CN1488350A - Eye preparation for mulating prescription suitable for ciprofloxacin and use method thereof - Google Patents
Eye preparation for mulating prescription suitable for ciprofloxacin and use method thereof Download PDFInfo
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- CN1488350A CN1488350A CNA031528058A CN03152805A CN1488350A CN 1488350 A CN1488350 A CN 1488350A CN A031528058 A CNA031528058 A CN A031528058A CN 03152805 A CN03152805 A CN 03152805A CN 1488350 A CN1488350 A CN 1488350A
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- prescription
- buffer system
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- ciprofloxacin
- polymer
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Abstract
The invention refers to an eye preparation, concretely a formula to use dissimilar-molecule- or different-viscidity same-molecule-copolymerized high-molecular material and buffer nutrition system design. The formula is mainly composed of medical liquid carrier, drug, buffer system and dissimilar-molecule- and/or same-molecule-copolymer 0.001%-25%.
Description
Technical field
The present invention relates to ophthalmic preparation, specifically be to use the ophthalmic preparation prescription and the using method thereof that are applicable to ciprofloxacin of the designs such as same molecule copolymerized macromolecule material, buffering nutrition system of different molecule or different viscosities.
Background technology
Up to the present, external is the most frequently used approach of ocular administration.But owing to the metabolism of tear makes our be difficult to the interior therapeutic drug levels of certain hour in definite ocular tissue with drainage.The Fickian diffusion requires to keep certain Concentraton gradient in a period of time.
Yet this requires the prolong drug dosage form giving snack made with traditional Chinese medicines or giving the snack made with traditional Chinese medicines time of staying on every side.For any non-type administering mode that enters, this all means the time of staying of wanting prolong drug.This point is especially true for ocular administration.But the limit problem that has a range of viscosities here, this limit should be able to be improved bioavailability of medicament to greatest extent, makes the patient that good tolerability is arranged again simultaneously.
Ciprofloxacin is a third generation Comprecin, is a kind of to multiple Gram-positive and all effective broad ectrum antibiotic of gram negative bacteria.Ciprofloxacin uses existing certain history as ophthalmic preparation.The ciprofloxacin eye drop of the commodity of being produced with Alcon company of famous multinational corporations U.S. ophthalmic preparation enterprise CILOXAN by name is an example, and this product pH is 4.5 (pH scope 4.0-5.0), and osmotic pressure is 300mOsm/kg.
The CILOXAN eye drop prescription of table one U.S. Alcon company
| Component | W/W％ |
| Ciprofloxacin | 0.35 |
| Sodium acetate trihydrate | |
| Acetic acid | |
| Benzalkonium chloride | 0.006 |
| Disodium edetate | 0.050 |
| Mannitol | 4.60 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | ?4.0-5.0 |
| Osmotic pressure | 260-300mOsm/kg |
| Character | Light yellow clear liquid |
Wherein W/W represents weight ratio.
The United States Patent (USP) of CILOXAN company expired this year (2003).Part haves much room for improvement below this product and commercially available similar products all exist: 1, certain zest is arranged.2, product is shorter in the eyeball surface time of staying, and the patient needs to drip once every 1-2 hour.
Summary of the invention
The object of the present invention is to provide a kind of ophthalmic preparation prescription and using method thereof that is applicable to ciprofloxacin, formation with control cornea surface aggregate thing film, keep the needed enough flowabilities of eye external preparation, prolong the administration time of ciprofloxacin at eyeball surface, and lubricated and nutrition eyeball, attenuating or elimination ophthalmic preparation are to the stimulation and the burn feeling of eyes.
Another importance is: the present invention uses the adjuvant of these ophthalmic preparation components as pharmaceutical composing prescription, to strengthen the response of medicine, can obtain better bioavailability thus, reduces the medication number of times.
According to design provided by the present invention, this prescription is mainly by pharmaceutically acceptable liquid carrier, the effectively medicine, buffer system of therapeutic dose and 0.001% to 25% different molecule co-polymer and/or form with the molecule co-polymer.
Described ciprofloxacin is base or hydrochlorate or lactate.
Described different molecule co-polymer and/or with the molecule co-polymer be poloxamer (poloxamers) or protect beautiful look bright (poloxmines) or hydroxypropyl methylcellulose or polyvinyl alcohol and/or hydrophile-lipophile balance value HLB from 5～35 other different molecule co-polymer and/or with the molecule co-polymer.
Wherein reasonable different molecule copolymer is Pluronic F-127.
Described different molecule copolymer and/or be with viscosity grade and/or different viscosities grade with the molecule co-polymer.
Described pharmaceutically acceptable liquid carrier is by weight or the liquid carrier formed of volume 75～100% water.
Described buffer system be acetate buffer system or phosphoric acid buffer system or borate buffer system or citric acid buffer system or triple buffer system or mix buffer system and/or other biology buffer system.
