CN106256351A - Olopatadine hydrochloride gel eyedrop and preparation method thereof - Google Patents
Olopatadine hydrochloride gel eyedrop and preparation method thereof Download PDFInfo
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- CN106256351A CN106256351A CN201510339919.8A CN201510339919A CN106256351A CN 106256351 A CN106256351 A CN 106256351A CN 201510339919 A CN201510339919 A CN 201510339919A CN 106256351 A CN106256351 A CN 106256351A
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- olopatadine hydrochloride
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Abstract
The invention discloses a kind of Olopatadine hydrochloride gel eyedrop and preparation method thereof, it is with Olopatadine hydrochloride as primary raw material, add the adjuvants such as gel-type vehicle, isoosmotic adjusting agent, preservative, water for injection, swelling stir, after adjusting pH sterilizing, i.e. prepare 0.1%-0.2% Olopatadine hydrochloride gel eyedrop.Purpose is to provide practical, convenient for clinic, treat the ophthalmic preparation of allergy reliably, solves the problem that eye drop drug form is short in the eye holdup time, drug absorption is poor.
Description
Technical field
The present invention relates to a kind of Olopatadine hydrochloride gel eyedrop and preparation method thereof, belong to technical field of pharmaceuticals.
Background technology
Olopatadine hydrochloride (Olopatadine hydrochloride), chemical name: Z-11-(3-dimethylamino acrylic)-6,11-dihydro-dibenzo [b, e] oxa--2-acetic acid hydrochloride, chemical structural formula:
Molecular formula: C21H23NO3 •HCl, 373.87
Olopatadine hydrochloride is the potent safe antiallergic agent of the third generation, by the exploitation of consonance fermentation company of Japan, in 1997 and calendar year 2001 respectively in the U.S. and Japan's listing.Alcon company is developed into the eye drop of 0.1% and 0.2%, and trade name is respectively Patanol and Pataday, is used for treating anaphylaxis conjunctivitis.Olopatadine hydrochloride has suppression histamine release and the dual function of selectivity antagonism H1 receptor, and without the common central nervous system impression of H1 receptor antagonist class antiallergic agent and Cardiotoxity, clinic is used for treating allergic rhinitis, urticaria, dermatitis etc., is the antiallergic drug of first choice of a new generation.
At present, its regular dosage form is eye drop, eye drop have with low cost, prepare the features such as easy, easy to use, accepted by extensive patients.But eye drop exists, and bioavailability is low, need long term administration, it is easy to cause the problems such as locally or systemically physiological-toxicity reaction.It is used for multiple times that to be easily caused patient acceptability bad for a long time.
Therefore, it is an object of the invention to overcome above deficiency, it is provided that a kind of Olopatadine hydrochloride gel eyedrop and preparation method thereof.
Summary of the invention
The invention discloses a kind of Olopatadine hydrochloride gel eyedrop and preparation method thereof, it is with Olopatadine hydrochloride as primary raw material, add the adjuvants such as gel-type vehicle, isoosmotic adjusting agent, preservative, water for injection, swelling stir, after adjusting pH sterilizing, i.e. prepare 0.1%～0.2% Olopatadine hydrochloride gel eyedrop.
Inventive gel eye drop consists of the following composition:
Olopatadine hydrochloride 0.1%～0.2%, substrate 0.1%～25%, preservative 0.01%～0.1%, isoosmotic adjusting agent 0.1%～10%, surplus is water for injection.
Substrate is selected from following: the mixture of the one or more than one in carbomer, poloxamer, hydroxypropyl methyl cellulose, methylcellulose, hyaluronate sodium etc..
Preservative is selected from following: the mixture of the one or more than one in Metagin, second, propyl ester, benzalkonium chloride, benzalkonium bromide etc..
The isoosmotic adjusting agent one or more mixture in sodium chloride, glucose, mannitol, glycerol, sorbitol, propylene glycol etc..
The present invention is achieved through the following technical solutions:
Step one, the gel-type vehicle of accurate weighed recipe quantity, the most swelling in the lower water for injection adding about 60% total amount of stirring, filter, obtain clarifying viscous solution；Step 2, the Olopatadine hydrochloride of accurate weighed recipe quantity, other adjuvants in addition to gel-type vehicle, add the water for injection of about 40% total amount, after stirring and dissolving, through filtering with microporous membrane sterilizing；Under step 3, stirring, step 2 gained solution is added in step one gained viscous solution, be sufficiently stirred for making uniformly；Step 4, regulate pH to 6-8 with certain density hydrochloric acid or sodium hydroxide solution, use flowing steam sterilization, to obtain final product.
