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39 results about "Enalapril Maleate" patented technology
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The maleate salt form of enalapril, a dicarbocyl-containing peptide and angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, enalapril is converted by de-esterification into its active form enalaprilat. Enalaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Enalapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
Stable formulations of ace inhibitors, and methods for preparation thereof
InactiveUS20080221156A1Easy to produceBiocidePeptide/protein ingredientsTime efficientIndustrial scale
The present invention provides stable formulations of ACE inhibitors, especially enalapril maleate, that can be manufactured in a time efficient, cost effective manner. Such formulations can be prepared simply and on a large industrial scale. The present invention also provides methods for the preparation of stable formulations of ACE inhibitors, especially enalapril maleate.
Owner:MUTUAL PHARMA CO INC
Enalapril maleate tablet and preparation method thereof
ActiveCN101721383AImprove stabilityLow costPill deliveryCardiovascular disorderPharmaceutical industryMedicine
The invention discloses an enalapril maleate tablet and a preparation method thereof, belonging to the technical field of chemical pharmaceutical industry. The enalapril maleate tablet mainly contains 3 to 9 parts of enalapril maleate, 40 to 60 parts of filling agent, 0 to 35 parts of disintegrating agent, 0 to 2 parts of caking agent, 0.1 to 4 parts of lubricating agent and 0.1 to 3 parts of flow aid. Compared with the conventional merchant enalapril maleate tablet, the enalapril maleate table provided by the invention adopts auxiliary materials which have poorer compatibility with the enalapril maleate technical on the traditional conception and ensures that the enalapril maleate tablet produced by using common auxiliary materials has excellent stability by utilizing the specified proportions among raw and auxiliary materials and the specific preparation process; and after being detected, the material qualities of batches of products are all not more than 3.0 percent, the quality stability thereof is superior to the same product from other enterprises, and the cost is saved to the largest extent at the same time of improving the stability.
Owner:JIANGSU PENGYAO PHARMA
Enalapril maleate tablet composition and its preparation and use
ActiveCN102357084AGood storage stabilityDipeptide ingredientsPill deliveryOrganic acidActive component
The invention relates to the field of hypertension treatment medicinal preparations, and provides an enalapril maleate tablet composition. The enalapril maleate tablet composition comprises enalapril maleate as an active component, one or more organic acids and auxiliary materials. The enalapril maleate tablet composition is characterized in that the one or more organic acids selected from malic acid, tartaric acid and taurine. The enalapril maleate tablet composition improves greatly enalapril maleate tablet storage stability, guarantees medical efficacy and reduces toxicity.
Owner:广东彼迪药业有限公司
Medicinal composition comprising quick-release pellets containing Enalapril or Enalapril-acid addition salt and slow-release pellets containing Felodipine
ActiveCN102247366AEffective plasma concentrationSmooth releasePharmaceutical delivery mechanismCardiovascular disorderBlood concentrationPatient compliance
The invention relates to a medicinal composition containing Enalapril or Enalapril-acid addition salt and Felodipine, prepared by putting slow-release pellets containing Felodipine and quick-release pellets containing Enalapril or Enalapril-acid addition salt in capsules. Each dosage unit of the medicinal composition contains 2.5-25mg of Enalapril maleate and 2.5-25mg of Felodipine. The medicinal composition can stabilize blood pressure quickly, and keep effective blood concentration for 24 hours, with increasing patient compliance. The medicinal composition is administered only once a day.
Owner:白云山威灵药业有限公司
Stable enalapril maleate capsules and preparation method thereof
InactiveCN105125514AHigh hardnessImprove the disintegration effectPill deliveryPharmaceutical non-active ingredientsLACTOSE MONOHYDRATEArginine
The invention relates to stable enalapril maleate capsules and a preparation method thereof, and belongs to the technical field of medicine. Enalapril maleate, lactose monohydrate, microcrystalline cellulose, startch, hydroxypropyl methyl cellulose, sodium alga acid, poloxamer 407, polyethylene glycol 4000 and L-arginine are preferably used as medical components of the stable enalapril maleate capsules, the degradation speed of the enalapril maleate is remarkably decreased through the mutual synergistic effect, the stability of the enalapril maleate capsules is greatly improved, and it is ensured that clinical medicine is safe, effective and capable of being stored for a long time.
