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Externally used antofloxacin medicine for local eyes or ears or noses or skins, and composition thereof

A technology for external use of drugs and compositions, applied in drug combinations, skin diseases, drug delivery, etc., can solve problems such as unsatisfactory effect of antofloxacin, worthless oral tablets or capsules, and intramuscular injection only

Inactive Publication Date: 2018-03-30
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A drug may show different effects and toxic reactions after being administered by different administration routes or administration sites, which is very common in pharmacy. Oral or intravenous administration of gatifloxacin and moxifloxacin can be used In the treatment of ophthalmic diseases [Document 1, Chen Zuji, the application research progress of gatifloxacin in ophthalmology, Journal of Optometry & Ophthalmology, Chinese Journal of Optometry & Ophthalmology, 2006, 8(6): 400-402; Document 2, Chen Zuji; Broad Spectrum Highly effective new fluoroquinolone antibacterial drug moxifloxacin and its application in ophthalmology, Ophthalmology Research, Chinese Ophthalmic Research, 2005, 06: 656-659;], however, cephalexin and cefadroxil can only be taken orally and cannot be injected The drug or the effect is very poor, ceftriaxone sodium, cefminox sodium, etc. can only be given by injection and cannot be taken orally or it is almost ineffective. Topical administration of cromolyn sodium eye drops or sprays can treat conjunctivitis or allergies or asthma etc. are effective, and are popular and commonly used drugs in the world, but the convenient oral tablets or capsules are worthless; a typical but not widely known example may also be: the toxicity of spectinomycin hydrochloride by intravenous injection is much higher than that by intramuscular injection Toxicity at the time, so that the drug can not be administered intravenously at therapeutic doses and can only be injected intramuscularly
[0015] In addition, our research found that the effect of low-dose antofloxacin is not satisfactory. In order to improve the compliance and efficacy of treatment, it is necessary to study whether antofloxacin can be used in the preparation of ophthalmic drugs or ophthalmic drugs for local administration of anti-infective diseases, etc. Obtaining valuable applications in otic medicine or skin external application, as well as suitable or valuable administration concentration or dosage or combined administration with steroidal or non-steroidal anti-inflammatory drugs, etc., etc., in On the basis of safety to improve curative effect, shorten the course of treatment, etc.

Method used

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  • Externally used antofloxacin medicine for local eyes or ears or noses or skins, and composition thereof
  • Externally used antofloxacin medicine for local eyes or ears or noses or skins, and composition thereof
  • Externally used antofloxacin medicine for local eyes or ears or noses or skins, and composition thereof

Examples

Experimental program
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preparation example Construction

[0163] In the preparation process or method of each embodiment of the present invention, in the case where the prescription of the embodiment has defined the name of each component, for the sake of simplicity, the names of each component in the prescription can be simplified or omitted.

[0164] Concentration units used in the description of the present invention have molar concentration (M) or (mol / L) or equivalent concentration (N), or percentage concentration etc., time unit can use second (s), minute (min), hour (h) Etc., volume unit can use liter (l or L), milliliter (ml), microliter (μl), mass unit can use gram (g), milligram (mg) and so on.

[0165] The appropriate amount in "appropriate amount of water for injection", "appropriate amount of sodium chloride", "appropriate amount of ethanol", etc. all refer to the appropriate small amount or the minimum amount or the optimal amount that can process the raw materials or preparations to the desired state or Optimal dosage....

Embodiment 1

[0169] Example 1 Preparation of Antofloxacin Hydrochloride Eye Drops

[0170]

[0171]

[0172] Preparation process: Take the prescribed amount of sodium hyaluronate, add it to 700ml of water for injection, heat to dissolve and let it cool, and take another antofloxacin hydrochloride and dissolve it in 200ml of water for injection, and then add the prescribed amount of boric acid, borax, taurine, poly Quaternary ammonium salt-1, stir to dissolve, then add sodium hyaluronate solution to the solution, stir and mix, adjust the pH value to 6.6 with citric acid solution and sodium hydroxide solution, adjust the pH of the solution with an appropriate amount of sodium chloride The osmotic pressure is about 306mOsmol / k, add water to the full amount, pressurize and filter through a 0.45μm microporous membrane, after the measurement is qualified, fill in 5ml / bottle, seal, sterilize at 121°C, let cool, inspect, and pack.

[0173] Take 10 bottles of the above-mentioned samples and p...

Embodiment 2

[0174] Example 2 Preparation of Antofloxacin Hydrochloride Eye Drops

[0175]

[0176] Preparation process: Take the prescribed amount of sodium hyaluronate, add it to 700ml of water for injection, heat to dissolve and let it cool, and take another antofloxacin hydrochloride and dissolve it in 200ml of water for injection, and then add the prescribed amount of sodium dihydrogen phosphate and disodium hydrogen phosphate , polyquaternium-1, stirring to dissolve, then mixing it with sodium hyaluronate solution, stirring and mixing, adjusting the pH value to 6.7 with lactic acid solution and sodium citrate solution, adjusting the pH of the solution with an appropriate amount of sodium chloride The osmotic pressure is about 306mOsmol / k, add water to the full amount, pressurize and filter through a 0.65μm microporous membrane, after the measurement is qualified, fill in 8ml / bottle, seal, sterilize at 121°C, let cool, inspect, and pack.

[0177] Take 10 bottles of the above sample...

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Abstract

The invention provides a composition containing an effective dose of antofloxacin or a pharmaceutically acceptable salt thereof or / and an effective dose of an anti-inflammatory steroid or non-steroidanti-inflammatory medicine or / and an effective dose of a water-retaining or wetting agent or an anti-xerophthalmia medicine, and an application of the composition in the preparation of an externally used antofloxacin medicine for local eyes or ears or noses or skins, used for preventing or treating conjunctivitis, angular blepharitis, keratitis, scleritis, trachoma, xerophthalmia, cataract, otitisexterna, otitis media, folliculitis and impetigo in humans or mammals. The medicine obtained in the invention has good curative effects or good therapeutic compliance.

Description

technical field [0001] The present invention relates to the technical field of medicine, and specifically provides antofloxacin or its pharmaceutically acceptable salts for the prevention or treatment of human or mammalian conjunctivitis, canthus blepharitis, trachoma, keratitis, cataract, ophthalmic perioperative Drugs or pharmaceutical compositions for topical ophthalmic or nasal or ear application, or skin external application for aseptic treatment of period, dry eye disease, otitis externa, otitis media, folliculitis, furunculosis, impetigo, trauma infection and eczema infection in the application. Background technique [0002] Antofloxacin is the first domestic innovative quinolone drug developed by the Shanghai Institute of Materia Medica for more than ten years (patent number: ZL97106728.7). It has the characteristics of long biological half-life, broad antibacterial spectrum, strong antibacterial activity, wide tissue distribution, good absorption, high bioavailabil...

Claims

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Application Information

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IPC IPC(8): A61K31/5383A61K9/00A61K45/06A61P27/02A61P27/16A61P11/02A61P29/00A61P31/02A61P31/04A61P27/12A61P17/00A61P17/02A61K9/06A61K9/08A61K31/192A61K31/198A61K31/196A61K31/416A61K31/436A61K31/56A61K31/57A61K31/573A61K31/58A61K31/7072A61K47/10A61K47/12A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44
Inventor 刘力
Owner 刘力
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