CN1215844C - Gatifloxacin gels foreye and its preparing method - Google Patents

Gatifloxacin gels foreye and its preparing method Download PDF

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Publication number
CN1215844C
CN1215844C CN200410026893.3A CN200410026893A CN1215844C CN 1215844 C CN1215844 C CN 1215844C CN 200410026893 A CN200410026893 A CN 200410026893A CN 1215844 C CN1215844 C CN 1215844C
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China
Prior art keywords
water
gatifloxacin
distilled water
gel
injection
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Expired - Fee Related
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CN200410026893.3A
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Chinese (zh)
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CN1562033A (en
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李东
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Shenzhen Huahui Biological Science And Technology Co Ltd
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Individual
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Abstract

The present invention discloses gatifloxacin eye gel and a preparation method thereof. The present invention aims to overcome the defects of drug tolerance caused by the longtime use of the existing ear drops and many medication times of patients, so the gatifloxacin eye gel is provided. The gatifloxacin eye gel contains the drugs: 0.05 wt% to 0.4 wt% of gatifloxacin, 0.5 wt% to 1.5 wt% of carbomer and 1 wt% to 2 wt% of triethanolmine. The preparation method comprises the steps that carbomer is taken, is spread at the surface of glycerol, is ground, is infiltrated, then is added to distilled water and is ground to make the carbomer fully swollen; triethanolmine is taken, is dissolved in distilled water, is added to supernatant fluid and is ground to prepare a gel ground substance (III); gatifloxacin is added in distilled water, is stirred, is dissolved, then is added to propanediol and is evenly stirred to prepare mixed liquor (IV); the mixed liquor (IV) is slowly added in the gel ground substance, is added to distilled water to the full quantity and is evenly ground to prepare the gatifloxacin eye gel.

