor inhibitor and azelnidipine calcium antagonist. When the compound preparation disclosed by the invention is used, the dose and application times of the medicine are reduced, side effects are reduced, the patient compliance is improved and the treatment effect is enhanced.