36 results about "Benazepril" patented technology

The invention discloses a graphene oxide supported benazepril compound as well as a preparation method and application thereof. The compound comprises graphene oxide and benazepril; and the surface of the graphene oxide contains one or more of hydroxyl, carbonyl, carboxyl and epoxy group; and the benazepril is adsorbed on the surface of a graphene oxide molecule. The preparation method disclosed by the invention comprises the following steps of: evenly mixing the graphene oxide with a benazepril solution according to a certain volume ratio; oscillating over the night, centrifuging the mixed solution at a certain rotating speed, taking sediment, and freezing and drying to obtain graphene oxide-medicine compound. The compound disclosed by the invention can be applied as a controlled release carrier of the benazepril. The compound disclosed by the invention is high in supporting rate; the release has pH response characteristic; the action time of the benazepril can be prolonged by application of the compound; and the frequency of medication is reduced.

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.

The invention discloses a synthetic method of Benazepril key intermediate S-amino substance, comprising the following steps of: (1) amination: in a sealed reaction vessel, introducing ammonia gas to 3-bromine-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate shown as formula (II) with the existence of a cupric salt catalyst and an organic solvent until the reaction pressure is 2.0MPa to 5.0MPa, evenly mixing, raising the temperature to 50 to 120 DEG C, reacting for 1 to 5 hours, and after the reaction is finished, obtaining 3-amino group-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate with the (S, R) configuration after the post-treatment of the reaction solution; and (2) resolving reaction: stirring the product obtained in step (1) at the reaction temperature of 30-70 DEG C for 0.5 to 8 hours in amino acid resolving agent and resolving solvent, and after the reaction is finished, obtaining optically pure (S)-3-amino group-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate by the separation treatment of reaction products. The method takes the cupric salt as the catalyst, and the amination is executed under normal medium pressure, therefore, the conversion rate is high and the pollution is light.

The present invention relates to an improved process for the preparation of trifluoromethanesulfonic ester of ethyl (R)-2-hydroxy-4-phenylbutyrate, referred to here as triflate in structural Formula I, and to the use of this compound as intermediate for the preparation of ACE (Angiotensin Converting Enzyme) inhibitor, benazepril.

The invention discloses a traditional Chinese medicine for treating hypertension early-stage kidney damage and a preparation method thereof. The traditional Chinese medicine for treating hypertension early-stage kidney damage disclosed by the invention mainly comprises radix rehmanniae preparata, fructus corni, yam, cortex eucommiae, radix salviae miltiorrhizae and tortoise shell, and is preparedinto various common preparations by the traditional technology of traditional Chinese medicine. The traditional Chinese medicine for treating hypertension early-stage kidney damage disclosed by the invention can effectively relieve the kidney fibrosis progress of the patient suffering hypertension early-stage kidney damage, reduces the kidney burden of the patient, and effectively controls the disease progression; in combination with the oral hypotensor benazepril, a synergistic effect is realized for the blood pressure reducing effect; and compared with the oral hypotensor benazepril only, the traditional Chinese medicine disclosed by the invention takes effect quickly in reducing blood pressure, and the final blood pressure reducing effect is better. Compared with the prior art, the invention has outstanding substantial characteristics and obvious progress.

This invention is a multilayer tablet contains calcium channel acceptor retarder and ACE inhibitor. Its feature is that it contains calcium channel acceptor retarder pleated sheet and ACE inhibitor pleated sheet. The calcium channel acceptor retarder pleated sheet contains levamlodipine or amoldipine or salt that can be accepted on pharmacy of them. The ACE inhibitor pleated sheet contains methylphenidate or its pharmacy accepted salt. They can be produced by normal medicine equipment, and preparation is easy, the multilayer tablet made can be quickly disintegrated, main medicine component can be quickly stripped, and its quality stability is good.

