Cyproheptadine hydrocloride
Cyproheptadine hydrochloride
CAS: 969-33-5
Molecular Formula: C21H22ClN
Cyproheptadine hydrocloride - Names and Identifiers
Cyproheptadine hydrocloride - Physico-chemical Properties
| Molecular Formula | C21H22ClN |
| Molar Mass | 323.86 |
| Melting Point | 254-256.5 °C(Solv: ethanol (64-17-5); ethyl ether (60-29-7)) |
| Solubility | ethanol: soluble |
| Color | Crystals from EtOH/Et2O |
| Storage Condition | Inert atmosphere,Room Temperature |
| Use | Cyproheptadine HCl is the Cyproheptadine hydrochloride form and is a histamine receptor antagonist that acts on the 5-HT2 receptor with an IC50 of 0.6 nM. |
Cyproheptadine hydrocloride - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | TM7050000 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 orl-rat: 295 mg/kg DRUGAY 6,340,82 |
Cyproheptadine hydrocloride - Standard
Authoritative Data Verified Data
This product is 1-methyl -4-(5h-dibenzo [a,d] cycloheptriene -5-subunit) piperidine hydrochloride sesquihydrate. The content of C21H21N • HCl shall not be less than 98.5% calculated as anhydrous.
Last Update：2024-01-02 23:10:35
Cyproheptadine hydrocloride - Trait
Authoritative Data Verified Data
- This product is white to yellowish crystalline powder; Almost odorless.
- This product is soluble in methanol, dissolved in chloroform, slightly soluble in ethanol, slightly soluble in water, almost insoluble in ether.
Last Update：2022-01-01 15:35:42
Cyproheptadine hydrocloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.088 ml | 15.439 ml | 30.878 ml |
| 5 mM | 0.618 ml | 3.088 ml | 6.176 ml |
| 10 mM | 0.309 ml | 1.544 ml | 3.088 ml |
| 5 mM | 0.062 ml | 0.309 ml | 0.618 ml |
Last Update：2024-01-02 23:10:35
Cyproheptadine hydrocloride - Differential diagnosis
Authoritative Data Verified Data
- take this product, add anhydrous ethanol to dissolve and dilute to make a solution containing about 16ug per lml, and measure by UV-Vis spectrophotometry (General 0401), there is a maximum absorption at a wavelength of 286nm and a minimum absorption at a wavelength of 264nm; The ratio of the absorbance at a wavelength of 286nm to the absorbance at a wavelength of 264nm should be 1.6 to 1.8.
- The infrared absorption spectrum of this product should be consistent with that of the control (Spectrum set 404).
- this product of saturated aqueous solution chloride identification (1) of the reaction (General 0301).
Last Update：2022-01-01 15:35:42
Cyproheptadine hydrocloride - Exam
Authoritative Data Verified Data
acidity
take this product l.Og, add water 25ml, shake, add methyl red indicator solution 1 drop, with sodium hydroxide titration solution (0.lmol/L) titration to the solution yellow, consumption of sodium hydroxide titration solution (0.lmol/L) not over 0.15.
Related substances
take an appropriate amount of this product, add mobile phase A to dissolve and dilute to make A solution containing about 2mg per 1ml as A test solution; Take 1ml for precision measurement and put it in A 100ml measuring flask, dilute to the scale with mobile phase A, shake well, take 1ml accurately, put it in A 10ml measuring flask, dilute to the scale with mobile phase A, shake well, and use it as A control solution; Take impurity I about 2mg, in A 100ml measuring flask, add an appropriate amount of mobile phase A to dissolve, add 1ml of test solution, dilute to the scale with mobile phase A, and shake well to serve as A system applicable solution. According to the high performance liquid chromatography (General 0512) test, using octyl silane bonded silica gel as filler, potassium dihydrogen phosphate buffer (take potassium dihydrogen phosphate 6.12g, add water to dissolve, adjust pH to 4.5 with phosphoric acid, dilute to ML with water-acetonitrile (6:4) as mobile phase A, potassium dihydrogen phosphate buffer-acetonitrile (4:6) as mobile Phase B, the gradient elution was carried out according to the following table, and the detection wavelength was 230nm. Take the system applicable solution 10 u1, inject human liquid chromatography, record the chromatogram, the separation degree of impurity I peak and cyproheptadine peak should be greater than 7.0. The sample solution and the control solution are respectively injected into the liquid chromatograph to record the chromatogram. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 1.5 times (0.15%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 5 times (0.5%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which were 0.5 times smaller than the main peak area of the control solution were ignored.
moisture
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 7.0% ~ 9.0%.
ignition residue
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
Heavy metals
The residue left under the item of taking the ignition residue shall not contain more than 20 parts per million of heavy metal when examined by law (General rule 0821, Law II).