Owner:CSPC OUYI PHARM CO LTD
Preparation method of N-carboxyalkyl dipeptide type angiotensin converting enzyme inhibitor
InactiveCN1429835ASimple and efficient processSuitable for industrialized mass productionDipeptidesCardiovascular disorderDipeptideDepressant
A process for preparing N-carboxyalkyl dipeptide type angiotensin converting enzyme (ACE) depressant (such as enalapril maleate, ramipril, etc) includes such steps as preparing N-carboxylic acid anhydride from bis (trichloromethyl) carbonate, and coupling with relative alpha-amino acid.
Owner:SHANGHAI INST OF PHARMA IND CO LTD
Medicine composition containing Enalapril maleate, folic acid and acid stabilizer
ActiveCN107007838AImprove stabilityStable than commercially availableOrganic active ingredientsPill deliveryLACTOSE MONOHYDRATEDissolution
The invention provides a new Enalapril maleate and folic acid composite preparation. An acid stabilizer with weight ratio of 1%-5% is added in the preparation to improve the stability of the preparation at high temperature and long-term standing condition; and meanwhile, a mixture of microcrystalline cellulose and lactose monohydrate is selected asfiller, the dissolution of the folic acid in the 0.1M hydrochloric acid medium is improved, and a finally prepared tablet is basically consistent with the market tablet. The composition disclosed by the invention is good in stability, capable of guaranteeing the clinical safe use of the medicine, simple in process operation, and suitable for industrial production.
Owner:NANJING YOKO PHARMA +2
Preparation method for enalapril maleate orally disintegrating tablets
ActiveCN103393612ASave electricityNo pollution in the processUrinary disorderPill deliveryHigh absorptionIrritation
The invention relates to a preparation method for enalapril maleate orally disintegrating tablets. The formula comprises the following ingredients, by weight, enalapril maleate, diluents, disintegrating agents, lubricants and corrective agents with a ratio of 1:(5-6):(3.5-4.5):(0.1-0.3):(0.05-0.15). The diluents, the disintegrating agents, the lubricants and the corrective agents can be substances generally used in pharmaceutical field. Enalapril maleate is crushed by a micropowder machine, and the particle sizes of 90% of the particles are less than 80 microns. Then the diluents, part of the disintegrating agents, the corrective agents are added, mixed uniformly and subjected to dry granulation. Then part of the disintegrating agents, the lubricants are added, mixed totally, and subjected to tabletting, and enalapril maleate orally disintegrating tablets are obtained. The enalapril maleate orally disintegrating tablets are advantaged by rapid disintegration, rapid onset, high absorption and high bioavailability. The enalapril maleate orally disintegrating tablets can reduce irritation effects of medicines on oesophaguses and gastrointestinal tracts and are well suitable for some critical patients to take.
Owner:青岛国海生物制药有限公司
Enalapril maleate granules and preparation method thereof
InactiveCN104473877AImprove stabilityImprove the dosage formDipeptide ingredientsGranular deliveryCyclodextrinPharmaceutical drug
The invention discloses enalapril maleate granules and aims to provide a granule prescription which can improve the drug stability. The enalapril maleate granules prepared by the method have the advantages that the enalapril maleate granules can be directly swallowed and can be further mixed in water to drink and can be quickly dissolved when coming across water; the enalapril maleate granules are good in taste, convenient to apply and carry, accurate to quantify, quick to take effect and high in availability. Meanwhile, the invention further discloses a preparation method of the enalapril maleate granules. By adopting a cyclodextrin inclusion technique, medicinal raw materials are included by virtue of a saturated aqueous solution method, so that the drug stability is improved. The process is simple to operate and low in cost, and the industrial amplifying application is increased.
Owner:万全万特制药(厦门)有限公司
Enalapril maleate preparation and application thereof
ActiveCN107951835AImprove stabilityImprove bioavailabilityInorganic non-active ingredientsPharmaceutical delivery mechanismAngiotensin-converting enzymeDiketopiperazines
The invention relates to the technical field of pharmaceutical preparations, in particular to an enalapril maleate preparation and application thereof. PH of the enalapril maleate preparation is 6.4-7.4. By controlling pH of enalapril maleate preparation, stability of the enalapril maleate preparation can be effectively enhanced, impurities such as DPK (diketopiperazine), enalaprilat, N-[1-(S)-(ethoxycarbonyl)-3-phenylpropyl]-L-alanine (impurity B) and the like generated by degradation of enalapril maleate in the enalapril maleate preparations in different dosage forms such as powder, granulesand tablets can be effectively controlled, bioavailability is fully improved, and the preparation can be used for preparing angiotensin converting enzyme inhibitor drugs.
