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Compound aminoglycoside drug composition for local administration

An aminoglycoside, topical drug delivery technology, used in drug combinations, pharmaceutical formulations, drug delivery, etc., can solve problems such as the worthlessness of oral tablets or capsules, unknown efficacy or adverse reactions, toxicity or irritation, and only intramuscular injection.

Inactive Publication Date: 2018-04-03
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] 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; a broad-spectrum and 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 but cannot be injected or the effect is very poor, and ceftriaxone Sodium pine and cefminox sodium can only be administered by injection, but cannot be administered orally or are almost ineffective when administered orally. Topical administration such as sodium cromoglycate eye drops or sprays is effective in the treatment of conjunctivitis, allergies or asthma, and is a popular and commonly used drug in the world. , but the convenient oral tablets or capsules are worthless; typical but not widely known examples may also include: the toxicity of aminoglycoside spectinomycin hydrochloride is much higher than that of intramuscular injection, As a result, the drug cannot be given intravenously at therapeutic doses and can only be given intramuscularly
However, there is currently no public literature reporting the combined administration of etimicin and dexamethasone for the treatment of ophthalmic diseases or the clinical efficacy or toxicity of local administration, and its efficacy or adverse effects at different dosages are unknown. Reaction or toxicity or irritation to the retina or cornea, etc., the toxic effects of drugs on the eye are diverse and complex
The eye is the window of 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. In recent years, there are still unexplained severe blinding adverse reactions of perfluoropropane gas for ophthalmic use in the case of passing the inspection, resulting in dozens of blindness

Method used

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  • Compound aminoglycoside drug composition for local administration
  • Compound aminoglycoside drug composition for local administration
  • Compound aminoglycoside drug composition for local administration

Examples

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preparation example Construction

[0201] In the preparation process of each embodiment of the present invention, in the case where the prescription of the embodiment has defined the names of the components, for the sake of simplicity, the names of the components in the prescription can be simplified or omitted.

[0202] 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.

[0203] 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 Optimum dosage.

Embodiment 1

[0206] The preparation of embodiment 1 compound etimicin in situ gel eye drops

[0207] Prescription: etimicin sulfate (calculated as etimicin) 3.0g, pranoprofen 0.5g, poloxamer 188 50g, trehalose 10g, disodium hydrogen phosphate 4.2g, lysine 3g, editidine 0.3 g of disodium acid, appropriate amount of 2M citric acid solution and sodium hydroxide solution, and dilute the volume to 1000 ml with water for injection.

[0208] Preparation process: Weigh the prescribed amount of poloxamer 188 and place it in a beaker of 700ml water for injection, stir to dissolve, and take the prescribed amount of etimicin sulfate, pranoprofen, lysine, trehalose, phosphoric acid respectively Put disodium hydrogen in a beaker of 200ml water for injection, stir to dissolve, mix the two solutions, use 2M citric acid solution and sodium hydroxide solution to adjust the pH value of the solution to 6.8, add water for injection to dilute to 1000ml, and the above drug The liquid is filtered through a 2 μm ...

Embodiment 2

[0209] The preparation of embodiment 2 compound etimicin gel eye drops

[0210] Prescription: etimicin sulfate (calculated as etimicin) 3.0g, hydrocortisone sodium succinate 0.25g, carbomer 9406g, polyvinyl alcohol 2g, trehalose 3g, taurine 5g, benzalkonium bromide Ammonium 0.01g, edetate disodium 0.3g, polysorbate 80 1g, 2M citric acid solution and 2M sodium hydroxide solution in appropriate amount, and dilute to 1000g with water for injection.

[0211] Preparation process: Take the prescribed amount of Carbomer 940 and polyvinyl alcohol in a beaker, add about 850ml of water, let it stand still to make it swell, adjust the pH value to neutral with 2M citric acid solution and 2M sodium hydroxide, and obtain the matrix. Take etimicin sulfate, hydrocortisone sodium succinate, trehalose, taurine, benzalkonium bromide, and polysorbate-80 respectively, add water and stir to make them miscible, slowly add them to the above matrix, and stir evenly , add water to 1000g, vacuum degass...

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Abstract

The invention provides a composition comprising an effective dose of etimicin or a pharmaceutically acceptable salt thereof, an anti-inflammatorily effective dose of steroids or non-steroid anti-inflammatory drugs, and an effective dose of a water-retaining or wetting agent or anti-xerophthalmia drug, and application of the composition to preparation of external drugs for local administration of the eyes, the nose or skin and for prevention and treatment of conjunctivitis in human beings or mammals, angular blepharitis, keratitis, scleritis, trachoma, xerophthalmia, cataract, otitis externa, otitis media, folliculitis, furuncle, pustule and the like. The composition provided by the invention has better curative effect or treatment compliance.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide the prevention or treatment of conjunctivitis, canthal blepharitis, trachoma, keratitis, dry eye syndrome, otitis externa, otitis media, cataract, folliculitis, furunculosis, impetigo An effective dose of etimicin or its pharmaceutically acceptable salt and an effective dose of dexamethasone or its derivatives for topical ophthalmic or ear or nasal or skin external application Or oral pharmaceutical composition 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 o...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/7036A61P31/04A61P29/00A61P1/02A61P17/00A61P17/02A61P27/02A61P27/12A61P27/16A61K31/573A61K31/192A61K31/57A61K31/58A61K31/56
CPCA61K9/0014A61K9/0043A61K9/0046A61K9/0048A61K9/0053A61K31/192A61K31/56A61K31/57A61K31/573A61K31/58A61K31/7036A61K45/06A61K2300/00
Inventor 刘力
Owner 刘力
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