CN102552889A - Biologically sterilizing eye drop preparation - Google Patents
Biologically sterilizing eye drop preparation Download PDFInfo
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- CN102552889A CN102552889A CN2010106167043A CN201010616704A CN102552889A CN 102552889 A CN102552889 A CN 102552889A CN 2010106167043 A CN2010106167043 A CN 2010106167043A CN 201010616704 A CN201010616704 A CN 201010616704A CN 102552889 A CN102552889 A CN 102552889A
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Abstract
The invention belongs to the field of medical preparations and particularly relates to a biologically sterilizing eye drop preparation. The preparation comprises the following biologically sterilizing components in percentage by weight: 0.0001 to 1 percent of biologically sterilizing component, 0.001 to 10 percent of negative charge biological adhesive material and 0.001 to 10 percent of buffer solution. Compared with the traditional eye drop, the sterilizing eye drop preparation disclosed by the invention has the advantages that the bioavailability of medicaments in eyes can be obviously improved and the sterilizing efficiency of the biologically sterilizing component in the eyes can be obviously improved.
Description
Technical field
The invention belongs to the medical preparation field, relate to a kind of biological antibiotic eye drop preparation specifically.
Background technology
Clinical common infectious eye disease, many like eye conjunctivitis and keratitis is main with bacterial infection.The analysis of lots of clinical nosetiology shows that gram-positive cocci is main pathogenic bacterium like staphylococcus epidermidis staphylococcus aureus and micrococcus luteus etc.; Gram negative bacilli takes second place like Pseudomonas aeruginosa and escherichia coli etc.The ratio of gram positive bacteria infection has the trend that increases year by year, and gram negative bacilli is on a declining curve.At present, bacillary curing eye diseases is mainly commonly used with the antibiotic eye drop, but is easy to generate drug resistance.Along with antibiotic extensive application, Resistant strain also constantly increases.And the antibiotic collyrium is because of the unsuitable life-time service of its side effect.Therefore, new being used to of the development ophthalmic preparation of treating bacillary oculopathy just becomes the focus of research.In recent years, both at home and abroad the biofungicide of the unique bactericidal activity of novel antibacterial medicine-have such as staphylococcus lysozyme, lysozyme and antibacterial peptide more and antibacterial peptide come to receive publicity more.Staphylococcus lysozyme is that Staphylococus Simulans staphylococcus is secreted the protein product outside born of the same parents, and molecular weight is 27kDa, contains 246 aminoacid, is a kind of endopeptidase, and isoelectric point, IP is 10.4～11.4, and is positively charged under the physiological condition.This enzyme can cut off the pentaglycine peptide bond bridge construction in the aureus cell wall Peptidoglycan, thereby reaches the purpose of rapid dissolving and killing bacteria.Even the drug resistance staphylococcus aureus, MRSA and " superbacteria ", staphylococcus lysozyme has very strong bactericidal action too, and is not easy to induce the generation Resistant strain, and has excellent biological compatibility.Lysozyme (lysozyme) is one type can make antibacterial, amide yeast or the dissolving of fungal cell wall, causes the bacteriolyze factor of microbial death, and isoelectric point, IP is 10.7-11.0.The gram-positive bacterium cell wall mainly is made up of Peptidoglycan polysaccharide such as (Peptidoglycan) and small-molecular peptides albumen, and glycosidic bond and peptide bond are its main connecting keys in the RF of cell wall.Lysozyme can be through the glycosidic bond (β-1 between-acetylmuramic acid C-1 and the N-acetylglucosamine C-4 of Peptidoglycan in hydrolysis cell wall and the theca externa; Peptide bond etc. between 4 glycosidic bonds, peptide bond such as D-Ala and Lys) and amido link (like amido link between wall acid of N-acetyl and Ala etc.); The bacteria cell wall RF is destroyed, cell wall lysis and death.Antibacterial peptide be in the organism through the micromolecule polypeptide of a kind of biologically active of inducing generation, molecular weight is made up of 20～60 amino acid residues about 2000～7000.This type active polypeptide majority has characteristics such as strong basicity, heat stability and broad-spectrum antiseptic.
Since traditional ophthalmic preparation exist some significant disadvantages as: medicine is short in the eye diseased region time of staying, absorbs not good enoughly, needs frequent drug administration etc.Therefore how improving biofungicide in ocular absorption, improve its therapeutic index, reduce its untoward reaction, is the problem that the present invention need solve.