Last Update：2022-01-01 15:35:43
Cyproheptadine hydrocloride - Content determination
Authoritative Data Verified Data
take this product about 0.3g, precision weighing, add anhydrous formic acid 10ml and acetic anhydride 40ml, according to the potential titration method (General rule 0701 ), 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 32.39mg of C21H21N-HCl.
Last Update：2022-01-01 15:35:43
Cyproheptadine hydrocloride - Category
Authoritative Data Verified Data
antihistamines.
Last Update：2022-01-01 15:35:44
Cyproheptadine hydrocloride - Storage
Authoritative Data Verified Data
light shielding, sealed storage.
Last Update：2022-01-01 15:35:44
Cyproheptadine hydrocloride - Cyproheptadine Hydrochloride Tablets
Authoritative Data Verified Data
This product contains anhydrous cyproheptadine hydrochloride (C21H21N • HCl) should be the label amount of 93.0% ~ 107.0%.
trait
This product is white tablet.
identification
- The test solution under the item of content measurement was taken, and the same results were obtained according to the item of identification (1) under the item of cyproheptadine hydrochloride.
- take an appropriate amount of fine powder of this product (about 20mg equivalent to anhydrous cyproheptadine hydrochloride), place it in a separatory funnel, Add 10ml of water and O. 1 mol / L sodium hydroxide solution 2.5ml, cyproheptadine hydrochloride was dissolved by shaking, extracted by shaking with 10ml of dichloromethane, and allowed to stand to separate layers. The dichloromethane layer was filtered through a filter covered with absorbent cotton and anhydrous sodium sulfate, the filtrate was evaporated to dryness, and the residue was taken and measured according to law (General rule 0402). The infrared absorption spectrum of this product should be consistent with the spectrum of the control (Spectrum set 404 figure).
- Take appropriate amount of fine powder of this product (about equivalent to anhydrous cyproheptadine hydrochloride 20mg ), add water 7ml, shake to dissolve cyproheptadine hydrochloride, filter, filtrate chloride identification (1) response (General rule 0301).
examination
- Content uniformity take 1 tablet of this product, put it in a 100ml measuring flask, add 2.0ml of hydrochloric acid solution (9-50), shake to disintegrate, and follow the method under the content determination item, from "add about 50ml of anhydrous ethanol", the content shall be determined according to law, and shall comply with the regulations (General rule 0941).
- dissolution: according to the method of dissolution and release determination (General rule 0931, second method), ML of 0.lmol/L hydrochloric acid solution was used as the dissolution medium, and the rotation speed was 50 rpm, operate according to law, after 30 minutes, take the appropriate amount of the solution, filter, take the filtrate as the test solution; Take the llmg of cyproheptadine hydrochloride as the reference substance, weigh it accurately, put it in a 100ml measuring flask, add an appropriate amount of ethanol, shake to dissolve, dilute to the scale with ethanol, shake well, take 2ml accurately, put it in a 100ml measuring flask, use 0.1 mol/L hydrochloric acid solution was diluted to the scale and shaken as a reference solution. According to the determination by high performance liquid chromatography (General rule 0512), with octanosilane bonded silica gel as filler, potassium dihydrogen phosphate buffer solution (take potassium dihydrogen phosphate 6.12g, add water 900ml to dissolve, the pH was adjusted to 4.5 with phosphoric acid and diluted with water to ML)-acetonitrile (60:40) as the mobile phase at the detection wavelength of 285nm. The number of theoretical plates shall not be less than 2000 based on the calculation of cyproheptadine peak, and the tailing factor shall not exceed 2.5. 25 u1 of each of the reference solution and the test solution were respectively injected into the liquid chromatograph, and the chromatograms were recorded. The dissolution amount of each tablet was calculated by the peak area according to the external standard method. The limit is 80% of the labeled amount and shall be in accordance with the provisions.
- others shall be in accordance with the relevant provisions under the item of tablets (General rule 0101).
