CN1194686C - Eye drops of fluconazole - Google Patents
Eye drops of fluconazole Download PDFInfo
- Publication number
- CN1194686C CN1194686C CNB021176183A CN02117618A CN1194686C CN 1194686 C CN1194686 C CN 1194686C CN B021176183 A CNB021176183 A CN B021176183A CN 02117618 A CN02117618 A CN 02117618A CN 1194686 C CN1194686 C CN 1194686C
- Authority
- CN
- China
- Prior art keywords
- fluconazole
- eye drops
- present
- water
- fluconazol
- 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.)
- Expired - Lifetime
Links
- RFHAOTPXVQNOHP-UHFFFAOYSA-N fluconazole Chemical compound C1=NC=NN1CC(C=1C(=CC(F)=CC=1)F)(O)CN1C=NC=N1 RFHAOTPXVQNOHP-UHFFFAOYSA-N 0.000 title claims abstract description 31
- 239000003889 eye drop Substances 0.000 title claims abstract description 20
- 229940012356 eye drops Drugs 0.000 title claims abstract description 16
- 229960004884 fluconazole Drugs 0.000 title claims abstract description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 16
- 229960000686 benzalkonium chloride Drugs 0.000 claims abstract description 11
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims abstract description 11
- 238000000034 method Methods 0.000 claims abstract description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 39
- 239000000203 mixture Substances 0.000 claims description 8
- 238000002360 preparation method Methods 0.000 claims description 7
- 230000001954 sterilising effect Effects 0.000 claims description 6
- 238000002347 injection Methods 0.000 claims description 5
- 239000007924 injection Substances 0.000 claims description 5
- 230000003020 moisturizing effect Effects 0.000 claims description 4
- 238000012856 packing Methods 0.000 claims description 4
- 239000000243 solution Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 10
- 239000008215 water for injection Substances 0.000 abstract description 8
- 229940079593 drug Drugs 0.000 abstract description 7
- 229940126701 oral medication Drugs 0.000 abstract description 4
- 230000004888 barrier function Effects 0.000 abstract description 2
- 230000007547 defect Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000001647 drug administration Methods 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- ULWHHBHJGPPBCO-UHFFFAOYSA-N propane-1,1-diol Chemical compound CCC(O)O ULWHHBHJGPPBCO-UHFFFAOYSA-N 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 description 7
- 206010017533 Fungal infection Diseases 0.000 description 4
- 208000031888 Mycoses Diseases 0.000 description 4
- 230000008901 benefit Effects 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 230000003203 everyday effect Effects 0.000 description 3
- 238000004659 sterilization and disinfection Methods 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 description 2
- 230000000843 anti-fungal effect Effects 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 208000030533 eye disease Diseases 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N 2-propanol Substances CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
- MFYSYFVPBJMHGN-ZPOLXVRWSA-N Cortisone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 MFYSYFVPBJMHGN-ZPOLXVRWSA-N 0.000 description 1
- 206010070840 Gastrointestinal tract irritation Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 229960002179 ephedrine Drugs 0.000 description 1
- 229940084434 fungoid Drugs 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000002045 lasting effect Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to eye drops prepared from a drug effective component, namely fluconazole for the first time and applied to the treatment of mycotic infection in the field of ophthalmology. The present invention aims to enhance the bioavailability of the drug effective component, a therapeutic effect and medication safety. The eye drops are prepared into fluconazole for the first time in the present invention, and the defects that drug administration quantity is large, and an oral drug passes through a blood-eye barrier with difficulty are overcome. Use quantity is few. The present invention has the main technique contents that fluconazole, the drug effective component and propanediol are fully ground and mixed, are added to a proper quantity of water for injection and are dissolved; benzalkonium chloride is added to a proper quantity of water for injection and is dissolved; both are mixed, are evenly stirred to replenish water to full quantity, are hotly pressed and are sterilized to prepare stable eye drops. The present invention is mainly used for ophthalmological diseases, etc.
Description
Affiliated technical field
---fluconazol---makes eye drop first to the present invention relates to a kind of effective ingredient, is applied to the ophthalmology treatment of fungal infections.