The present invention provides one kind of medicine composition of benazepril and its preparation process. The present invention solves the problem of benazepril with low dissolution and the problems of the preparation process in medicine sticking and medicine degradation. The preparation process combines solid dispersing technology and traditional tablet preparation, and is simple, accurate in dosage control and high in production efficiency.

The present invention provides a method of converting an intermediate compound to the desired S,S diastereomer for efficiently making benazepril and analogues thereof.

The invention discloses a liposome solid preparation of benazepril / hydrochlorothiazide and a preparation method thereof. The liposome solid preparation is prepared mainly by the liposome made of 1 portion of hydrochloric acid benazepril, 1.25 portions of hydrochlorothiazide, 50-200 portions of soya bean lecithin, 20-100 portions of octadecylamine and 5-60 portions of cholesterol acetyl lipide measured based on weight, the benazepril / hydrochlorothiazide liposome, and the other excipients typically used in pharmacy. According to the invention, the product quality of the preparation is improved,the toxic and side effects are reduced, the stability, dissolution and bioavailability of the medicine are greatly improved, and a stable and enduring function and remarkable therapeutic effects are achieved.

A stable pharmaceutical composition consisting of (a) benazepril, in free or pharmaceutically acceptable salt form; and (b) amlodipine, in free or pharmaceutically acceptable salt form. The composition is free of alkali and alkaline earth metal carbonates and phosphates. The composition is also free of excipients which increase the pH of microenvironment above 5. It is therefore not required to physically separate the two drugs from each other.

The present invention relates to an improved process for the preparation of trifluoromethanesulfonic ester of ethyl (R)-2-hydroxy-4-phenylbutyrate- , referred to here as triflate in structural Formula I, and to the use of this compound as intermediate for the preparation of ACE (Angiotensin Converting Enzyme) inhibitor, benazepril.

The present invention relates to a medicine composition containing enalapril or benazepril and sotalol. It is a new type hypotensor medicine composition. The content of enalapril or benazepril is 5-40 mg and the sotalol content is 20-160mg.

The invention relates to a solid medicine composition system and a preparation method thereof, wherein the solid medicine composition system contains lercanidipine which is an antihypertensive drug, pharmaceutical acceptable salts of lercanidipine, benazepril which is also an antihypertensive drug, pharmaceutical acceptable salts of benazepril, and a disintegrating agent which is capable of ensuring release of lercanidipine and benazepril. A certain amount of the disintegrating agent is added, so that the solid medicine composition is excellent and stable in dissolution rate, and is capable of maintaining stable plasma concentration, drug administration frequency is reduced, drug administration intervals are prolonged, and treatment cost is reduced. The solid medicine composition is capable of increasing medicine compliance of patient, and reducing production cost. In addition, compared with combined utilization of lercanidipine and benazepril, addition amount of auxiliary materials is reduced.

The invention relates to a pharmaceutical composition comprising an angiotensin converting enzyme inhibitor (ACEI), an enkephalinase inhibitor, a folic acid compound and a pharmaceutically acceptable carrier, wherein the ACEI is selected from the group consisting of enalapril, benazepril, ramipril, fosinopril, cilazapril, perindopril and the like, and the content is 1.25-75 mg; the enkephalinase inhibitor is sacubitril, and the content is 10-120 mg; and the folic acid compound is selected from the group consisting of folic acid, 5-methyltetrahydrofolate, calcium formyltetrahydrofolate, leucovorin, calcium levofolinate and the like, and the content is 0.1-5 mg. The invention provides the use of the pharmaceutical composition in the preparation of a medicament for the treatment of chronic heart failure and the prevention of stroke. By the implementation of the invention, the pharmaceutical composition can also improve the compliance of patients and improve the therapeutic effect by providing the pharmaceutical composition for a specific use to the patients.

