CN101264053B - Oxybuprocaine hydrochloride eye drops and preparation thereof - Google Patents
Oxybuprocaine hydrochloride eye drops and preparation thereof Download PDFInfo
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- CN101264053B CN101264053B CN2008100113911A CN200810011391A CN101264053B CN 101264053 B CN101264053 B CN 101264053B CN 2008100113911 A CN2008100113911 A CN 2008100113911A CN 200810011391 A CN200810011391 A CN 200810011391A CN 101264053 B CN101264053 B CN 101264053B
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- oxybuprocaine
- eye drops
- gram
- purified water
- polyvinyl alcohol
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- 239000003889 eye drop Substances 0.000 title claims abstract description 30
- 229940012356 eye drops Drugs 0.000 title claims abstract description 27
- 238000002360 preparation method Methods 0.000 title claims abstract description 13
- PRGUDWLMFLCODA-UHFFFAOYSA-N oxybuprocaine hydrochloride Chemical compound [Cl-].CCCCOC1=CC(C(=O)OCC[NH+](CC)CC)=CC=C1N PRGUDWLMFLCODA-UHFFFAOYSA-N 0.000 title claims description 25
- 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 29
- 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 29
- 239000003814 drug Substances 0.000 claims abstract description 18
- 229960003502 oxybuprocaine Drugs 0.000 claims abstract description 16
- CMHHMUWAYWTMGS-UHFFFAOYSA-N oxybuprocaine Chemical compound CCCCOC1=CC(C(=O)OCCN(CC)CC)=CC=C1N CMHHMUWAYWTMGS-UHFFFAOYSA-N 0.000 claims abstract description 16
- 239000002994 raw material Substances 0.000 claims abstract description 13
- 239000008213 purified water Substances 0.000 claims description 30
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 30
- 229940068984 polyvinyl alcohol Drugs 0.000 claims description 28
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims description 28
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 20
- 125000001246 bromo group Chemical group Br* 0.000 claims description 20
- 229940087511 calcium disodium versenate Drugs 0.000 claims description 20
- 239000000243 solution Substances 0.000 claims description 8
- 230000001954 sterilising effect Effects 0.000 claims description 8
- 238000004659 sterilization and disinfection Methods 0.000 claims description 8
- 238000003756 stirring Methods 0.000 claims description 8
- 230000000694 effects Effects 0.000 abstract description 12
- 230000009471 action Effects 0.000 abstract description 5
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 abstract description 4
- 206010002091 Anaesthesia Diseases 0.000 abstract description 4
- 230000037005 anaesthesia Effects 0.000 abstract description 4
- 210000004877 mucosa Anatomy 0.000 abstract description 3
- 230000008901 benefit Effects 0.000 abstract description 2
- 230000007794 irritation Effects 0.000 abstract description 2
- 239000003109 Disodium ethylene diamine tetraacetate Substances 0.000 abstract 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 abstract 1
- 238000010521 absorption reaction Methods 0.000 abstract 1
- 229960002233 benzalkonium bromide Drugs 0.000 abstract 1
- KHSLHYAUZSPBIU-UHFFFAOYSA-M benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 abstract 1
- 235000019301 disodium ethylene diamine tetraacetate Nutrition 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 238000002474 experimental method Methods 0.000 abstract 1
- 230000008595 infiltration Effects 0.000 abstract 1
- 238000001764 infiltration Methods 0.000 abstract 1
- 239000002574 poison Substances 0.000 abstract 1
- 231100000614 poison Toxicity 0.000 abstract 1
- 238000012360 testing method Methods 0.000 description 7
- 238000002691 topical anesthesia Methods 0.000 description 5
- 230000003444 anaesthetic effect Effects 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 230000004410 intraocular pressure Effects 0.000 description 3
- 231100000331 toxic Toxicity 0.000 description 3
- 230000002588 toxic effect Effects 0.000 description 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- 206010017012 Foreign body in eye Diseases 0.000 description 2
- JEIPFZHSYJVQDO-UHFFFAOYSA-N ferric oxide Chemical compound O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 239000003589 local anesthetic agent Substances 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- OUROWMSQIGUYLY-UHFFFAOYSA-N C(=O)O.C1(=CC=CC=C1)OC(CC)CN Chemical compound C(=O)O.C1(=CC=CC=C1)OC(CC)CN OUROWMSQIGUYLY-UHFFFAOYSA-N 0.000 description 1
- 208000028006 Corneal injury Diseases 0.000 description 1