Background technology
Nearly ten or twenty is over year, and fungal infection oculopathy increases gradually, and extensive use antibiotic, 17-hydroxy-11-dehydrocorticosterone and immune formulation have especially clinically more increased the ascendant trend of fungoid oculopathy.The domestic antifungal medicament for the eyes that does not also have topical application generally adopts injection or oral formulations to treat clinically at present.The report that fluconazol yet there are no research and produces as eye drop.
Summary of the invention
Anti-fungal infection medicine fluconazol is made into eye drop first, and it is big not only to overcome dosage, and oral drugs are difficult to the deficiency by blood-eye barrier, and use amount is few, improves the bioavailability of effective ingredient, increases curative effect and drug safety.
Technical scheme of the present invention is: fluconazol ingredient and propylene glycol mix, and make it fully to be uniformly dispersed, and add injection water dissolving back and mix with Benza, make eye drop, are used for the ophthalmology treatment of fungal infections, and use amount is few and effect is lasting.Its concrete feature is as follows:
The eye drops of fluconazole single preparations of ephedrine, its formal name: eye drops of fluconazole; Two (1H-1.2.4-the triazol radical)-2-propanol eye drops of chemical name: 2-(2.4-difluorophenyl)-1.3-; English name: Fluconazole EyeDrops; The Chinese phonetic alphabet: Fukangzuo Diyanye; Trade name: Pu Fen.Medicine and main adjunct ingredient and the preparation of forming in following ratio that is applied to ophthalmology illness thereof: wherein containing fluconazol is 0.1-2.5% (w/w); Containing propylene glycol is 0-10.0% (w/w); Containing benzalkonium chloride is 0-0.1% (w/w).The fluconazol effective ingredient fully mixes with propylene glycol, makes it fully to be uniformly dispersed; Add an amount of water for injection and grind dissolving; Benzalkonium chloride adds an amount of water for injection dissolving; The two mixing stirs, and moisturizing is to full dose; Pressure sterilizing; Filter; Packing; Promptly.Among the above-mentioned preparation technology, its core technology is: (1) fluconazol ingredient is fully mixed with propylene glycol, grinds to make it to be uniformly dispersed; (2) add injection water dissolving back and benzalkonium chloride liquid mix homogeneously; (3) completion amount post-heating (115 ℃ of temperature, 30 minutes time) sterilization.
Good effect of the present invention: the development of eye drops of fluconazole and exploitation have following advantage: (1), lower than oral administration cost, oral every day, dosage was 300-600mg, and the eye drops of fluconazole drug content is 0.5%, the about 1.50-2.25ml of use amount every day, ingredient use amount every day is 7.5-12.5mg.(2), eye drops of fluconazole directly acts on the affected part, can play a role fully effectively, the GI irritation that oral drug therapy brought and other side effect that can avoid oral drug therapy to bring.(3), with respect to other ophthalmic preparation, ophthalmic preparation of fluconazole has unrivaled advantage: be difficult for being diluted by tear, within the eye the time of staying long, help the abundant absorption and the utilization and easy to use of principal agent.This Products Development is successful, not only can fill up a blank of domestic ophthalmic remedy, also can bring good social benefit and economic benefit.(4), our enterprise is the ophthalmic remedy manufacturer of domestic specialty, is devoted to production, development, the exploitation of medicament for the eyes over more than 30 year always, actively participates in work for the public good, ophthalmic remedy accounts for more than 90% of the gross output value.
Embodiment
Prescription 1:
Fluconazol 5.0g
Propylene glycol 22.0g
Benzalkonium chloride 0.1g
Water for injection adds to full dose
Make 1000ml
Operating process:
1. get the fluconazol of recipe quantity, mix, make it fully to be uniformly dispersed with propylene glycol;
2. add an amount of water for injection, dissolving;
3. get benzalkonium chloride in addition, be dissolved in water, join 2., stir;
4. moisturizing filters to full dose, heat sterilization, and packing, promptly.
Prescription 2:
Fluconazol 1.0-25.0g
Propylene glycol 0-110.0g
Benzalkonium chloride 0-0.5g
Water for injection adds to full dose
Make 1000ml
Operating process:
1. get the fluconazol of recipe quantity, mix, make it fully to be uniformly dispersed with propylene glycol;
2. add an amount of water for injection, dissolving;
3. get benzalkonium chloride in addition, be dissolved in water, join 2., stir;
4. moisturizing filters to full dose, heat sterilization, and packing, promptly.
