Inosine is an organic compound with chemical formula CtenHtwelveNfourOfiveIt is a nucleoside compound formed by the combination of hypoxanthine and ribose. It is applicable to leukopenia, thrombocytopenia, various heart diseases, acute and chronic hepatitis, cirrhosis, etc. caused by various reasons, and can also treat central retinitis, optic atrophy, etc.
Reference value for drainage parameter calculation (XlogP): None
Number of hydrogen bond donors: 4
Number of hydrogen bond receptors: 6
Number of rotatable chemical bonds: 2
Number of tautomers: 3
Topological molecular polar surface area: 129
Number of heavy atoms: 19
Surface charge: 0
Complexity: 405
Number of isotope atoms: 0
Determine the number of atomic structure centers: 4
Number of uncertain atomic structure centers: 0
Determine the number of chemical bond structure centers: 0
Number of uncertain chemical bond structure centers: 0
Number of covalent bond units: 1[2]
purpose
It is used as coenzyme medicine.Inosine is a component of ATP, coenzyme A, ribonucleic acid and deoxyribonucleic acid in the body, participating in the material metabolism and energy metabolism of the body.It can improve the level of ATP in the body, can be converted into a variety of nucleotides, and participate in protein synthesis.Inosine has good permeability to cell membrane. It can enter cells directly, transform into nucleotide, and then further transform into ATP to participate in metabolism. It can promote the recovery of liver cells, prevent fatty liver, improve the activity of various enzymes, and stimulate the body to produce antibodies.Inosine can be used as an auxiliary liver protection drug and can also be used to rescue liver coma when acute, chronic hepatitis and cirrhosis lead to abnormal liver function.[1]
Pharmacopoeia information
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essential information
This product is 9β-D-ribose hypoxanthine, calculated as dry product, containing CtenHtwelveNfourOfiveIt should be 98.0%~102.0%.
character
This product is white crystalline powder, odorless, slightly bitter in taste.
This product is slightly soluble in water, insoluble in ethanol, and easily soluble in dilute hydrochloric acid and sodium hydroxide test solution.
identify
1. Take an appropriate amount of 0.01% test solution, add equal volume of 3.5-dihydroxytoluene solution (take 0.1g of 3,5-dihydroxytoluene and ferric chloride respectively, add hydrochloric acid to make 100mL), mix well, heat in the water bath for about 10 minutes, and it will turn green.
2. 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.
3. The infrared absorption spectrum of this product should be consistent with the control spectrum (spectrum set 605 figure).
inspect
Transmittance of solution
Take 0.5g of this product, add 50mL of water to dissolve it, and measure the transmittance at the wavelength of 430nm according to the ultraviolet visible spectrophotometry (general rule 0401), which shall not be less than 98.0% (for injection).
Related substances
Determine according to the method of high performance liquid chromatography (general rule 0512).
Test solution: take this product, add water to dissolve and dilute it to make a solution containing about 0.5mg per 1mL.
Reference solution: precisely measure 1mL of the test solution, place it in a 1000mL volumetric flask, dilute it with water to the scale, and shake it up.
System suitability solution: Take about 10mg of inosine reference substance, add 1ml of 1mol/L hydrochloric acid solution at 80 ℃, heat it in a water bath for 10 minutes, cool it, add 1ml of 1mol/L sodium hydroxide solution, and add water to 50mL.
Chromatographic conditions: octadecyl silane bonded silica gel is used as the filler, methanol water (10:90) is used as the mobile phase, the detection wavelength is 248 nm, and the injection volume is 20 μ L.
System suitability requirements: in the system suitability solution chromatogram, the resolution between the inosine peak and the adjacent impurity peak should meet the requirements, and the number of theoretical plates should not be less than 2000 based on the inosine peak.
Determination method: Precisely measure the test solution and the reference solution, respectively inject them into the liquid chromatograph, and record the retention time of the chromatogram to the main component peak twice.
Limit: If there are impurity peaks in the chromatogram of the test solution, the sum of the peak areas of each impurity shall not be greater than the main peak area of the reference solution (1.0%).
