{"id":26052,"date":"2025-11-05T10:34:33","date_gmt":"2025-11-05T03:34:33","guid":{"rendered":"https:\/\/nhathuocngocanh.com\/bp\/?p=26052"},"modified":"2025-11-05T10:34:33","modified_gmt":"2025-11-05T03:34:33","slug":"oxybuprocaine-hydrochloride","status":"publish","type":"post","link":"https:\/\/nhathuocngocanh.com\/bp\/oxybuprocaine-hydrochloride\/","title":{"rendered":"Oxybuprocaine Hydrochloride"},"content":{"rendered":"

(Ph. Eur. monograph 1251)<\/p>\n

C_{17<\/sub>H_{29<\/sub>ClN_{2<\/sub>O_{3<\/sub>\u00a0 \u00a0 \u00a0 \u00a0 \u00a0344.9\u00a0 \u00a0 \u00a0 \u00a0 \u00a0 \u00a05987-82-6<\/p>\n}}}}

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

Local anaesthetic.<\/p>\n

Preparation<\/strong><\/p>\n

Oxybuprocaine Eye Drops<\/p>\n

DEFINITION<\/h2>\n
2-(Diethylamino)ethyl 4-amino-3-butoxybenzoate hydrochloride.<\/p>\n
Content<\/h3>\n
98.5 per cent to 101.5 per cent (dried substance).<\/p>\n
CHARACTERS<\/h2>\n
Appearance<\/h3>\n
White or almost white, crystalline powder or colourless crystals.<\/p>\n
Solubility<\/h3>\n
Very soluble in water, freely soluble in ethanol (96 per cent).<\/p>\n
It shows polymorphism (5.9).<\/p>\n
IDENTIFICATION<\/h2>\n
First identification: B, D.<\/p>\n
Second identification: A, C, D.<\/p>\n
A. Melting point (2.2.14): 158 \u00b0C to 162 \u00b0C.<\/p>\n
B. Infrared absorption spectrophotometry (2.2.24).<\/p>\n
Preparation: Discs.<\/p>\n
Comparison: oxybuprocaine hydrochloride CRS.<\/p>\n
If the spectra obtained show differences, dissolve the substance to be examined and the reference substance separately in methanol R, evaporate to dryness and record new spectra using the residues.<\/p>\n
C. Thin-layer chromatography (2.2.27).<\/p>\n
Test solution: Dissolve 40 mg of the substance to be examined in methanol R and dilute to 10 mL with the same solvent.<\/p>\n
Reference solution (a): Dissolve 40 mg of oxybuprocaine hydrochloride CRS in methanol R and dilute to 10 mL with the same solvent.<\/p>\n
Reference solution (b): Dissolve 20 mg of procaine hydrochloride R in reference solution (a) and dilute to 5 mL with reference solution (a).<\/p>\n
Plate: TLC silica gel F254 plate R.<\/p>\n
Mobile phase: anhydrous formic acid R, methanol R, water R, ethyl acetate R (10:15:15:60 V\/V\/V\/V).<\/p>\n
Application: 5 \u03bcL.<\/p>\n
Development: Over a path of 10 cm.<\/p>\n
Drying: In a current of warm air for 10 min.<\/p>\n
Detection: Spray with dimethylaminobenzaldehyde solution R7 and examine in ultraviolet light at 254 nm.<\/p>\n
System suitability: Reference solution (b):<\/p>\n
\u2014 the chromatogram shows 2 clearly separated spots.<\/p>\n
Results: The principal spot in the chromatogram obtained with the test solution is similar in position, colour and size to the principal spot in the chromatogram obtained with reference solution (a).<\/p>\n
D. Dilute 0.2 mL of solution S (see Tests) to 2 mL with water R. The solution gives reaction (a) of chlorides (2.3.1).<\/p>\n
TESTS<\/h2>\n
Solution S<\/h3>\n
Dissolve 5.0 g in carbon dioxide-free water R and dilute to 50 mL with the same solvent.<\/p>\n
Appearance of solution<\/h3>\n
Solution S is clear (2.2.1) and not more intensely coloured than reference solution Y_{5<\/sub> (2.2.2, Method II).<\/p>\n}
pH (2.2.3)<\/h4>\n
4.5 to 6.0 for solution S.<\/p>\n
Related substances<\/h3>\n
Liquid chromatography (2.2.29).<\/p>\n
Buffer solution pH 2.5: Add 6 mL of perchloric acid solution R and 12 mL of dilute phosphoric acid R to 950 mL of water R. Adjust to pH 2.5 with a 40 g\/L solution of sodium hydroxide R and dilute to 1000.0 mL with water R.<\/p>\n
Test solution: Dissolve 10.0 mg of the substance to be examined in the mobile phase and dilute to 25.0 mL with the mobile phase.<\/p>\n
Reference solution (a): Dilute 1.0 mL of the test solution to 20.0 mL with the mobile phase. Dilute 5.0 mL of this solution to 100.0 mL with the mobile phase.<\/p>\n
