CN1456157A - Ophthalmic gel of L-ofloxacin - Google Patents
Ophthalmic gel of L-ofloxacin Download PDFInfo
- Publication number
- CN1456157A CN1456157A CN 02117617 CN02117617A CN1456157A CN 1456157 A CN1456157 A CN 1456157A CN 02117617 CN02117617 CN 02117617 CN 02117617 A CN02117617 A CN 02117617A CN 1456157 A CN1456157 A CN 1456157A
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- CN
- China
- Prior art keywords
- levofloxacin
- gel
- ofloxacin
- eye
- ingredient
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Abstract
A levo-ofloxacin gel for treating bacterial infection of eye, such as bacterial conjunctivitis, ophthalmomyositis, dacryocystitis, etc is prepared from levo-ofloxacin, boric acid, hydrogenated and hardened castor oil, hydroxyphenyl ethylester, propanediol, sodium hyaluronate, etc. Its advantages are long stay time in eye and high curative effect.
Description
Affiliated technical field
---levofloxacin---makes gel for eye use first to the present invention relates to a kind of effective ingredient, is applied to the treatment of ophthalmology bacterial infection.
Background technology
The levofloxacin ophthalmic preparation in exploitation of report has at present: 0.3% levofloxacin lactate eye drop, 0.3% levofloxacin hydrochloride eye ointment.The report that ophthalmic gel of L-ofloxacin yet there are no research and produces.
Summary of the invention
Big in order to overcome dosage, oral drugs are difficult to the deficiency by blood-eye barrier, invent a kind of gel for eye use, the ophthalmology topical, not only solved eye drop and easily diluted by tear, the defective that the ophthalmic time of staying is short, and use amount is few, improve the bioavailability of effective ingredient, increase curative effect and drug safety.
Technical scheme of the present invention is: the levofloxacin effective ingredient forms stable transparent mastic with card pool nurse gel-type vehicle and sodium hyaluronate solution, uses the back and forms the gas-pervious reticular membrane of one deck at the eye table, and effect is lasting.
The ophthalmic gel of L-ofloxacin single preparations of ephedrine, its chemistry is by name: (-)-9-fluoro-2,3-dihydro-3-methyl isophthalic acid 0-(4-methyl isophthalic acid-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de]-[1,4] benzoxazinyl-6-carboxylic acid gel for eye use; Common name: ophthalmic gel of L-ofloxacin; English name: Levofloxacin EyeGel; The Chinese phonetic alphabet: Zuoxuan Yangfushaxing Yanyong Ningjiao; Levofloxacin ingredient and main adjunct ingredient and the preparation of forming in following ratio that is applied to ophthalmology illness thereof: wherein containing levofloxacin is 0.1-1.0% (w/w); Containing card pool nurse is 0-3.0% (w/w); Containing the hydrogenation hardened castor oil is 0-5.0% (w/w); Containing hyaluronate sodium is 0-0.2% (w/w).The levofloxacin effective ingredient mixes with an amount of water for injection under acid condition, grinds to form superfine powder; Respectively with sodium chloride, Oleum Ricini, ethyl hydroxybenzoate, propylene glycol, stir, add water, heating makes whole dissolvings.Card pool nurse is swelled into aqueous solution, adds the right amount of boron processed with acid and becomes transparent emulsifiable paste, joins in the above-mentioned cooled levofloxacin aqueous solution, stirs, and continues cooling, adds hyaluronate sodium.It is transparent to be stirred to mastic, filters packing, packing.In addition, substrate such as levofloxacin effective ingredient and hydroxypropyl methylcellulose series, methylcellulose series, polyvinyl alcohol series all can form gel, and card pool nurse series substrate effect is best.Among the above-mentioned preparation technology, its core technology is: (pH=5.0-6.5) dissolving under (1) levofloxacin ingredient acid condition, (2) be to guarantee the transparent key of mastic with adjunct ingredient Hybrid Heating dissolving (temperature range 60-80 ℃), (3) card pool nurse swelling (concentration range 1.5-3.0%) is made transparent emulsifiable paste, and (4) hyaluronate sodium mixes with mastic.