Summary of the invention
The technical issues that need to address of the present invention provide a kind of long in the eye holdup time, the biological antibiotic eye drop preparation that bactericidal potency is strong.
Design of the present invention is such:
Microsphere or nanoparticle are that the dosing eyes system of carrier compares with traditional eye drop, can significantly improve the bioavailability of medicine at eye.In addition, the polymer that hyaluronic acid, sodium carboxymethyl cellulose, carbomer, chondroitin sulfate etc. have the bio-adhesive characteristic can combine with conjunctiva is mucoprotein, and the prolong drug particle is in the holdup time in cornea proparea.Biofungicide among the present invention (staphylococcus lysozyme, lysozyme and antibacterial peptide) is a kind of alkaline protein or polypeptide; Be bordering in vivo under the neutral pH environment and have a large amount of positive charges; Can interact through positive and negative charge with electronegative bio-adhesive material and form nanoparticle or microgranule, thereby the synergistic effect that can produce drug effect improves the fungicidal effectiveness of enzyme at eye.
Technical scheme of the present invention is following:
A kind of biological antibiotic eye drop preparation, by weight percentage, its component comprises: biological antibiotic composition 0.0001～1%; Negative charge bio-adhesive material 0.001～10%, antibacterial 0～0.4%, buffer surplus.
Described biofungicide is one or more in lysozyme, staphylococcus lysozyme and the antibacterial peptide.
Described negative charge bio-adhesive material is one or more in hyaluronate sodium, dextran sulfate, sodium carboxymethyl cellulose, carbomer, chondroitin sulfate, the sodium alginate.
Described antibacterial be hibitane, chlorobutanol, phenoxyethanol one or more.
Described buffer is a kind of in phosphate buffer, borate buffer solution, lucky Fei Shi buffer, the sodium acetate-borate buffer.
The specific embodiment
The preparation of embodiment 1 antibacterial peptide-chondroitin sulfate eye drop
Get antibacterial peptide 12mg and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Get chondroitin sulfate 0.1g and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Antibacterial peptide solution after filtering and chondroitin sulfate cellulose solution are mixed stirring,, promptly get antibacterial peptide-chondroitin sulfate eye drop with 1000 times of phosphate buffer (pH 6.5) dilutions.
The preparation of embodiment 2 lysozyme-hyaluronate sodium eye drop
Get lysozyme 120mg and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Get hyaluronate sodium 0.1g and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Lysozyme soln after filtering and sodium hyaluronate solution are mixed stirring,, promptly get lysozyme-hyaluronate sodium eye drop with 1000 times of borate buffer solution (pH 7.4) dilutions.
The preparation of embodiment 3 staphylococcus lysozymes-dextran sulfate eye drop
Get staphylococcus lysozyme 120mg and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Get dextran sulfate 1g and add the 1ml water dissolution, 0.22 μ m membrane filtration degerming.Dissolving staphylococcal bacteria enzymatic solution after filtering and sodium alginate soln are mixed stirring,, promptly get staphylococcus lysozyme-dextran sulfate eye drop with 1000 times of sodium acetate-borate buffer (pH 7.4) dilutions.
Embodiment 4 antibacterial peptides-chondroitin sulfate eye drop is to the bactericidal action of staphylococcus aureus
Behind antibacterial peptide in the artificial tears-chondroitin sulfate eye drop and staphylococcus aureus (ATCC43300) the Resistant strain effect 10min, the coated plate counting, its sterilizing rate is 99.9%.
Claims (5)
1. a biological antibiotic eye drop preparation is characterized in that, by weight percentage, its composition comprises biological antibiotic composition 0.0001～1%, negative charge bio-adhesive material 0.001～10%, antibacterial 0～0.4%, buffer surplus.
2. described biofungicide is one or more in lysozyme, staphylococcus lysozyme and the antibacterial peptide.
3. biological antibiotic eye drop preparation as claimed in claim 1 is characterized in that, described negative charge bio-adhesive material is one or more in hyaluronate sodium, dextran sulfate, sodium carboxymethyl cellulose, carbomer, chondroitin sulfate, the sodium alginate.
4. biological antibiotic eye drop preparation as claimed in claim 2 is characterized in that, described antibacterial be hibitane, chlorobutanol, phenoxyethanol one or more.
