XYLOMETAZOLIN HYDROCHLORIDE
xylometazoline hcl
CAS: 1218-35-5
Molecular Formula: C16H25ClN2
XYLOMETAZOLIN HYDROCHLORIDE - Names and Identifiers
| Name | xylometazoline hcl |
| Synonyms | Olynth Novorin Therapin Galazolin Neo-Rinoleina Neo-Synephrine II xylometazoline hcl otrivinhydrochloride otrivinehydrochloride XYLOMETAZOLIN HYDROCHLORIDE XYLOMETAZOLINE HYDROCHLORIDE XYLOMETAZOLINE HCL (OXYMETAZOLINE EP IMPURITY B HCL) 2-(4-TERT-BUTYL-2,6-DIMETHYLBENZYL)-2-IMIDAZOLINE HYDROCHLORIDE 2-(4-tert-butyl-2,6-dimethylbenzyl)-2-imidazolinmonohydrochloride 2-(4-tert-butyl-2,6-dimethylbenzyl)-4,5-dihydro-1H-imidazol-1-ium chloride 2-[[4-(1,1-dimethylethyl)-2,6-dimethylphenyl]methyl]-4,5-dihydro-1h-imidazol |
| CAS | 1218-35-5 |
| EINECS | 214-936-4 |
| InChI | InChI=1/C16H24N2.ClH/c1-11-8-13(16(3,4)5)9-12(2)14(11)10-15-17-6-7-18-15;/h8-9H,6-7,10H2,1-5H3,(H,17,18);1H |
XYLOMETAZOLIN HYDROCHLORIDE - Physico-chemical Properties
| Molecular Formula | C16H25ClN2 |
| Molar Mass | 280.84 |
| Melting Point | 131-133 C |
| Boling Point | 394.2°C at 760 mmHg |
| Flash Point | 192.2°C |
| Solubility | DMSO 27 mg/mL;Water 56 mg/mL;Ethanol 56 mg/mL |
| Vapor Presure | 4.56E-06mmHg at 25°C |
| Appearance | White to off-white crystalline powder |
| Color | Crystals |
| Merck | 14,10086 |
| Storage Condition | 2-8°C |
| MDL | MFCD00238707 |
XYLOMETAZOLIN HYDROCHLORIDE - Risk and Safety
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | NJ2390000 |
| HS Code | 29332900 |
| Hazard Class | 6.1 |
| Packing Group | III |
| Toxicity | LD50 orl-rat: 230 mg/kg KSRNAM 5,555,71 |
XYLOMETAZOLIN HYDROCHLORIDE - Standard
Authoritative Data Verified Data
This product is 2-(4-tert-butyl-2, 6-dimethylbenzyl)-2-imidazoline hydrochloride. Based on the dry product, the content of C16H24N2 • HCl shall not be less than 99.0%.
Last Update：2024-01-02 23:10:35
XYLOMETAZOLIN HYDROCHLORIDE - Trait
Authoritative Data Verified Data
- This product is white or off-white crystalline powder; Odorless.
- This product is soluble in ethanol, soluble in water or chloroform, almost insoluble in ether.
Last Update：2022-01-01 15:35:45
XYLOMETAZOLIN HYDROCHLORIDE - Differential diagnosis
Authoritative Data Verified Data
- take about 3mg of this product, add 3ml of water to dissolve, add 1 ml of sodium nitroprusside test solution and 0.5ml of sodium hydroxide test solution, place it for 10 minutes, add 4ml of sodium bicarbonate test solution, and shake it to be purple.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 657).
- the aqueous solution of this product was chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:35:46
XYLOMETAZOLIN HYDROCHLORIDE - Exam
Authoritative Data Verified Data
acidity
take 0.50g of this product, Add 10ml of water, shake to dissolve, according to the law (General 0631),pH value should be 5.0~6.6.