Owner:湖南千金湘江药业股份有限公司
Stable hydrochlorothiazide crystalline compound, and composite enalapril maleate pharmaceutical composition thereof
InactiveCN104744404ASimple production methodLow costOrganic active ingredientsDipeptide ingredientsEnalapril+hydrochlorothiazideSolubility
The invention belongs to the technical field of medicines, and provides a stable hydrochlorothiazide crystalline compound, and a composite enalapril maleate pharmaceutical composition thereof, and a preparation method. The method comprises the following steps: dissolving hydrochlorothiazide sold into water; dropwise adding a mixed solvent of absolute ethyl alcohol and trichloromethane; and carrying out heat-preservation stirring, cooling, carrying out heat-preservation stirring, filtering, washing and drying in vacuum to obtain the hydrochlorothiazide crystalline compound. The hydrochlorothiazide crystalline compound is high in yield, high in purity, good in water solubility and stable in quality. The invention further provides a composite enalapril maleate pharmaceutical composition containing the stable hydrochlorothiazide crystalline compound and a preparation method of the composite enalapril maleate pharmaceutical composition. The composite enalapril hydrochlorothiazide pharmaceutical composition prepared by the preparation formula and the preparation technology is stable in quality; and industrialized implementation is easily to realize.
Owner:张旻
Isomer impurities in bulk pharmaceutical chemicals of enalapril maleate and synthesis method of isomer impurities
ActiveCN110117309ABiological material analysisPeptide preparation methodsChromatographic separationTert-Butyloxycarbonyl protecting group
The invention provides isomer impurities in bulk pharmaceutical chemicals of enalapril maleate and a preparing method of the isomer impurities. N-t-butyloxycarboryl-D-alanine (a compound I) and D-proline benzyl ester (II) are subjected to a condensation acylation reaction to prepare an intermediate compound III, then Boc deprotection is conducted to obtain an intermediate compound IV, the intermediate IV and ethyl 2-oxo-4-phenylbutyrate (V) are subjected to reductive amination to obtain a compound VI, then the compound VI is subjected to hydrogenation to remove benzyl groups, then a mixture ofenalapril enantiomers (TM1) and diastereoisomers (TM2), and then the enalapril enantiomers (TM1) and diastereoisomers (TM2) are obtained through preparative chromatographic separation.
Owner:CHANGZHOU PHARMA FACTORY
Pharmaceutical composition of enalapril maleate folic acid and preparation method thereof
InactiveCN106963938AGood compatibilityImprove stabilityOrganic active ingredientsDipeptide ingredientsCross-linkMannitol
The invention provides a pharmaceutical composition of enalapril maleate folic acid. The composition comprises enalapril maleate, folic acid, filler, a disintegrant, a binder and a lubricant. The composition is characterized in that the filler is selected from composition, lactose anhydrous or mannitol, the disintegrant is selected from one or more of cross-linked sodium carboxymethylcellulose or low substituted hydroxypropyl cellulose, the binder is selected from povidone K30, hydroxypropyl methyl cellulose E5, hydroxypropyl cellulose SL-FP or hydroxypropyl methylcellulose 603, and the lubricant is selected from talcum powder, sodium stearyl fumarate or glyceryl behenate. The excipients and raw materials selected by the invention have good compatibility, the preparation obtained by dry granulation has good stability, can ensure safe use of drugs in clinical practice, and the technological operation is simple and is suitable for industrial production.
Owner:NANJING YOKO PHARMA +2
Enalapril maleate oral solution and preparation method thereof
InactiveCN104055730AGreat tasteEasy to takeDipeptide ingredientsPharmaceutical delivery mechanismMedicineCardiac failures
The invention discloses a stable enalapril maleate powder composition which is taken orally, and specifically relates to a stable enalapril maleate oral solution composition. The enalapril maleate composition disclosed by the invention can be used for treating hypertension, cardiac failure, ventricular dysfunction and the like. The composition disclosed by the invention is superior to enalapril, can be better absorbed by body, is good in mouthfeel, is suitable for the children and the old, and remarkably increases medication compliance of a patient.
