CN102885768A - Pranoprofen in-situ gelling eye drop and preparation method thereof - Google Patents
Pranoprofen in-situ gelling eye drop and preparation method thereof Download PDFInfo
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- CN102885768A CN102885768A CN2012104394056A CN201210439405A CN102885768A CN 102885768 A CN102885768 A CN 102885768A CN 2012104394056 A CN2012104394056 A CN 2012104394056A CN 201210439405 A CN201210439405 A CN 201210439405A CN 102885768 A CN102885768 A CN 102885768A
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Abstract
A pranoprofen in-situ gelling eye drop is disclosed. The pranoprofen in-situ gelling eye drop comprises the components by mass percent: 0.1% of pranoprofen, 1%-40% of thickening agent, 0.03%-1.0% of pH adjusting agent, 0.01%-0.03% of bacteria inhibitor, 0.005%-0.2% of antioxidant, 0.01%-0.05% of chelating agent, and 0.1%-4.0% of solubilizing agent. The pranoprofen in-situ gelling eye drop disclosed by the invention has the characteristics that a material (e.g., poloxamer 407 and sodium alginate) with good biocompatibility and having the feature of temperature sensitivity, pH sensitivity or ion sensitivity is used as a matrix, the eye drop is administered in vitro under a solution state, phase change occurs immediately at the administered site in vivo in accordance with different environments inside and outside human body, so as to form in-situ gel; and the eye drop is convenient to use, high in bioavailability and long in residence time and results in good compliance of patients. The invention further discloses a preparation method of the pranoprofen in-situ gelling eye drop.
Description
Technical field
The invention belongs to medical technical field, be specifically related to a kind of eye drop that contains pranoprofen and preparation method thereof.
Background technology
Mainly adopt the use in conjunction control postoperative infection such as antibiotic and hormone behind the operated eye clinically at present, in order to avoid bring out disease.Glucocorticoid is control external eyes and the non-infection inflammation of anterior chamber of eye and the active drug of inflammation, but the eye use can cause the untoward reaction such as glaucoma, the infection of Secondary cases antibacterial.Therefore develop a kind of effectively and the medicine of few side effects has wide market prospect.
Pranoprofen, chemistry (RS)-2-(10-hydrogen-9-Evil-1-naphthazine-6-yl) propanoic acid by name, be the phenoxy propionic acid nonsteroid anti-inflammatory drugs, its mechanism of action is mainly and suppresses cyclooxygenase (COX) activity, synthesizing of blocking-up Eicosatetraenoic acid derivates, suppress the synthetic of prostaglandin, stabilizing cell membrane, the amelioration of inflammation reaction belongs to nonsteroidal antiinflammatory drug.Antiinflammation is better than aspirin and ibuprofen.
Present domestic pranoprofen eye drop goes on the market, but has no report and the Related product listing of pranoprofen original position gel eye drop and preparation thereof.
Pranoprofen is poor stability in aqueous solution, especially to photo-labile, and easily degraded in the long preservation process.Common eye use eye drop is shorter in the eye holdup time, and for guaranteeing to reach therapeutic effect, the patient often needs multiple dosing, and is extremely inconvenient, and patient compliance is poor.
Summary of the invention
The present invention mainly solves pranoprofen aqueous eye drops poor stability and short problem of holdup time, prepares a kind of pranoprofen original position gel eye drop, and its preparation method is provided.
The prepared pranoprofen original position gel eye drop of the present invention mainly comprises the pharmaceutic adjuvants such as principal agent pranoprofen, thickening agent, pH adjusting agent, antibacterial, antioxidant, chelating agen, solubilizing agent.
Thickening agent refers to one or more in poloxamer, sodium alginate, the carbomer etc.
PH adjusting agent refers to one or more in borate buffer solution system, acetate salt buffer liquid system, tartrate buffer system, the carbonate buffer solution system etc.
Antibacterial refers to one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, chlorobutanol, boric acid, thimerosal, the benzalkonium chloride etc.
Antioxidant refers to one or more in 2,6 ditertiary butyl p cresol (BHT), hydroxyanisol (BHA), sodium thiosulfate, hydroxyanisol, the 1-benzopyran derivatives etc.
Chelating agen refers to one or more in citric acid, the disodium edetate (EDTA-2Na) etc.
Solubilizing agent refers to one or more in tween 80 (2%), Polyethylene Glycol, the polyoxyethylene hydrogenated Oleum Ricini (2.5%) etc.
Technical scheme of the present invention is as follows:
A kind of pranoprofen original position gel eye drop, it is characterized in that: its quality group becomes pranoprofen 0.1%; Thickening agent 1%～40%; PH adjusting agent 0.03%～1.0%; Antibacterial 0.01%～0.03%; Antioxidant 0.005%～0.2%; Chelating agen 0.01%～0.05%; Solubilizing agent 0.1%～4.0%.