- 108090000371 Esterases Proteins 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 1
- 108010052164 Sodium Channels Proteins 0.000 description 1
- 102000018674 Sodium Channels Human genes 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 230000004308 accommodation Effects 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 229940124326 anaesthetic agent Drugs 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 229960004194 lidocaine Drugs 0.000 description 1
- 229960005015 local anesthetics Drugs 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000036407 pain Effects 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 210000001747 pupil Anatomy 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229960002372 tetracaine Drugs 0.000 description 1
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000012876 topography Methods 0.000 description 1
- 231100000820 toxicity test Toxicity 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a surface anesthesia drug, in particular to a eye drops using oxybuprocaine as main component and the preparation method, which is prepared by following raw material according to weight account: oxybuprocaine 2 to 7, benzalkonium bromide 0.05 to 0.15, disodium edta 0.05 to 0.15, polyvinyl alcohol 8 to 15. The eye drops using oxybuprocaine as main component has the advantages of smaller irritation of mucosa, rapid action, wide diffusing surface, fast efficacy, strong infiltration, quick absorption, long action time, strong surface anesthesia action and small poison and side effect through experiment showing.
Description
Technical field
The present invention relates to a kind of topical anesthesia medicine, particularly relating to a kind of is the eye drop and preparation method thereof of main component with the Oxybuprocaine.
Background technology
At present clinically be used to measure examination of eyes such as intraocular pressure, gonioscope, three mirror contact lens, shallowly remove at corneal foreign body, lacrimal style inserts and the dress of cloudy shape lens such as wears at the surgery anesthesia effect.Existing topical anesthesia medicine such as lignocaine, tetracaine etc., there is the danger that produces toxic and side effects in they, especially in some operated eyes, very easily cause corneal injury, bring misery to the patient.And the problem that more existing general surface local anesthetics also exist, and onset is slow, action time is short.
Also having some is injection site anaesthetics, owing to need injection, therefore can cause injector's misery, has increased patient's pain, makes topography cure mainly malformation simultaneously, makes the difficulty that becomes of performing the operation.
Summary of the invention
The present invention provides a kind of rapid-action, long action time, topical anesthesia medicine Oxybuprocaine hydrochloride eye drops that toxic and side effects is little in order to solve the problems of the technologies described above.
Another object of the present invention provides the preparation method of the simple Oxybuprocaine hydrochloride eye drops of a kind of processing technique.
In order to solve the problems of the technologies described above, the present invention realizes like this, Oxybuprocaine hydrochloride eye drops, it is to be prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 2-7 part, bromo geramine 0.05-0.15 part, Calcium Disodium Versenate 0.05-0.15 part, polyvinyl alcohol 8-15 part.
Described Oxybuprocaine hydrochloride eye drops, it is to be prepared from by following preferred weight umber by following raw material medicaments: Oxybuprocaine 3-5 part, bromo geramine 0.08-0.12 part, Calcium Disodium Versenate 0.08-0.12 part, polyvinyl alcohol 10-12 part.
Described Oxybuprocaine hydrochloride eye drops, it is to be prepared from by following optimum weight umber by following raw material medicaments: 4 parts of Oxybuprocaines, 0.1 part of bromo geramine, 0.1 part of Calcium Disodium Versenate, polyvinyl alcohol 10-12 part.
The preparation method of described Oxybuprocaine hydrochloride eye drops is as follows: getting the polyvinyl alcohol that meets described parts by weight, to add purified water sterilization back standby; Get the bromo geramine, Calcium Disodium Versenate and the Oxybuprocaine that meet described parts by weight with the purified water dissolving after, add above-mentioned poly-vinyl alcohol solution, and add purified water, stir evenly, filter, embedding promptly.