Good effect of the present invention: the application of ophthalmic gel of L-ofloxacin has following advantage: (1), lower than oral administration cost, oral every day, dosage was 300-600mg, and the ophthalmic gel of L-ofloxacin drug content is 0.5%, use the about 150-225mg of gel content every day, levofloxacin use amount every day is 0.75-1.25mg.(2), ophthalmic gel of L-ofloxacin directly acts on the affected part, can play a role fully effectively, GI irritation and other side effect that can avoid oral drug therapy to bring.(3), with respect to other ophthalmic preparation, gel has unrivaled advantage, compare ophthalmic gel of L-ofloxacin with eye drop and be difficult for being diluted by tear, within the eye the time of staying long, help the abundant absorption and the utilization of principal agent; Compare with the eye ointment of vaseline substrate, the ophthalmic gel of L-ofloxacin good water solubility is cleaned easily, and pollution clothes is not easy to use.On the other hand, ophthalmic gel of L-ofloxacin does not cause the visual field fuzzy, all can use round the clock.
Embodiment writes out a prescription 1:
Levofloxacin ... 0.5g card pool nurse ... 0.6g
Sodium chloride ... 0.5g boric acid ... 1.0g
The hydrogenation hardened castor oil ... 1.0g ethyl hydroxybenzoate ... 0.025g
Propylene glycol ... 1.0g hyaluronate sodium ... 0.05g
Make ... 100.0g operating process:
1.. the levofloxacin porphyrize, with sodium chloride, Oleum Ricini, ethyl hydroxybenzoate, propylene glycol, stir, add water, heating makes whole dissolvings.
2.. boric acid, card are moored nurse, are stirred, in the adding 1..
3.. heating stirs.
3.. heating stirs.
4.. cooling below 40 ℃, adds hyaluronate sodium.
5.. filter, packing, packing, promptly.Prescription 2:
Levofloxacin ... 0.1-1.0g card pool nurse ... 0.1-3.0g
Sodium chloride ... 0.1-1.0g boric acid ... 0.5-2.0g
The hydrogenation hardened castor oil ... 0.1-5.0g ethyl hydroxybenzoate ... 0.025-0.1g
Propylene glycol ... 0.5-5.0g hyaluronate sodium ... 0.01-0.1g
Make ... 100.0g operating process:
1.. the levofloxacin porphyrize, with sodium chloride, Oleum Ricini, ethyl hydroxybenzoate, propylene glycol, stir, add water, heating makes whole dissolvings.
2.. boric acid, card are moored nurse, are stirred, in the adding 1..
3.. heating stirs.
4.. cooling below 40 ℃, adds hyaluronate sodium.
5.. filter, packing, packing, promptly.
Fig. 1 is a levofloxacin gel for eye use preparation technology flow chart.