Related substances
take this product, add the mobile phase to dissolve and dilute to make a solution containing about 0.5mg per lml, as a test solution; Take the appropriate amount of precision, solutions containing 1UG and 0.25ug per 1 ml were prepared as control solution (1) and control solution (2) by quantitative dilution with mobile phase. According to the high performance liquid chromatography (General 0512) test, with eighteen alkyl silane bonded silica gel as filler, 0.1% triethylamine (with glacial acetic acid to adjust the pH value to 5.0)-acetonitrile (45:55) as mobile phase, the detection wavelength was 220nm. Take about 12.5mg of this product, put it in a 25ml measuring flask, add lmol / L sodium hydroxide solution 10ml, shake, water bath heating for about 5 minutes, so as to produce N-(2-aminoethyl)-2-[4-(1, 1-dimethylethyl)-2, 6-dimethylphenyl] acetamide (impurity), cool, after 10ml of 1 mol / L hydrochloric acid solution is added and neutralized, dilute to scale with water, shake well, use 10ul as the applicable solution for the system, inject into the liquid chromatograph, record the chromatogram, the impurity I Peak (relative retention time of about 0.8) should be separated from the ciloxazoline peak by greater than 2.5. 10ul of the control solution (2) was injected into the liquid chromatograph, and the signal-to-noise ratio of the xyloazoline peak was not less than 10; 10ul of the sample solution and the control solution (1) were accurately measured, injected into the liquid chromatograph respectively, the chromatogram was recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of impurity I peak multiplied by the correction factor of 1.55 shall not be greater than the area of the main peak (0.2%) of the control solution (1), other single impurity peak area shall not be greater than the main peak area (0.2%) of the control solution (1), and the sum of other impurity peak areas shall not be greater than 2.5 times (0.5%) of the main peak area of the control solution (1). The chromatographic peaks in the chromatogram of the test solution which are smaller than the main peak area of the control solution (2) are ignored.
loss on drying
take this product, dry to constant weight at 105°C, weight loss shall not exceed 0.5% (General rule 0831).
ignition residue
not more than 0.1% (General rule 0841).
Last Update：2022-01-01 15:35:47
XYLOMETAZOLIN HYDROCHLORIDE - Content determination
Authoritative Data Verified Data
take this product about 0.22g, precision weighing, add anhydrous glacial acetic acid 60ml to dissolve, add acetic anhydride 5ml, according to the potential titration method (General rule 0701), with potassium nitrate saturated anhydrous methanol solution as salt bridge solution, with perchloric acid titration solution (0.1 mol/L) titration, and the results of the titration were corrected with a blank test. Each 1 ml perchloric acid titration solution (0.1 mol/L) corresponds to 28.08mg of C16H24N2 • HCl.
Last Update：2022-01-01 15:35:48
XYLOMETAZOLIN HYDROCHLORIDE - Category
Authoritative Data Verified Data
vasoconstrictor.
Last Update：2022-01-01 15:35:48
XYLOMETAZOLIN HYDROCHLORIDE - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 15:35:48
XYLOMETAZOLIN HYDROCHLORIDE - Xylometazoline Hydrochloride Nasal Drops
Authoritative Data Verified Data
This product shall contain 90.0% ~ 110.0% of the labeled amount of ciloxazoline hydrochloride (C16H24N2 • HCI).
trait
This product is a colorless clear liquid.
identification
- take an appropriate amount of this product (equivalent to 3mg of ciloxazoline hydrochloride), add 1 ml of sodium nitroprusside test solution and 0.5ml of sodium hydroxide test solution for 10 minutes, and add 4ml of sodium bicarbonate test solution, which should be purple after shaking.
- in the chromatogram recorded under the content determination item, the retention time of the main peak of the test solution should be consistent with the retention time of the main peak of the reference solution.
examination
- the pH value should be 5.6 to 6.6 (General 0631).
- impurity I: take an appropriate amount of this product and dilute it with water if necessary to make a solution containing 0.5mg of ciloxazoline hydrochloride per 1 ml as a test solution. Take 1 ml for precision measurement and put it in a 100ml measuring flask, as a control solution, it was diluted to the scale with water and shaken. According to the chromatographic conditions of the related substances of the hydrochloride, 10ul of the test solution and the control solution are respectively injected into the liquid chromatograph, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If there is a chromatographic peak of impurity I in the chromatogram of the test solution, the peak area multiplied by the correction factor 1.55 shall not be greater than 1.5 times (1.5%) of the main peak area of the control solution.
- others should comply with the relevant provisions under nasal preparations (General rule 0106).
