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. |
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 |
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.
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 |
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.
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.
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 7.0% ~ 9.0%.
take l.Og of this product and check it according to law (General rule 0841). The residue left shall not exceed 0.1%.
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).
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.
antihistamines.
light shielding, sealed storage.
This product contains anhydrous cyproheptadine hydrochloride (C21H21N • HCl) should be the label amount of 93.0% ~ 107.0%.
This product is white tablet.
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.
with cyproheptadine hydrochloride.
2mg (based on C21H21N • HCl)
light shielding, sealed storage.
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 |