{"id":16504,"date":"2025-10-21T11:09:21","date_gmt":"2025-10-21T04:09:21","guid":{"rendered":"https:\/\/nhathuocngocanh.com\/bp\/?p=16504"},"modified":"2025-10-21T11:09:21","modified_gmt":"2025-10-21T04:09:21","slug":"irbesartan","status":"publish","type":"post","link":"https:\/\/nhathuocngocanh.com\/bp\/irbesartan\/","title":{"rendered":"Irbesartan"},"content":{"rendered":"<p><em>(Ph. Eur. monograph 2465)<\/em><\/p>\n<p>C<sub>25<\/sub>H<sub>28<\/sub>N<sub>6<\/sub>O 428.5 138402-11-6<\/p>\n<p><strong>Action and use<\/strong><\/p>\n<p>Angiotensis II (AT<sub>1<\/sub>) receptor antagonist.<\/p>\n<p><strong>Preparation<\/strong><\/p>\n<p>Irbesartan Tablets<\/p>\n<h2>DEFINITION<\/h2>\n<p>2-Butyl-3-[[2\u2032-(1H-tetrazol-5-yl)[1,1\u2032-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one.<\/p>\n<h3>Content<\/h3>\n<p>99.0 per cent to 101.0 per cent (anhydrous substance).<\/p>\n<h2>CHARACTERS<\/h2>\n<h3>Appearance<\/h3>\n<p>White or almost white, crystalline powder.<\/p>\n<h3>Solubility<\/h3>\n<p>Practically insoluble in water, sparingly soluble in methanol, slightly soluble in methylene chloride.<\/p>\n<p>It shows polymorphism (5.9).<\/p>\n<h2>IDENTIFICATION<\/h2>\n<p>Infrared absorption spectrophotometry (2.2.24).<\/p>\n<p>Comparison: irbesartan CRS.<\/p>\n<p>If the spectra obtained in the solid state show differences, dissolve the substance to be examined and the reference substance separately in methanol R, evaporate to dryness at 60 \u00b0C and record new spectra using the residues.<\/p>\n<h2>TESTS<\/h2>\n<h3>Appearance of solution<\/h3>\n<p>The solution is clear (2.2.1) and not more intensely coloured than reference solution B7 (2.2.2, Method II).<\/p>\n<p>Dissolve 0.50 g in a mixture of 1 volume of 2 M sodium hydroxide R and 9 volumes of methanol R2 and dilute to 10 mL with the same mixture of solvents.<\/p>\n<h3>Impurity B<\/h3>\n<p>Liquid chromatography (2.2.29). Prepare the solutions immediately before use.<\/p>\n<p>Test solution: Dissolve 0.100 g of the substance to be examined in the mobile phase and dilute to 5.0 mL with the mobile phase.<\/p>\n<p>Reference solution: Dissolve 25.0 mg of sodium azide R (sodium salt of impurity B) in the mobile phase and dilute to 100.0 mL with the mobile phase. Dilute 0.25 mL of the solution to 200.0 mL with the mobile phase.<\/p>\n<p>Precolumn (used to prevent saturation of the column with irbesartan):<\/p>\n<p>\u2014 size: l = 0.05 m, \u00d8 = 4 mm;<\/p>\n<p>\u2014 stationary phase: strongly basic anion-exchange resin for chromatography R (8.5 \u03bcm).<\/p>\n<p>Column:<\/p>\n<p>\u2014 size: l = 0.25 m, \u00d8 = 4 mm;<\/p>\n<p>\u2014 stationary phase: strongly basic anion-exchange resin for chromatography R (8.5 \u03bcm).<\/p>\n<p>Mobile phase: 4.2 g\/L solution of sodium hydroxide R in carbon dioxide-free water R.<\/p>\n<p>Flow rate: 1.0 mL\/min.<\/p>\n<p>Detection: Conductivity detector with a sensitivity of 3 \u03bcS; use a self-regenerating anion suppressor.<\/p>\n<p>Neutralisation of the eluent: Either chemical or electrochemical:<\/p>\n<p>\u2014 chemical: by continuous countercurrent circulation in a neutralising micromembrane, performed before detection:<\/p>\n<p>\u2014 neutralising solvent: 0.025 M sulfuric acid;<\/p>\n<p>\u2014 flow rate: 10 mL\/min;<\/p>\n<p>\u2014 pressure: about 100 kPa.<\/p>\n<p>\u2014 electrochemical: 300 mA (for example).<\/p>\n<p>Injection 200 \u03bcL; after each injection of the test solution, rinse the precolumn with a mixture of mobile phase and methanol R (40:60 V\/V) for 10 min; equilibrate to initial conditions as necessary; a switch valve can be used to avoid disconnecting the precolumn from the column.<\/p>\n<p>Run time: 25 min.<\/p>\n<p>Retention time: Impurity B = about 14 min.<\/p>\n<p>System suitability: Reference solution:<\/p>\n<p>\u2014 signal-to-noise ratio: minimum 10 for the peak due to impurity B.<\/p>\n<p>Limit:<\/p>\n<p>\u2014 impurity B: not more than the area of the corresponding peak in the chromatogram obtained with the reference solution (10 ppm).<\/p>\n<h3>Related substances<\/h3>\n<p>Liquid chromatography (2.2.29).<\/p>\n<p>Buffer solution pH 3.2 Mix 5.5 mL of phosphoric acid R and 950 mL of water for chromatography R and adjust to pH 3.2 with triethylamine R.<\/p>\n<p>Test solution: Dissolve 50 mg of the substance to be examined in methanol R2 and dilute to 50.0 mL with the same solvent.<\/p>\n<p>Reference solution (a): Dilute 1.0 mL of the test solution to 100.0 mL with methanol R2. Dilute 1.0 mL of this solution to 10.0 mL with methanol R2.