Content determination
- measured by high performance liquid chromatography (General 0512).
- chromatographic conditions and system suitability test using eighteen alkyl silane bonded silica gel as filler; 0.1% triethylamine (with glacial acetic acid to adjust the pH value to 5.0)-acetonitrile (45:55) as mobile phase; the detection wavelength was 220nm. Add 10ml of 1 mol/L sodium hydroxide solution to a 25ml measuring flask, shake well, and heat with water bath for about 5 minutes to generate impurity I, after 10ml of 1 mol/L hydrochloric acid solution is added and neutralized, dilute to scale with water, shake well, use 10ul as the applicable solution for the system, inject into the liquid chromatograph, record the chromatogram, the impurity I Peak (relative retention time of about 0.8) should be separated from the ciloxazoline peak by greater than 2.5.
- precision measurement: take an appropriate amount of this product and quantitatively dilute it with water to make a solution containing about 50 tons of sulfoazoline hydrochloride per 1 ml, as a test solution, and inject the LOL into the liquid chromatograph with precision measurement, record the chromatogram; Take an appropriate amount of the reference substance of ciloxazoline hydrochloride, weigh it accurately, dissolve it with water and dilute it quantitatively to make a solution containing 50% per 1 ml, and determine it by the same method. According to the external standard method to calculate the peak area, that is.
category
The same as the same as the hydrochloride.
specification
(l ) 5ml:2.5mg ( 2 ) 5ml:5mg (3 ) 10ml:5mg (4) 10ml:1Omg
storage
sealed storage.
Last Update：2022-01-01 15:35:49
XYLOMETAZOLIN HYDROCHLORIDE - Reference Information
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
| Overview | Cylosazoline hydrochloride has the effect of directly stimulating the α1-adrenergic receptor of the nasal mucosa blood vessels and causing vasoconstriction, thereby reducing blood flow and reducing The congestion and edema caused by inflammation are clinically used to reduce the symptoms of nasal congestion caused by diseases such as acute and chronic rhinitis, sinusitis, allergic rhinitis, and hypertrophic rhinitis, it has the characteristics of fast onset, long-lasting effect and small side effects. |
| pharmacological action | this product is an imidazoline derivative, which belongs to adrenergic receptor agonist and has a special excitatory effect on α receptor. This product directly acts on the alpha receptor on the small blood vessels of the nasal mucosa to produce vasoconstriction, thereby reducing blood flow and reducing nasal mucosal congestion and edema caused by inflammation. |
| Indications | Cylosazoline hydrochloride is a new type of long-acting nasal vasoconstrictor, which can effectively relieve the congestion and swelling of the nasal mucosa. It has the advantages of fast onset, strong effect, long curative effect, and small adverse reactions. It is an ideal long-acting nasal vasoconstrictor. It is suitable for alleviating nasal congestion caused by acute and chronic rhinitis, sinusitis, allergic rhinitis, hypertrophic rhinitis and other diseases. It should be reminded that the biggest side effect of this vasoconstrictor is repeated contraction of nasal blood vessels, especially excessive spraying can easily cause rebound nasal congestion, and the elasticity of the mucous membranes or cilia in the nasal cavity is reduced. Long-term use can cause drug-induced rhinitis. Therefore, it must be used strictly according to the recommended dosage, and the maximum continuous use shall not exceed 7 days; children under 6 years old should be used under the guidance of a doctor, and generally use it continuously for no more than 5 days. If you need to continue using it, you should consult a doctor. Infants and young children's central nervous system is immature, easily affected by drugs, and the nasal mucosa is thin and tender, the blood vessels are rich, and the external drugs are quickly absorbed through the nasal mucosa, which is easy to cause poisoning, so children under 2 years old are prohibited. |
