{"id":31042,"date":"2025-11-12T16:58:31","date_gmt":"2025-11-12T09:58:31","guid":{"rendered":"https:\/\/nhathuocngocanh.com\/bp\/?p=31042"},"modified":"2025-11-12T16:58:31","modified_gmt":"2025-11-12T09:58:31","slug":"vardenafil-hydrochloride-trihydrate","status":"publish","type":"post","link":"https:\/\/nhathuocngocanh.com\/bp\/vardenafil-hydrochloride-trihydrate\/","title":{"rendered":"Vardenafil Hydrochloride Trihydrate"},"content":{"rendered":"

Edition: BP 2025 (Ph. Eur. 11.6 update)<\/p>\n

Action and use<\/strong><\/p>\n

Selective inhibitor of cyclic GMP-specific phosphodiesterase type V with vasodilator action; treatment of erectile dysfunction.<\/p>\n

Preparations<\/strong><\/p>\n

Vardenafil Orodispersible Tablets Vardenafil Tablets<\/p>\n

DEFINITION<\/h2>\n
2-[2-Ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate.<\/p>\n
Content<\/strong><\/p>\n
98.0 per cent to 102.0 per cent (anhydrous substance).<\/p>\n
CHARACTERS<\/h2>\n
Appearance<\/h3>\n
White or slightly brown or yellow powder.<\/p>\n
Solubility<\/h3>\n
Slightly soluble in water, freely soluble in anhydrous ethanol, practically insoluble in heptane.<\/p>\n
IDENTIFICATION<\/h2>\n
A. Infrared absorption spectrophotometry (2.2.24).<\/p>\n
Comparison\u00a0 vardenafil hydrochloride CRS.<\/p>\n
B. Water (see Tests).<\/p>\n
C. It gives reaction (a) of chlorides (2.3.1).<\/p>\n
TESTS<\/h2>\n
Related substances<\/h3>\n
Liquid chromatography (2.2.29). Protect the solutions from light. Solvent mixture acetonitrile R, mobile phase A (20:80 V\/V).<\/p>\n
Test solution (a) Dissolve 50.0 mg of the substance to be examined in 20 mL of acetonitrile R and dilute to 100.0 mL with mobile phase A.<\/p>\n
Test solution (b)\u00a0 Dilute 15.0 mL of test solution (a) to 50.0 mL with the solvent mixture.<\/p>\n
Reference solution (a) Dissolve 50.0 mg of vardenafil hydrochloride CRS in 20 mL of acetonitrile R and dilute to 100.0 mL with mobile phase A. Dilute 15.0 mL of the solution to 50.0 mL with the solvent mixture.<\/p>\n
Reference solution (b) Dilute 1.0 mL of test solution (a) to 100.0 mL with the solvent mixture. Dilute 1.0 mL of this solution to 10.0 mL with the solvent mixture.<\/p>\n
Reference solution (c)\u00a0 Dissolve 5 mg of vardenafil for system suitability CRS (containing impurity A) in 2 mL of acetonitrile R and dilute to 10 mL with mobile phase A.<\/p>\n
Column:<\/p>\n
\u2014 size: l = 0.25 m, \u00d8 = 3.0 mm;<\/p>\n
\u2014 stationary phase: end-capped polar-embedded octadecylsilyl amorphous organosilica polymer R (5 \u00b5m);<\/p>\n
\u2014 temperature: 45 \u00b0C.<\/p>\n
Mobile phase:<\/p>\n
\u2014 mobile phase A: solution containing 0.7 g\/L of disodium hydrogen phosphate dihydrate R and 1.3 g\/L of potassium dihydrogen phosphate R;<\/p>\n
\u2014 mobile phase B: acetonitrile for chromatography R;<\/p>\n\n\n\n\n\n\n
Time (min)<\/strong><\/td>\n Mobile phase A (per cent V\/V)<\/strong><\/td>\n Mobile phase B (per cent V\/V)<\/strong><\/td>\n<\/tr>\n
0 – 2<\/td>\n 80<\/td>\n 20<\/td>\n<\/tr>\n
2 – 22<\/td>\n 80 \u2192 25<\/td>\n 20 \u2192 75<\/td>\n<\/tr>\n
22 – 27<\/td>\n 25<\/td>\n 75<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n
Flow rate\u00a0 0.5 mL\/min.<\/p>\n
Detection\u00a0 Spectrophotometer at 242 nm.<\/p>\n
Injection\u00a0 10 \u00b5L of test solution (a) and reference solutions (b) and (c).<\/p>\n
Identification of impurities Use the chromatogram supplied with vardenafil for system suitability CRS and the chromatogram obtained with reference solution (c) to identify the peak due to impurity A.<\/p>\n
Relative retention\u00a0 With reference to vardenafil (retention time = about 16 min): impurity A = about 0.8.<\/p>\n