Claims (2)
1. ophthalmic gel of L-ofloxacin single preparations of ephedrine that is used for the treatment of bacterial infection, is applied to treat ophthalmology illness, its chemistry is by name: (-)-9-fluoro-2,3-dihydro-3-methyl isophthalic acid 0-(4-methyl isophthalic acid-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de]-[1,4] benzoxazinyl-6-carboxylic acid gel for eye use; Common name: ophthalmic gel of L-ofloxacin; English name: Levofloxacin Eye Gel; The Chinese phonetic alphabet: Zuoxuanyangfushaxing Yanyong Ningjiao; Medicine and main adjunct ingredient and the preparation of forming in following ratio that is applied to ophthalmology thereof: wherein containing levofloxacin is 0.1-1.0% (w/w); Containing card pool nurse is 0-3.0% (w/w); Containing Oleum Ricini is 0-5.0% (w/w); Containing hyaluronate sodium is 0-0.2% (w/w).And, the relevant ophthalmic preparation of content ratio therewith; With above-mentioned levofloxacin effective ingredient, under acid condition, mix with an amount of water for injection, grind to form superfine powder; Respectively with sodium chloride, Oleum Ricini, ethyl hydroxybenzoate, propylene glycol, stir, add water, heating makes whole dissolvings.Card pool nurse is swelled into aqueous solution, adds the right amount of boron processed with acid and becomes transparent emulsifiable paste, joins in the above-mentioned cooled levofloxacin aqueous solution, stirs, and continues cooling, adds hyaluronate sodium.It is transparent to be stirred to mastic, filters packing, packing.In addition, substrate such as levofloxacin effective ingredient and hydroxypropyl methylcellulose series, methylcellulose series, polyvinyl alcohol series all can form gel, and card pool nurse series substrate effect is best.Among the above-mentioned preparation technology, its core technology is: (pH=5.0-6.5) dissolving under (1) levofloxacin ingredient acid condition, (2) be to guarantee the transparent key of mastic with adjunct ingredient Hybrid Heating dissolving (temperature range 60-80 ℃), (3) card pool nurse swelling (concentration range 1.5-3.0%) is made transparent emulsifiable paste, and (4) hyaluronate sodium mixes with mastic.
2. according to the described ophthalmic gel of L-ofloxacin of claim 1, it is characterized in that this effective ingredient levofloxacin makes gel for eye first, medicine and main adjunct ingredient and the preparation of forming in following ratio that is applied to the ophthalmology illness treatment thereof: wherein levofloxacin is its effective ingredient, and concentration is 0.1-1.0% (w/w); It is 0-3.0% (w/w) that main adjuvant contains card pool nurse; Containing the hydrogenation hardened castor oil is 0-5.0% (w/w); Containing hyaluronate sodium is 0-0.2% (w/w).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02117617 CN1456157A (en) | 2002-05-10 | 2002-05-10 | Ophthalmic gel of L-ofloxacin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 02117617 CN1456157A (en) | 2002-05-10 | 2002-05-10 | Ophthalmic gel of L-ofloxacin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1456157A true CN1456157A (en) | 2003-11-19 |
Family
ID=29410322
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 02117617 Pending CN1456157A (en) | 2002-05-10 | 2002-05-10 | Ophthalmic gel of L-ofloxacin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1456157A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100361658C (en) * | 2005-06-15 | 2008-01-16 | 刘继东 | In situ-forming eye gel composition of ganciclovir and preparation method thereof |
| WO2009006130A3 (en) * | 2007-06-28 | 2009-09-17 | Bausch & Lomb Incorporated | Salt free hyaluronate ophthalmic solution |
| WO2013122801A1 (en) * | 2012-02-13 | 2013-08-22 | Bausch & Lomb Incorporated | Ophthalmic pharmaceutical compositions and methods of making and using same |
| RU2669768C1 (en) * | 2017-12-26 | 2018-10-16 | Илья Александрович Марков | Gel drops for treating inflammatory eye diseases, including infectious and sustainable to antibiotics diseases |
-
2002
- 2002-05-10 CN CN 02117617 patent/CN1456157A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100361658C (en) * | 2005-06-15 | 2008-01-16 | 刘继东 | In situ-forming eye gel composition of ganciclovir and preparation method thereof |
| WO2009006130A3 (en) * | 2007-06-28 | 2009-09-17 | Bausch & Lomb Incorporated | Salt free hyaluronate ophthalmic solution |
| WO2013122801A1 (en) * | 2012-02-13 | 2013-08-22 | Bausch & Lomb Incorporated | Ophthalmic pharmaceutical compositions and methods of making and using same |
| US9278132B2 (en) | 2012-02-13 | 2016-03-08 | Bausch & Lomb Incorporated | Ophthalmic pharmaceutical compositions and methods of making and using same |
| RU2669768C1 (en) * | 2017-12-26 | 2018-10-16 | Илья Александрович Марков | Gel drops for treating inflammatory eye diseases, including infectious and sustainable to antibiotics diseases |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |