39 results about "Candesartan cilexitil" patented technology

The present invention provides an improved synthesis for the manufacture of candesartan and pharmaceutically acceptable salts and esters thereof as active ingredients of a medicament for the treatment of hypertension and related diseases and conditions which comprises the removal of the tetrazolyl protecting group in an organic solvent, and in the presence of a Lewis acid.

The invention relates to a candesartan cilexetil self-microemulsion soft capsule and a preparation method thereof. The soft capsule comprises capsule liquid and content medicine liquid. The preparation method is as follows: 100-130 parts of gelatin is arranged in mixing solution for swelling, wherein the mixing solution is formed by 18-30 parts of glycerol, 20-30 parts of sorbic alcohol and 100-120 parts of water; then 0.1-0.3 part of ethylparaben is added, heating is carried out until the gelatin is dissolved, the mixture is stirred uniformly and is filtered, and vacuum defoaming and heat insulation are carried out, thus obtaining the capsule liquid; 1-2 parts of candesartan cilexetil, 20-40 parts of assistant emulsifiers, 10-30 parts of oil phase and 80-100 parts of emulsifiers are mixed uniformly, and then the mixture is heated and stirred until the uniform and transparent content solution is formed; and the prepared capsule liquid and the prepared content solution the weight percentage ratio of which is 4:3 are moulded and pressed into soft capsules by rotating a mould press, and then drying and surface treatment are carried out on the soft capsules, thus obtaining the finished products. In the invention, the bioavailability of the candesartan cilexetil is improved, and the preparation method is simple relatively, the production is easy, thus the application prospect is wide.

The invention provides a method for preparing candesartan cilexetil, which can solve the problems of longer reaction route, easy remaining of toxic substances in medicines and lower total yield existing in the prior art. In the method, the candesartan cilexetil is finally prepared by using 2-amino-3-nitrobenzoic acid as an initial raw material through esterification reaction, N-alkylation reaction, nitro reduction reaction, cyclization reaction, hydrolysis reaction, esterification reaction and tetrazole protecting group deprotection reaction. The synthetic method has simple steps and high yield, greatly reduces the participation and generation of toxic products in the reaction process, reduces the release of waste and is beneficial to clean production.

The invention discloses a brand-new oral solid pharmaceutical composition. The pharmaceutical composition is an oral preparation prepared from hydrochlorothiazide, levamlodipine, candesartan cilexetil and pharmaceutically acceptable auxiliary materials. The oral preparations include but are not limited to tablets or capsules. The composition contains the following raw materials in parts by weight: 5-25 parts by weight of hydrochlorothiazide, 2.5-5 parts by weight of levamlodipine, 4-20 parts by weight of candesartan cilexetil, and 30-60 parts by weight of microcrystalline cellulose 30-60 parts by weight of compressible starch, 30-50 parts by weight of cross-linked polyvinylpyrrolidone, 1-2 parts by weight of silicon dioxide and 0.5-2 parts by weight of magnesium stearate. The medicinal composition of the invention has scientific and reasonable prescription, low auxiliary material content and high bioavailability, and is the first choice medicine for treating hypertension.

The preparation method of candesartan cilexetil and its precursor compound. The precursor compound is 2-ethoxy-1-[[2′-(1-R-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H -Benzimidazole-7-carboxylic acid 1-(cyclohexyloxycarbonyloxy)ethyl ester (III), from 2-ethoxy-1-(4'-halophenyl)methyl-1H-benzene Imidazole-7-carboxylic acid 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester (I) and 2-(1-R-1H-tetrazol-5-yl)phenylboronic acid or 2- (1-R-1H-tetrazol-5-yl) phenyl borate (II) reacts in a soluble organic reaction medium and in the presence of a catalyst and a water-soluble basic compound allowed by the Suzuki reaction get. The precursor compound can be further hydrolyzed under acidic conditions to obtain candesartan cilexetil which can be used as medicine. The method can conveniently and advantageously prepare the candesartan cilexetil compound.

The invention discloses a hydrochlorothiazide crystal and a candesartan cilexetil hydrochlorothiazide medicinal combination thereof. The characteristic peaks of the hydrochlorothiazide crystal in an X-ray powder diffraction pattern, which are measured and obtained by using a Cu-K[alpha] ray, are displayed when 2[theta] is 4.1 degrees, 8.2 degrees, 9.8 degrees, 12.1 degrees, 15.1 degrees, 16.7 degrees, 19.3 degrees, 20.0 degrees, 22.1 degrees, 23.3 degrees and 26.8 degrees. The combination comprises 4-20 parts of candesartan cilexetil, 10-15 parts of the hydrochlorothiazide crystal, 10-50 parts of pregelatinized starch, 15-35 parts of microcrystalline cellulose PH102, 10-45 parts of crosslinked polyvinylpyrrolidone and 0.5-1 part of magnesium stearate. The medicinal combination has a reasonable prescription, stable and reliable quality, and better disintegration time limit and dissolution rate; a direct powder tabletting process is adopted; the process is simple; the production period is short; the production cost is low; and the industrialized production is facilitated.

The invention relates to a brand new drug composition containing levamlodipine besylate and candesartan cilexetil and a preparation method thereof. The composition comprises the active ingredients such as levamlodipine besylate and candesartan cilexetil and pharmaceutically acceptable auxiliaries, wherein levamlodipine besylate is levamlodipine besylate crystals; and the characteristic peak in the X-ray powder diffraction pattern obtained after measuring the crystals with a Cu-Kalpha ray is displayed at 2theta, namely 8.0 degrees, 12.1 degrees, 15.4 degrees, 17.0 degrees, 19.8 degrees, 21.6 degrees, 23.0 degrees, 24.3 degrees, 25.7 degrees, 27.4 degrees, 30.7 degrees and 33.5 degrees. The drug composition and the preparation method have the following advantages: the crystals can improve the solubility of levamlodipine besylate to some extent, thus amlodipine besylate in the drug composition is dissolved out more quickly and the drug composition has a better curative effect and good stability; and the method adopts a direct powder compression technology, has the advantages of simple technology, short production period and low production cost and is easy to realize industrial production.