CN1543952A - Enoxacin ocular sustained release gelata and preparation thereof - Google Patents
Enoxacin ocular sustained release gelata and preparation thereof Download PDFInfo
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- CN1543952A CN1543952A CNA2003101051939A CN200310105193A CN1543952A CN 1543952 A CN1543952 A CN 1543952A CN A2003101051939 A CNA2003101051939 A CN A2003101051939A CN 200310105193 A CN200310105193 A CN 200310105193A CN 1543952 A CN1543952 A CN 1543952A
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Abstract
The invention relates to an eye use Enoxacin slow release gelling agent and its preparation method, which comprises the following constituents (by weight proportions), Enoxacin 0.1-1, and thickening agent 0.1-40, preservative agent 0.001-3, isotonic conditioning agent 0.1-10, pH=4.5-9 of pH modifier, and balancing water. The preparation process comprises dissolving the Enoxacin into water, adding thickening agent and stewing, charging preservative agent, isotonic conditioning agent, stirring to dissolve, regulating pH=4.5-9 with pH modifier, subjecting the solution to filtration by microporous filtering film, watering to total amount from the filter.
Description
Technical field:
The present invention relates to medical technical field, exactly it is a kind of enoxacin sustain-released ophthalmic gels and preparation method thereof.
Background technology:
According to statistics, the patient more than 80% is that ophthalmology infects in the patient that ophthalmology is gone to a doctor.Ophthalmology infects and comprises conjunctivitis, keratitis and global inflammation etc.; Divide from pathogen, comprise bacterial infection and fungal infection.Bacterial infection can use anti-infectives, but owing to there is blood-ocular barrier, causes medicine can not all penetrate ophthalmic, and the drug level in the eye inner tissue is low.Therefore the anti-infective that is used for ophthalmology is the good anti-infectives of those permeabilitys, as tobramycin, lincomycin and chloromycetin etc.In recent years, quinolones increases rapidly in the application of ophthalmology, as ofloxacin, levofloxacin, norfloxacin, ciprofloxacin and enoxacin etc.Cephalosporins commonly used is because permeability difference and drug resistance problem and the less ophthalmology that is applied to.The sickness rate of fungal infection has the trend that increases, but the ophthalmic remedy of anti-fungal infection seldom.
Current clinical anti-infectives commonly used is conventional dosage forms such as eye drop and eye ointment mostly.Eye drop after the administration, by tear is diluted to 0.1% of original concentration in a few minutes as the most frequently used dosage form of ophthalmology, bioavailability is low, only is 1%-10%, therefore needs to increase the eye dripping frequency, the patient uses inconvenience, poor compliance, and may cause general toxic reaction.Though the eye ointment release is slow, owing to being substrate with vaseline, greasy feeling is strong easily to produce " paste is looked " phenomenon, thereby the not very willing use of patient.And gel for eye adopts hydrophilic matrix, excellent biological compatibility is arranged, zest is little, some advantages that not only have Eye ointments, as increasing the time of contact in medicine and affected part, the effect time limit of prolong drug, and can alleviate medicine to the friction of eyeball with overcome the problem of " paste is looked ".The development work that this just impels people to carry out eye-gel preparation, for example the Chinese patent CN1374085A of Zhao new people's application is a kind of aseptic eye-gel preparation, its effective ingredient is a levofloxacin, is mainly used in non-treatment ocular infection.Finland Sang Dun company has applied for that in China a key name is called the patent of invention of " ophthalmic composition with decreased viscosity ", application number is 95192185, its objective is medicine can controllably be absorbed within the eye, and the viscosity of reduction medicine, thereby it is had treat handling property preferably, Germany lid Hartmann chemical pharmacy company limited has applied for that in China a key name is called the patent of invention of " aseptic dropped in eyes gel preparation and preparation method thereof ", application number is 96192797, and its purpose also is the action time of prolong drug.
Summary of the invention:
The purpose of this invention is to provide a kind of enoxacin sustain-released ophthalmic gels and preparation method thereof, it is a kind of ophthalmic preparation of water white semifluid gel state, can keep the drug level of long period, and zest is little, improves curative effect.It is an active component with the anti-inflammation agent, is aided with isoosmotic adjusting agent, pH regulator agent, antiseptic, thickening agent, water etc. and makes eye-gel preparation.