Owner:AVENTIS PHARMA HAINAN
Stable enalapril maleate tablet and preparation method thereof
InactiveCN106963738ALittle changeStable enalaprilat contentInorganic non-active ingredientsPill deliveryGlycerolLactose
The invention discloses a stable enalapril maleate tablet and a preparation method thereof, and belongs to the technical field of the pharmaceutic preparation. The enalapril maleate tablet is prepared by the following components by weight: 0.255-1.02 parts of enalapril maleate, 7-9 parts of lactose, 0.6-1.8 parts of corn starch, 0.1-0.3 parts of glycerol distearate, and 0.1-0.2 parts of lake or ferric oxide. The selected accessories and the preparation technology are capable of remarkably reducing the degrading speed of the enalapril maleate through the mutual synergistic effect, greatly improving the stability of the enalapril maleate tablet product, and solving the quality problem existing in the current product all the time. The lake or ferric oxide is added in the tablet for the good shading function, so the enalapril maleate photosensitivity problem can be effectively solved.
Owner:HUAYI PHARMA ANHUI CO LTD
Storage-stable and bio-stable formulations of ACE inhibitors, and methods for preparation thereof
InactiveCN1758921APeptide/protein ingredientsHeterocyclic compound active ingredientsTime efficientQuinapril Hydrochloride
The present invention provides storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, that can be manufactured in a time efficient and cost effective manner. Such formulations can be prepared simply and on a large industrial scale using conventional methods and equipment. The present invention also provides methods for the preparation of highly manufacturable, storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride. Methods for treatment of cardiovascular disorders using storage-stable and bio-stable formulations of ACE inhibitors, especially enalapril maleate and quinapril hydrochloride, are also provided.
Owner:SIGMAPHARM
Pharmaceutical composition for treating hypertension
ActiveCN103239708AGood dispersionGood membrane permeabilityOrganic active ingredientsDipeptide ingredientsSolubilityHard Capsule
The invention provides a pharmaceutical composition for treating hypertension. The invention relates to a pharmaceutical composition comprising therapeutic doses of lercanidipine hydrochloride and enalapril maleate, and a proper amount of oil, a surfactant and an assisted surfactant. Preparative dosage forms particularly hard capsules and soft capsules are provided. The pharmaceutical composition increases solubility of a poorly soluble drug of lercanidipine hydrochloride and stability of enalapril maleate, and is suitable for the treatment of hypertension.
Owner:CHONGQING SHENGHUAXI PHARMA CO LTD +1
Enalapril maleate tablet and preparation method thereof
InactiveCN106924201AImprove stabilityLittle degree of degradationDipeptide ingredientsInorganic non-active ingredientsAdhesiveFiller Excipient
The invention provides an enalapril maleate tablet and a preparation method thereof. The enalapril maleate tablet comprises the following raw and auxiliary materials in parts by weight: 4-10 parts of enalapril maleate, 2-8 parts of citric acid, 45-65 parts of filler, 0-30 parts of disintegrating agent, 0-2 parts of adhesive and 0.2-3 parts of lubricant, wherein the lubricant is a mixture of nanometer silicon dioxide and talcum powder. The preparation method comprises the following steps: 1) uniformly mixing the enalapril maleate with the filler in the manner of equivalent gradual adding, sieving with a 100-mesh sieve for later use 2) uniformly mixing the power acquired in the step 1) with the prescription amount of disintegrating agent, and sieving with the 100-mesh sieve for later use; and 3) uniformly mixing the powder acquired in the step 2) with the prescription amounts of adhesive, lubricant and citric acid, sieving with the 100-mesh sieve and performing dry powder tabletting on the powder, thereby acquiring the enalapril maleate tablet. The tablet has the advantages of high stability, simple raw and auxiliary materials and high dissolving speed.
Owner:HUAYI PHARMA ANHUI CO LTD
Preparation method of enalapril maleate
InactiveCN112225778AReduce usageStarting materials are safe and readily availablePeptide preparation methodsEthyl butyratePhenyl group
The invention discloses a preparation method of enalapril maleate. The preparation method comprises the following steps of adding L-alanine, alkali and water into a container, cooling, adding a (Boc)2O solution, performing heating, stirring and reacting to obtain an intermediate 1; adding the intermediate 1 into a solvent, cooling, adding a chlorination reagent under the protection of nitrogen, and performing stirring for reaction to obtain an intermediate 2; adding L-proline and alkali into water for reaction, then adding the intermediate 2, and carrying out heat preservation reaction to obtain an intermediate 3; adding 2-oxo-4-phenyl ethyl butyrate, the intermediate 3, a molecular sieve and a reducing agent into a solvent, and reacting under set pressure to obtain an enalapril crude product; and dissolving the enalapril crude product, adding maleic acid, and stirring for reaction to obtain enalapril maleate. The method has the advantages of safe and easily available starting materials, low price, relatively short reaction steps, avoidance of the use of toxic reagents, relatively small generation amount of three wastes, relatively simple operation, high product purity, high yield, and suitableness for industrial production.
