Local delivery eye medicine composition

Abstract

The invention provides an application of etimicin and pharmacologically acceptable salt or inclusion compounds thereof in preparation of a local eye medicine or medicine composition for preventing ortreating eye diseases, xerophthalmia or dry eye syndromes, caused by conjunctivitis, angular blepharitis, keratitis, scleritis, trachoma and sensitive bacterium infection, of people or mammals. Eye preparations comprise eye drops, eye gel and the like. The medicine has better safety and effectiveness in a certain range.

Description

technical field [0001] The present invention relates to the technical field of medicine, and in particular provides a topical etimicin ophthalmic agent for preventing or treating conjunctivitis, canthal blepharitis, trachoma, keratitis, dry eye disease or dry eye syndrome or dry eye syndrome, etc. Pharmaceutical composition and its preparation and use. Background technique [0002] Etimicin is an aminoglycoside drug developed in China, and it is currently listed as the fourth-generation semi-synthetic water-soluble aminoglycoside antibiotics internationally (document: Chaudhary M1, Kesava Naidu G, Kumar S, PayasiA. Comparative antibacterial activity of A novel semisynthetic antibiotic: etimicin sulphate and other aminoglycosides. World J Microbiol Biotechnol. 2012Dec; 28(12): 3365-71.), its mechanism of action is to inhibit the normal protein synthesis of sensitive bacteria, and its ear and kidney toxicity is low. The subacute toxicity tests of etimicin by research institut...

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Problems solved by technology

[0008] A drug may exhibit different effects and toxic reactions after being administered by different routes of administration or administration sites. One route of administration is effective, but another route of administration is ineffective or poorly effective, or different drugs are administered in different The toxicity in the route of administration is different, which is very common in pharmacy. At present, gatifloxacin and moxifloxacin, which are administered orally or intravenously, have been clearly used for the treatment of ophthalmic diseases (document 1 , Chen Zuji, the application research progress of gatifloxacin in ophthalmology, Chinese Journal of Optometry & Ophthalmology, 2006, 8(6):400-402; Document 2, Chen Zuji; broad-spectrum and high-efficiency new fluoroquinolone antibacterial Moxifloxacin and its application in ophthalmology, Ophthalmology Research, Chinese Ophthalmic Research, 2005 06 period: 656-659;), however, cephalexin and cefadroxil can only be taken orally and cannot be injected or the effect is very poor. Trixone sodium and cefminox sodium can only be administered by injection, but cannot be administered orally or are almost ineffective. Local administration such as cromolyn sodium eye drops or sprays is effective in the treatment of conjunctivitis, allergies or asthma, etc., which are popular and commonly used in the world Oral tablets or capsules that are convenient to carry are worthless; typical but not widely known examples may also include: Spectinomycin hydrochloride, an aminoglycoside, has much higher toxicity when injected intravenously than intramuscularly , resulting in the drug not being administered intravenously at therapeutic doses but only intramuscularly

However, the current open literature does not report whether etimicin is sufficient for the treatment of ophthalmic diseases or the clinical efficacy or the toxicity of local administration, etc. etimicin sulfate is currently used for the treatment of systemic infectious diseases in the form of injection administration. There are reports of topical drug treatment, but its curative effect and local toxicity are unknown, and its curative effect or adverse reactions at different doses, or toxicity or irritation to the retina or cornea, etc., cannot be inferred from intravenous administration. The toxicity of the eye is strong or weak, and the toxic effects of drugs on the eye are diverse and complex

The eye is the window to the human soul and one of the most important organs of animals. The cornea of ​​the eye is very sensitive to drugs. Once the exposure to chemical substances is uncomfortable or causes serious adverse reactions, the result of a slight difference in production is likely to cause serious adverse reactions Or blindness, etc. Perfluoropropane gas for ophthalmology still has unexplained severe blinding adverse reactions after passing the inspection, resulting in dozens of blindness

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