Description

Gatifloxacin eye gel and preparation method thereof
Technical field
The present invention relates to a kind of external used medicine for the treatment of ocular infection and preparation method thereof, particularly a kind of spacetabs type eye gel for the treatment of ocular infection and preparation method thereof.
Background technology
So far, the antibiotic medicine of treatment ocular infection disease, kind is few, the aging of product.The antibiotic medicine of present clinical first-selection is ciprofloxacin, tobramycin and dexamethasone compound preparation (trade name: Tobrex).The shortcoming of Tobrex is the price comparison costliness, and by contrast, the price of disposable levofloxacin hydrochloride eye drops is then cheaper.But disposable levofloxacin hydrochloride eye drops is bigger to the eye zest, and the patient is difficult for accepting.Particularly the old antibiotic eye drop of prolonged application causes antibiotic fastbacteria increasing, so this type of antibiotic therapeutical effect weakens; And, also needing multiple dosing on the one during use, the patient is difficult for accepting.
The English name of Gatifloxacin is Gatifloxacin, is abbreviated as GFLX, and the commodity of external listing Tequin by name belongs to novel fluoroquinolone antibacterial agent thing of the 4th generation.From the characteristics of structure and antimicrobial spectrum, have good pharmacokinetics and pharmacodynamic profile, phototoxicity obviously reduces, and is difficult for producing drug resistance, and antimicrobial spectrum is wider.It at first went on the market in the U.S. in December in 1999 on the 27th, was subjected to the welcome of extensive patients deeply.Its characteristics can reduce: 1. has a broad antifungal spectrum.Except that gram negative bacteria being had the strong antibiotic activity, also have than the more powerful resisting gram-positive bacteria of other quinolones and the activity of pathogen such as anaerobe resistant, gonococcus, mycoplasma, chlamydia and mycobacterium.2. antibacterial activity is higher than ciprofloxacin and levofloxacin.3. safety is good.The clinical practice person of having no side effect accounts for 96.5%.Though the report that utilizes GFLX intravenous injection and oral administration treatment eye inflammation is arranged abroad, and effect is better.But this therapeutic modality is very inconvenient to the patient.
Gel for eye is to be adjuvant with natural, semi-synthetic or complete synthesis gel, the pharmaceutical preparation of making.Adjuvant can be selected materials such as polyacrylamide, carbopol 910, carbopol 940 for use.It is big and be easy to and features such as tear mixes that it has viscosity, and prolong drug improves bioavailability in the holdup time on eye surface.The external gel for eye use that medicines such as N-ethyl-N-(.gamma.-picolyl)tropamide, pilocarpine, chloromycetin and betamethasone are arranged of development and Application, but still do not have the report that the GFLX eye-gel preparation is studied at present.
Summary of the invention
The purpose of this invention is to provide a kind of with the Gatifloxacin be main component, have efficient sterilizing, long action time, a spacetabs type gel eye drop that adverse effect is low.
GFLX eye gel of the present invention contains the medicine of following percentage by weight:
Gatifloxacin 0.05%~0.4%
Carbomer 0.5%~1.5%
Triethanolamine 1%~2%
The preferred technical solution of the present invention is the medicine that also comprises following percentage by weight on the basis of such scheme:
Propylene glycol 8%~12%
Glycerol 8%~12%
Distilled water or purified water or water for injection add to 100%
The Gatifloxacin general by name of above-mentioned Gatifloxacin, English name are Gatifloxacin, and molecular formula is C 19H 22FN 3O 41.5H 2O, chemistry 1-cyclopropyl-6 fluoro-7-(3-methyl piperazine-1-yl) by name-8-methoxyl group-1,4-dihydro-4-oxygen-quinoline-3-carboxylic acid 1/2 hydrate; The English name of propylene glycol is PropyleneGlycol; The English name of glycerol is Glycerol; The English name of carbomer is Carbomer; The English name of triethanolamine is Trolamine; The English name of purified water is Purified Water; The English name of water for injection is Water for Injection.
Manufacturing method for above mentioned medicine is for comprising the following steps:
(1) according to dosage gets carbomer and be sprinkled into the glycerol surface, carbomer is mixed fully with glycerol with polishing; Add 150~250ml distilled water or purified water or water for injection and be ground to exquisiteness, add distilled water or purified water or the water for injection of 350~450ml again, make the abundant swelling of carbomer, be statically placed in the container, make mixed liquor (I);
According to dosage get in the distilled water or purified water or water for injection of triethanolamine adding 50~150ml, stirring is fully dissolved it and is made solution (II);
Mixed liquor (I) is added solution (II), continue again to grind, make gel-type vehicle (III);
(2) get an amount of purified water or water for injection or distilled water in addition, according to dosage add Gatifloxacin, stirring is fully dissolved it; According to dosage add propylene glycol again, stir and make its mix homogeneously, make mixed liquor (IV);
(3) under grinding, mixed liquor (IV) is slowly added in the gel-type vehicle (III), again distilled water or purified water or water for injection are added to full dose, continue to be ground to evenly;
(4) aforesaid liquid is carried out just filter and fine straining, carry out fill and sterilization again and promptly get eye gel of the present invention.
The invention has the beneficial effects as follows: because it is the gel rubber sustained-release dosage form, particularly its substrate carbomer has inherent peculiar cross-linked structure, and viscosity that it is good and hydrophilic gel make it have slow releasing function preferably.Therefore this dosage form has the advantage that viscosity is big and be easy to absorb, can prolong drug in the holdup time of mucomembranous surface, thereby fully improve the advantage of the bioavailability of novel fluoroquinolone antibacterial agent thing of the 4th generation of GFLX and pharmaceutics, pharmacodynamics; In clinical practice, can reduce administration time, prolong dosing interval, reduce whole body and absorb the untoward reaction that brings, help improving patient's compliance.Simultaneously, it has overcome old kind medicine to the drug resistance that the patient brings, and has solved the urgent need of clinical eye anti-infectious disease new drug.
Concrete embodiment
Below in conjunction with illustrated embodiments the present invention is described in further detail.
Embodiment one.Gatifloxacin eye gel is to be made by the medicine of following percentage by weight:
Gatifloxacin 0.3%
Propylene glycol 10%
Glycerol 10%
Acritamer 940 1%
Triethanolamine 1.35%
Distilled water or purified water or water for injection add to 100%
It is as follows to utilize medicine of the present invention to carry out the situation of clinical experiment:
Therapeutic Method
Group technology by the order of seeing and treating patients, is divided into 4 groups with 100 routine patients.A, B are the treatment group for two groups, bacterial conjunctivitis 25 examples (A group) wherein, and bacterial keratitis 25 examples (B group) are with the treatment of Gatifloxacin gel eye drop, each 1~2, every day 2 times.C, D are matched group for two groups, bacterial conjunctivitis 25 examples (C group) wherein, and bacterial keratitis 25 examples (D group), with the treatment of 0.3% ciprofloxacin eye drops, each 1~2, per 2 hours are once.
The treatment standard
Bacterial conjunctivitis is cured: subjective symptoms, hyperemia and secretions disappear; Produce effects: subjective symptoms alleviates, and hyperemia alleviates, and secretions reduces; Invalid: symptom no change or subjective symptoms increase the weight of.
Bacterial keratitis is cured: subjective symptoms, hyperemia and secretions disappear, the corneal ulcer healing; Produce effects: subjective symptoms alleviates, hyperemia alleviates, secretions reduces, the little or minimizing of corneal ulcer reduction of area; Invalid: symptom no change or subjective symptoms increase the weight of.
Therapeutic outcome
The clinical effectiveness of Gatifloxacin gel eye drop
Bacterial conjunctivitis Bacterial keratitis
Not healing meter x is cured in grouping 2Value P value (%) (%) Not healing meter x is cured in grouping 2Value P value (%) (%)
Treatment group matched group A 24 1 25 (96) (4) 4.15 <0.05 C 19 6 25 (76) (24) B 23 2 25 (92) (8) 4.5 <0.05 C 17 8 25 (68) (32)