Above-described Olopatadine hydrochloride gel eyedrop and preparation method thereof, obtained eye drop is 0.1%～0.2% Olopatadine hydrochloride gel eyedrop.
The present invention, compared with ordinary eye drops dosage form, has the following characteristics that (1) this product selects substrate to be hydrophilic material, and viscosity is moderate, and lubricity is good, to part tissue of eye nonirritant；(2) this product can adhere to eyeball surface after instilling ophthalmic, increases medicine and the time of contact of eye and area, so that medicine slowly discharges, length of holding time, reduces times for spraying, reduces the zest to eye；(3) this product decreases medicine simultaneously and flows into the sense of discomfort that mouth and nose cause.
Detailed description of the invention
Embodiment 1:
Take about 6kg water for injection, the lower carbomer 80g that adds of stirring, abundant swelling rear filtration, obtain clarification viscous solution.Take water for injection about 4kg, add Olopatadine hydrochloride 10g, benzalkonium chloride 1g, sodium chloride 50g, be stirred to dissolve, after filtering with microporous membrane sterilizing, add in carbomer viscous solution, be sufficiently stirred for making uniformly.PH to 6～8 is regulated with 2mol/L hydrochloric acid or sodium hydroxide solution, after flowing steam sterilization, aseptic subpackaged, to obtain final product.
Embodiment 2:
Take about 6kg water for injection, the lower carbomer 70g that adds of stirring, the most swelling after, filter, obtain clarification viscous solution.Take water for injection about 4kg, add Olopatadine hydrochloride 20g, benzalkonium chloride 1g, sodium chloride 50g, be stirred to dissolve, after filtering with microporous membrane sterilizing, add in carbomer viscous solution, be sufficiently stirred for making uniformly.PH to 6～8 is regulated with 2mol/L hydrochloric acid or sodium hydroxide solution, after flowing steam sterilization, aseptic subpackaged, to obtain final product.
Embodiment 3:
Take about 6kg water for injection, the lower carbomer 80g that adds of stirring, the most swelling after, filter, obtain clarification viscous solution.Take water for injection about 4kg, add Olopatadine hydrochloride 10g, methyl hydroxybenzoate 3g, sodium chloride 50g, be stirred to dissolve, after filtering with microporous membrane sterilizing, add in carbomer viscous solution, be sufficiently stirred for making uniformly.PH to 6～8 is regulated with 2mol/L hydrochloric acid or sodium hydroxide solution, after flowing steam sterilization, aseptic subpackaged, to obtain final product.
Embodiment 4:
Take about 6kg water for injection, the lower carbomer 80g that adds of stirring, the most swelling after, filter, obtain clarification viscous solution.Take water for injection about 4kg, add Olopatadine hydrochloride 20g, methyl hydroxybenzoate 3g, sodium chloride 50g, be stirred to dissolve, after filtering with microporous membrane sterilizing, add in carbomer viscous solution, be sufficiently stirred for making uniformly.PH to 6～8 is regulated with 2mol/L hydrochloric acid or sodium hydroxide solution, after flowing steam sterilization, aseptic subpackaged, to obtain final product.
Above example discloses the present invention, and so it is not intended to limiting the invention, and the technical scheme that all employing equivalents or equivalent transformation mode are obtained, within all falling within protection scope of the present invention.
Claims (6)
1. an Olopatadine hydrochloride gel eyedrop, is made up of following raw materials by weight: Olopatadine hydrochloride 0.1%～0.2%, substrate 0.1%～25%, preservative 0.01%～0.1%, isoosmotic adjusting agent 0.1%～10%, and surplus is water for injection.
Gel eyedrop the most according to claim 1, it is characterised in that: substrate is selected from following: the mixture of the one or more than one in carbomer, poloxamer, hydroxypropyl methyl cellulose, methylcellulose, hyaluronate sodium etc..
Gel eyedrop the most according to claim 1, it is characterised in that: preservative is selected from following: the mixture of the one or more than one in Metagin, second, propyl ester, benzalkonium chloride, benzalkonium bromide etc..
Gel eyedrop the most according to claim 1, it is characterised in that: the mixture of isoosmotic adjusting agent one or more than one in sodium chloride, glucose, mannitol, glycerol, sorbitol, propylene glycol etc..
5. the preparation method of the gel eyedrop described in claim 1, it is characterised in that: specifically include following steps:
Step one, the gel-type vehicle of accurate weighed recipe quantity, the most swelling in the lower water for injection adding about 60% total amount of stirring, filter, obtain clarifying viscous solution；Step 2, the Olopatadine hydrochloride of accurate weighed recipe quantity, other adjuvants in addition to gel-type vehicle, add the water for injection of about 40% total amount, after stirring and dissolving, through filtering with microporous membrane sterilizing；Under step 3, stirring, step 2 gained solution is added in step one gained viscous solution, be sufficiently stirred for making uniformly；Step 4, regulate pH to 6-8 with certain density hydrochloric acid or sodium hydroxide solution, use flowing steam sterilization, to obtain final product.
The preparation method of Olopatadine hydrochloride gel eyedrop the most according to claim 5, it is characterised in that: obtained eye drop is 0.1%-0.2% Olopatadine hydrochloride gel eyedrop.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510339919.8A CN106256351A (en) | 2015-06-18 | 2015-06-18 | Olopatadine hydrochloride gel eyedrop and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510339919.8A CN106256351A (en) | 2015-06-18 | 2015-06-18 | Olopatadine hydrochloride gel eyedrop and preparation method thereof |
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| CN106256351A true CN106256351A (en) | 2016-12-28 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN201510339919.8A Pending CN106256351A (en) | 2015-06-18 | 2015-06-18 | Olopatadine hydrochloride gel eyedrop and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112603884A (en) * | 2020-12-24 | 2021-04-06 | 苏州工业园区天龙制药有限公司 | Eye drops containing olopatadine hydrochloride and preparation method thereof |
| CN115887367A (en) * | 2022-11-21 | 2023-04-04 | 山东诺明康药物研究院有限公司 | Olopatadine hydrochloride in-situ gel eye drops and preparation method and application thereof |
| CN119345125A (en) * | 2024-12-25 | 2025-01-24 | 广州市桐晖药业有限公司 | Azelastine hydrochloride eye drops |
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| WO2008011836A2 (en) * | 2006-07-25 | 2008-01-31 | Osmotica Corp. | Ophthalmic solutions |
| CN101180038A (en) * | 2005-03-23 | 2008-05-14 | 伊兰制药国际有限公司 | Nanoparticulate corticosteroid and antihistamine formulations |
| WO2008120249A1 (en) * | 2007-03-30 | 2008-10-09 | Sifi S.P.A. | Pharmaceutical formulations based on apolar and polar lipids for ophthalmic use |
| CN101766617A (en) * | 2010-01-12 | 2010-07-07 | 北京华禧联合科技发展有限公司 | Compound composition of intal and Statins |
| CN101966144A (en) * | 2009-07-28 | 2011-02-09 | 胡容峰 | Preparation and application of olopatadine in-situ gel |
| WO2011141929A2 (en) * | 2010-05-11 | 2011-11-17 | Cadila Healthcare Limited | Aqueous pharmaceutical compositions of fluticasone and olopatadine |
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2015
- 2015-06-18 CN CN201510339919.8A patent/CN106256351A/en active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101180038A (en) * | 2005-03-23 | 2008-05-14 | 伊兰制药国际有限公司 | Nanoparticulate corticosteroid and antihistamine formulations |
| WO2008011836A2 (en) * | 2006-07-25 | 2008-01-31 | Osmotica Corp. | Ophthalmic solutions |
| WO2008120249A1 (en) * | 2007-03-30 | 2008-10-09 | Sifi S.P.A. | Pharmaceutical formulations based on apolar and polar lipids for ophthalmic use |
| CN101966144A (en) * | 2009-07-28 | 2011-02-09 | 胡容峰 | Preparation and application of olopatadine in-situ gel |
| CN101766617A (en) * | 2010-01-12 | 2010-07-07 | 北京华禧联合科技发展有限公司 | Compound composition of intal and Statins |
| WO2011141929A2 (en) * | 2010-05-11 | 2011-11-17 | Cadila Healthcare Limited | Aqueous pharmaceutical compositions of fluticasone and olopatadine |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112603884A (en) * | 2020-12-24 | 2021-04-06 | 苏州工业园区天龙制药有限公司 | Eye drops containing olopatadine hydrochloride and preparation method thereof |
| CN115887367A (en) * | 2022-11-21 | 2023-04-04 | 山东诺明康药物研究院有限公司 | Olopatadine hydrochloride in-situ gel eye drops and preparation method and application thereof |
| CN119345125A (en) * | 2024-12-25 | 2025-01-24 | 广州市桐晖药业有限公司 | Azelastine hydrochloride eye drops |
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Application publication date: 20161228 |