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Topically administered pharmaceutical composition

A composition and topical technology, applied in the field of medical technology, can solve problems such as unknown efficacy or adverse reactions, toxicity or irritation, blinding adverse reactions, and worthless oral tablets or capsules

Inactive Publication Date: 2018-03-27
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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  • Topically administered pharmaceutical composition
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Examples

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preparation example Construction

[0191] 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.

[0192] 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.

[0193] 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

[0196] Example 1 Preparation of Compound Etimicin Sulfate Dexamethasone Sodium Phosphate Eye Drops

[0197] Prescription: etimicin sulfate (calculated as etimicin) 1g, dexamethasone sodium phosphate 1g, sodium hyaluronate 0.5g, sodium borate 1g, sorbic acid 1g, taurine 5g, appropriate amount of sodium chloride, 2M Appropriate amount of L-malic acid solution, appropriate amount of 1M sodium hydroxide solution, add water for injection to 1000ml

[0198] Preparation process: Take the prescribed amount of sodium hyaluronate, add it to 900ml of water for injection, heat to dissolve, let it cool, then add the prescribed amount of etimicin sulfate, dexamethasone sodium phosphate, sodium borate, sorbic acid, and taurine in sequence, Stir to dissolve, stir, adjust the pH value to 6.5 with L-malic acid solution and sodium hydroxide solution, adjust the osmotic pressure of the solution to about 300mOsmol / k with an appropriate amount of sodium chloride, add water to the full amount, and f...

Embodiment 2

[0199] Example 2 Preparation of Compound Etimicin Sulfate Dexamethasone Sodium Phosphate Eye Drops

[0200] Prescription: etimicin sulfate (calculated as etimicin) 2g, dexamethasone sodium phosphate 1g, sodium hyaluronate 1g, boric acid 0.5g, sodium borate 2g, thimerosal 0.05g, taurine 5g, sodium chloride Appropriate amount, appropriate amount of 2M malic acid solution, appropriate amount of 1M sodium hydroxide solution, add water for injection to 1000ml

[0201] Preparation process: Take the prescribed amount of sodium hyaluronate, add it to 900ml of water for injection, heat to dissolve, let it cool, then add the prescribed amount of etimicin sulfate, dexamethasone sodium phosphate, boric acid, sodium borate, thimerosal, and taurine , stir to dissolve, stir, adjust the pH value to 6.5 with malic acid solution and sodium hydroxide solution, adjust the osmotic pressure of the solution with an appropriate amount of sodium chloride to about 298mOsmol / k, add water to the full amo...

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Abstract

The present invention provides a composition containing an effective dose of etimicin or a pharmaceutically acceptable salt thereof and an anti-inflammatory effective dose of dexamethasone or a pharmaceutically acceptable derivative thereof, and applications of the composition in preparation of topical ophthalmic or aural or nasal or skin external application drugs for prevention or treatment of human or mammalian conjunctivitis, angular blepharitis, keratitis, scleritis, trachoma, xerophthalmia, otitis externa, otitis media, folliculitis, furuncle, impetigo and the like. According to the present invention, the drug has good safety and good efficacy compared to etimicin.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular to provide prevention or treatment of conjunctivitis, canthal blepharitis, trachoma, keratitis, dry eye syndrome, otitis externa, otitis media, folliculitis, boils, impetigo, trauma An effective dose of etimicin or its pharmaceutically acceptable salts and an effective dose of dexamethasone or its derivatives for topical ophthalmic or ear or nasal or external skin or oral Pharmaceutical compositions and uses. 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7036A61K9/08A61K47/36A61K47/32A61K47/22A61K9/10A61K47/38A61K47/10A61K9/06A61K47/26A61K47/44A61K47/18A61K47/14A61K9/70A61K31/573
CPCA61K9/0046A61K9/0048A61K9/006A61K9/06A61K9/08A61K9/10A61K9/7007A61K9/7023A61K31/573A61K31/7036A61K47/10A61K47/183A61K47/22A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61K2300/00
Inventor 刘力
Owner 刘力
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