An angiotensin converting enzyme (ACE) inhibitor is mainly used for treating diseases such as hypertension, congestive heart failure, myocardial infarction, renal dysfunction, etc. The existing medicines in the market comprise captopril, enalapril, benazepril, and the like, which have obvious adverse reactions such as severe dry cough, parageusia, proteinuria, hematuria, hypotension, and the like, and the medicines have some adverse reactions that threaten life such as acute thrombocytopenia, hyperkalemia, severe arrhythmia and renal failure. The invention relates to a technical scheme for chemosynthesis of a 2-alkoxycarbonyl-3-phenylpropionic acid ester derivative with the characteristic of the structural general formula I and provides a 2-alkoxycarbonyl-3-phenylpropionic acid ester derivative with the characteristic of the structural general formula I and the derivative is taken as an ACE inhibitor for treating diseases such as hypertension, congestive heart failure, myocardial infarction and renal dysfunction, and lowering blood sugar and blood lipid, etc. R1, R2, R3 and R4 are -H, C1-3-alkyl, C1-3-alkenylnyl, C1-3-alkoxy, aryloxy, arylalkoxyl, heterocycles, heteroarylalkyl, acyl, acyloxy, hydroxy C1-3-alkyl, hydroxy, amino, halogen, nitro, cyano, formyl, acylamino, C1-3-alkyamino, C1-3-alkoxycarbonylamino, C1-3-alkylcarbonylamino, C1-3-alkylsulfonyl and arylsulfonyl.

The invention relates to a medicinal composition for lowering blood pressure, which consists of trichlormethiazide and angiotensin converting enzyme inhibitor which serve as active ingredients and a pharmaceutical carrier, wherein the angiotensin converting enzyme inhibitor may be enalapril, cilazapril, benazepril, captopril, ramipril, perindopril and fosinopril. The unit dosage of trichlormethiazide is 0.5 to 8 milligrams, preferably 2 to 4 milligrams. The unit dosage of angiotensin converting enzyme inhibitor is 1.5 to 50 milligrams. The medicinal composition can be made into various oral preparations including conventional tablets, capsules, chewable tablets, dispersible tablets and effervescent tablets.

The invention discloses a compound glucose-reducing preparation containing phenformin and a preparation method of the compound glucose-reducing preparation. The compound glucose-reducing preparation consists of the following components: the phenformin, water-soluble dietary fibers, vinpocetine, vitamin B1, gastric inhibitory peptide, glutamine dipeptide, benazepril, prostaglandin A1, sophorin A, beta-glucosidase, chitosan oligosaccharide, indapamide, curcumin and sodium ferulate. The compound preparation disclosed by the invention, on the basis of the combined action of various medicinal components, is capable of promoting secretion of insulin, so that the purpose of reducing glucose is achieved; the compound preparation is capable of effectively improving immunity of a patient and preventing various diabetic complications; and moreover, the compound preparation is significant in glucose-reducing effect, low in side effects and free from adverse effects on the patient in a long term of using, and the compound preparation has a broad application prospect.

The invention relates to an oral hard capsule and particularly relates to a tablet capsule formed by filling benazepril tablets and amlodipine tablets in a capsule. The tablet capsule provided by the invention is composed of a capsule and tablets filled in the capsule, wherein the capsule comprises an upper capsule body and a lower capsule body, and the capsule is internally filled with at least one tablet with the benazepril as an active ingredient and at least one tablet with amlodipine as an active ingredient. The active ingredients in the capsule are not in mutual contact with each other, so that no chemical compatibility and byproducts are generated between the ingredients, the stability of a product is improved, a degradation product generated after the benazepril and the amlodipine are in contact is reduced, and relevant substances of the product provided by the invention are still controlled within the amount alone brought by the benazepril (seven) and the benazepril (seven).

The invention provides a new pharmaceutical composition for treating hypertension, and relates particularly to a composition comprising S-metoprolol and angiotensin converting enzyme inhibitor including enalapril, captopril, lisinopril, perindopril, benazepril and fosinopril, wherein the weight ratio of S-metoprolol to angiotensin converting enzyme inhibitor is (1-35):1, preferably (3-25):1, morepreferably (7.5-18):1. The inventive composition is very important for long-term survival rate of hypertensive patients, and has a positive impact on the prognosis of hypertension for patients.