Advantage of the present invention and effect are as follows:
It has mucosa irritation for a short time Oxybuprocaine hydrochloride eye drops of the present invention through following evidence, and effect is rapidly, diffusion is wide, rapid-action, and is strong to tissue penetration, absorb rapidly, and long action time, the effect of topical anesthesia is strong, the characteristics that toxic and side effects is low.Eye drop of the present invention is used to measure examination of eyes such as intraocular pressure, gonioscope, three mirror contact lens, shallowly removes at corneal foreign body, lacrimal style inserts and the dress of contact lens surgery anesthesia such as to wear effective.Below further specify the effect of medicine of the present invention by test.
Following test is carried out according to conventional method, and concrete result of the test is as follows:
Pharmacological testing:
The ophthalmology topical anesthetic cream.After the administration of this product eye drip, rapid-action, be about 16 seconds, continue about 15 minutes.The effect of its topical anesthesia is strong.This product pharmacological mechanism is thought and the inboard receptors bind in neuron membrane sodium channel, thereby is stoped Na
+Interior stream produces local anesthetic action.
Toxicological test:
The toxicity test result of medicine eye drop of the present invention shows: a little less than the injury effect of its corneal, pupil diameter, ocular accommodation, intraocular pressure etc. are not all had influence.
The pharmacokinetics test:
This product can be absorbed by mucosa, under the esterase effect, resolves into 4-amino-3-butyl phenyl ether formic acid and two basic ammonia alcohol rapidly.The human plasma half-life of measuring in test tube is about 2 ~ 3 minutes or is slightly short.
The specific embodiment
Below description by the specific embodiment the present invention is described in further detail; but this is not to be limitation of the present invention; those skilled in the art are according to basic thought of the present invention; can make various modifications or improvement; but only otherwise break away from basic thought of the present invention, all within protection scope of the present invention.
Embodiment 1:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 4 gram, bromo geramine 0.1 gram, Calcium Disodium Versenate 0.1 gram, polyvinyl alcohol 10 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 10 gram polyvinyl alcohol, to add 100-300 purified water sterilization back standby; Get 0.1 gram bromo geramine, 0.1 gram Calcium Disodium Versenate and 4 gram Oxybuprocaines with the dissolving of 100-300 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Embodiment 2:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 2 gram, bromo geramine 0.05 gram, Calcium Disodium Versenate 0.05 gram, polyvinyl alcohol 8 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 8 gram polyvinyl alcohol, to add 100-200 purified water sterilization back standby; Get 0.05 gram bromo geramine, 0.05 gram Calcium Disodium Versenate and 2 gram Oxybuprocaines with the dissolving of 100-200 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Embodiment 3:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 7 gram, bromo geramine 0.15 gram, Calcium Disodium Versenate 0.15 gram, polyvinyl alcohol 15 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 15 gram polyvinyl alcohol, to add 200-400 purified water sterilization back standby; Get 0.15 gram bromo geramine, 0.15 gram Calcium Disodium Versenate and 7 gram Oxybuprocaines with the dissolving of 200-400 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Embodiment 4:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 3 gram, bromo geramine 0.08 gram, Calcium Disodium Versenate 0.08 gram, polyvinyl alcohol 10 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 10 gram polyvinyl alcohol, to add 200-250 purified water sterilization back standby; Get 0.08 gram bromo geramine, 0.08 gram Calcium Disodium Versenate and 3 gram Oxybuprocaines with the dissolving of 200-250 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Embodiment 5:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 5 gram, bromo geramine 0.12 gram, Calcium Disodium Versenate 0.12 gram, polyvinyl alcohol 12 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 12 gram polyvinyl alcohol, to add 200-300 purified water sterilization back standby; Get 0.12 gram bromo geramine, 0.12 gram Calcium Disodium Versenate and 5 gram Oxybuprocaines with the dissolving of 200-300 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Embodiment 6:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 4 gram, bromo geramine 0.1 gram, Calcium Disodium Versenate 0.1 gram, polyvinyl alcohol 10 or 12 grams add purified water and make 1000 milliliters and make Oxybuprocaine hydrochloride eye drops.