System suitability\u00a0 Reference solution (c):<\/p>\n
\u2014 resolution: minimum 5.0 between the peaks due to impurity A and vardenafil.<\/p>\n
Calculation of percentage contents:<\/p>\n
\u2014 for each impurity, use the concentration of vardenafil hydrochloride trihydrate in reference solution (b).<\/p>\n
Limits:<\/p>\n
\u2014 impurity A: maximum 0.15 per cent;<\/p>\n
\u2014 unspecified impurities: for each impurity, maximum 0.10 per cent;<\/p>\n
\u2014 total: maximum 0.3 per cent;<\/p>\n
\u2014 reporting threshold: 0.05 per cent.<\/p>\n
Sulfates (2.4.13)<\/strong><\/p>\n
Maximum 400 ppm.<\/p>\n
Suspend 0.5 g in 20 mL of a 5.15 g\/L solution of hydrochloric acid R and stir for 15 min. Filter if complete dissolution is not obtained.<\/p>\n
Water (2.5.12)<\/strong><\/p>\n
8.8 per cent to 10.5 per cent, determined on 60.0 mg.<\/p>\n
Sulfated ash (2.4.14)<\/strong><\/p>\n
Maximum 0.1 per cent, determined on 1.0 g.<\/p>\n
ASSAY<\/h2>\n
Liquid chromatography (2.2.29) as described in the test for related substances with the following modification.<\/p>\n
Injection\u00a0 10 \u00b5L of test solution (b) and reference solution (a).<\/p>\n
Calculate the percentage content of C_{23<\/sub>H_{33<\/sub>ClN_{6<\/sub>O_{4<\/sub>S taking into account the assigned content of vardenafil hydrochloride CRS.<\/p>\n}}}}
IMPURITIES<\/h2>\n
Specified impurities\u00a0 A.<\/em><\/p>\n
Other detectable impurities (the following substances would, if present at a sufficient level, be detected by one or other of the tests in the monograph. They are limited by the general acceptance criterion for other\/unspecified impurities and\/or by the general monograph Substances for pharmaceutical use (2034). It is therefore not necessary to identify these impurities for demonstration of compliance. See also 5.10. Control of impurities in substances for pharmaceutical use) B, C.<\/em><\/p>\n
A. 2-[2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5,7-dimethylimidazo[5,1-f][1,2,4]triazin-4(3H)-one,<\/p>\n
B. 4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)benzenesulfonic acid,<\/p>\n
C. 2,2\u2032-[piperazine-1,4-diylbis[(sulfonyl)(4-ethoxybenzene-1,3-diyl)]]bis[5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin- 4(3H)-one].<\/p>\n","protected":false},"excerpt":{"rendered":"
Edition: BP 2025 (Ph. Eur. 11.6 update) Action and use Selective inhibitor of cyclic GMP-specific phosphodiesterase type V with vasodilator action; treatment of erectile dysfunction. Preparations Vardenafil Orodispersible Tablets Vardenafil Tablets DEFINITION 2-[2-Ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate. Content 98.0 per cent to 102.0 per cent (anhydrous substance). CHARACTERS Appearance White or slightly brown or yellow powder. Solubility…<\/p>\n","protected":false},"author":5,"featured_media":31043,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[174],"tags":[],"class_list":["post-31042","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\/31042","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\/5"}],"replies":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/comments?post=31042"}],"version-history":[{"count":2,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/31042\/revisions"}],"predecessor-version":[{"id":31049,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/31042\/revisions\/31049"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media\/31043"}],"wp:attachment":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media?parent=31042"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/categories?post=31042"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/tags?post=31042"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}

