CN106963726A - A kind of gel for eye use and preparation method thereof, purposes and application method - Google Patents

A kind of gel for eye use and preparation method thereof, purposes and application method Download PDF

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Publication number
CN106963726A
CN106963726A CN201710374599.9A CN201710374599A CN106963726A CN 106963726 A CN106963726 A CN 106963726A CN 201710374599 A CN201710374599 A CN 201710374599A CN 106963726 A CN106963726 A CN 106963726A
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CN
China
Prior art keywords
gel
eye use
eye
preparation
value
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.)
Withdrawn
Application number
CN201710374599.9A
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Chinese (zh)
Inventor
樊莲莲
麦刚
张标
苏文成
张培雯
巫奇
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Peoples Hospital of Deyang City
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Peoples Hospital of Deyang City
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Publication date
Application filed by Peoples Hospital of Deyang City filed Critical Peoples Hospital of Deyang City
Priority to CN201710374599.9A priority Critical patent/CN106963726A/en
Publication of CN106963726A publication Critical patent/CN106963726A/en
Withdrawn legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The invention discloses a kind of gel for eye use and preparation method thereof, purposes and application method.The gel for eye use is mainly made up of the raw material of following masses percentage:Lavo-ofloxacin hydrochloride 0.1~1.5%, triamcinolone acetonide acetate 0~0.5%, Acritamer 940 P0.2~1.5%, HPMCK4M0.25~5.0%, pure water 91.5~99.45%;The pH value of the gel for eye use is 4.0~5.0.The present invention is in administration; it can realize and fast, easily be administered; the site of action of eye can quick, timely, hygienic, be reliably and efficiently covered again; can also the surface of eyeball in time, health, it is reliable, good protective film is stably formed, so that antibacterials can be good at stable playing its antibacterial curative effect;In addition, the present invention can realize stabilization, reliably long-acting administration, and then play its quick, lasting, bactericidal effect longer.