Owner:CISEN PHARMA
Enalapril maleate tablet and preparation method thereof
ActiveCN101721383BImprove stabilityLow costPill deliveryHeterocyclic compound active ingredientsMedicinePharmaceutical industry
Owner:JIANGSU PENGYAO PHARMA
Drug composition for treating chronic cardiac failure and application thereof
ActiveCN108524762ADialectically accurate and completeSignificant effectOrganic active ingredientsDipeptide ingredientsSide effectRadix Ophiopogonis
Owner:上海市静安区中医医院
A kind of pharmaceutical composition containing enalapril maleate, folic acid and acid stabilizer
InactiveCN107007838BImprove stabilityStable than commercially availableOrganic active ingredientsPill deliveryPharmacologyPolypill
Owner:NANJING YOKO PHARMA +2
Enalapril maleate tablet composition and its preparation and use
ActiveCN102357084BGood storage stabilityDipeptide ingredientsPharmaceutical non-active ingredientsOrganic acidActive component
The invention relates to the field of hypertension treatment medicinal preparations, and provides an enalapril maleate tablet composition. The enalapril maleate tablet composition comprises enalapril maleate as an active component, one or more organic acids and auxiliary materials. The enalapril maleate tablet composition is characterized in that the one or more organic acids selected from malic acid, tartaric acid and taurine. The enalapril maleate tablet composition improves greatly enalapril maleate tablet storage stability, guarantees medical efficacy and reduces toxicity.
Owner:广东彼迪药业有限公司
Method for treating diabetes by combining traditional Chinese medicine and western medicine
InactiveCN103550227AEnhance physical fitnessImprove microcirculationDipeptide ingredientsMetabolism disorderFormularyHypoproteinemia
The invention relates to a method for treating diabetes by combining traditional Chinese medicine and western medicine. The method specifically comprises the following steps: (1) general treatment; (2) western medicine treatment, namely, controlling blood glucose and blood pressure, and controlling the blood glucose through gliquidone tablets; treating severe patients by cooperatively using insulin; reducing the blood pressure through enalapril maleate tablets; dosing albumin intravenous drip to patients suffering hypoproteinemia, oliguria and severe edema and treating by utilizing equilibrium liquid; and (3) traditional Chinese medicine treatment method, namely mixing 2-5 parts of ginseng, 3-5 parts of lucid ganoderma, 2-5 parts of astragalus root, 4-8 parts of wine-treated rhubarb, 6-9 parts of yam, 3-5 parts of cornus, 4-8 parts of radix rehmanniae, 1-3 parts of leech, 3-5 parts of safflower, 5-8 parts of salviae miltiorrhizae, 10-20 parts of rhizoma smilacis glabrae, 2-6 parts of rhizoma alismatis and 1-4 parts of licorice to a traditional Chinese medicine decoction, and decocting the traditional Chinese medicine in water when in use. The traditional Chinese medicine formulation has the functions of invigorating qi, tonifying kidney, detoxifying, promoting diuresis, promoting blood circulation to remove meridian obstruction, strengthening body resistance and eliminating evil, and the combined treatment manner has a certain curative effect on diabetics.
Owner:李文芝 +1
A kind of pharmaceutical composition for treating hypertension
Owner:CHONGQING SHENGHUAXI PHARMA CO LTD +1
Enalapril maleate capsules and preparation method thereof
InactiveCN107049968AImprove stabilityLow costDipeptide ingredientsPill deliveryFiller ExcipientGlycerol
The invention provides enalapril maleate capsules and a preparation method thereof. The enalapril maleate capsules comprise the following raw and auxiliary materials in parts by weight: 3-5 parts of enalapril maleate, 60-80 parts of filler, 0.2-3 parts of zinc stearate and 1-3 parts of glycerol distearate. The preparation method comprises the following steps: 1) uniformly mixing enalapril maleate and the filler in an equivalently increasingly adding manner, and screening the mixture through a 100-mesh sieve for later use; and 2) uniformly mixing the powder obtained in the step 1) with zinc stearate and glycerol distearate in prescription amounts in an equivalently increasingly adding manner, screening the mixture through a 100-mesh sieve, and tabletting the dry powder to obtain the enalapril maleate capsules. The capsules prepared from simple raw and auxiliary materials are high in stability and high in dissolving rate.
