Clarithromycin sub-microemulsion injection and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparation, and in particular relates to a clarithromycin submicron emulsion injection using phospholipid compound to carry medicine and a preparation method thereof. By 100 milliliters of the injection, the clarithromycin submicron emulsion injection comprises 0.05 to 0.5 gram of clarithromycin phospholipid compound in terms of clarithromycin, 10 to 20 grams of medium chain fatty acid triglyceride, 0 to 10 grams of soybean oil for injection, 0.2 to 2 grams of soya lecithin, 0.2 to 1 gram of Pluronic F-68, 0 to 0.5 gram of Tween-80, 0.01 to 0.05 gram of L-cysteine, 0.05 to 0.3 gram of sodium oleate, 2 to 5 grams of glycerin, and 70 to 90 grams of water for injection, wherein the mass ratio of clarithromycin in the clarithromycin phospholipid compound to the soya lecithin is between 1 to 1 and 1 to 12. The clarithromycin submicron emulsion injection has the advantages that the clarithromycin submicron emulsion injection has physical and chemical properties meeting requirement of medicine use for veins, not only can sterilize at high temperature, but also has favorable physical and chemical stability for long term storage, has little stimulation to the veins, improves adaptability of a patient, and is suitable for clinical application.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, relates to a clarithromycin submicroemulsion injection loaded with a phospholipid complex and a preparation method thereof. Background technique [0002] Clarithromycin (clarithromycin) is a macrolide antibiotic developed by Taisho Pharmaceutical Company of Japan in 1981. Its chemical name is 6-O-methylerythromycin, and its chemical structure is as follows: [0003] [0004] Clarithromycin binds to the 50S subunit of the bacterial ribosome. By blocking the effect of transpeptidation and the process of mRNA translocation, it prevents the elongation of the peptide chain and inhibits the synthesis of bacterial protein, thereby producing antibacterial effects. Clarithromycin is mainly used in the treatment of local infections to treat respiratory tract infections, skin and soft tissue infections and urinary tract infections; in the treatment of digestive system diseases,...

AI Technical Summary

Problems solved by technology

The clarithromycin emulsion obtained in this way also limits its sterilization method due to the presence of oleic acid and caproic acid, and does not mention how to sterilize it in the instructions

[0008] Clarithromycin is a drug that is insoluble in oil and water. There is no report in the prior art that this type of drug is prepared into a submicroemulsion injection. The injection was successfully prepared, and all its indicators met the requirements of the State Food and Drug Administration for new drug research and development

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