The preparation method of Oxybuprocaine hydrochloride eye drops is as follows: getting 10 or 12 gram polyvinyl alcohol, to add 100-300 purified water sterilization back standby; Get 0.1 gram bromo geramine, 0.1 gram Calcium Disodium Versenate and 4 gram Oxybuprocaines with the dissolving of 100-300 purified water after, add above-mentioned poly-vinyl alcohol solution, and add purified water to full dose, stir evenly, filter, embedding promptly.
Claims (4)
1. Oxybuprocaine hydrochloride eye drops is characterized in that being prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 2-7 part, bromo geramine 0.05-0.15 part, Calcium Disodium Versenate 0.05-0.15 part, polyvinyl alcohol 8-15 part.
2. Oxybuprocaine hydrochloride eye drops according to claim 1 is characterized in that being prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 3-5 part, bromo geramine 0.08-0.12 part, Calcium Disodium Versenate 0.08-0.12 part, polyvinyl alcohol 10-12 part.
3. Oxybuprocaine hydrochloride eye drops according to claim 1 is characterized in that being prepared from by following parts by weight by following raw material medicaments: 4 parts of Oxybuprocaines, 0.1 part of bromo geramine, 0.1 part of Calcium Disodium Versenate, polyvinyl alcohol 10-12 part.
4. the preparation method of the described Oxybuprocaine hydrochloride eye drops of claim 1, it is characterized in that getting the polyvinyl alcohol that meets described parts by weight, to add purified water sterilization back standby; Get the bromo geramine, Calcium Disodium Versenate and the Oxybuprocaine that meet described parts by weight with the purified water dissolving after, add above-mentioned poly-vinyl alcohol solution, and add purified water, stir evenly, filter, embedding promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100113911A CN101264053B (en) | 2008-05-13 | 2008-05-13 | Oxybuprocaine hydrochloride eye drops and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100113911A CN101264053B (en) | 2008-05-13 | 2008-05-13 | Oxybuprocaine hydrochloride eye drops and preparation thereof |
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| Publication Number | Publication Date |
|---|---|
| CN101264053A CN101264053A (en) | 2008-09-17 |
| CN101264053B true CN101264053B (en) | 2010-09-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008100113911A Active CN101264053B (en) | 2008-05-13 | 2008-05-13 | Oxybuprocaine hydrochloride eye drops and preparation thereof |
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| Country | Link |
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| CN (1) | CN101264053B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104983786B (en) * | 2015-07-14 | 2020-03-10 | 泊诺(天津)创新医药研究有限公司 | Polyvinyl alcohol composition |
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- 2008-05-13 CN CN2008100113911A patent/CN101264053B/en active Active
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| Publication number | Publication date |
|---|---|
| CN101264053A (en) | 2008-09-17 |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
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| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| EC01 | Cancellation of recordation of patent licensing contract |
Assignee: Shenyang Oasis Pharmaceutical Co., Ltd. Assignor: Lai Fuping Contract record no.: 2011210000072 Date of cancellation: 20110628 |
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| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: Shenyang Oasis Pharmaceutical Co., Ltd. Assignor: Lai Fuping Contract record no.: 2011210000072 Denomination of invention: Oxybuprocaine hydrochloride eye drops and preparation thereof Granted publication date: 20100915 License type: Exclusive License Open date: 20080917 Record date: 20110627 Assignee: Shenyang Oasis Pharmaceutical Co., Ltd. Assignor: Lai Fuping Contract record no.: 2011210000075 Denomination of invention: Oxybuprocaine hydrochloride eye drops and preparation thereof Granted publication date: 20100915 License type: Exclusive License Open date: 20080917 Record date: 20110628 |
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Owner name: SHENYANG OASIS PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: LAI FUPING Effective date: 20150731 |
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Effective date of registration: 20150731 Address after: Dong Daying, Xinmin Economic Development Zone, Shenyang Patentee after: Shenyang Oasis Pharmaceutical Co., Ltd. Address before: 110016 No. 165-9 Youth Street, Shenhe District, Liaoning, Shenyang Patentee before: Lai Fuping |