CN112545985A - Eye drops containing netilmicin sulfate and preparation method thereof - Google Patents
Eye drops containing netilmicin sulfate and preparation method thereof Download PDFInfo
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- CN112545985A CN112545985A CN202011621221.2A CN202011621221A CN112545985A CN 112545985 A CN112545985 A CN 112545985A CN 202011621221 A CN202011621221 A CN 202011621221A CN 112545985 A CN112545985 A CN 112545985A
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- purified water
- netilmicin sulfate
- preservative
- netilmicin
- eye drops
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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- Life Sciences & Earth Sciences (AREA)
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- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses an eye drop containing netilmicin sulfate, wherein each 1000ml of the eye drop comprises the following components: 1-10g of netilmicin sulfate, 60-80g of preservative, 1-10g of isoosmotic adjusting agent and the balance of purified water. The main drug in the eye drops provided by the invention is netilmicin sulfate, and the auxiliary materials are preservative, isotonic conditioning agent and purified water. The whole preparation process is simple, the production efficiency is high, and the preparation method can be used for treating various eye infections sensitive to netilmicin.
Description
Technical Field
The invention relates to the technical field of medicines, and in particular relates to eye drops containing netilmicin sulfate.
Background
Netilmicin sulfate has good curative effect on various ophthalmic infections of sensitive bacteria, but no ophthalmic preparation is clinically used at present. The 2002 patent (ZL02138662.5) discloses the application of netilmicin sulfate in the preparation of eye drop preparations, but no product is clinically applied in the prior art. The patent also comprises an antioxidant, an antioxidant synergist, a preservative, a pH regulator, an isotonic regulator, a stabilizer and a solvent besides the main raw material netilmicin sulfate, and the technical preparation has the defects of complex components, easy reaction risk of main medicines and various auxiliary materials in product preservation, difficult industrial production and the like.
Disclosure of Invention
It is an object of the present invention to provide an eye drop containing netilmicin sulfate that solves one or more of the above-mentioned problems of the prior art.
The invention provides an eye drop containing netilmicin sulfate, wherein each 1000ml of the eye drop comprises the following components: 1-10g of netilmicin sulfate, 60-80g of preservative, 1-10g of isoosmotic adjusting agent and the balance of purified water.
In certain embodiments, the preservative is selected from one or more of benzalkonium chloride, benzalkonium bromide, chlorhexidine.
In certain embodiments, the isotonicity adjusting agent is selected from one or more of sodium chloride, sorbitol, glycerin, PEG, propylene glycol.
The invention provides a preparation method of eye drops containing netilmicin sulfate, which comprises the following steps:
step 1): weighing netilmicin sulfate, adding 200ml of purified water, and stirring until the netilmicin sulfate is completely dissolved;
step 2): adding a prescription amount of preservative into the solution obtained in the step 1), stirring uniformly, filtering, washing a filter membrane with purified water, and collecting filtrate and washing liquid;
step 3): weighing the formula amount of the isotonic regulator, dissolving with purified water, and filtering;
step 4): adding the filtrate and washing liquid obtained in the step 2) into the isotonic regulator solution obtained in the step 3), supplementing the solution to 1000ml with purified water, filtering, measuring the content, and subpackaging in eye drops.
In certain embodiments, the filtration in steps 2) to 4) is through a 0.22 μm microporous membrane.
In certain embodiments, the amount of purified water used to flush the filter in step 2) is 50 ml.
In certain embodiments, 200ml of purified water is used to dissolve the isotonic adjusting agent in step 3).
In some embodiments, the eye drop bottle of step 4) is pre-sterilized and dried.
Compared with the prior art, the invention has the beneficial effects that: the main drug in the eye drops provided by the invention is netilmicin sulfate, and the auxiliary materials are preservative, isotonic conditioning agent and purified water. The whole preparation process is simple, the production efficiency is high, and the preparation method can be used for treating various eye infections sensitive to netilmicin.
Detailed Description
The present invention will be described in further detail below with reference to embodiments.
The invention discloses an eye drop containing netilmicin sulfate, wherein each 1000ml of the eye drop comprises the following components: 1-10g of netilmicin sulfate, 60-80g of preservative, 1-10g of isoosmotic adjusting agent and the balance of purified water. The preservative is one or more selected from benzalkonium chloride, benzalkonium bromide and chlorhexidine. The isotonic regulator is selected from one or more of sodium chloride, sorbitol, glycerol, PEG, and propylene glycol.
The invention also discloses a preparation method of the eye drops, which comprises the following steps:
step 1): weighing netilmicin sulfate, adding 200ml of purified water, and stirring until the netilmicin sulfate is completely dissolved;
step 2): adding a prescription amount of preservative into the solution obtained in the step 1), stirring uniformly, filtering, washing a filter membrane with purified water, and collecting filtrate and washing liquid;
step 3): weighing the formula amount of the isotonic regulator, dissolving with purified water, and filtering;
step 4): adding the filtrate and washing liquid obtained in the step 2) into the isotonic regulator solution obtained in the step 3), supplementing the solution to 1000ml with purified water, filtering, measuring the content, and subpackaging in eye drops.