Owner:HUAYI PHARMA ANHUI CO LTD
Method for preparing enalapril maleate tablets
InactiveCN109350733AGuaranteed storage stabilitySimple preparation processDipeptide ingredientsInorganic non-active ingredientsMedicineEnalapril Maleate
The invention relates to a method for preparing enalapril maleate tablets, and belongs to the field of pharmaceutical preparations. The method for preparing the stable enalapril maleate tablets is discovered pertinently for the problems of increase of related substances in enalapril maleate tablet long-term storage procedures and instable quality of products. The method for preparing the enalaprilmaleate tablets has the advantages that the method is simple, industrial production can be facilitated, and the quality of products can be guaranteed.
Owner:SHANDONG POLYTECHNIC COLLEGE +1
A kind of pharmaceutical composition for treating chronic heart failure and its application
ActiveCN108524762BDialectically accurate and completeSignificant effectOrganic active ingredientsDipeptide ingredientsSide effectRadix Ophiopogonis
The invention relates to a drug composition for treating chronic cardiac failure and application thereof. The drug composition comprises a traditional Chinese medicine composition, Enalapril Maleate-Folate tablets and metoprolol tablets. The traditional Chinese medicine composition is prepared from rehmannia roots, radix aconiti lateralis preparata, cassia twigs, radix ophiopogonis, Chinese yam, dogwood, the fruit of Chinese magnoliavine, Codonopsis pilosula, white poria and rhizoma alismatis. The invention further provides application of the traditional Chinese medicine for preparing medicinefor treating chronic cardiac failure. The drug composition has the advantages that the selected traditional Chinese medicines and the ratio are carefully screened, and the effect is remarkable; the preparation method is simple, and the drug composition is convenient for a patient to use; the drug effect is high, no toxic or side effect is caused, no adverse reaction is caused, the clinical symptoms of the patient suffering from chronic cardiac failure can be obviously improved, the heart rate variability of the patient is regulated, the good clinic effect is achieved, and the good applicationprospect is achieved.
Owner:上海市静安区中医医院
Separate detection method of ACEI-contained composition and relevant substances
PendingCN110320288AEfficient separationImprove stabilityComponent separationPhosphateGradient elution
The invention provides an analytic detection method for simultaneous determination of enalapril maleate-folate and relevant substances thereof. According to the method, gradient elution is performed through a high-performance liquid chromatograph by using octyl bonded silica gel as a filler and using a phosphate buffer solution with pH ranging from 2.0 to 3.0 and acetonitrile as mobile phases, wherein detection wavelength ranges from 210nm to 220nm, and column temperature ranges from 40 DEG C to 60 DEG C. Through the method, effective separation of all impurities is realized by the adoption ofgradient elution, the separation degree at each absorption peak is greater than 5, feeding precision is good, and RSD is smaller than 1%; and the method is good in durability, and the system applicable solution is good in stability.
Owner:NANJING YOUKE BIOLOGICAL MEDICAL RES +3
A kind of preparation method of enalapril maleate
ActiveCN109021064BReduce pollutionStrengthen labor protectionPeptide preparation methodsPeptides with abnormal peptide linkDisodium phosphateHydrogen phosphate
The invention discloses a preparation method of enalapril maleate, which comprises dissolving disodium hydrogen phosphate in water, adding dichloromethane, N-[(S)-1-ethoxycarbonyl-3-phenylpropyl] ‑L‑alanine, dripping triphosgene solution at room temperature generates key intermediate N‑[(S)‑1‑ethoxycarbonyl‑3‑phenylpropyl]‑L‑alanine‑N‑carboxylic acid anhydride, and then Condensation with L-proline and salification of maleic acid can produce crude enalapril maleate, which can be purified with high purity enalapril maleate after one water purification. The preparation method of the invention fully utilizes the theory of atomic economy, and is easy to operate, low in cost and pollution-free. It is suitable for large-scale industrial production; and after only one refinement, the chromatographic purity can reach more than 99.7%, and the total yield is more than 50%. In addition, the preparation method has mild reaction conditions, less pollution, high yield and product purity, and is more suitable for industrial production.
Owner:YANGTZE RIVER PHARM GRP CO LTD
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