Time (min)<\/strong><\/td>\n	Mobile phase A (per cent V\/V)<\/strong><\/td>\n	Mobile phase B (per cent V\/V)<\/strong><\/td>\n<\/tr>\n
0 – 2<\/td>\n	80<\/td>\n	20<\/td>\n<\/tr>\n
2 – 22<\/td>\n	80 \u2192 25<\/td>\n	20 \u2192 75<\/td>\n<\/tr>\n
22 – 27<\/td>\n	25<\/td>\n	75<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n Flow rate\u00a0 0.5 mL\/min.<\/p>\n Detection\u00a0 Spectrophotometer at 242 nm.<\/p>\n Injection\u00a0 10 \u00b5L of test solution (a) and reference solutions (b) and (c).<\/p>\n Identification of impurities Use the chromatogram supplied with vardenafil for system suitability CRS and the chromatogram obtained with reference solution (c) to identify the peak due to impurity A.<\/p>\n Relative retention\u00a0 With reference to vardenafil (retention time = about 16 min): impurity A = about 0.8.<\/p>\n System suitability\u00a0 Reference solution (c):<\/p>\n \u2014 resolution: minimum 5.0 between the peaks due to impurity A and vardenafil.<\/p>\n Calculation of percentage contents:<\/p>\n \u2014 for each impurity, use the concentration of vardenafil hydrochloride trihydrate in reference solution (b).<\/p>\n Limits:<\/p>\n \u2014 impurity A: maximum 0.15 per cent;<\/p>\n \u2014 unspecified impurities: for each impurity, maximum 0.10 per cent;<\/p>\n \u2014 total: maximum 0.3 per cent;<\/p>\n \u2014 reporting threshold: 0.05 per cent.<\/p>\n Sulfates (2.4.13)<\/strong><\/p>\n Maximum 400 ppm.<\/p>\n Suspend 0.5 g in 20 mL of a 5.15 g\/L solution of hydrochloric acid R and stir for 15 min. Filter if complete dissolution is not obtained.<\/p>\n Water (2.5.12)<\/strong><\/p>\n 8.8 per cent to 10.5 per cent, determined on 60.0 mg.<\/p>\n Sulfated ash (2.4.14)<\/strong><\/p>\n Maximum 0.1 per cent, determined on 1.0 g.<\/p>\n ASSAY<\/h2>\n Liquid chromatography (2.2.29) as described in the test for related substances with the following modification.<\/p>\n Injection\u00a0 10 \u00b5L of test solution (b) and reference solution (a).<\/p>\n Calculate the percentage content of C_{23<\/sub>H_{33<\/sub>ClN_{6<\/sub>O_{4<\/sub>S taking into account the assigned content of vardenafil hydrochloride CRS.<\/p>\n}}}} IMPURITIES<\/h2>\n Specified impurities\u00a0 A.<\/em><\/p>\n Other detectable impurities (the following substances would, if present at a sufficient level, be detected by one or other of the tests in the monograph. They are limited by the general acceptance criterion for other\/unspecified impurities and\/or by the general monograph Substances for pharmaceutical use (2034). It is therefore not necessary to identify these impurities for demonstration of compliance. See also 5.10. Control of impurities in substances for pharmaceutical use) B, C.<\/em><\/p>\n A. 2-[2-ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5,7-dimethylimidazo[5,1-f][1,2,4]triazin-4(3H)-one,<\/p>\n B. 4-ethoxy-3-(5-methyl-4-oxo-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-2-yl)benzenesulfonic acid,<\/p>\n C. 2,2\u2032-[piperazine-1,4-diylbis[(sulfonyl)(4-ethoxybenzene-1,3-diyl)]]bis[5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin- 4(3H)-one].<\/p>\n","protected":false},"excerpt":{"rendered":" Edition: BP 2025 (Ph. Eur. 11.6 update) Action and use Selective inhibitor of cyclic GMP-specific phosphodiesterase type V with vasodilator action; treatment of erectile dysfunction. Preparations Vardenafil Orodispersible Tablets Vardenafil Tablets DEFINITION 2-[2-Ethoxy-5-[(4-ethylpiperazin-1-yl)sulfonyl]phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate. Content 98.0 per cent to 102.0 per cent (anhydrous substance). CHARACTERS Appearance White or slightly brown or yellow powder. Solubility…<\/p>\n","protected":false},"author":5,"featured_media":31043,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[174],"tags":[],"class_list":["post-31042","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\/31042","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\/5"}],"replies":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/comments?post=31042"}],"version-history":[{"count":2,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/31042\/revisions"}],"predecessor-version":[{"id":31049,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/31042\/revisions\/31049"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media\/31043"}],"wp:attachment":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media?parent=31042"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/categories?post=31042"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/tags?post=31042"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}

Appearance<\/h3>\nWhite or slightly brown or yellow powder.<\/p>\n

Solubility<\/h3>\nSlightly soluble in water, freely soluble in anhydrous ethanol, practically insoluble in heptane.<\/p>\n

IDENTIFICATION<\/h2>\nA. Infrared absorption spectrophotometry (2.2.24).<\/p>\nComparison\u00a0 vardenafil hydrochloride CRS.<\/p>\nB. Water (see Tests).<\/p>\nC. It gives reaction (a) of chlorides (2.3.1).<\/p>\n

TESTS<\/h2>\n

Appearance<\/h3>\n
White or slightly brown or yellow powder.<\/p>\n

Solubility<\/h3>\n
Slightly soluble in water, freely soluble in anhydrous ethanol, practically insoluble in heptane.<\/p>\n

IDENTIFICATION<\/h2>\n
A. Infrared absorption spectrophotometry (2.2.24).<\/p>\n
Comparison\u00a0 vardenafil hydrochloride CRS.<\/p>\n
B. Water (see Tests).<\/p>\n
C. It gives reaction (a) of chlorides (2.3.1).<\/p>\n