Sustain-released ophthalmic gels of the present invention, form by following component:
Constituent content (weight %)
Anti-inflammation agent 0.1-1
Thickening agent 0.1-40
Antiseptic 0.001-3
Isoosmotic adjusting agent 0.1-10
It is the amount of 4.5-9 that the preparation pH value is regulated in the pH regulator agent
Water surplus.
Active component in the sustain-released ophthalmic gels of the present invention: enoxacin
Thickening agent be selected from following: the mixture of one or more in polyvinyl alcohol (PVA, Polyvinyl Alcohol), hyaluronic acid sodium (HA, Sodium Hyaluronat), methylcellulose (EC, Methyl Cellulose), the hydroxypropyl emthylcellulose (HPMC, Hydroxypropyl Methylcellulose).The polyvinyl alcohol molecular weight is 3 * 10
4-20 * 10
4, the methylcellulose molecular weight is 2 * 10
4-38 * 10
4, the hydroxypropyl emthylcellulose molecular weight is 26000～86000.
Antiseptic be selected from following: the mixture of one or more in benzyl alcohol, chlorobutanol, thimerosal, hibitane, benzalkonium chloride, benzalkonium bromide, Metagin, second, the propyl ester;
Isoosmotic adjusting agent is to be selected from sodium chloride, glucose, mannitol, mountain plough alcohol or suchlike material;
The pH regulator agent is to adopt sodium hydroxide and/or hydrochloric acid, citric acid, sodium citrate, glacial acetic acid, triethanolamine.
The preparation method of sustain-released ophthalmic gels of the present invention
Step is as follows: by the weighing of above-mentioned prescription with anti-inflammation agent stirring and dissolving in water, standing over night behind the adding thickening agent, adding antiseptic, isoosmotic adjusting agent again, stir and make dissolving, is 4.5-9 with pH regulator agent regulator solution pH value, solution passes through filtering with microporous membrane, add water to total amount again on filter, Quality Identification is carried out in sampling, qualified after, be sub-packed in eye drip with in the bottle under gnotobasis, packing promptly.
The physicochemical character of formulation products of the present invention:
This product is water white mobile semisolid.
Ophthalmic preparation of the present invention is applicable to by multiple eye infections such as the pathogenic microbial conjunctivitis of sensitivity, keratitis.Every day 1～2 time, be applied to ophthalmic with 0.5 inch gel respectively at every turn.
Advantage of the present invention is: eye-gel preparation of the present invention is a kind of preparation that is used for the treatment of ocular infection, this gel for eye use within the eye the time of staying longer, be difficult for to run off, can keep active drug concentration, and zest is little, toxicity is low, the compatibility is good.
The specific embodiment:
Following example will the present invention is further elaborated, but do not limit content of the present invention.
Embodiment 1:
Remove ionized water 39kg, add enoxacin 0.15kg, stir and make dissolving.Get sodium alginate 2kg, be sprinkled in the above-mentioned solution.Standing over night adds benzalkonium bromide 0.001kg again, sodium chloride 0.4kg, stirring and dissolving.Regulating pH with 10%NaOH solution is 7.4, and dissolving adds water to total amount 50kg by the 0.22um microporous filter membrane on filter.Quality Identification is carried out in sampling, and qualified back is sub-packed in eye drip with in the bottle under gnotobasis, and packing promptly.
Embodiment 2:
Remove ionized water 39kg, add enoxacin 0.15kg, stir and make dissolving.Get hydroxypropyl emthylcellulose (HPMC F4M) 1.5kg, be sprinkled in the above-mentioned solution.Standing over night adds benzalkonium bromide 0.001kg again, sodium chloride 0.4kg, stirring and dissolving.Regulating pH with boric acid is 7, and dissolving adds water to total amount 50kg by the 0.22um microporous filter membrane on filter.Quality Identification is carried out in sampling, and qualified back is sub-packed in eye drip with in the bottle under gnotobasis, and packing promptly.
Embodiment 3:
Remove ionized water 39kg, add enoxacin 0.15kg, stir and make dissolving.Get methylcellulose 2kg, be sprinkled in the above-mentioned solution.Standing over night adds benzalkonium bromide 0.001kg again, sodium chloride 0.4kg, stirring and dissolving.Regulating pH with 10%NaOH solution is 7, and dissolving adds water to total amount 50kg by the 0.22um microporous filter membrane on filter.Quality Identification is carried out in sampling, and qualified back is sub-packed in eye drip with in the bottle under gnotobasis, and packing promptly.