<\/p>\n<p>Reference solution (b): Dissolve 5 mg of the substance to be examined and 5 mg of irbesartan impurity A CRS inmethanol R2 and dilute to 10 mL with the same solvent. Dilute 1 mL of the solution to 10 mL with methanol R2.<\/p>\n<p>Column:<\/p>\n<p>\u2014 size: l = 0.25 m, \u00d8 = 4 mm;<\/p>\n<p>\u2014 stationary phase: end-capped octadecylsilyl silica gel for chromatography R (5 \u03bcm).<\/p>\n<p>Mobile phase: acetonitrile R1, buffer solution pH 3.2 (33:67 V\/V).<\/p>\n<p>Flow rate: 1.0 mL\/min.<\/p>\n<p>Detection: Spectrophotometer at 220 nm.<\/p>\n<p>Injection: 10 \u03bcL.<\/p>\n<p>Run time: 1.4 times the retention time of irbesartan.<\/p>\n<p>Identification of impurities: Use the chromatogram obtained with reference solution (b) to identify the peak due to impurity A.<\/p>\n<p>Relative retention: With reference to irbesartan (retention time = about 23 min): impurity A = about 0.7.<\/p>\n<p>System suitability: Reference solution (b):<\/p>\n<p>\u2014 resolution: minimum 3.0 between the peaks due to impurity A and irbesartan.<\/p>\n<p>Limits:<\/p>\n<p>\u2014 impurity A: not more than 1.5 times the area of the principal peak in the chromatogram obtained with reference solution (a) (0.15 per cent);<\/p>\n<p>\u2014 unspecified impurities: for each impurity, not more than the area of the principal peak in the chromatogram obtained with reference solution (a) (0.10 per cent);<\/p>\n<p>\u2014 total: not more than twice the area of the principal peak in the chromatogram obtained with reference solution (a) (0.2 per cent);<\/p>\n<p>\u2014 disregard limit: 0.5 times the area of the principal peak in the chromatogram obtained with reference solution (a) (0.05 per cent).<\/p>\n<h3>Water (2.5.12)<\/h3>\n<p>Maximum 0.5 per cent, determined on 1.00 g.<\/p>\n<h3>Sulfated ash (2.4.14)<\/h3>\n<p>Maximum 0.1 per cent, determined on 1.0 g.<\/p>\n<h2>ASSAY<\/h2>\n<p>Dissolve 0.300 g in 50 mL of anhydrous acetic acid R. Titrate with 0.1 M perchloric acid, determining the end-point potentiometrically (2.2.20).<\/p>\n<p>1 mL of 0.1 M perchloric acid is equivalent to 42.85 mg of C<sub>25<\/sub>H<sub>28<\/sub>N<sub>6<\/sub>O.<\/p>\n<h2>IMPURITIES<\/h2>\n<p>Specified impurities A, B.<\/p>\n<p><img loading=\"lazy\" decoding=\"async\" class=\"alignnone size-medium wp-image-16802\" src=\"https:\/\/nhathuocngocanh.com\/bp\/wp-content\/uploads\/2025\/10\/2-247-300x163.jpg\" alt=\"Irbesartan\" width=\"300\" height=\"163\" srcset=\"https:\/\/nhathuocngocanh.com\/bp\/wp-content\/uploads\/2025\/10\/2-247-300x163.jpg 300w, https:\/\/nhathuocngocanh.com\/bp\/wp-content\/uploads\/2025\/10\/2-247-1024x555.jpg 1024w, https:\/\/nhathuocngocanh.com\/bp\/wp-content\/uploads\/2025\/10\/2-247-768x416.jpg 768w, https:\/\/nhathuocngocanh.com\/bp\/wp-content\/uploads\/2025\/10\/2-247.jpg 1200w\" sizes=\"auto, (max-width: 300px) 100vw, 300px\" \/><\/p>\n<p>A. 1-(pentanoylamino)-N-[[2\u2032-(1H-tetrazol-5-yl)[1,1\u2032-biphenyl]-4-yl]methyl]cyclopentane-1-carboxamide,<\/p>\n<p>B. N<sub>3<\/sub><sup>&#8211;<\/sup>\u00a0 : trinitride (azide).<\/p>\n","protected":false},"excerpt":{"rendered":"<p>(Ph. Eur. monograph 2465) C25H28N6O 428.5 138402-11-6 Action and use Angiotensis II (AT1) receptor antagonist. Preparation Irbesartan Tablets DEFINITION 2-Butyl-3-[[2\u2032-(1H-tetrazol-5-yl)[1,1\u2032-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one. Content 99.0 per cent to 101.0 per cent (anhydrous substance). CHARACTERS Appearance White or almost white, crystalline powder. Solubility Practically insoluble in water, sparingly soluble in methanol, slightly soluble in methylene chloride. It shows polymorphism&#8230;<\/p>\n","protected":false},"author":4,"featured_media":16801,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[174],"tags":[],"class_list":["post-16504","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-medicinal-substances"],"acf":[],"_links":{"self":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/16504","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/users\/4"}],"replies":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/comments?post=16504"}],"version-history":[{"count":3,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/16504\/revisions"}],"predecessor-version":[{"id":16809,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/16504\/revisions\/16809"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media\/16801"}],"wp:attachment":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media?parent=16504"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/categories?post=16504"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/tags?post=16504"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}