Content determination
Take 20 tablets of this product, precision weighing, fine, precision weighing an appropriate amount (equivalent to anhydrous cyproheptadine hydrochloride 1.5 mg ), put it in a 100ml measuring flask, add hydrochloric acid solution (9-50)2.0ml, shake for 2~3 minutes, add about 50ml of anhydrous ethanol, shake for 10 minutes, dissolve cyproheptadine hydrochloride, dilute to the scale with anhydrous ethanol, shake well, centrifuge, take the supernatant as the test solution, measure the absorbance at the wavelength of 286nm according to ultraviolet-visible spectrophotometry (General rule 0401), and calculate as the absorption coefficient of C21H21N • HCl is 353, that's right.
category
with cyproheptadine hydrochloride.
specification
2mg (based on C21H21N • HCl)
storage
light shielding, sealed storage.
Last Update：2022-01-01 15:35:45
Cyproheptadine hydrocloride - Reference Information
| Introduction | cyproheptadine hydrochloride, also known as diphenylcycloheptadine, metapantin, ethylphenylcycloheptadine, A hexahydropyridine antihistamine that competes with histamine released from tissues for H1 receptors on effector cells, thereby preventing the onset of allergic reactions, relieve histamine induced spasmolysis and hyperemia, the goods have a strong H1 receptor antagonism, antihistamine effect than chlorpheniramine, promethazine strong. Mild to moderate anti-serotonin and anti-cholinergic effects. In addition, there is the role of stimulating appetite, after a certain period of time visible weight gain. |
| properties | cyproheptadine hydrochloride is a white or yellowish crystalline powder, almost odorless and slightly bitter in taste. Soluble in methanol, dissolved in chloroform, slightly soluble in ethanol, slightly soluble in water, almost insoluble in ether. |
| Clinical application | clinically cyproheptadine hydrochloride is mainly used for acute and chronic urticaria (especially cold urticaria has good effect), papular urticaria, angioedema, allergic eczema, contact dermatitis, food allergy, drug allergy, allergic rhinitis, hay fever, allergic conjunctivitis, insect sting allergy and migraine. It has a certain therapeutic effect on bronchial asthma. Can be used for Cushing's syndrome, acromegaly adjuvant therapy. It can also be used as an appetite enhancer for anorexia nervosa. Treatment of acanthosis nigricans and prevention of necrotizing pyoderma have been reported. |
| side effects | 1. Drowsiness or drowsiness, dry mouth, bitter mouth, thick sputum, constipation, etc. Rash, increased photosensitivity, hypotension, tachycardia, extrasystoles, anaphylactic shock, hemolytic anemia, leukopenia, thrombocytopenia, Fatigue, Head Pain, Sleep Initiation and Maintenance Disorders, paresthesia, convulsions, hallucinations, reports of hysteria and other adverse reactions. 2. Long-term medication may lead to increased appetite and weight gain. |
| biological activity | Cyproheptadine HCl is the hydrochloride salt form of Cyproheptadine, a histamine receptor antagonist that acts at the 5-HT2 receptor, the IC50 was 0.6 nM. |
| Target | Value |
Last Update：2024-04-09 02:00:12
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View History
Cyproheptadine hydrocloride
T Cell Receptor Peptide V.beta.8.2 (39-59) (murine)
Cyclobutanecarboxylic acid, 1-[3-(trifluoromethyl)phenyl]-
4-(2-Hydroxyethyl)piperazine-1-(2-hydroxy propanesulfonic acid)
ETHYL 5-[(4-METHOXYPHENYL)SULFANYL]-3-PHENYL-1,2,4-TRIAZINE-6-CARBOXYLATE
339991-01-4
对三氟甲氧基肉桂酸
2-甲基嘧啶基-4(3H)-酮
[5-(羟甲基)四氢呋喃-2-基]甲醇
BOC-11-AMINOUNDECANOIC ACID
T Cell Receptor Peptide V.beta.8.2 (39-59) (murine)
Cyclobutanecarboxylic acid, 1-[3-(trifluoromethyl)phenyl]-
4-(2-Hydroxyethyl)piperazine-1-(2-hydroxy propanesulfonic acid)
ETHYL 5-[(4-METHOXYPHENYL)SULFANYL]-3-PHENYL-1,2,4-TRIAZINE-6-CARBOXYLATE
339991-01-4
对三氟甲氧基肉桂酸
2-甲基嘧啶基-4(3H)-酮
[5-(羟甲基)四氢呋喃-2-基]甲醇
BOC-11-AMINOUNDECANOIC ACID