Edition: BP 2025 (Ph. Eur. 11.6 update)<\/p>\n
Action and use<\/strong><\/p>\n Dopamine receptor antagonist; neuroleptic.<\/p>\n Preparation<\/strong><\/p>\n Zuclopenthixol Acetate Injection<\/p>\n Zuclopenthixol Acetate is (Z)-2-4-[3-(2-chlorothioxanthene-9-ylidene)propyl]piperazin-1-ylethyl acetate. It contains not less than 98.0% and not more than 102.0% of C24<\/sub>H27<\/sub>ClN2<\/sub>O2<\/sub>S, calculated with reference to the dried substance.<\/p>\n A yellowish, viscous oil.<\/p>\n Very slightly soluble in water; very soluble in dichloromethane, in ethanol (96%) and in ether.<\/p>\n A. The light absorption of a 0.0015% w\/v solution in ethanol (96%), Appendix II B, in the range 210 to 350 nm exhibits two maxima at 230 and 268 nm. The absorbances at the maxima are about 1.18 and 0.51 respectively.<\/p>\n B. The infrared absorption spectrum, Appendix II A, is concordant with the reference spectrum of zuclopenthixol acetate\u00a0(RS 363).<\/p>\n Carry out the method for thin-layer chromatography, Appendix III A, using the following solutions protected from light.<\/p>\n (1) 0.250% w\/v of the substance being examined in dichloromethane.<\/p>\n (2) Dilute 1 volume of solution (1) to 100 volume with dichloromethane, further dilute 1 volume of this solution to 10 volumes with the same solvent.<\/p>\n (3) Dilute 1 volume of solution (2) to 2 volumes with dichloromethane.<\/p>\n (4) 0.00050% w\/v of 2- chlorothioxanthone BPCRS in dichloromethane.<\/p>\n (5) 0.000625% w\/v of zuclopenthixol hydrochloride BPCRS in a solution containing 3 drops of diethylamine in dichloromethane.<\/p>\n (a) Use as the coating silica gel F254 (Merck silica gel 60 F254 plates are suitable).<\/p>\n (b) Use an unlined tank and the mobile phase as described below.<\/p>\n (c) Apply 4 \u03bcL of each solution.<\/p>\n (d) Develop the plate to 10 cm.<\/p>\n (e) After removal of the plate, allow it to dry in air, spray with a mixture of equal volumes of sulfuric acid and absolute ethanol, heat at 110\u00b0 for 5 minutes and examine under ultraviolet light (365 nm) immediately.<\/p>\n 10 volumes of diethylamine, 40 volumes of dichloromethane and 50 volumes of cyclohexane.<\/p>\n In the chromatogram obtained with solution (1):<\/p>\n any spot corresponding to 2-chlorothioxanthone is not more intense than the spot in the chromatogram obtained with solution (4) (0.2%);<\/p>\n any spot corresponding to zuclopenthixol is not more intense than the spot in the chromatogram obtained with solution (5) (0.25%);<\/p>\n any other secondary spot is not more intense than the spot in the chromatogram obtained with solution (2) (0.1%);<\/p>\n not more than three other secondary spots are more intense than the spot in the chromatogram obtained with solution (3) (0.05%).<\/p>\n Carry out the method for liquid chromatography, Appendix III D, using the following solutions in dichloromethane protected from light.<\/p>\n (1) 0.040% w\/v of the substance being examined.<\/p>\n (2) 0.00046% w\/v of trans-clopenthixol acetate dihydrochloride BPCRS (equivalent to 0.00040% w\/v of trans-clopenthixol acetate).<\/p>\n (3) 0.020% w\/v of the substance being examined and 0.023% w\/v of trans-clopenthixol acetate dihydrochloride BPCRS.<\/p>\n (a) Use stainless steel column (25 cm x 4.6 mm) packed with silica gel for chromatography (5 \u00b5m) (Spherisorb S 5W is suitable).<\/p>\n (b) Use isocratic elution and the mobile phase described below.<\/p>\n (c) Use a flow rate of 2 mL per minute.<\/p>\n (d) Use ambient temperature.<\/p>\n (e) Use a detection wavelength of 254 nm.<\/p>\n (f) Inject 15 \u03bcL of each solution.<\/p>\n 0.03 volume of 13.5M ammonia, 45 volumes of dichloromethane, 45 volumes of heptane and 50 volumes of acetonitrile.<\/p>\n The test is not valid unless, in the chromatogram obtained with solution (3), the resolution between the principal peaks is at least 2.6.<\/p>\n In the chromatogram obtained with solution (1), the area of any peak corresponding to trans-clopenthixol acetate is not greater than the area of the peak in the chromatogram obtained with solution (2) (1%).<\/p>\n When dried at 60\u00b0 at a pressure not exceeding 0.7 kPa for 3 hours, loses not more than 0.4% of its weight, Appendix XI D. Use 1 g.<\/p>\n Not more than 0.1%, Appendix IX A.<\/p>\n Dissolve 0.2 g in 50 mL of anhydrous acetic acid and carry out Method I for non-aqueous titration, Appendix VIII A, determining the end point potentiometrically. Each mL of 0.1M perchloric acid VS is equivalent to 22.15 mg of C24<\/sub>H27<\/sub>ClN2<\/sub>O2<\/sub>S.<\/p>\n Zuclopenthixol Acetate should be protected from light and stored at a temperature not exceeding -20\u00b0.<\/p>\n A. trans-clopenthixol acetate(trans-isomer),<\/p>\n B. 2-chlorothioxanthone,<\/p>\n C. zuclopenthixol.<\/p>\n","protected":false},"excerpt":{"rendered":" Edition: BP 2025 (Ph. Eur. 11.6 update) Action and use Dopamine receptor antagonist; neuroleptic. Preparation Zuclopenthixol Acetate Injection DEFINITION Zuclopenthixol Acetate is (Z)-2-4-[3-(2-chlorothioxanthene-9-ylidene)propyl]piperazin-1-ylethyl acetate. It contains not less than 98.0% and not more than 102.0% of C24H27ClN2O2S, calculated with reference to the dried substance. CHARACTERISTICS A yellowish, viscous oil. Very slightly soluble in water; very…<\/p>\n","protected":false},"author":5,"featured_media":32020,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[174],"tags":[],"class_list":["post-32018","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\/32018","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=32018"}],"version-history":[{"count":2,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/32018\/revisions"}],"predecessor-version":[{"id":32033,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/32018\/revisions\/32033"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media\/32020"}],"wp:attachment":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media?parent=32018"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/categories?post=32018"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/tags?post=32018"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}DEFINITION<\/h2>\n
CHARACTERISTICS<\/h2>\n
IDENTIFICATION<\/h2>\n
TESTS<\/h2>\n
Related substances<\/h3>\n
CHROMATOGRAPHIC CONDITIONS<\/h4>\n
MOBILE PHASE<\/h4>\n
LIMITS<\/h4>\n
trans-Isomer<\/h3>\n
CHROMATOGRAPHIC CONDITIONS<\/h4>\n
MOBILE PHASE<\/h4>\n
SYSTEM SUITABILITY<\/h4>\n
LIMITS<\/h4>\n
Loss on drying<\/h3>\n
Sulfated ash<\/h3>\n
ASSAY<\/h2>\n
STORAGE<\/h2>\n
IMPURITIES<\/h2>\n