Erythromycin ethylsuccinate, English name, Chinese alias: erythromycin ethyl succinate, erythromycin succinate, erythromycin ethyl succinate, erythromycin ethylsuccinate, erythromycin ethylsuccinate, western medicine.Commonly used pharmaceutical preparations include granules, tablets, capsules, etc.
This product is erythromycin ethyl succinate.Calculated as anhydrous substance, the potency per 1mg shall not be less than 765 erythromycin units.
character
This product is white powder or crystalline powder;Odorless and tasteless.
This product is easily soluble in absolute ethanol, acetone or chloroform, slightly soluble in ether, and almost insoluble in water.
identify
(1) Take about 5mg of this product, add 3-5 drops each of the saturated methanol solution of hydroxylamine hydrochloride and the saturated methanol solution of sodium hydroxide, heat it on the water bath to generate bubbles, cool it, add hydrochloric acid solution (4.5 → 100) to make it acidic, add 0.5ml of ferric chloride test solution, and the solution turns purple red.
(2) Take this product and erythromycin ethylsuccinate standard, add acetone to prepare a solution containing 4mg each in 1ml, test according to the thin-layer chromatography conditions under the item of related substances, take 10 μ l each of the above two solutions, and dot them on the same thin-layer plate respectively. The position and color of the main spot of the test solution should be the same as that of the standard solution.
(3) The infrared absorption spectrum of this product should be consistent with the reference spectrum (Figure 1059 of Pharmaceutical Infrared Spectrum Collection).If found at 1260cm-1If the absorption peak at is not consistent with the control map, take an appropriate amount of this product, dissolve it in absolute ethanol, evaporate it on a water bath, place it in a phosphorus pentoxide dryer and dry it under reduced pressure, and then determine[2]。
inspect
PH
Take this product, add water to make a suspension containing 10mg per 1ml, take the supernatant, and determine according to the law (Appendix VI H, Part II, Pharmacopoeia 2010 Edition). The pH value should be 6.0~8.5.
Related substances
Take this product, precisely weigh it, add acetone to quantitatively prepare a solution containing 4mg per 1ml as the test solution;Take erythromycin standard, weigh it precisely, add acetone to prepare a solution containing 0.2mg per 1ml quantitatively as the control solution.Test according to thin layer chromatography (Appendix Ⅴ B, Part II of Pharmacopoeia, 2010 Edition), take 10 μ l of each of the above two solutions, dab them on the same silica gel G thin layer plate respectively, use trichloromethane ethanol 15% ammonium acetate solution (85:15:1), adjust the pH value to 7.0 with ammonia solution when in use temporarily, place them in the separation funnel, shake and stand them, take the lower layer as the developing agent, develop them, and dry them in air,Spray color developing solution (take 0.5ml of p-methoxybenzaldehyde, add 10ml of glacial acetic acid, 85ml of methanol and 5ml of sulfuric acid, and mix), heat it at 110 ℃ until spots appear.If the test solution shows erythromycin spots, its color shall not be deeper than the color of the spots at the corresponding positions shown in the control solution.
water content
Take an appropriate amount of this product, add 10% imidazole anhydrous methanol solution to dissolve it, and measure it according to the moisture determination method (Appendix VIII M, Method A, Part II, Pharmacopoeia 2010 Edition). The moisture content should not exceed 3.0%.
Ignition residue
Not more than 0.5% (Appendix Ⅷ N, Part II, Pharmacopoeia 2010).
Assay
Accurately weigh an appropriate amount of this product, add ethanol (add 4ml ethanol every 10mg according to erythromycin ethylsuccinate) to dissolve it, dilute it quantitatively with phosphate buffer (pH 7.8) to make a solution containing about 500 units per 1ml, and place it at room temperature for 16 hours or at 40 ℃ for 6 hours to make the hydrolysis complete;Take another 25mg of erythromycin standard, precisely weigh it, add 12.5ml of ethanol to dissolve it, use phosphate buffer solution (pH 7.8) to make a solution containing 500 units per 1ml, and measure it according to the item of erythromycin under the Antibiotic Microbiological Test Method (Appendix XI A of Pharmacopoeia Volume II, 2010 Edition, Tube dish Method or Turbidity Method).1000 erythromycin unit is equivalent to 1mg of Cthirty-sevenHsixty-sevenNOthirteen[2]。
Pharmacopoeia of the People's Republic of China (2010)[2]
Drug description
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classification
Antibiotics>Macrolides
Dosage form
1. Tablets: 0.1g, 0.125g;
2. Particles: 0.05g, 0.1g, 0.125g, 0.25g.
pharmacological action
Erythromycin ethylsuccinate in the treatment of diphtheria
This product belongs to macrolide antibiotics, which is ethyl succinate of erythromycin, and is more stable than erythromycin in gastric acid.It has antibacterial activity against Staphylococcus (except for methicillin resistant strains), Streptococcus and Gram positive bacteria in each group.[3]
Pharmacokinetics
Erythromycin ethylsuccinate is easy to be absorbed by oral administration, the drug is stable in gastric acid, and is absorbed in the intestinal tract in the form of matrix and ester.Erythromycin ethylsuccinate 500mg was taken orally on an empty stomach, and the blood concentration reached the peak after 0.5-2.5 hours.After drug absorption, except for cerebrospinal fluid and brain tissue, it is widely distributed in various tissues and body fluids, especially in liver, bile and spleen, where the concentration is higher (can be more than ten to ten times higher than the blood concentration).The drug is not easy to penetrate the blood cerebrospinal fluid barrier. When the meninges are inflamed, the concentration in cerebrospinal fluid is only 10% of the blood drug concentration.Erythromycin ethylsuccinate can enter fetal blood circulation and breast milk.Erythromycin ethylsuccinate is metabolized into inactive metabolite by liver.Drugs are mainly concentrated in the liver and discharged from bile to carry out intestinal hepatic circulation, and drug accumulation may occur in patients with liver function damage.About 2% - 5% of the oral dose is discharged from the body through glomerular filtration, and the rest is discharged through feces.The half-life of the drug is about 1.4~2.0h, and the half-life of patients with renal function damage is relatively prolonged.