The invention is further illustrated by the following specific examples.
Example 1
The present embodiment discloses an eye drop containing netilmicin sulfate, which comprises the following main components: netilmicin sulfate 2g, benzalkonium bromide solution 2g, sodium chloride 10g, purified water to 1000 ml.
The preparation method comprises the following steps: precisely measuring 2g of netilmicin sulfate, adding 200ml of purified water, stirring until the netilmicin sulfate is completely dissolved, adding 2g of benzalkonium bromide, stirring, filtering through a 0.22-micron microporous membrane, washing the membrane with 50ml of purified water, and collecting filtrate and washing liquid for later use.
10g of sodium chloride serving as an isotonic regulator is precisely weighed, dissolved in 200ml of purified water and filtered by a 0.22 mu m microporous filter membrane.
Adding the filtrate and washing solution into isoosmotic adjusting agent solution, adding purified water to 1000ml, filtering with 0.22 μm microporous membrane, measuring content, and packaging into sterilized dry eye drop bottle.
Example 2
The present embodiment discloses an eye drop containing netilmicin sulfate, which comprises the following main components: 3g of netilmicin sulfate, 3g of benzalkonium bromide solution, 9g of sodium chloride and purified water are added to 1000 ml.
The preparation method comprises the following steps: precisely measuring 3g of netilmicin sulfate, adding 200ml of purified water, stirring until the netilmicin sulfate is completely dissolved, adding 3g of benzalkonium bromide, stirring, filtering through a 0.22-micron microporous membrane, washing the membrane with 50ml of purified water, and collecting filtrate and washing liquid for later use.
9g of sodium chloride serving as an isotonic regulator is precisely weighed, dissolved in 200ml of purified water and filtered by a 0.22 mu m microporous filter membrane.
Adding the filtrate and washing solution into isoosmotic adjusting agent solution, adding purified water to 1000ml, filtering with 0.22 μm microporous membrane, measuring content, and packaging into sterilized dry eye drop bottle.
Example 3
The present embodiment discloses an eye drop containing netilmicin sulfate, which comprises the following main components: 3g of netilmicin sulfate, 3g of benzalkonium chloride solution, 9g of sorbitol and purified water are added to 1000 ml.
The preparation method comprises the following steps: precisely measuring 3g of netilmicin sulfate, adding 200ml of purified water, stirring until the netilmicin sulfate is completely dissolved, adding 3g of benzalkonium chloride solution, stirring uniformly, filtering through a 0.22-micron microporous membrane, washing the membrane with 50ml of purified water, and collecting filtrate and washing liquid for later use.
9g of isoosmotic adjusting agent sorbitol is precisely weighed and dissolved in 200ml of purified water, and the solution is filtered by a 0.22 mu m microporous filter membrane.
Adding the filtrate and washing solution into isoosmotic adjusting agent solution, adding purified water to 1000ml, filtering with 0.22 μm microporous membrane, measuring content, and packaging into sterilized dry eye drop bottle.
Example 4
The present embodiment discloses an eye drop containing netilmicin sulfate, which comprises the following main components: 9g of netilmicin sulfate, 6g of chlorhexidine solution, 7g of propylene glycol and purified water are added to 1000 ml.
The preparation method comprises the following steps: precisely measuring 9g of netilmicin sulfate, adding 200ml of purified water, stirring until the netilmicin sulfate is completely dissolved, adding 6g of chlorhexidine solution, stirring uniformly, filtering through a 0.22 mu m microporous membrane, washing the membrane with 50ml of purified water, and collecting filtrate and washing liquid for later use.
6g of propylene glycol serving as an isotonic regulator is precisely weighed, dissolved in 200ml of purified water and filtered by a 0.22 mu m microporous filter membrane.
Adding the filtrate and washing solution into isoosmotic adjusting agent solution, adding purified water to 1000ml, filtering with 0.22 μm microporous membrane, measuring content, and packaging into sterilized dry eye drop bottle.
The netilmicin sulfate belongs to aminoglycoside antibiotics, the antibacterial spectrum of the netilmicin sulfate is similar to that of gentamicin, and the netilmicin sulfate-containing eye drops disclosed by the invention are stable to aminoglycoside acetyltransferase AAC (3) through experiments. The present invention is sensitive to strains that produce the enzyme and are resistant to drugs such as kanamycin, gentamicin, tobramycin, sisomicin, and the like. The half-life of the invention is 2-2.5 hours, which is not changed with the administration route, but the half-life can be prolonged when the dosage is increased (the dosage is 3mg/kg, and t1/2 is 3 hours). 80% of the drug is excreted in the urine within 24 hours, and the urine drug concentration may exceed 100. mu.g/ml.
After being used, the eye drops disclosed by the invention are widely distributed in various main organs and various body fluids, but have low concentration in cerebrospinal fluid and bile. Since the product can enter ascites or edema fluid, the blood concentration of such patients is often lower than that of other patients. The blood concentration of the patient with fever is usually lower than that of the patient without fever, but the blood concentration can be slightly increased after fever abating. The antibacterial action of the eye drops disclosed by the invention is basically similar to that of gentamicin, and the eye drops have good antibacterial action on enterobacteriaceae bacteria such as escherichia coli, klebsiella, enterobacter, proteus, shigella, salmonella, citric acid bacillus, serratia, pseudomonas aeruginosa, nitrate negative bacillus and the like.
The above description is only a preferred embodiment of the present invention, and it should be noted that, for those skilled in the art, various changes and modifications can be made without departing from the inventive concept of the present invention, and these should be considered as within the scope of the present invention.
Claims (8)
1. An eye drop containing netilmicin sulfate is characterized in that each 1000ml of eye drop comprises the following components: 1-10g of netilmicin sulfate, 60-80g of preservative, 1-10g of isoosmotic adjusting agent and the balance of purified water.
2. An ophthalmic solution containing netilmicin sulfate as claimed in claim 1, wherein the preservative is selected from benzalkonium chloride, benzalkonium bromide and chlorhexidine.
3. An ophthalmic solution containing netilmicin sulphate as claimed in claim 2, wherein the isotonicity adjusting agent is selected from one or more of sodium chloride, sorbitol, glycerol, PEG, propylene glycol.
4. A method for preparing an ophthalmic solution according to claim 3, comprising the steps of:
step 1): weighing netilmicin sulfate, adding 200ml of purified water, and stirring until the netilmicin sulfate is completely dissolved;
step 2): adding a prescription amount of preservative into the solution obtained in the step 1), stirring uniformly, filtering, washing a filter membrane with purified water, and collecting filtrate and washing liquid;
step 3): weighing the formula amount of the isotonic regulator, dissolving with purified water, and filtering;
step 4): adding the filtrate and washing liquid obtained in the step 2) into the isotonic regulator solution obtained in the step 3), supplementing the solution to 1000ml with purified water, filtering, measuring the content, and subpackaging in eye drops.
5. The method for producing eye drops according to claim 4, wherein the filtration in the step 2) to the step 4) is performed by filtration through a 0.22 μm microfiltration membrane.
6. The process for producing ophthalmic solutions according to claim 5, wherein the amount of purified water used for washing the filter in the step 2) is 50 ml.
7. A process for the preparation of ophthalmic solutions according to claim 6, wherein the isotonic adjusting agent is dissolved in 200ml of purified water in step 3).
8. The method for producing eye drops according to claim 7, wherein the eye drop bottle in the step 4) is preliminarily sterilized and dried.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011621221.2A CN112545985A (en) | 2020-12-30 | 2020-12-30 | Eye drops containing netilmicin sulfate and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011621221.2A CN112545985A (en) | 2020-12-30 | 2020-12-30 | Eye drops containing netilmicin sulfate and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN112545985A true CN112545985A (en) | 2021-03-26 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202011621221.2A Pending CN112545985A (en) | 2020-12-30 | 2020-12-30 | Eye drops containing netilmicin sulfate and preparation method thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1502335A (en) * | 2002-11-21 | 2004-06-09 | 安徽省安泰医药生物技术有限责任公司 | Application of Netilmicin sulfate in preparation of eye drops |
| RU2580630C1 (en) * | 2015-03-19 | 2016-04-10 | Общество с ограниченной ответственностью "Научно-внедренческий центр Агроветзащита" | Antibacterial drug in form of drops for treating eye diseases in animals |
-
2020
- 2020-12-30 CN CN202011621221.2A patent/CN112545985A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1502335A (en) * | 2002-11-21 | 2004-06-09 | 安徽省安泰医药生物技术有限责任公司 | Application of Netilmicin sulfate in preparation of eye drops |
| RU2580630C1 (en) * | 2015-03-19 | 2016-04-10 | Общество с ограниченной ответственностью "Научно-внедренческий центр Агроветзащита" | Antibacterial drug in form of drops for treating eye diseases in animals |
Non-Patent Citations (1)
| Title |
|---|
| 安媛等: "硫酸奈替米星滴眼液的制备与质量控制", 《中国医院药学杂志》 * |
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Address after: 219 Furong Zhongsi Road, Xishan Economic and Technological Development Zone, Wuxi City, Jiangsu Province, 214000 Applicant after: Zhuohe Pharmaceutical Group Co.,Ltd. Address before: 219 Furong Zhongsi Road, Xishan Economic and Technological Development Zone, Wuxi City, Jiangsu Province, 214000 Applicant before: Zhuohe Pharmaceutical Group Co.,Ltd. |
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| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20210326 |