CN102885768A - Pranoprofen in-situ gelling eye drop and preparation method thereof - Google Patents

Pranoprofen in-situ gelling eye drop and preparation method thereof Download PDF

Info

Publication number
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
Authority
CN
China
Prior art keywords
pranoprofen
eye drop
original position
solution
refers
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
CN2012104394056A
Other languages
Chinese (zh)
Inventor
兰雪莲
陈建
赵雷
郦红岩
吴修艮
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.)
JIANGSU JIBEIER PHARM CO Ltd
Original Assignee
JIANGSU JIBEIER PHARM 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 JIANGSU JIBEIER PHARM CO Ltd filed Critical JIANGSU JIBEIER PHARM CO Ltd
Priority to CN2012104394056A priority Critical patent/CN102885768A/en
Publication of CN102885768A publication Critical patent/CN102885768A/en
Pending legal-status Critical Current

Links

Landscapes

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

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

Pranoprofen original position gel eye drop and preparation method thereof
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.
CN2012104394056A 2012-11-02 2012-11-02 Pranoprofen in-situ gelling eye drop and preparation method thereof Pending CN102885768A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN2012104394056A CN102885768A (en) 2012-11-02 2012-11-02 Pranoprofen in-situ gelling eye drop and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2012104394056A CN102885768A (en) 2012-11-02 2012-11-02 Pranoprofen in-situ gelling eye drop and preparation method thereof

Publications (1)

Publication Number Publication Date
CN102885768A true CN102885768A (en) 2013-01-23

Family

ID=47529589

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2012104394056A Pending CN102885768A (en) 2012-11-02 2012-11-02 Pranoprofen in-situ gelling eye drop and preparation method thereof

Country Status (1)

Country Link
CN (1) CN102885768A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
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

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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)

* Cited by examiner, † Cited by third party
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

Similar Documents

Publication Publication Date Title
JP6444308B2 (en) Tetracycline topical formulation, its preparation and use
CA3000306A1 (en) Compositions including meloxicam-cyclodextrin inclusion complexes and methods of treating acute pain
JP5989095B2 (en) Transdermal composition of ibuprofen and method of use thereof
TWI283573B (en) Nateglinide containing preparations
AU2007339312B2 (en) Pharmaceutical compositions and method for treating inflammation in cattle and other animals
JP6117939B2 (en) Diclofenac composition
US11938109B2 (en) Methods for the preparation of a levothyroxine solution
TWI401078B (en) Chemically stable compositions of 4-hydroxy tamoxifen
AU2018420535A1 (en) Edaravone pharmaceutical composition
CN104902874A (en) Injectable depot formulation comprising optically active tolvaptan and process of producing the same
CA2748896C (en) Pharmaceutical composition comprising aleglitazar
EP2817069A1 (en) Composition comprising a retinoid and benzoyl peroxide
CN102885768A (en) Pranoprofen in-situ gelling eye drop and preparation method thereof
AU2017209981A1 (en) Process of preparing active pharmaceutical ingredient salts
CN103690516A (en) Aripiprazole oral membrane and preparation method thereof
CN103932974B (en) Ciclopirox olamine vaginal suppository composition and preparation method thereof
CN105213303A (en) A kind of bromfenac sodium hydrate thermosensitive type situ-gel eye drop and preparation method thereof
CN101978945B (en) A kind of ibuprofen medicinal composition
CN101278895A (en) Instant type gel preparation for eye and method of producing the same
JP2021536485A (en) Injectable sustained release antibiotic formulation
JP6925275B2 (en) Pharmaceutical composition for skin
US9775832B2 (en) Pharmaceutical composition for oral administration
CN107007559B (en) Stable oral pharmaceutical composition and preparation method thereof
CN102716107B (en) water-soluble ibuprofen pharmaceutical composition
CN105407882A (en) Pharmaceutical formulations comprising agomelatine in the form of agomelatine co-crystal with an organic acid

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130123