Claims (4)

1. Gatifloxacin eye gel is characterized in that containing the medicine of following percentage by weight:
Gatifloxacin 0.05%-0.4%
Carbomer 0.5%-1.5%
Triethanolamine 1%-2%.
2. Gatifloxacin eye gel according to claim 1 is characterized in that also containing the medicine of following percentage by weight:
Propylene glycol 8%-12%
Glycerol 8%-12%
Distilled water or pure water or water for injection add to 100%.
3. Gatifloxacin eye gel according to claim 1 and 2 is characterized in that being made by the medicine of following percentage by weight:
Gatifloxacin 0.3%
Propylene glycol 10%
Glycerol 10%
Acritamer 940 1%
Triethanolamine 1.35%
Distilled water or pure water or water for injection add to 100%.
4. according to the preparation method of claim 1 or 2 or 3 described medicines, it is characterized in that comprising the following steps:
(1) according to dosage gets carbomer and be sprinkled into the glycerol surface, carbomer is mixed fully with glycerol with polishing; Add 150-250ml distilled water or pure water or water for injection and be ground to exquisiteness, add distilled water or pure water or the water for injection of 350-450ml again, make the abundant swelling of carbomer, be statically placed in the container, make mixed liquor (I);
According to dosage get in the distilled water or pure water or water for injection of triethanolamine adding 50-150ml, stirring is fully dissolved it and is made mixed liquor (II);
Mixed liquor (I) is added mixed liquor (II), continue again to grind, make gel-type vehicle (III);
(2) get an amount of distilled water or pure water or water for injection in addition, according to dosage add Gatifloxacin, stirring is fully dissolved it; According to dosage add propylene glycol again, stir and make its mix homogeneously, make mixed liquor (IV);
(3) under grinding, mixed liquor (IV) is slowly added in the gel-type vehicle (III), again distilled water or pure water or water for injection are added to full dose, continue to be ground to evenly;
(4) aforesaid liquid is carried out just filter and fine straining, carry out fill and sterilization again and promptly get eye of the present invention gelling.
CN200410026893.3A 2004-04-18 2004-04-18 Gatifloxacin gels foreye and its preparing method Expired - Fee Related CN1215844C (en)

Priority Applications (1)

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Application Number Priority Date Filing Date Title
CN200410026893.3A CN1215844C (en) 2004-04-18 2004-04-18 Gatifloxacin gels foreye and its preparing method

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CN1562033A CN1562033A (en) 2005-01-12
CN1215844C true CN1215844C (en) 2005-08-24

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Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1307995C (en) * 2005-10-12 2007-04-04 周卓和 Gatifloxacin eye drop and its preparing method
CN102078284B (en) 2009-11-27 2013-06-12 沈阳兴齐眼药股份有限公司 Gatifloxacin-containing gel for eyes and preparation method thereof
CN103142463B (en) * 2013-03-05 2015-09-09 宁夏康亚药业有限公司 Medical composite for eye, its preparation method and application

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Granted publication date: 20050824

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