Loss on drying
Take this product, dry it at 105 ℃ to constant weight, and the weight loss shall not exceed 1.0% (general rule 0831).
Ignition residue
Not more than 0.1% (for injection), or not more than 0.2% (for oral use) (General Rule 0841).
heavy metal
Take 1.0g of this product and check it according to the law (General Rule 0821, the second method). The content of heavy metals should not exceed 10% per million.
Abnormal toxicity
Take this product, add sodium chloride injection to make a solution containing 10mg per 1mL, check according to the law (general rule 1141), and give it by intravenous injection, which should meet the requirements (for injection).
Assay
Determine according to the method of high performance liquid chromatography (general rule 0512).
Test solution
Take an appropriate amount of this product, weigh it precisely, add water to dissolve it and dilute it quantitatively to make a solution containing about 20 µ g per 1mL, and shake it well.
Reference solution
Take an appropriate amount of inosine reference substance, weigh it precisely, add water to dissolve it and dilute it quantitatively to prepare a solution containing about 20 µ g per 1mL, and shake it well.
System suitability Solution, chromatographic conditions and system suitability requirements
See related substances.
Assay
Accurately measure the test solution and the reference solution, respectively inject them into the liquid chromatograph, and record the chromatogram.Calculate by peak area according to external standard method.
category
Cell metabolism improver.
Storage
Protect from light and store in an airtight manner.
preparation
1. Inosine oral solution.
2. Inosine tablets.
3. Inosine capsules.
4. Inosine injection.
5. Inosine glucose injection.
6. Inosine and sodium chloride injection.
7. Inosine for injection.[3]
Brief Introduction to Drugs
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pharmacological action
This medicine is a normal component of human body and a precursor of adenine. It can enter somatic cells directly through the cell membrane and participate in nucleic acid metabolism, energy metabolism and protein synthesis in the body.
This medicine can activate the pyruvate oxidase system, improve the activity of coenzyme A, activate the liver function, and enable the tissue cells in the state of low-energy hypoxia to continue to metabolize, contributing to the recovery of damaged liver cell function.It also participates in energy metabolism and protein synthesis.
This drug can increase ATP level and can be converted into various nucleotides.It can stimulate the production of antibodies in the body, improve the intestinal absorption of iron, activate liver function, and accelerate the repair of liver cells.It can enhance the proliferation of white blood cells.
Applicability
1. It is used to treat leukopenia and thrombocytopenia.
2. Treatment of acute hepatitis and chronic hepatitis, cirrhosis, hepatic encephalopathy.
3. It is used as an auxiliary drug for coronary atherosclerotic heart disease (coronary heart disease), myocardial infarction, rheumatic heart disease, and pulmonary heart disease.
4. It is used to prevent and reduce the toxic reaction of heart and liver caused by schistosomiasis control drugs.
5. It is used as an auxiliary drug for ophthalmic diseases (central retinitis, optic atrophy).
contraindication
It is prohibited to mix with chloramphenicol, dipyridamole and other injections.
Adverse reactions
Occasionally, stomach discomfort and mild diarrhea can be seen, and intravenous injection can cause flushing, nausea and abdominal burning sensation.
Usage and dosage
1. Oral: 0.2-0.4g per time for adults, three times a day, and the dosage can be doubled if necessary for liver diseases;Children: 0.1-0.2g each time, three times a day.
2. Intravenous injection: 0.2-0.6g each time, 1-2 times a day.
3. Intravenous drip: 0.2-0.6g per time for adults, diluted with 5% glucose injection or 20mL of normal saline for injection, 1-2 times a day;Children: 0.1-0.2g each time, once a day.
matters needing attention
This product cannot be compatible with chloramphenicol, dipyridamole, thiopental sodium, whey acid and other injections.
Drug interaction
Inosine cannot be compatible with whey acid, chloramphenicol, dipyridamole, thiopental sodium and other injections.
security information
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Safety terminology
S24/25：Avoid contact with skin and eyes.
Avoid skin and eye contact.
Risk terminology
R36/37/38：Irritating to eyes, respiratory system and skin.