Description

A kind of gel for eye use and preparation method thereof, purposes and application method
Technical field
The present invention relates to ophthalmic remedy, specifically a kind of gel for eye use for preventing and treating eye bacterium infection, and this is ophthalmically acceptable solidifying Preparation method, purposes and the application method of glue.
Background technology
The eye medicinal of preventing and treating eye bacterium infection generally has eye drops, eye ointment and gel for eye use.Wherein, gel for eye use The medicine retention time is between eye drops and eye ointment, and easy cleaning.
However, existing most of gel for eye use is unreasonable based on formulation selection and preparation technology, its finished product state is Semisolid shape.In administration, the gel for eye use of such a semi-solid can not reliably, quickly and efficiently cover patient's eyeball surface Infected zone, it, which is not only existed, is administered relatively cumbersome technical problem;Moreover, the gel for eye use of such a semi-solid, it is impossible to In time, the protective film that can play antibacterial curative effect voluntarily wholesomely is formed, it is necessary to carry out in patient's eyeball surface infected zone Human assistance processing, is unfavorable for the stable of antibacterial curative effect and plays and be also easy to produce new infection, poor reliability;Further, since it is partly The state of solid-like is single, in administration in the absence of the time and space of State Transferring, upon administration the i.e. quick release property of medicine, it is impossible to Realize reasonable, reliably long-acting administration.
The content of the invention
The technical purpose of the present invention is:There is provided one kind liquid can be realized to half for above-mentioned the deficiencies in the prior art Solid State Transformation, be administered it is quick and convenient and hygienic, be conducive to antibacterial curative effect stable and the long-acting gel for eye use reliably played, and should Preparation method, purposes and the application method of gel for eye use.
The present invention realizes its technical purpose the technical scheme adopted is that a kind of gel for eye use, the gel for eye use is main It is made up of the raw material of following masses percentage:
The pH value of the gel for eye use is 4.0~5.0.
Preferably, the pH value of the gel for eye use is with appropriate triethanolamine regulation.
A kind of preparation method of above-mentioned gel for eye use, the preparation method comprises the following steps:
Raw material components Acritamer 940 P and HPMC K4M are thrown in pure water by step 1., make Acritamer 940 P and HPMC K4M is in uniform shape on pure water liquid level;It is swelled overnight, stirs to obtain settled solution;
Lavo-ofloxacin hydrochloride is added in the solution of step 1 by step 2., stirring and dissolving;
The pH value of the solution of step 3. regulating step 2 is 4.0~5.0, produces gel for eye use.
Preferably, before the pH value regulation of step 3, triamcinolone acetonide acetate is added in the solution of step 2.
Preferably, the pH value regulation of step 3 is adjusted with appropriate triethanolamine.
A kind of purposes of above-mentioned gel for eye use, the gel for eye use is used to treat non-viral and fungus-caused eye bacterium Infection.
A kind of application method of above-mentioned gel for eye use, the application method is that the gel for eye use is uniformly applied into conjunctiva On capsule, light ball 5 minutes in an instant of mesh are closed, you can.
The method have the benefit that:The present invention is aided with mutual compatibility using lavo-ofloxacin hydrochloride as main component Triamcinolone acetonide acetate, Acritamer 940 P and the HPMC K4M of collaboration, its finished product are the gel to pH sensitive, according to this characteristic It is set to realize liquid and semisolid transformation because of the change of pH environment, i.e., for liquid, when entering eye because of eye when in vitro The stronger pH sensitiveness of eyeball and be changed into semisolid;In this way, the present invention can be realized and be fast, easily administered, again in administration Can it is quick, in time, health, the site of action for reliably and efficiently covering eye, moreover it is possible to the surface of eyeball in time, health, can Lean on, be stably formed good protective film, so that antibacterials, which can be good at stabilization, plays its antibacterial curative effect, can be special The prevention and treatment for local infection of being performed the operation for ophthalmology I, II class;In addition, this liquid of the present invention is changed into semisolid spy Property, the slow-release capability of the property of medicine can be effectively extended, so as to realize stabilization, reliably long-acting administration, in artificial tears In be able to maintain that more than 24 hours, can be achieved once a day to be administered, so play that it is quick, continue, longer bactericidal make With.
Embodiment
The present invention is ophthalmic remedy, specifically a kind of gel for eye use for preventing and treating eye bacterium infection, and the gel for eye use Preparation method, purposes and application method.The technology contents of the present invention are carried out with multiple embodiments below detailed, clear, complete Site preparation illustrates that wherein embodiment 1 to 10 is the formula technique scheme of eye gel, in order that content is convenient, clear, now with list Form is expressed, and the gel for eye use raw material proportioning in each embodiment in embodiment 1 to 10 is to calculate by percentage to the quality, specifically As shown in table 1.
The concrete component material proportion data (mass percent) of the embodiment of the present invention 1 to 10 of table 1
The deployed gel for eye use of the various embodiments described above carries out pH value regulation with appropriate triethanolamine, and finished product is ophthalmically acceptable solidifying The pH value of glue needs to be in the interval range of 4.0~5.0 this pH value, such as pH value is 4.0,4.5 or 5.0 (in interval Specific pH value value depending on application requirement).
Embodiment 11
The preparation method of the present invention comprises the following steps:
(or other embodiments, such as embodiment 2,3,4,6,7,8,9 or formula ratio 10) are accurate with embodiment 1 for step 1. Standby each raw material;
Raw material components Acritamer 940 P and HPMC K4M are thrown in pure water, make Acritamer 940 P and HPMC K4M pure Water level is in uniform shape;It is swelled overnight, stirs to obtain settled solution;
Lavo-ofloxacin hydrochloride is added in the solution of step 1 by step 2., stirring and dissolving;
Triamcinolone acetonide acetate is added in the solution of step 2 by step 3., stirring and dissolving;
Appropriate triethanolamine is added in previous solu and carries out pH value regulation so that the pH value range of solution is in 4.0 ~5.0 is interval interior, such as pH value is 4.0,4.5 or 5.0 (value of the specific pH value in interval is depending on application requirement), i.e., Obtain gel for eye use.
Embodiment 12
The preparation method of the present invention comprises the following steps:
Step 1. prepares each raw material with the formula ratio of embodiment 5;
Raw material components Acritamer 940 P and HPMC K4M are thrown in pure water, make Acritamer 940 P and HPMC K4M pure Water level is in uniform shape;It is swelled overnight, stirs to obtain settled solution;
Lavo-ofloxacin hydrochloride is added in the solution of step 1 by step 2., stirring and dissolving;
Step 3. adds appropriate triethanolamine in the solution of step 2 and carries out pH value regulation so that the pH value model of solution Enclose be in 4.0~5.0 it is interval in, (value of the specific pH value in interval regards application will such as pH value is 4.0,4.5 or 5.0 Depending on asking), produce gel for eye use.
Embodiment 13
With the gel for eye use that any technical measures are obtained in above-described embodiment 1 to 12, the purposes of its purposes-i.e. of the invention It is, for treating non-viral and fungus-caused eye bacterium infection, to be particularly suitable for the part to ophthalmology I, the operation of II class The prevention and treatment of infection.
In the treatment for non-viral and fungus-caused eye bacterium infection, application method of the invention is, by eye Uniformly it is applied to gel on conjunctival sac, closes light ball 5 minutes in an instant of mesh, you can.
Various embodiments above is only to illustrate the present invention, rather than its limitations;Although with reference to the various embodiments described above to this hair It is bright to be described in detail, it will be understood by those within the art that:The present invention still can be to the various embodiments described above In concrete technical scheme modify, or to which part technical characteristic carry out equivalent substitution, and these modification or replace Change, the essence of appropriate technical solution is departed from the spirit and scope of the present invention.

