CN101264074B - Oxybuprocaine gel and preparation thereof - Google Patents
Oxybuprocaine gel and preparation thereof Download PDFInfo
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- CN101264074B CN101264074B CN2008100111507A CN200810011150A CN101264074B CN 101264074 B CN101264074 B CN 101264074B CN 2008100111507 A CN2008100111507 A CN 2008100111507A CN 200810011150 A CN200810011150 A CN 200810011150A CN 101264074 B CN101264074 B CN 101264074B
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- oxybuprocaine
- gel
- purified water
- methylcellulose
- calcium disodium
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Abstract
The invention discloses a surface anesthesia drug, in particular to a gel preparation using oxybuprocaine as main component and the preparation method, which is prepared by following raw material according to weight account: oxybuprocaine 1 to 5, benzalkonium bromide 0.05 to 0.15, disodium edta 0.05 to 0.15, methyl cellulose 12 to 22. The gel preparation using oxybuprocaine as main component has the advantages of fast efficacy, strong infiltration, quick absorption, long action time 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 gel preparation and preparation method thereof of main component with the Oxybuprocaine.
Background technology
Clinical topical anesthesia and the lubricated pain relieving that is used for each section's inspection, disposal, minor operation at present often adopts the topical anesthesia medicine to play the effect of local anesthesia analgesic.Existing topical anesthesia medicine such as lignocaine, tetracaine etc., there is the danger that produces toxic and side effects in they, especially in some cosmetic surgerys, for example in the operated eye, 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 needing injection, therefore can cause injector's misery, has increased patient's pain, and topography simultaneously cures mainly malformation, makes operation become difficult.
Summary of the invention
The present invention provides a kind of rapid-action, long action time, topical anesthesia medicine Oxybuprocaine gel 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 gel of a kind of processing technique.
In order to solve the problems of the technologies described above, the present invention realizes like this, Oxybuprocaine gel, it is to be prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 1-5 part, bromo geramine 0.05-0.15 part, Calcium Disodium Versenate 0.05-0.15 part, methylcellulose 12-22 part.
Described Oxybuprocaine gel, it is to be prepared from by following preferred weight umber by following raw material medicaments: Oxybuprocaine 2-4 part, bromo geramine 0.08-0.12 part, Calcium Disodium Versenate 0.08-0.12 part, methylcellulose 15-20 part.
Described Oxybuprocaine gel, it is to be prepared from by following optimum weight umber by following raw material medicaments: 3 parts of Oxybuprocaines, 0.1 part of bromo geramine, 0.1 part of Calcium Disodium Versenate, 17 parts of methylcellulose.
The preparation method of Oxybuprocaine gel is as follows: gets purified water, adds methylcellulose, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; Oxybuprocaine, bromo geramine, Calcium Disodium Versenate, with after the purified water dissolving, add above-mentioned methocel solution, add purified water again, stir evenly, filter, embedding is promptly.
Advantage of the present invention and effect are as follows:
It has rapid-actionly Oxybuprocaine gel of the present invention through following evidence, and penetration is strong, absorbs rapidly long action time, the characteristics that toxic and side effects is little.Following test is carried out according to conventional method, and concrete result of the test is as follows:
Pharmacological testing:
Local anesthetic.Onset in 4 minutes after this product administration can obtain sufficient anaesthetic effect in 8 minutes, continued drug effect more than 40 minutes.Animal topical anesthesia result of the test shows: surface anesthetic effect is strong.The inboard receptors bind in mechanism of action and neuron membrane sodium channel, thus Na stoped
+Interior stream produces local anesthetic action.
Toxicological test:
The acute toxicity testing result of this product shows: to the median lethal dose(LD 50) (LD of mice
50) be 6.8mg/kg, be 4.2mg/kg to Cavia porcellus.LD during subcutaneous administration
50To mice is 42.5mg/kg, is 60mg/kg to rat, is 21mg/kg to Cavia porcellus, is 30mg/kg to rabbit.