Reference solution (b): Mix 1.0 mL of the test solution with 1 mL of a 40 g\/L solution of sodium hydroxide R and allow to stand for 20 min. Add 1 mL of dilute phosphoric acid R and dilute to 100.0 mL with the mobile phase. Dilute 25 mL of this solution to 100.0 mL with the mobile phase.<\/p>\n
Column:<\/p>\n
\u2014 size: l = 0.15 m, \u00d8 = 3.9 mm;<\/p>\n
\u2014 stationary phase: octadecylsilyl silica gel for chromatography R1 (5 \u03bcm) with a pore size of 10 nm and a carbon loading of 19 per cent;<\/p>\n
\u2014 temperature: 35 \u00b0C.<\/p>\n
Mobile phase: acetonitrile R, buffer solution pH 2.5 (25:75 V\/V).<\/p>\n
Flow rate: 1 mL\/min.<\/p>\n
Detection: Spectrophotometer at 309 nm.<\/p>\n
Injection: 20 \u03bcL.<\/p>\n
Run time: 4 times the retention time of oxybuprocaine.<\/p>\n
Retention time: Oxybuprocaine = about 9 min.<\/p>\n
System suitability: Reference solution (b):<\/p>\n
\u2014 resolution: minimum 12 between the peaks due to oxybuprocaine and impurity B (hydrolysis product).<\/p>\n
Limits:<\/p>\n
\u2014 any impurity: for each impurity, not more than 0.4 times the area of the principal peak in the chromatogram obtained with reference solution (a) (0.1 per cent);<\/p>\n
\u2014 total: not more than the area of the principal peak in the chromatogram obtained with reference solution (a) (0.25 per cent);<\/p>\n
\u2014 disregard limit: 0.05 times the area of the principal peak in the chromatogram obtained with reference solution (a) (0.0125 per cent).<\/p>\n
Loss on drying (2.2.32)<\/h4>\n
Maximum 0.5 per cent determined on 1.000 g by drying in an oven at 105 \u00b0C.<\/p>\n
Sulfated ash (2.4.14)<\/h4>\n
Maximum 0.1 per cent, determined on 1.0 g.<\/p>\n
ASSAY<\/h2>\n
Dissolve 0.300 g in a mixture of 20 mL of anhydrous acetic acid R and 20 mL of acetic anhydride R. Titrate with 0.1 M perchloric acid, determining the end-point potentiometrically (2.2.20).<\/p>\n
1 mL of 0.1 M perchloric acid is equivalent to 34.49 mg of C_{17<\/sub>H_{29<\/sub>ClN_{2<\/sub>O_{3<\/sub>.<\/p>\n}}}}
STORAGE<\/h2>\n
Protected from light.<\/p>\n
IMPURITIES<\/h2>\n
$\"Oxybuprocaine$ <\/p>\n
A. 4-aminobenzoic acid,<\/p>\n
$\"Oxybuprocaine$ <\/p>\n
B. 4-amino-3-butoxybenzoic acid,<\/p>\n
$\"Oxybuprocaine$ <\/p>\n
C. 4-amino-3-hydroxybenzoic acid.<\/p>\n","protected":false},"excerpt":{"rendered":"
(Ph. Eur. monograph 1251) C17H29ClN2O3\u00a0 \u00a0 \u00a0 \u00a0 \u00a0344.9\u00a0 \u00a0 \u00a0 \u00a0 \u00a0 \u00a05987-82-6 Action and use Local anaesthetic. Preparation Oxybuprocaine Eye Drops DEFINITION 2-(Diethylamino)ethyl 4-amino-3-butoxybenzoate hydrochloride. Content 98.5 per cent to 101.5 per cent (dried substance). CHARACTERS Appearance White or almost white, crystalline powder or colourless crystals. Solubility Very soluble in water, freely soluble…<\/p>\n","protected":false},"author":2,"featured_media":26060,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"_acf_changed":false,"footnotes":""},"categories":[174],"tags":[],"class_list":["post-26052","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\/26052","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\/2"}],"replies":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/comments?post=26052"}],"version-history":[{"count":2,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/26052\/revisions"}],"predecessor-version":[{"id":26063,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/posts\/26052\/revisions\/26063"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media\/26060"}],"wp:attachment":[{"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/media?parent=26052"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/categories?post=26052"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/nhathuocngocanh.com\/bp\/wp-json\/wp\/v2\/tags?post=26052"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}