indication
1. Mycoplasma pneumonia.
2. Newborn conjunctivitis and infant pneumonia caused by chlamydia trachomatis.
11. Long term prevention of rheumatic fever and prevention of endocarditis.
12. Campylobacter jejuni enteritis, gonorrhea, syphilis, acne, etc.
Usage and dosage
Oral, 1.6g per day for adults, divided into 2~4 times.Legionellosis should be used in large quantities, 0.4~1.0g each time, 4 times a day.The daily dose for adults should not exceed 4g.Children take 7.5~12.5 mg/kg orally by weight 4 times a day;Or twice a day, 15-25mg/kg each time;In case of severe infection, the daily dose can be doubled and taken four times.Children with pertussis take 10~12.5 mg/kg orally four times a day for 14 days..
Adverse reactions
Hepatotoxic reactions after taking this product are more common than taking other erythromycin preparations;It can cause gastrointestinal reactions: nausea, vomiting, anorexia, abdominal distention, diarrhea, rash, drug fever, headache and pseudomembranous colitis in individual cases.Tinnitus and hearing damage may occur when the dosage is too large;It can cause acute pancreatitis and granulocytopenia.
taboo
This product can enter the milk, and lactating women should use it carefully.
It is forbidden for patients with chronic liver disease, those with liver function damage and pregnant women.
matters needing attention
1. Cross allergy: When patients are allergic to one macrolide, they may also be allergic to other macrolides.
2. Effect of drugs on pregnancy: erythromycin ethylsuccinate can enter the fetal circulation through the placenta. Although there is no evidence in animal experiments that erythromycin is teratogenic, it is still advisable to weigh the advantages and disadvantages when pregnant women use it.
3. The influence of drugs on the test value or diagnosis: (1) Erythromycin ethylsuccinate can interfere with the fluorescence measurement of the Higerty method, causing a false increase in the measured value of urinary catecholamine;(2) A few patients may have elevated serum alkaline phosphatase, bilirubin, alanine aminotransferase and aspartate aminotransferase after treatment.
4. Liver function should be routinely monitored during long-term drug use;Erythromycin ethylsuccinate can accumulate when liver function is damaged, so the blood concentration level should be monitored when large doses of drugs are used.
5. Generally, patients with renal function decline need not reduce the dosage, but the dosage of this product should be appropriately reduced for those with severe renal function damage.
Drug interaction
1. Erythromycin ethylsuccinate can inhibit the metabolism of carbamazepine when used together with carbamazepine, leading to the increase of the blood concentration of carbamazepine and toxic reaction;Moreover, carbamazepine can reduce the efficacy of erythromycin ethylsuccinate through liver microsomal oxidase.
2. The combination of erythromycin ethylsuccinate and cyclosporine can promote the absorption of cyclosporine and interfere with its metabolism. The clinical manifestations are abdominal pain, hypertension and liver dysfunction.
3. The combination of erythromycin ethylsuccinate and xanthines (except for dihydroxypropyltheophylline) can reduce the liver clearance of aminophylline, leading to the increase of serum aminophylline concentration and (or) the increase of toxic reaction.
4. Erythromycin ethylsuccinate combined with lovastatin can inhibit the metabolism of lovastatin and increase its blood concentration, which may cause rhabdomyolysis.
5. The combination of erythromycin ethylsuccinate and other hepatotoxic drugs may enhance hepatotoxicity.
6. The combination of erythromycin ethylsuccinate and digoxin can clear the intestinal flora that can inactivate digoxin, thus leading to the intestinal liver circulation of digoxin, and increasing the blood concentration of digoxin, leading to toxic reactions.
7. The combination of erythromycin ethylsuccinate, astemizole, terfenadine and other antihistamines can increase cardiac toxicity and cause arrhythmia.
8. Erythromycin ethylsuccinate combined with ergotamine tartrate can cause acute ergot poisoning (such as peripheral vasospasm).
9. The application of erythromycin ethylsuccinate in patients taking warfarin for a long time can lead to the prolongation of prothrombin time, thus increasing the risk of bleeding.
10. Erythromycin ethylsuccinate is antagonistic to chloramphenicol and lincomycin.
11. The combination of erythromycin ethylsuccinate and β - lactam drugs can reduce their antibacterial activities.
Expert comments
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In China, 1530 patients with upper respiratory tract infection were treated with erythromycin ethylsuccinate, 300mg per time for adults and 12.5mg/kg per time for children, 3-4 times per day. The treatment course was 9 days for the elderly and 2 days for the short.After treatment, 1388 cases were cured, 96 cases were effective, and the total effective rate was 97%. In another report, 2070 patients with respiratory system infection were treated with erythromycin ethylsuccinate, 500 mg per time for adults, 3 times per day, and 30~50 mg/kg per day for children. The effective rates for upper respiratory tract infection, bronchiectasis, and bronchopneumonia were 97%, 91.5%, and 92.9%, respectively.Erythromycin ethylsuccinate is tasteless, stable in gastric juice, and can be made into a variety of oral preparations for children and adults.The clinical indications are the same as erythromycin, but the blood concentration in the body is high and the antibacterial activity is strong. It is the first choice drug resistant to infections caused by Staphylococcus aureus and hemolytic streptococcus[4]。