The pharmacokinetics test:
This product penetration is strong, absorbs rapidly, and is rapid-action; Can under the esterase effect, resolve into 4-amino-3-butyl phenyl ether formic acid and two basic ammonia alcohol rapidly.The human plasma half-life of measuring in the test tube that exsomatizes 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 3 grams, bromo geramine 0.1 gram, Calcium Disodium Versenate 0.1 gram, methylcellulose 17 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 100-300 milliliter, adds methylcellulose 17 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; Oxybuprocaine 3 grams, bromo geramine 0.1 gram, Calcium Disodium Versenate 0.1 add above-mentioned methocel solution, and add purified water to full dose after restraining, dissolving with purified water 100-300, stir evenly, and filter, and embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Embodiment 2:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 1 gram, bromo geramine 0.05 gram, Calcium Disodium Versenate 0.05 gram, methylcellulose 12 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 100-200 milliliter, adds methylcellulose 12 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; After Oxybuprocaine 1 gram, bromo geramine 0.05 gram, Calcium Disodium Versenate 0.05 restrain, dissolve with purified water 100-150, add above-mentioned methocel solution, and add purified water, stir evenly to full dose, filter, embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Embodiment 3:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 5 grams, bromo geramine 0.15 gram, Calcium Disodium Versenate 0.15 gram, methylcellulose 22 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 200-400 milliliter, adds methylcellulose 22 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; After Oxybuprocaine 5 grams, bromo geramine 0.15 gram, Calcium Disodium Versenate 0.15 restrain, dissolve with purified water 200-300, add above-mentioned methocel solution, and add purified water, stir evenly to full dose, filter, embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Embodiment 4:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 2 grams, bromo geramine 0.08 gram, Calcium Disodium Versenate 0.08 gram, methylcellulose 20 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 200-300 milliliter, adds methylcellulose 20 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; After Oxybuprocaine 2 grams, bromo geramine 0.08 gram, Calcium Disodium Versenate 0.08 restrain, dissolve with purified water 100-200, add above-mentioned methocel solution, and add purified water, stir evenly to full dose, filter, embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Embodiment 5:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 4 grams, bromo geramine 0.12 gram, Calcium Disodium Versenate 0.12 gram, methylcellulose 15 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 200-300 milliliter, adds methylcellulose 15 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; After Oxybuprocaine 4 grams, bromo geramine 0.12 gram, Calcium Disodium Versenate 0.12 restrain, dissolve with purified water 200-300, add above-mentioned methocel solution, and add purified water, stir evenly to full dose, filter, embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Embodiment 6:
It is to be prepared from by following weight by following raw material medicaments: Oxybuprocaine 2.5 grams, bromo geramine 0.15 gram, Calcium Disodium Versenate 0.1 gram, methylcellulose 18 grams add purified water and make 1000 milliliters of Oxybuprocaine gels.
The preparation method of Oxybuprocaine gel is as follows: gets purified water 200-300 milliliter, adds methylcellulose 18 grams, allow its natural water absorption and swelling, and after treating to dissolve fully, standby; After Oxybuprocaine 2.5 grams, bromo geramine 0.15 gram, Calcium Disodium Versenate 0.1 restrain, dissolve with purified water 200-300, add above-mentioned methocel solution, and add purified water, stir evenly to full dose, filter, embedding promptly gets 1000 milliliters of sour oxybuprocaine gels.
Claims (4)
1. Oxybuprocaine gel is characterized in that it is to be prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 1-5 part, bromo geramine 0.05-0.15 part, Calcium Disodium Versenate 0.05-0.15 part, methylcellulose 12-22 part.
2. Oxybuprocaine gel according to claim 1 is characterized in that described Oxybuprocaine gel is to be prepared from by following parts by weight by following raw material medicaments: Oxybuprocaine 2-4 part, bromo geramine 0.08-0.12 part, Calcium Disodium Versenate 0.08-0.12 part, methylcellulose 15-20 part.
3. Oxybuprocaine gel according to claim 1 is characterized in that described Oxybuprocaine gel is to be prepared from by following parts by weight by following raw material medicaments: 3 parts of Oxybuprocaines, 0.1 part of bromo geramine, 0.1 part of Calcium Disodium Versenate, 17 parts of methylcellulose.
4. the preparation method of the described Oxybuprocaine gel of claim 1 is characterized in that getting purified water, adds methylcellulose, allows its natural water absorption and swelling, and is after treating to dissolve fully, standby; Oxybuprocaine, bromo geramine, Calcium Disodium Versenate add above-mentioned methocel solution after dissolving with purified water, add purified water again, stir evenly, and filter, and embedding promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100111507A CN101264074B (en) | 2008-04-23 | 2008-04-23 | Oxybuprocaine gel and preparation thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100111507A CN101264074B (en) | 2008-04-23 | 2008-04-23 | Oxybuprocaine gel and preparation thereof |
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| Publication Number | Publication Date |
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| CN101264074A CN101264074A (en) | 2008-09-17 |
| CN101264074B true CN101264074B (en) | 2010-09-08 |
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| CN2008100111507A Active CN101264074B (en) | 2008-04-23 | 2008-04-23 | Oxybuprocaine gel and preparation thereof |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6218428B1 (en) * | 2000-04-28 | 2001-04-17 | Emil Chynn | Ophthalmic composition |
-
2008
- 2008-04-23 CN CN2008100111507A patent/CN101264074B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6218428B1 (en) * | 2000-04-28 | 2001-04-17 | Emil Chynn | Ophthalmic composition |
Non-Patent Citations (3)
| Title |
|---|
| 庄靖玲.盐酸奥布卡因表面麻醉下行小梁切除术26例.交通医学21 3.2007,21(3),320. * |
| 毕殿洲.药剂学(国家执业药师资格考试应试指南).中国医药科技出版社,2000,182-184. * |
| 王海莲等.局麻药利多卡因与丁卡因乳膏经皮吸收的观察与临床应用.中华麻醉学杂志19 5.1999,19(5),310. * |
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| CN101264074A (en) | 2008-09-17 |
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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 gel and preparation thereof Granted publication date: 20100908 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 gel and preparation thereof Granted publication date: 20100908 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 |