CN102949334A - Levofloxacin hydrochloride gel-type eye-drops - Google Patents

Levofloxacin hydrochloride gel-type eye-drops Download PDF

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Publication number
CN102949334A
CN102949334A CN2011102395967A CN201110239596A CN102949334A CN 102949334 A CN102949334 A CN 102949334A CN 2011102395967 A CN2011102395967 A CN 2011102395967A CN 201110239596 A CN201110239596 A CN 201110239596A CN 102949334 A CN102949334 A CN 102949334A
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CN
China
Prior art keywords
levofloxacin hydrochloride
hydrochloride gel
drops
eye drop
water
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.)
Pending
Application number
CN2011102395967A
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Chinese (zh)
Inventor
张伟明
徐向
张艳
王少平
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SUZHOU BEAUTY OF TAIHU-LAKE MEDICINE Co Ltd
Original Assignee
SUZHOU BEAUTY OF TAIHU-LAKE MEDICINE Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by SUZHOU BEAUTY OF TAIHU-LAKE MEDICINE Co Ltd filed Critical SUZHOU BEAUTY OF TAIHU-LAKE MEDICINE Co Ltd
Priority to CN2011102395967A priority Critical patent/CN102949334A/en
Publication of CN102949334A publication Critical patent/CN102949334A/en
Pending legal-status Critical Current

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses levofloxacin hydrochloride gel-type eye-drops comprising levofloxacin hydrochloride, poloxamer, another auxiliary material, and water. The water is injection water. The other auxiliary material is a pH regulating agent which is one or a complex of the components selected from sodium dihydrogen phosphate, potassium dihydrogen phosphate, borax, acetic acid, sodium acetate, and sodium hydroxide. The levofloxacin hydrochloride gel-type eye-drops have high medicine concentration in cornea and aqueous humor. Therefore, the levofloxacin hydrochloride gel-type eye-drops are beneficial for controlling bacteria reproduction and growth, shortening disease course, and improving curative rate.

Description

A kind of eye drop of Levofloxacin Hydrochloride Gel type
Technical field
The present invention relates to a kind of eye drop of Levofloxacin Hydrochloride Gel type, belong to technical field of pharmaceuticals.
Background technology
0.3% its Main Ingredients and Appearance of Levofloxacin Hydrochloride Gel type eye drop is levofloxacin (Levofloxacin).Levofloxacin is a kind of broad-spectrum long-acting fluoroquinolone antibacterial agent, it is the S type laevoisomer of ofloxacin, being 8~128 times of ofloxacin R type dextroisomer to the inhibition ability of Gram-positive and negative bacteria breeding, is 2 times of racemic modification ofloxacin.Levofloxacin is brought into play bactericidal action by suppressing DNA gyrase activity.Levofloxacin eye drops clinical practice has a broad antifungal spectrum has stronger antibacterial action to Gram-positive, negative bacteria.Clinical ophthalmology is mainly used in bacillary eye surface diseases.At present, bacterial keratitis and conjunctivitis are ophthalmology common disease, frequently-occurring disease, and therefore researching and developing antibiotics collyrium safe, long-acting, comfortable dosage form has important clinical meaning.
Summary of the invention
In view of the defective that above-mentioned prior art exists, the objective of the invention is to propose a kind of eye drop of Levofloxacin Hydrochloride Gel type.
Purpose of the present invention will be achieved by the following technical programs:
A kind of eye drop of Levofloxacin Hydrochloride Gel type comprises levofloxacin hydrochloride, poloxamer and other adjuvants and water in the described eye drop, described water is water for injection;
Described other adjuvants are the PH regulator, and described PH regulator is that in sodium dihydrogen phosphate, potassium dihydrogen phosphate, Borax, acetic acid, sodium acetate, the sodium hydroxide one or more are composite.
The eye drop of a kind of Levofloxacin Hydrochloride Gel type as previously discussed, wherein said eye drop also comprise one or more assembly in stabilizing agent, the thickening agent.
Outstanding effect of the present invention is: the temperature of this dosage form before undergoing phase transition is the lower mobile liquid condition of a kind of viscosity below 30 ℃ the time, can evenly distribute and the rapid gel that forms under the effect of temperature after splashing into ophthalmic, adhere to eyeball surface, thereby medicine is slowly discharged in conjunctival sac, keep the long duration, can be as most of loss the behind the eye drop eye drip.
Below in conjunction with embodiment, the specific embodiment of the present invention is described in further detail, so that technical solution of the present invention is easier to understand, grasp.
The specific embodiment
A kind of eye drop of Levofloxacin Hydrochloride Gel type comprises levofloxacin hydrochloride, poloxamer and other adjuvants and water in the described eye drop, also comprise one or more assembly in stabilizing agent, the thickening agent.Described water is water for injection; Described other adjuvants are the PH regulator, and described PH regulator is that in sodium dihydrogen phosphate, potassium dihydrogen phosphate, Borax, acetic acid, sodium acetate, the sodium hydroxide one or more are composite.
The preparation method of the eye drop of the above Levofloxacin Hydrochloride Gel type specifically comprises the steps:
The levofloxacin hydrochloride of step 1, accurate weighing recipe quantity adds in the water for injection of about 70% total amount and stirs, and adopts magnetic agitation, and rotating speed is 65 to turn/min, to fully dissolving, the liquid that obtains clarifying;
Other adjuvants in step 2, the accurate weighing prescription except poloxamer add in the solution of step 1 gained successively, and stirring and dissolving is even, obtains clarifying mixed solution, and gained solution is tentatively filtered with microporous filter membrane;
Step 3, the solution of step 2 gained is cooled to 0 ℃~4 ℃, the poloxamer that adds the recipe quantity of accurate weighing carries out swelling, swelling fully after, add water to recipe quantity, obtain clarifying the solution of thickness;
Step 4 is filtered behind the solution left standstill to the step 3 gained, adopts flowing steam sterilization, namely obtains the eye drop of Levofloxacin Hydrochloride Gel type.
The eye drop preparation method of above-described a kind of Levofloxacin Hydrochloride Gel type, its eye drop that makes are the eye drop of 0.3% Levofloxacin Hydrochloride Gel type.
Levofloxacin Hydrochloride Gel type eye drop rabbit intraocular pharmacokinetic result of study shows, single eye drip cornea and aqueous humor Chinese medicine concentration in 180min are significantly higher than the eye drop group, and bioavailability is better than the eye drop group.Cornea and aqueous humor Chinese medicine concentration are significantly higher than the eye drop group behind the Levofloxacin Hydrochloride Gel type eye drop multiple dosing in 240min.This illustrates the number of times of conventional eye drip, and Levofloxacin Hydrochloride Gel type eye drop has high drug level in cornea and aqueous humor, is beneficial to the Growth and Reproduction of control antibacterial, shortens the course of disease, improves cure rate.
The present invention still has numerous embodiments, and all employing equivalents or equivalent transformation and all technical schemes of forming all drop within protection scope of the present invention.

