Name | pyrithioxin dihydrochloride |
Synonyms | bonifen Pyritinol HCl Pyrithioxine hcl Pyritinol hydrochloride PYRITINOL HYDROCHLORIDE PYRITINOL DIHYDROCHLORIDE pyritinol dihydrochloride Pyrithioxine hydrochloride PYRITHIOXIN DIHYDROCHLORIDE pyrithioxin dihydrochloride pyridin-2(1H)-one hydrochloride 3,3'-(dithiodimethylene)bis(5-hydroxy-6-methyl-4-pyridinemethanodihydrochl 5,5'-dithiodimethylenebis(2-methyl-3-hydroxy-4-hydroxymethylpyridine)dihydro 3,3'-dithiodimethylenebis(5-hydroxy-6-methyl-4-pyridinemethanol)dihydrochlor 5,5'-(disulfanediyldimethanediyl)bis[4-(hydroxymethyl)-2-methylpyridin-3-ol] 3,3'-dithiobis(methylene)bis(5-hydroxy-6-methyl-4-pyridinemethanol)dihydroch 5,5'-(disulfanediyldimethanediyl)bis[4-(hydroxymethyl)-2-methylpyridin-3-ol] dihydrochloride |
CAS | 10049-83-9 |
EINECS | 233-178-5 |
InChI | InChI=1/C5H5NO.ClH/c7-5-3-1-2-4-6-5;/h1-4H,(H,6,7);1H |
InChIKey | HRZWYHGGJOWGRI-UHFFFAOYSA-N |
Molecular Formula | C16H22Cl2N2O4S2 |
Molar Mass | 441.39 |
Melting Point | 184 °C |
Boling Point | 330.9°C at 760 mmHg |
Flash Point | 153.9°C |
Vapor Presure | 0.000117mmHg at 25°C |
Appearance | neat |
Storage Condition | Sealed in dry,Room Temperature |
WGK Germany | 2 |
RTECS | UT4900000 |
This product is 3,3 '-(dithiomethylene) BIS (5-hydroxy-6-methyl-4-pyridinmethanol) dihydrochloride monohydrate. The content of C16H20N204S2 · 2HC1 should be between 97.0% and 103.0% based on the water content.
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.266 ml | 11.328 ml | 22.656 ml |
5 mM | 0.453 ml | 2.266 ml | 4.531 ml |
10 mM | 0.227 ml | 1.133 ml | 2.266 ml |
5 mM | 0.045 ml | 0.227 ml | 0.453 ml |
take 0.10g of this product, Add 10ml of water to dissolve, check according to law (General 0631) ,pH value should be 2.0~3.5 (for injection).
take l.Og of this product, add 10ml of water to dissolve, the solution should be clear and colorless. If it is turbid, it should not be more concentrated compared with No. 1 turbidity standard solution (General 0902 method 1), orange or yellow-green standard colorimetric solution No. 5 (for oral use or comparison with yellow or yellow-green standard colorimetric solution No. 2 (for injection) (General rule 0901 method 1), shall not be deeper.
take this product, add water to dissolve and dilute to make a solution containing about 0.2 mg per lml as a test solution; Take lml 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. Test according to high performance liquid chromatography (General 0512). Silica gel was bonded with eighteen alkyl silane as filler; The mobile phase was perchloric acid solution (0.82 -1000, adjusted to pH 3.0 with triethylamine)-methanol (75:25); The detection wavelength was 295mn. The number of theoretical plates shall not be less than 2000 based on the calculation of pyritinol peak, and the separation degree between pyritinol peak and adjacent impurity peak shall meet the requirements. 20ul of the test solution and the control solution were respectively injected into the liquid chromatograph, and the chromatogram was recorded to 2 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 a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than the main peak area of the control solution (1.0%).
take this product, according to the moisture determination method (General 0832 first method 1), the moisture content should be 3.5% ~ 4.5%.
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 10 parts per million of heavy metal when examined by law (General Principles 0821, Law II).
take this product, according to the law inspection (General 1101), should comply with the provisions. (For aseptic dispensing)
take an appropriate amount of this product, precision weighing, add 0.01mol/ L hydrochloric acid solution to dissolve and quantitatively dilute to prepare a solution containing about 10ug per lml, the absorbance was measured at a wavelength of 0401 NM according to ultraviolet-visible spectrophotometry (General Rule 403), and the absorption coefficient of C16H20N204S2 · 2HC1 was calculated.
cerebral metabolism improving drugs.
light shielding, sealed storage.
This product contains pyritinol hydrochloride (C16H20N204S2 • 2HCI • H20) should be 93.0% ~ 107.0% of the label amount.
This product is white or white-like tablets or sugar-coated tablets, white or white after removing the coating.
take an appropriate amount of the fine powder of this product, and show the same reaction according to the tests (1) and (3) under the item of pyritinol hydrochloride.
should be in accordance with the relevant provisions under The tablet item (General rule 0101).
Take 20 tablets of this product (sugar-coated tablets should be removed from the coating), finely grind, accurately weigh appropriate amount (about equivalent to pyritinol hydrochloride 0.lg), put it in a 100ml measuring flask, and add O.Olmol/L hydrochloric acid solution to pyritinol hydrochloride dissolved and diluted to the scale, shake, filter, precision volume filtrate 2ml, 200ml flask, with 0.01mol/L hydrochloric acid solution to the scale, shake, UV-visible spectrophotometry (General 0401), at the wavelength of 295nm absorbance, the absorption coefficient of C16H20N204S2 · 2HC1 · H20 was calculated as 388.
with pyritinol hydrochloride.
0.lg
light shielding, sealed storage.
This product is a sterile aqueous solution of pyritinol hydrochloride. Pyritinol hydrochloride, calculated as C16H20N2O4S2 • 2HC1, shall be 93.0% ~ 107.0% of the labeled amount.
This product is colorless to yellowish clear liquid.
precision take the right amount of this product, with O.Olmol/L hydrochloric acid solution is quantitatively diluted to prepare a solution containing about 10ug of pyritinol hydrochloride (based on Cl6H20N204S2 • 2HC1) per 1 ml, which is obtained by the method under the item of pyritinol hydrochloride content determination.
with pyritinol hydrochloride.
calculated by C16H20N204S2 • 2HC1 (l)2ml:0.1g(2)2ml:0.2g (3)5ml:0.2g
light shielding, closed storage.
This product contains pyritinol hydrochloride (C16H20N204S2 • 2HCl • H20) should be 93.0% ~ 107.0% of the label amount.
The content of this product is white or white powder.
should comply with the relevant provisions under the capsule (General rule 0103).
take the contents under the difference of loading amount, mix evenly, weigh an appropriate amount (about 0.1g of pyritinol hydrochloride) accurately, put it in a 100ml measuring flask, and add 0.Olmol/L hydrochloric acid solution to pyritinol hydrochloride dissolved and diluted to the scale, shake, filtered, precision volume of filtrate continued 2ml, 200ml flask, with O.Olmol/L hydrochloric acid solution to the scale, shake, according to UV-visible spectrophotometry (General 0401), at the wavelength of 295nm absorbance, the absorption coefficient of C16H20N204S2 · 2HC1 · H20 was calculated as 388.
with pyritinol hydrochloride.
O.lg
light shielding, sealed storage.
This product is pyritinol hydrochloride sterile powder or sterile lyophilized. Based on the average loading, pyritinol hydrochloride shall be calculated as C16H20N204S2 • 2HC1 and shall be 93.0% ~ 107.0% of the labeled amount.
This product is white or off-white crystalline powder or freeze-dried loose lumps; Odorless.
take this product, according to the item of pyritinol hydrochloride identification (1), (3) test, show the same reaction.
take the contents under the difference of loading amount, mix evenly, weigh the appropriate amount accurately, and add O.Olmol/L hydrochloric acid solution is dissolved and quantitatively diluted to prepare a solution containing about 10ug of pyritinol hydrochloride (as calculated by C16H20N2O4S2 • 2HC1) per 1 ml, which is obtained according to the method under the item of pyritinol hydrochloride content determination.
with pyritinol hydrochloride.
calculated as C16H20N2O4S2 • 2HC1 (l)0.1g (2)0.2g
light shielding, closed storage.
central stimulant | pyritinol hydrochloride, also known as naofuxin, is a central stimulant. This product is a derivative of vitamin B6, which can promote the metabolism of glucose and amino acids in the brain, increase carotid blood flow, increase cerebral blood flow, and improve systemic assimilation. Mainly used for the improvement of symptoms such as headache, dizziness, insomnia, memory loss, inattention, and emotional changes in cerebral concussion syndrome, brain trauma sequelae, encephalitis and meningitis sequelae; also used for cerebral arteriosclerosis, Alzheimer's psychosis, etc. |
traits | white crystalline powder, odorless. Easily soluble in water, high temperature, alkaline solution, sunlight are easy to destroy. |
pharmacokinetics | oral administration is rapidly and completely absorbed, plasma protein binding rate is very low, and it quickly enters brain tissue and other body organs and tissues. It is mainly metabolized in the liver and excreted by the kidneys. |
pharmacological action | pyritinol hydrochloride is a derivative of vitamin B6, which is formed by connecting two molecules of vitamin B6 with disulfide bonds and has the effects of promoting intelligence and brain activation. This drug can activate the cholinergic system in the brain, increase the activity of postsynaptic cholinergic neurons in the cerebral cortex, increase the second messenger cGMP, reduce γ-aminobutyric acid, and activate dopamine in the brain to enhance the brain Tolerance to hypoxia. It can also promote glucose and amino acid metabolism in the brain and improve systemic assimilation. It can also increase carotid blood flow, improve cerebral blood flow and brain bioelectrical activity. |
clinical application | 1. it is used to improve symptoms such as dizziness, pain, insomnia, memory loss, inattention, mood changes, etc. caused by sequelae of brain trauma, encephalitis and meningitis. It is also used to improve cerebral arteriosclerosis and senile dementia mental symptoms. 2. For rheumatoid arthritis. |
adverse reactions | 1. the nervous system can occasionally cause dizziness, dizziness and headache. 2. Gastrointestinal tract can occasionally cause nausea. 3. Skin can occasionally cause rash. 4. Phlebitis and pain may occur at other injection sites, which can disappear after drug withdrawal. |
precautions | 1. contraindications are allergic to this drug. 2. Use with caution ① Liver insufficiency. ② Diabetic patients. 3. Special population (1) Children: There is still a lack of research data on children's medication. Not recommended for children. (2) the elderly: elderly patients with no special medication. (3) Pregnant women: In animal experiments, this medicine has the tendency to cause cleft lip in offspring animals, so pregnant women should use it with caution. (4) lactating women: this medicine in the milk concentration is higher, lactating women should be used with caution. |