Claims (7)

1. a kind of gel for eye use, it is characterised in that the gel for eye use is mainly made up of the raw material of following masses percentage:
Lavo-ofloxacin hydrochloride 0.1~1.5%,
Triamcinolone acetonide acetate 0~0.5%,
Acritamer 940 P 0.2~1.5%,
HPMC K4M 0.25~5.0%,
Pure water 91.5~99.45%;
The pH value of the gel for eye use is 4.0~5.0.
2. gel for eye use according to claim 1, it is characterised in that the pH value of the gel for eye use is with three appropriate ethanol Amine is adjusted.
3. the preparation method of gel for eye use described in a kind of claim 1, it is characterised in that the preparation method includes following step Suddenly:
Raw material components Acritamer 940 P and HPMC K4M are thrown in pure water by step 1., make Acritamer 940 P and HPMC K4M It is in uniform shape in pure water liquid level;It is swelled overnight, stirs to obtain settled solution;
Lavo-ofloxacin hydrochloride is added in the solution of step 1 by step 2., stirring and dissolving;
The pH value of the solution of step 3. regulating step 2 is 4.0~5.0, produces gel for eye use.
4. the preparation method of gel for eye use according to claim 3, it is characterised in that before the pH value regulation of step 3, in step Triamcinolone acetonide acetate is added in rapid 2 solution.
5. the preparation method of gel for eye use according to claim 3, it is characterised in that the pH value regulation of step 3 is with appropriate Triethanolamine is adjusted.
6. the purposes of gel for eye use described in a kind of claim 1, it is characterised in that the gel for eye use be used to treating it is non-viral and Fungus-caused eye bacterium infection.
7. the application method of gel for eye use described in a kind of claim 1, it is characterised in that the application method is will be described ophthalmically acceptable Gel is uniformly applied on conjunctival sac, closes light ball 5 minutes in an instant of mesh, you can.
CN201710374599.9A 2017-05-24 2017-05-24 A kind of gel for eye use and preparation method thereof, purposes and application method Withdrawn CN106963726A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201710374599.9A CN106963726A (en) 2017-05-24 2017-05-24 A kind of gel for eye use and preparation method thereof, purposes and application method

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201710374599.9A CN106963726A (en) 2017-05-24 2017-05-24 A kind of gel for eye use and preparation method thereof, purposes and application method

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CN106963726A true CN106963726A (en) 2017-07-21

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2745998C1 (en) * 2020-01-17 2021-04-05 Акционерное Общество "Производственная Фармацевтическая Компания Обновление" Bioadhesive antibacterial composition, the method of its manufacture (options)

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
樊莲莲等: "左氧氟沙星和曲安奈德双载药眼用凝胶的制备", 《中国药房》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2745998C1 (en) * 2020-01-17 2021-04-05 Акционерное Общество "Производственная Фармацевтическая Компания Обновление" Bioadhesive antibacterial composition, the method of its manufacture (options)
WO2021145795A3 (en) * 2020-01-17 2021-09-23 Акционерное Общество "Производственная Фармацевтическая Компания Обновление" Bioadhesive antibacterial agent and method for manufacturing same (variants)

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Application publication date: 20170721