Content<\/h3>\n98.5 per cent to 101.5 per cent (dried substance).<\/p>\n

CHARACTERS<\/h2>\n

Appearance<\/h3>\nWhite or almost white, crystalline powder or colourless crystals.<\/p>\n

Solubility<\/h3>\nVery soluble in water, freely soluble in ethanol (96 per cent).<\/p>\nIt shows polymorphism (5.9).<\/p>\n

TESTS<\/h2>\n

Solution S<\/h3>\nDissolve 5.0 g in carbon dioxide-free water R and dilute to 50 mL with the same solvent.<\/p>\n

Appearance of solution<\/h3>\nSolution S is clear (2.2.1) and not more intensely coloured than reference solution Y5<\/sub> (2.2.2, Method II).<\/p>\n

pH (2.2.3)<\/h4>\n4.5 to 6.0 for solution S.<\/p>\n

Loss on drying (2.2.32)<\/h4>\nMaximum 0.5 per cent determined on 1.000 g by drying in an oven at 105 \u00b0C.<\/p>\n

Sulfated ash (2.4.14)<\/h4>\nMaximum 0.1 per cent, determined on 1.0 g.<\/p>\n

STORAGE<\/h2>\nProtected from light.<\/p>\n

Content<\/h3>\n
98.5 per cent to 101.5 per cent (dried substance).<\/p>\n

Appearance<\/h3>\n
White or almost white, crystalline powder or colourless crystals.<\/p>\n

Solubility<\/h3>\n
Very soluble in water, freely soluble in ethanol (96 per cent).<\/p>\n
It shows polymorphism (5.9).<\/p>\n

Solution S<\/h3>\n
Dissolve 5.0 g in carbon dioxide-free water R and dilute to 50 mL with the same solvent.<\/p>\n

Appearance of solution<\/h3>\n
Solution S is clear (2.2.1) and not more intensely coloured than reference solution Y_{5<\/sub> (2.2.2, Method II).<\/p>\n}

pH (2.2.3)<\/h4>\n
4.5 to 6.0 for solution S.<\/p>\n

Loss on drying (2.2.32)<\/h4>\n
Maximum 0.5 per cent determined on 1.000 g by drying in an oven at 105 \u00b0C.<\/p>\n

Sulfated ash (2.4.14)<\/h4>\n
Maximum 0.1 per cent, determined on 1.0 g.<\/p>\n

STORAGE<\/h2>\n
Protected from light.<\/p>\n