| usage and dosage | nasal drops: 10ml:5mg;10ml:10mg. Spray: 10ml:5mg;10ml:10mg. 1. Nose dripping: Adults use 0.1% solution, 2-3 drops at a time, 2 times a day; Children aged 6-12 years old use 0.05% solution, 2-3 drops at a time, 2 times a day. 2. Nasal spray: Adults spray 2~3 on one side once, once in the morning and once before going to bed. Continuous use shall not exceed 7 days. There should be intervals between long-term and extensive treatment sessions. |
| adverse reactions | 1. frequent medication is easy to cause rebound nasal congestion, and long-term use can cause drug-induced rhinitis. 2. A few people have mild burning sensation, acupuncture sensation, dry nasal mucosa, headache, dizziness, heart rate acceleration and other reactions. 3. Other similar drugs are similar and extremely rare systemic allergic reactions, such as dyspnea, angioedema, and mild or temporary visual disorders. |
| taboo | 1. atrophic rhinitis and nasal dryness are prohibited. 2. Children under 2 years old are prohibited. 3. Patients receiving monoamine oxidase inhibitors (such as isocarbazide, phenylhydrazine, isoniazid, etc.) or tricyclic antidepressants are contraindicated. 4. Those who are allergic to this drug are contraindicated. |
| Synthetic route | 1, 3-dimethyl-5-tert-butylbenzene is the starting material, and in the presence of a catalyst, it reacts with chloromethylation reagent to obtain 2, 6-dimethyl-4-tert-butyl-1-chloromethylbenzene; sodium cyanide is used for cyanidation to obtain 2, 6-Dimethyl-4-tert-butyl-1-phenylacetonitrile is then cyclized with ethylenediamine p-toluenesulfonate to obtain p-toluenesulfonate (11); the selozoline is free with alkali and then salt with hydrogen chloride to obtain selozoline hydrochloride. The shortcomings of this process route are: the market price of tert-butyl m-xylene is higher; chloromethyl ether is more toxic, has a low boiling point and a higher market price; carbon disulfide and other highly toxic solvents, and has a low boiling point. Poor reaction operability. Another synthetic route is: 2, 6-dimethyl-4-tert-butylaniline hydrochloride is used as the starting material to react with sodium nitrite, copper sulfate, and paraformaldehyde to produce 2, 6-dimethyl 4-tert-butylbenzaldehyde, which is reduced to alcohol, and then chloromethylation, hydrogenation, aminoesterification, cyclization, and salt formation to form cylosazoline hydrochloride. The synthesis route is long and the post-treatment is complicated; after analysis and comparison, the diazotization reaction in the synthesis method is generally not high in yield; and the use of thionyl chloride has a lot of pollution to the environment; it is difficult to scale up the production, and the resulting product There are many impurities and product purity. In short, the synthesis method has a long process route, cumbersome post-treatment, low yield of finished products, high production costs, and is difficult to achieve large-scale industrial production. |
| Use | is an α-adrenaline ligand agonist, which has the effect of constricting blood vessels. |
Last Update：2024-04-09 15:16:47
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View History
XYLOMETAZOLIN HYDROCHLORIDE
特班布林杂质25
2-{4-chloro-2-methyl-5-[(4-phenyl-1-piperazinyl)sulfonyl]phenoxy}acetamide
2-(PHENYLTHIO)THIOPHENE
(DIPHENYLIMINO-LAMBDA6-SULFANYL)ONE(WXC09774)
Ruthenium(2+), pentaammine(histidinato-N3)-, dichloride, monohydrochloride, (OC-6-22)- (9CI)
ETHYL 3-AMINO-3-(5-CHLORO-2-METHOXYPHENYL)PROPANOATE HYDROCHLORIDE
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693
5-Chloro-8-quinolinyl 2-(2-piperidinyl)ethylether hydrochloride
phenyl-(4-piperidinyl)methanone hydrochloride
特班布林杂质25
2-{4-chloro-2-methyl-5-[(4-phenyl-1-piperazinyl)sulfonyl]phenoxy}acetamide
2-(PHENYLTHIO)THIOPHENE
(DIPHENYLIMINO-LAMBDA6-SULFANYL)ONE(WXC09774)
Ruthenium(2+), pentaammine(histidinato-N3)-, dichloride, monohydrochloride, (OC-6-22)- (9CI)
ETHYL 3-AMINO-3-(5-CHLORO-2-METHOXYPHENYL)PROPANOATE HYDROCHLORIDE
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol GSK 690693
5-Chloro-8-quinolinyl 2-(2-piperidinyl)ethylether hydrochloride
phenyl-(4-piperidinyl)methanone hydrochloride