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Ophthalmic bacterial-infection resisting medicine for external use

An anti-bacterial and eye drop technology, applied in anti-bacterial drugs, drug combination, drug delivery, etc., can solve the problems of eye dehydration or edema, tablets not suitable for eye use, low pH value, etc., and achieve the effect of less toxic and side effects

Active Publication Date: 2012-07-04
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Linezolid intravenous injection and oral tablets currently in use cannot be used directly or after simple processing for external ocular use
Among them, it is obvious that tablets are not suitable for ophthalmic use; the reason why intravenous injections are not suitable for ophthalmic use is that ① the pH value is low, and direct eye drops are highly irritating, which not only causes eye pain and tearing, but also causes conjunctival and corneal damage; Isotonic, it will cause local dehydration or edema of the eye; ③ It does not contain preservatives, and it is easy to be contaminated by bacteria when used for many times, resulting in repeated eye infection

Method used

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  • Ophthalmic bacterial-infection resisting medicine for external use
  • Ophthalmic bacterial-infection resisting medicine for external use
  • Ophthalmic bacterial-infection resisting medicine for external use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0023] Example 1-3 Preparation of Linezolid Eye Drops Raw Material Components and Consumption

[0024]

[0025] According to the technical scheme of the present invention, the kinds of auxiliary materials that can be selected for preparing the linezolid eye drops are not limited to the kinds listed in the above table, and the following multiple choices can also be made:

[0026] Bacteriostatic agent: except phenylmercuric nitrate, any bacteriostatic agent known in pharmacy can be used, and its dosage is according to the conventional dosage in pharmacy. For example, ① thimerosal 0.002% to 0.005% (volume-weight percentage, that is, the number of grams per 100 ml, the same below); The effective concentration is 0.002% to 0.01%; ③alcohols, commonly used chlorobutanol 0.3~0.6%; ④parabens, commonly used ethylparaben, concentration 0.03~0.06%; The concentration is 0.01-0.08%.

[0027] Thickener: thickeners commonly used in pharmacy can be used, such as hypromellose, methylcellul...

Embodiment 4-6

[0030] Example 4-6 Preparation of Linezolid Ophthalmic Gel Raw Material Components and Consumption

[0031]

[0032] According to the technical solution of the present invention, the types of auxiliary materials that can be used to prepare the linezolid ophthalmic gel are not limited to those listed in the above table, and the following multiple options can also be selected:

[0033] Wherein, the kind selection and consumption of antibacterial agent are the same as embodiment 1~3.

[0034] The thickening agent is selected from one of hypromellose, methylcellulose, sodium hyaluronate, polyvinyl alcohol, polyvinylpyrrolidone, carboxymethylcellulose, carbomer, chondroitin sulfate or one of the varieties Any combination; the dosage ratio of the thickener to linezolid is 0.5-5 grams: 0.1-1.0 grams.

[0035] Use a pH regulator to adjust the pH value of the finished eye drops to 5.5 to 7.5; the pH regulator is any one of sodium hydroxide, hydrochloric acid, sodium citrate, citric...

Embodiment 7-9

[0037] Example 7-9 Preparation of Linezolid Ophthalmic Ointment Raw Material Components and Consumption

[0038] Raw material species

[0039] Preparation method: the eye ointment is prepared by the production method of eye ointment commonly used in pharmacy. The production method is to take linezolid, add an appropriate amount of sterilized and cooled liquid paraffin, grind it into a fine paste, pass through a 200-mesh sieve, then gradually add sterile and filtered lanolin and yellow petrolatum mixture, mix well, Instantly. All preparation equipment and packaging containers used must be sterilized.

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Abstract

The invention provides ophthalmic bacterial-infection resisting medicine for external use. Linezolid is adopted as medicative raw materials to prepare eye drops, ophthalmic gel and eye ointments. The content of the linezolid in every 100 parts by weight of a medicament is within 0.1 to 1.0 parts by weight. The medicine is for external use at partial positions of eyes, and has good intraocular penetrability and mild toxic as well as side effects; moreover, the medicine is suitable for treating as well as preventing bacterial infection at partial positions of the eyes, including diseases of conjunctivitis, keratitis, keratohelcosis, iritis, ocular traumas, chemical injuries, ophthalmic postoperative infections and the like.

Description

technical field [0001] The invention relates to a medical preparation, especially an external medicine for ophthalmic antibacterial infection. Background technique [0002] Local bacterial infection of the eye, including conjunctivitis, keratitis, corneal ulcer, iritis, eye trauma, chemical injury, infection after eye surgery, etc. Most of its pathogenic bacteria are Pseudomonas aeruginosa and Gram-positive cocci, such as Staphylococcus epidermidis, Staphylococcus saprophyticus, Staphylococcus aureus and Neisseria gonorrhoeae. Among them, Staphylococcus epidermidis was the first. [0003] Contemporary medicine confirms that because of the existence of the "blood-ocular barrier" in the human body, it is difficult to implement systemic medication for local bacterial infection of the eye, and topical application of antibacterial drugs to the eye is an effective way to combat local infection of the eye. Currently commonly used ophthalmic anti-infective drugs such as Tobramycin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377A61K9/08A61K9/00A61K9/06A61P27/02A61P31/02A61P31/04
CPCA61K31/132A61K31/192A61K31/136A61K31/14A61K9/0048A61P27/02A61P31/02A61P31/04
Inventor 叶成添吴绮峰王延东唐细兰刁红星
Owner GUANGDONG WHOLEWIN TECH
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