Embodiment 4:
Remove ionized water 39kg, add enoxacin 0.15kg, stir and make dissolving.Get polyvinyl alcohol 1kg, be sprinkled in the above-mentioned solution.Standing over night adds benzalkonium bromide 0.001Kg again, sodium chloride 0.4kg, stirring and dissolving.Regulating pH with boric acid is 7, and dissolving adds water to total amount 50kg by the 0.22um microporous filter membrane on filter.Quality Identification is carried out in sampling, and qualified back is sub-packed in eye drip with in the bottle under gnotobasis, and packing promptly.
Embodiment 5:
Remove ionized water 39kg, add enoxacin 0.15kg, stir and make dissolving.Get hyaluronic acid sodium 1kg, be sprinkled in the above-mentioned solution.Standing over night adds benzalkonium bromide 0.001kg again, sodium chloride 0.4kg, stirring and dissolving.Regulating pH with boric acid is 7, and dissolving adds water to total amount 50kg by the 0.22um microporous filter membrane on filter.Quality Identification is carried out in sampling, and qualified back is sub-packed in eye drip with in the bottle under gnotobasis, and packing promptly.
Claims (5)
1, enoxacin sustain-released ophthalmic gels is characterized in that: it is made up of following component:
Constituent content (weight %)
Enoxacin 0.1-1
Thickening agent 0.1-40
Antiseptic 0.001-3
Isoosmotic adjusting agent 0.1-10
It is the amount of 4.5-9 that the preparation pH value is regulated in the pH regulator agent
Water surplus.
2, enoxacin sustain-released ophthalmic gels according to claim 1 is characterized in that:
Described thickening agent be selected from following: the mixture of one or more in polyvinyl alcohol, hyaluronic acid sodium, sodium alginate, methylcellulose, the hydroxypropyl emthylcellulose;
Described antiseptic be selected from following: the mixture of one or more in benzyl alcohol, chlorobutanol, thimerosal, hibitane, benzalkonium chloride, benzalkonium bromide, Metagin, second, the propyl ester;
Described isoosmotic adjusting agent is to be selected from sodium chloride, glucose, mannitol, mountain plough alcohol or suchlike material;
Described pH regulator agent is to adopt sodium hydroxide and/or hydrochloric acid, citric acid, sodium citrate, glacial acetic acid, triethanolamine.
3, enoxacin sustain-released ophthalmic gels according to claim 2 is characterized in that: described polyvinyl alcohol English name Polyvinyl Alcohol, molecular weight is 3 * 10
4-20 * 10
4Methylcellulose English name Methyl Cellulose, molecular weight is 2 * 10
4-38 * 10
4Hydroxypropyl emthylcellulose English name Hydroxypropyl Methylcellulose, molecular weight is 26000～86000.
4, enoxacin sustain-released ophthalmic gels according to claim 1 is characterized in that: this gel preparation is mobile semi-solid preparation, and the gel viscosity reduces with the increase of external carbuncle.
5, a kind of preparation method of enoxacin sustain-released ophthalmic gels as claimed in claim 1, it is characterized in that: described preparation method step is, by the described prescription weighing of claim 1, enoxacin is dissolved in water, and standing over night behind the adding thickening agent adds antiseptic, isoosmotic adjusting agent again, stirring and dissolving, regulating pH with the pH regulator agent is 4.5-9, and solution adds water to total amount from filter again by filtering with microporous membrane.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2003101051939A CN100563657C (en) | 2003-11-26 | 2003-11-26 | Enoxacin sustain-released ophthalmic gels and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2003101051939A CN100563657C (en) | 2003-11-26 | 2003-11-26 | Enoxacin sustain-released ophthalmic gels and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1543952A true CN1543952A (en) | 2004-11-10 |
| CN100563657C CN100563657C (en) | 2009-12-02 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2003101051939A Expired - Fee Related CN100563657C (en) | 2003-11-26 | 2003-11-26 | Enoxacin sustain-released ophthalmic gels and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100563657C (en) |
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2003
- 2003-11-26 CN CNB2003101051939A patent/CN100563657C/en not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| CN100563657C (en) | 2009-12-02 |
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Granted publication date: 20091202 Termination date: 20141126 |
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