A kind of method for preparing above-mentioned original position gel eye drop, it is comprised of the following step:
Step 1. is pressed following mass percent proportioning following raw materials according: pranoprofen 0.1%; Thickening agent 1%～40%; PH adjusting agent 0.03%～1.0%; Antibacterial 0.01%～0.03%; Antioxidant 0.005%～0.2%; Chelating agen 0.01%～0.05%; Solubilizing agent 0.1%～4.0%.
Step 2. is dissolved in the thickening agent of said ratio in the water for injection, and 1. stand for standby use gets solution.
Step 3. is dissolved in pH adjusting agent, the antibacterial of said ratio in the water for injection, and heated and stirred makes dissolving fully, lets cool, and is for subsequent use, gets solution 2..
Step 4. is dissolved in chelating agen, antioxidant, the solubilizing agent of said ratio in the water for injection, and heated and stirred makes dissolving fully, lets cool, and is for subsequent use, gets solution 3..
3. step 5. is dissolved in solution with pranoprofen, stirs to make dissolving fully, gets solution 4..
Step 6. with solution 4. with 2. mix homogeneously of solution, get solution 5..
1. 5. step 7. mix solution with solution, supplies the injection water yield, stirs and make mix homogeneously, gets solution 6..
Step 8. 6. with filtering with microporous membrane, is sterilized solution, packing, and get final product.
This preparation method characteristic is: take good biocompatibility, have the material (such as poloxamer188, sodium alginate etc.) of the characteristics such as responsive to temperature, pH sensitivity or ion-sensitive as substrate, external with the solution state administration after, difference according to the human body internal and external environment undergoes phase transition at agents area immediately, form non-chemically crosslinked semi-solid preparation, namely be formed on the body gel, has the gentle controlled release ability of good compliance, and there is not the inaccurate defective of the external divided dose of general gel, easy to use, bioavailability is high, and the holdup time is long.
The specific embodiment
Embodiment 1
Take by weighing sodium alginate 5g, add water for injection 100mL, slowly stir and make dissolving, stand for standby use, as solution 1..Take by weighing benzalkonium chloride 0.13g, boric acid 8g adds an amount of water for injection, and heated and stirred makes dissolving, cooling, as solution 2..Take by weighing Borax 2.3g, EDTA-2Na0.15g, BHT0.025g, Tween-800.5g, heated and stirred makes dissolving, cooling, as solution 3..Take by weighing pranoprofen 0.5g, add solution 3., fully stir and make dissolving, as solution 4..With solution 2. with solution 4. mix and blend make into homogeneous system, add again solution 1., adding water for injection, to make the system final volume be 500mL, stirs and make mix homogeneously.With 0.22 μ m filtering with microporous membrane, sterilization, packing, and get final product.
Embodiment 2
Take by weighing poloxamer188 10g, add an amount of water for injection, fully stirring makes and is uniformly dispersed, and places more than the refrigerator cold-storage 12h, forms clear solution until polymer dissolves fully, stand for standby use, as solution 1..Take by weighing benzalkonium chloride 0.13g, boric acid 8g adds an amount of water for injection, and heated and stirred makes dissolving, cooling, as solution 2..Take by weighing Borax 2.3g, EDTA-2Na0.15g, BHT0.035g, Tween-800.75g, heated and stirred makes dissolving, cooling, as solution 3..Take by weighing pranoprofen 0.5g, add solution 3., fully stir and make dissolving, as solution 4..With solution 2. with solution 4. mix and blend make into homogeneous system, add again solution 1., adding water for injection, to make the system final volume be 500mL, stirs and make mix homogeneously.With 0.22 μ m filtering with microporous membrane, sterilization, packing, and get final product.
Embodiment 3
Take by weighing sodium alginate 8g, add water for injection 100mL, stir in the hot bath and make dissolving, stand for standby use, as solution 1..Take by weighing benzalkonium chloride 0.10g, boric acid 8g adds an amount of water for injection, and heated and stirred makes dissolving, cooling, as solution 2..Take by weighing Borax 2.3g, EDTA-2Na 0.15g, heated and stirred makes dissolving, cooling, as solution 3..Take by weighing BHT 0.075g, Tween-80 1.0g, heating makes dissolving, as solution 4..4. 3. solution mixed with solution, and stirring makes system even, gets solution 5..Take by weighing pranoprofen 0.5g, add solution 5., fully stir and make dissolving, as solution 6..With solution 2. with solution 6. mix and blend make into homogeneous system, add again solution 1., adding water for injection, to make the system final volume be 500mL, stirs and make mix homogeneously.With 0.22 μ m filtering with microporous membrane, sterilization, packing, and get final product.
Claims (7)
1. pranoprofen original position gel eye drop, it is characterized in that: its quality group becomes pranoprofen 0.1%; Thickening agent 1%～40%; PH adjusting agent 0.03%～1.0%; Antibacterial 0.01%～0.03%; Antioxidant 0.005%～0.2%; Chelating agen 0.01%～0.05%; Solubilizing agent 0.1%～4.0%.
2. pranoprofen original position gel eye drop according to claim 1, thickening agent refers to one or more in poloxamer, sodium alginate, the carbomer etc.