Creativeness of the present invention realizes by clinical, toxicology and pharmacology data, provides in the lump during examination as to substances.
Fig. 1 is an eye drops of fluconazole preparation technology flow chart.
Claims (6)
1. an eye drops of fluconazole is characterized in that by weight: contain fluconazol 0.5～2.5%, propylene glycol 2.2～10.0%, benzalkonium chloride 0.01～0.1%.
2. according to the eye drops of fluconazole of claim 1, it is characterized in that by weight: contain fluconazol 0.5%, propylene glycol 2.2%, benzalkonium chloride 0.01%.
3. the preparation method of the eye drops of fluconazole of claim 1: fluconazol is fully mixed with propylene glycol, add the injection water and grind dissolving; Benzalkonium chloride is dissolved in water; Above-mentioned two kinds of solution are mixed, and moisturizing is to full dose, and pressure sterilizing filters, packing, promptly.
4. according to the method for claim 4, it is characterized in that fluconazol is fully mixed with propylene glycol, grinding makes it to be uniformly dispersed.
5. according to the method for claim 4, it is characterized in that fluconazol and propylene glycol add the dissolving of injection water after, mix with Benza.
6. according to the method for claim 4, the temperature that it is characterized in that pressure sterilizing is 115 ℃, and the time is 30 minutes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021176183A CN1194686C (en) | 2002-05-10 | 2002-05-10 | Eye drops of fluconazole |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB021176183A CN1194686C (en) | 2002-05-10 | 2002-05-10 | Eye drops of fluconazole |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1456158A CN1456158A (en) | 2003-11-19 |
| CN1194686C true CN1194686C (en) | 2005-03-30 |
Family
ID=29410323
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB021176183A Expired - Lifetime CN1194686C (en) | 2002-05-10 | 2002-05-10 | Eye drops of fluconazole |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1194686C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1316969C (en) * | 2005-08-31 | 2007-05-23 | 四川升和制药有限公司 | Ophthalmic preparation of fluconazole and method for preparing the same |
-
2002
- 2002-05-10 CN CNB021176183A patent/CN1194686C/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| CN1456158A (en) | 2003-11-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: Shenyang Sinqi Pharmaceutical Co., Ltd. Assignor: Liu Jidong Contract fulfillment period: 2005.4.21 to 2010.4.21 Contract record no.: 2008210000061 Denomination of invention: Eye drops of fluconazole Granted publication date: 20050330 License type: Exclusive license Record date: 20081106 |
|
| LIC | Patent licence contract for exploitation submitted for record |
Free format text: EXCLUSIVE LICENSE; TIME LIMIT OF IMPLEMENTING CONTACT: 2005.4.21 TO 2010.4.21; CHANGE OF CONTRACT Name of requester: SHENYANG XING QI PHARMACEUTICAL CO., LTD. Effective date: 20081106 |
|
| ASS | Succession or assignment of patent right |
Owner name: SHENYANG XINGQI MEDICINE CO., LTD. Free format text: FORMER OWNER: LIU JIDONG Effective date: 20111013 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20111013 Address after: 110027 No. 12, 4, three street, Shenyang economic and Technological Development Zone, Liaoning, China Patentee after: Shenyang Sinqi Pharmaceutical Co., Ltd. Address before: 110027, Liaoning, Shenyang economic and Technological Development Zone, No. three, 12, No. 4, Shenyang Xing Qi Pharmaceutical Co., Ltd. Patentee before: Liu Jidong |
|
| C56 | Change in the name or address of the patentee |
Owner name: SHENYANG SINQI EYE PHARMACEUTICAL CO., LTD. Free format text: FORMER NAME: SHENYANG XINGQI MEDICINE CO., LTD. |
|
| CP03 | Change of name, title or address |
Address after: 110024, 4, 12, three street, Shenyang economic and Technological Development Zone Patentee after: Shenyang Sinqi Pharmaceutical Co., Ltd. Address before: 110027 No. 12, 4, three street, Shenyang economic and Technological Development Zone, Liaoning, China Patentee before: Shenyang Sinqi Pharmaceutical Co., Ltd. |
|
| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20050330 |