Claims (2)

1. the eye drop of a Levofloxacin Hydrochloride Gel type, it is characterized in that: comprise levofloxacin hydrochloride, poloxamer and other adjuvants and water in the described eye drop, described water is water for injection;
Described other adjuvants are the PH regulator, and described PH regulator is that in sodium dihydrogen phosphate, potassium dihydrogen phosphate, Borax, acetic acid, sodium acetate, the sodium hydroxide one or more are composite.
2. the eye drop of a kind of Levofloxacin Hydrochloride Gel type as claimed in claim 1, it is characterized in that: described eye drop also comprises one or more assembly in stabilizing agent, the thickening agent.
CN2011102395967A 2011-08-19 2011-08-19 Levofloxacin hydrochloride gel-type eye-drops Pending CN102949334A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN2011102395967A CN102949334A (en) 2011-08-19 2011-08-19 Levofloxacin hydrochloride gel-type eye-drops

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2011102395967A CN102949334A (en) 2011-08-19 2011-08-19 Levofloxacin hydrochloride gel-type eye-drops

Publications (1)

Publication Number Publication Date
CN102949334A true CN102949334A (en) 2013-03-06

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107224425A (en) * 2016-03-24 2017-10-03 湖北远大天天明制药有限公司 A kind of preparation method of the sterile gel of lavo-ofloxacin hydrochloride
CN112190558A (en) * 2020-10-20 2021-01-08 迪沙药业集团有限公司 Levofloxacin composition

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101278895A (en) * 2007-04-06 2008-10-08 北京华禧联合科技发展有限公司 Instant type gel preparation for eye and method of producing the same
CN101461777A (en) * 2009-01-06 2009-06-24 河北科技大学 Disposable levofloxacin hydrochloride eye drops without bacteriostatic agent and preparation method thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101278895A (en) * 2007-04-06 2008-10-08 北京华禧联合科技发展有限公司 Instant type gel preparation for eye and method of producing the same
CN101461777A (en) * 2009-01-06 2009-06-24 河北科技大学 Disposable levofloxacin hydrochloride eye drops without bacteriostatic agent and preparation method thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
高斐等: "《左氧氟沙星热敏型眼用凝胶的研制及体外释放研究》", 《中国药房》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107224425A (en) * 2016-03-24 2017-10-03 湖北远大天天明制药有限公司 A kind of preparation method of the sterile gel of lavo-ofloxacin hydrochloride
CN107224425B (en) * 2016-03-24 2021-05-25 湖北远大天天明制药有限公司 Preparation method of levofloxacin hydrochloride sterile gel
CN112190558A (en) * 2020-10-20 2021-01-08 迪沙药业集团有限公司 Levofloxacin composition

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Application publication date: 20130306