3. pranoprofen original position gel eye drop according to claim 1, pH adjusting agent refers to one or more in borate buffer solution system, acetate salt buffer liquid system, tartrate buffer system, the carbonate buffer solution system etc.
4. pranoprofen original position gel eye drop according to claim 1, antibacterial refers to one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, chlorobutanol, boric acid, thimerosal, the benzalkonium chloride etc.
5. pranoprofen original position gel eye drop according to claim 1, antioxidant refers to one or more in 2,6 ditertiary butyl p cresol (BHT), hydroxyanisol (BHA), sodium thiosulfate, hydroxyanisol, the 1-benzopyran derivatives etc.
6. pranoprofen original position gel eye drop according to claim 1, chelating agen refers to one or more in citric acid, the disodium edetate (EDTA-2Na) etc.
7. pranoprofen original position gel eye drop according to claim 1, solubilizing agent refers to one or more in tween 80 (2%), Polyethylene Glycol, the polyoxyethylene hydrogenated Oleum Ricini (2.5%) etc.
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| Application Number | Priority Date | Filing Date | Title |
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| CN2012104394056A CN102885768A (en) | 2012-11-02 | 2012-11-02 | Pranoprofen in-situ gelling eye drop and preparation method thereof |
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| CN2012104394056A CN102885768A (en) | 2012-11-02 | 2012-11-02 | Pranoprofen in-situ gelling eye drop and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014168595A1 (en) * | 2013-04-08 | 2014-10-16 | Yeditepe Universitesi | Polymer based hydrogel |
| WO2021157569A1 (en) * | 2020-02-03 | 2021-08-12 | 千寿製薬株式会社 | Use of polyether compound |
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| US4607038A (en) * | 1984-03-01 | 1986-08-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Ophthalmic pranoprofen compositions |
| 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 |
| CN101564374A (en) * | 2008-04-25 | 2009-10-28 | 北京和润创新医药科技发展有限公司 | Medicinal in situ forming eye gel |
| JP2011021003A (en) * | 2009-06-16 | 2011-02-03 | Rohto Pharmaceutical Co Ltd | Aqueous composition |
| JP2011136980A (en) * | 2009-12-01 | 2011-07-14 | Rohto Pharmaceutical Co Ltd | Ophthalmic composition for silicone hydrogel contact lens |
| CN102283805A (en) * | 2011-06-29 | 2011-12-21 | 扬子江药业集团有限公司 | Method for preparing eye drops containing non-ionic cellulose derivatives |
| JP2012031075A (en) * | 2010-07-29 | 2012-02-16 | Rohto Pharmaceutical Co Ltd | Ophthalmic composition for ionic silicone-hydrogel contact lens |
| JP2012067129A (en) * | 2004-02-27 | 2012-04-05 | Taisho Pharmaceutical Co Ltd | Ophthalmic solution |
| JP2012126734A (en) * | 2012-03-19 | 2012-07-05 | Taisho Pharmaceutical Co Ltd | Eyedrop medicine |
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- 2012-11-02 CN CN2012104394056A patent/CN102885768A/en active Pending
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| US4607038A (en) * | 1984-03-01 | 1986-08-19 | Yoshitomi Pharmaceutical Industries, Ltd. | Ophthalmic pranoprofen compositions |
| JP2012067129A (en) * | 2004-02-27 | 2012-04-05 | Taisho Pharmaceutical Co Ltd | Ophthalmic solution |
| 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 |
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| JP2011021003A (en) * | 2009-06-16 | 2011-02-03 | Rohto Pharmaceutical Co Ltd | Aqueous composition |
| JP2011136980A (en) * | 2009-12-01 | 2011-07-14 | Rohto Pharmaceutical Co Ltd | Ophthalmic composition for silicone hydrogel contact lens |
| JP2012031075A (en) * | 2010-07-29 | 2012-02-16 | Rohto Pharmaceutical Co Ltd | Ophthalmic composition for ionic silicone-hydrogel contact lens |
| CN102283805A (en) * | 2011-06-29 | 2011-12-21 | 扬子江药业集团有限公司 | Method for preparing eye drops containing non-ionic cellulose derivatives |
| JP2012126734A (en) * | 2012-03-19 | 2012-07-05 | Taisho Pharmaceutical Co Ltd | Eyedrop medicine |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014168595A1 (en) * | 2013-04-08 | 2014-10-16 | Yeditepe Universitesi | Polymer based hydrogel |
| US9655990B2 (en) | 2013-04-08 | 2017-05-23 | Yeditepe Universitesi | Polymer based hydrogel |
| WO2021157569A1 (en) * | 2020-02-03 | 2021-08-12 | 千寿製薬株式会社 | Use of polyether compound |
| EP4101469A1 (en) * | 2020-02-03 | 2022-12-14 | Senju Pharmaceutical Co., Ltd. | Use of polyether compound |
| EP4101469A4 (en) * | 2020-02-03 | 2024-05-29 | Senju Pharmaceutical Co., Ltd. | Use of polyether compound |
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Application publication date: 20130123 |