The invention relates to an integrated traditional Chinese and western medicine medicine for treating biliary dyskinesia syndrome and a preparation method thereof. The raw materials for making the active ingredients of the medicine include Chinese medicine ingredients, western medicine ingredients and related pharmaceutical excipients, and the Chinese medicine ingredients include Lycium barbarum Seedlings, Acanthopanax, Mountain Lettuce, Melon Seeds, White Pico, Lime, Coral Algae, Atractylodes Atractylodes, Hollyhock, Youcao, Liuqu, Sleeping Vegetables, Meigen, Luoxingcao and Lingchen; The western medicine ingredients include Qiangjiacoumarin, ursodeoxycholic acid, lentinan and mebrobenatezine; the medicine of the present invention selects Chinese herbal medicines with functions of invigorating the liver and kidney, clearing away heat and gallbladder, diuresis and treating stranguria, etc. The antispasmodic and choleretic Western medicine ingredients are used in combination. Both Chinese and Western ingredients can improve the immunity of patients. They have a significant effect on the treatment of biliary dyskinesia syndrome and its complications. The medicine is convenient to take and has no side effects, so it can be safely promoted.

The invention discloses a liposome solid preparation of benazepril / hydrochlorothiazide and a preparation method thereof. The liposome solid preparation is prepared mainly by the liposome made of 1 portion of hydrochloric acid benazepril, 1.25 portions of hydrochlorothiazide, 50-200 portions of soya bean lecithin, 20-100 portions of octadecylamine and 5-60 portions of cholesterol acetyl lipide measured based on weight, the benazepril / hydrochlorothiazide liposome, and the other excipients typically used in pharmacy. According to the invention, the product quality of the preparation is improved, the toxic and side effects are reduced, the stability, dissolution and bioavailability of the medicine are greatly improved, and a stable and enduring function and remarkable therapeutic effects are achieved.

The present invention relates to an improved process for preparation of highly pure benazepril of Formula I, wherein R is hydrogen or pharmacologically acceptable salt thereof by completely eliminating the impurity of 7-bromo analogue of benazepril of Formula Ia, wherein R is bromo group.

A stable pharmaceutical composition consisting of (a) benazepril, in free or pharmaceutically acceptable salt form; and (b) amlodipine, in free or pharmaceutically acceptable salt form. The composition is free of alkali and alkaline earth metal carbonates and phosphates. The composition is also free of excipients which increase the pH of microenvironment above 5. It is therefore not required to physically separate the two drugs from each other.

The present invention provides one kind of medicine composition of benazepril and its preparation process. The present invention solves the problem of benazepril with low dissolution and the problemsof the preparation process in medicine sticking and medicine degradation. The preparation process combines solid dispersing technology and traditional tablet preparation, and is simple, accurate in dosage control and high in production efficiency.

The invention discloses compound plaster for treating rhinitis. The compound plaster for treating rhinitis is prepared from the main raw materials in parts by weight: 11 to 17 parts of zidovudine, 4 to 6 parts of aspartic acid, 10 to 17 parts of calculus bovis factitious, 1 to 3 parts of guaifenesin, 4 to 8 parts of aloe vera gel, 11 to 15 parts of ribavirin, 5 to 8 parts of domiphen, 4 to 8 parts of fatty acid sucrose ester, 15 to 30 parts of chlorothiazide, and 8 to 20 parts of benazepril. The compound plaster prepared by the invention has an obvious curative effect of treating acute rhinitis and chronic rhinitis, and does not influence breath of a patient and normal discharge of nasal secretions when in use.

The invention relates to a Chinese and Western medicine composition for treating acute peritonitis and a preparation method thereof. The raw materials for making the active ingredients of the Chinese and Western medicine composition are composed of: white calamus, long stem orchid, ginger grass, cup chrysanthemum, ground loquat, Rattan, sour rattan wood, citronella, orange peel, camphor root, ginger, black cortex root, lysozyme, mebrobenatezine; the Chinese and Western medicine composition of the present invention combines traditional Chinese medicine and Western medicine, and has the functions of sterilizing, reducing inflammation, clearing away heat Detoxification, expelling wind and dampness, nourishing the spleen and stomach, dispelling cold and relieving the exterior, warming the middle and relieving pain, eliminating filth and harmonizing the middle, and can eliminate harmful bacteria in the intestinal tract, contribute to the growth of normal intestinal flora, improve digestive function, regulate Systemic immunity has definite curative effect on acute peritonitis, and the effect is quick. In terms of prescription selection, the present invention has certain innovativeness for treating acute peritonitis and has certain social and economic value.

The invention discloses a synthetic method of Benazepril key intermediate S-amino substance, comprising the following steps of: (1) amination: in a sealed reaction vessel, introducing ammonia gas to 3-bromine-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate shown as formula (II) with the existence of a cupric salt catalyst and an organic solvent until the reaction pressure is 2.0MPa to 5.0MPa, evenly mixing, raising the temperature to 50 to 120 DEG C, reacting for 1 to 5 hours, and after the reaction is finished, obtaining 3-amino group-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate with the (S, R) configuration after the post-treatment of the reaction solution; and (2) resolving reaction: stirring the product obtained in step (1) at the reaction temperature of 30-70 DEG C for 0.5 to 8 hours in amino acid resolving agent and resolving solvent, and after the reaction is finished, obtaining optically pure (S)-3-amino group-2, 3, 4, 5-tetrahydrogen-2-oxygen-1H-1-benzoaza-1-tert-butyl acetate by the separation treatment of reaction products. The method takes the cupric salt as the catalyst, and the amination is executed under normal medium pressure, therefore, the conversion rate is high and the pollution is light.

The invention discloses a compound for inhibiting combination of novel coronavirus spike protein and ACE2, the compound is a compound A or a compound B, the IC50 value of the compound A for inhibiting ACE2 is less than 50 [mu] M, and the IC50 value of the compound B for inhibiting ACE2 is less than 1 [mu] M; the compound A is dipeptide or tripeptide, hydrophobic amino acid residues exist at the C end of the compound A, and the hydrophobic amino acid residues comprise any one of residues of proline, tyrosine, phenylalanine and tryptophan; the compound B is a pril drug containing the structure of the compound A, and the pril drug comprises but is not limited to captopril, enalapril, lisinopril, fosinopril, perindopril, benazepril and eplerenone; the compound can be combined with an RBD region of a novel coronavirus S protein, competitively blocks combination of the RBD region and an ACE2 receptor, and has a positive effect on prevention of the novel coronavirus SARS-CoV-2.

According to the invention, extension primers with different molecular weights at different single nucleotide polymorphism (SNP) loci are utilized, and a plurality of loci are simultaneously detectedthrough matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI TOF MA), and finally, a method for guiding individualized medication of benazepril serving as antihypertensive drug by detecting a product is obtained. The method comprises the following steps: respectively designing multiple amplification primers and extension primers according to a plurality of to-be-detected target SNP loci; preparing a multiplex amplification primer reaction system and an extension primer reaction system; in the reaction systems, simultaneously and respectively carrying out amplification and single base extension reaction on the plurality of target SNP sites by using a plurality of primers; and carrying out time-of-flight mass spectrometry analysis on a product after the singlebase extension reaction, identifying genotypes of SNP related to different drug metabolism according to products of extension primers with different molecular weights represented by a mass spectrum peak, and guiding individualized medication of the antihypertensive drug benazepril. The method can simultaneously detect 9 SNP loci related to benazepril drug metabolism, and has the advantages of lowcost, no need of probe synthesis, short time consumption, simple and convenient result analysis and extremely wide application field.