5. biological antibiotic eye drop preparation as claimed in claim 1 is characterized in that, described buffer is a kind of in phosphate buffer, borate buffer solution, lucky Fei Shi buffer, the sodium acetate-borate buffer.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2010106167043A CN102552889A (en) | 2010-12-27 | 2010-12-27 | Biologically sterilizing eye drop preparation |
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| CN2010106167043A CN102552889A (en) | 2010-12-27 | 2010-12-27 | Biologically sterilizing eye drop preparation |
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| CN102552889A true CN102552889A (en) | 2012-07-11 |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104524557A (en) * | 2014-12-16 | 2015-04-22 | 杨陈 | Lysostaphin compound disinfection gel |
| CN105536026A (en) * | 2014-10-28 | 2016-05-04 | 无锡灵锡医疗器械科技有限公司 | Contact lens care composition |
| CN105622741A (en) * | 2014-10-28 | 2016-06-01 | 无锡灵锡医疗器械科技有限公司 | Preparation method of composition for contact lens surface antibacterial coating and application method |
| CN106668850A (en) * | 2015-11-05 | 2017-05-17 | 惠众国际医疗器械（北京）有限公司 | Natural bactericides/antibacterial agents |
| EP3287171A1 (en) * | 2013-02-28 | 2018-02-28 | Laboratoires Thea S.A.S. | Topical antimicrobial dermatological composition for ophtalmologic use |
| WO2019237633A1 (en) * | 2018-06-14 | 2019-12-19 | 陕西慧康生物科技有限责任公司 | Novel artificial tears containing recombinant human lysozyme and recombinant human epidermal growth factor |
| WO2019237634A1 (en) * | 2018-06-14 | 2019-12-19 | 陕西慧康生物科技有限责任公司 | Novel artificial tears containing recombinant human lysozyme |
| CN114106937A (en) * | 2021-11-26 | 2022-03-01 | 东南大学 | Contact lens care solution |
| CN115429749A (en) * | 2022-09-14 | 2022-12-06 | 昆山博青生物科技有限公司 | Composite lysozyme antibacterial gel and preparation method thereof |
-
2010
- 2010-12-27 CN CN2010106167043A patent/CN102552889A/en active Pending
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3287171A1 (en) * | 2013-02-28 | 2018-02-28 | Laboratoires Thea S.A.S. | Topical antimicrobial dermatological composition for ophtalmologic use |
| CN105536026A (en) * | 2014-10-28 | 2016-05-04 | 无锡灵锡医疗器械科技有限公司 | Contact lens care composition |
| CN105622741A (en) * | 2014-10-28 | 2016-06-01 | 无锡灵锡医疗器械科技有限公司 | Preparation method of composition for contact lens surface antibacterial coating and application method |
| CN104524557A (en) * | 2014-12-16 | 2015-04-22 | 杨陈 | Lysostaphin compound disinfection gel |
| CN106668850A (en) * | 2015-11-05 | 2017-05-17 | 惠众国际医疗器械（北京）有限公司 | Natural bactericides/antibacterial agents |
| WO2019237633A1 (en) * | 2018-06-14 | 2019-12-19 | 陕西慧康生物科技有限责任公司 | Novel artificial tears containing recombinant human lysozyme and recombinant human epidermal growth factor |
| WO2019237634A1 (en) * | 2018-06-14 | 2019-12-19 | 陕西慧康生物科技有限责任公司 | Novel artificial tears containing recombinant human lysozyme |
| US20210121540A1 (en) * | 2018-06-14 | 2021-04-29 | Shaanxi Huikang Bio-Tech Co., Ltd. | Novel artificial tears containing recombinant human lysozyme |
| AU2018428270B2 (en) * | 2018-06-14 | 2022-09-01 | Shaanxi Huikang Bio-Tech Co., Ltd. | Novel artificial tears containing recombinant human lysozyme |
| CN114106937A (en) * | 2021-11-26 | 2022-03-01 | 东南大学 | Contact lens care solution |
| CN115429749A (en) * | 2022-09-14 | 2022-12-06 | 昆山博青生物科技有限公司 | Composite lysozyme antibacterial gel and preparation method thereof |
| CN115429749B (en) * | 2022-09-14 | 2023-11-10 | 昆山博青生物科技有限公司 | Compound lysozyme antibacterial gel and preparation method thereof |
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Application publication date: 20120711 |