In described prescription, can contain antiseptic.And described antiseptic can be benzalkonium chloride or benzalkonium bromide or disodium edetate (EDTA), or other ophthalmic preparation is used the combination of antiseptic with antiseptic or ophthalmic preparation.
A kind of using method that is applicable to the ophthalmic preparation prescription of ciprofloxacin is characterized in that: the ophthalmic preparation prescription is used as eye drop or aural preparations or nasal drop or nasal spray.
The present invention is based on this discovery, that is: the above-mentioned drug effect that contains the eye prescription of viscosity intensifier is with the concentration of polymer in the prescription, rather than prescription viscosity positive correlation.
According to the present invention, we are verified from the angle of eyes to drug absorption, the importantly amount of polymer in the prescription, rather than the viscosity of prescription.Our prescription can contain not commensurability polymer, but similar viscosity, pH and absorption are arranged.Because active constituent is that high polymer keeps well, so its absorption of the prescription of higher polymer concentration is stronger.
For the stability and the effectiveness of active ingredient in guaranteeing to write out a prescription and antiseptic, we have estimated and have compared the stability of prescription and pH, osmotic pressure and active component and antiseptic when doing prescription research.In addition, we have also studied the physicochemical property of this prescription product under the condition of storage of acceleration stability test.
The specific embodiment
Following examples just illustrate the embodiment that the present invention is possible, rather than limit the scope of the invention.
Experimental example one
Through improved ciprofloxacin prescription also is aseptic, an isoosmotic aqueous eye drop.This write out a prescription hydrochloric ciprofloxacin 0.35% (containing base 0.3%), benzalkonium chloride 0.006%, sodium acetate, acetic acid, disodium edetate, mannitol, Pluronic F-127 and pure water.This prescription uses sodium hydroxide or hydrochloric acid to regulate pH to 4.0-5.0.
One of improved ciprofloxacin prescription of table 2
| Component | W/W％ |
| Ciprofloxacin | 0.350 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 2.000 |
| Disodium edetate | 0.050 |
| Sodium chloride | 0.010 |
| Potassium chloride | 0.010 |
| Mannitol | 4.600 |
| Benzalkonium chloride | 0.006 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | ?4.0-5.0 |
| Osmotic pressure | 260-300mOsm/kg |
| Character | Light yellow clear liquid |
Experimental example two
Two of the improved ciprofloxacin prescription of table 3
| Component | W/W％ |
| Ciprofloxacin | 0.350 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 2.000 |
| Disodium edetate | 0.050 |
| Sodium chloride | 0.050 |
| Potassium chloride | 0.010 |
| Sorbitol | 4.000 |
| Benzalkonium chloride | 0.006 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | 4.0-5.0 |
| Osmotic pressure | 260-300mOsm/kg |
| Character | Light yellow clear liquid |
Experimental example three
Three of the improved ciprofloxacin prescription of table 4
| Component | W/W％ |
| Ciprofloxacin | 0.350 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 5.000 |
| Disodium edetate | 0.050 |
| Sodium chloride | 0.010 |
| Glycerol | 0.200 |
| Sorbitol | 4.000 |
| Benzalkonium chloride | 0.006 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | 4.0-5.0 |
| Osmotic pressure | 240-320mOsm/kg |
| Character | Light yellow clear liquid |
Experimental example four
Four of the improved ciprofloxacin prescription of table 5
| Component | W/W％ |
| Ciprofloxacin | 0.350 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 10.00 |
| Disodium edetate | 0.050 |
| Sodium chloride | 0.010 |
| Potassium chloride | 0.010 |
| Sorbitol | 4.200 |
| Benzalkonium chloride | 0.006 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | 4.0-5.0 |
| Osmotic pressure | 250-310mOsm/kg |
| Character | Light yellow clear liquid |
Experimental example five
Five of the improved ciprofloxacin prescription of table 6
| Component | W/W％ |
| Ciprofloxacin | 0.350 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Hydroxypropyl methylcellulose (low viscosity) | 1.000 |
| Hydroxypropyl methylcellulose (high viscosity) | 0.500 |
| Disodium edetate | 0.050 |
| Sodium chloride | 0.010 |
| Potassium chloride | 0.010 |
| Mannitol | 4.400 |
| Benzalkonium chloride | 0.006 |
| Pure water | Add to 100 grams |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| pH | 4.0-5.0 |
| Osmotic pressure | 250-310mOsm/kg |
| Character | Light yellow clear liquid |
Experimental example six
Six of the improved ciprofloxacin prescription of table 7
| Component | W/W％ |
| Ciprofloxacin | 0.35 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 25.00 |
| EDTA | 0.001 |
| Mannitol | 2.00 |
| Benzalkonium chloride | 0.006 |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| Pure water | Add to 100 grams |
Experimental example seven
Seven of the improved ciprofloxacin prescription of table 8
| Component | W/W％ |
| Ciprofloxacin | 0.35 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Pluronic?F-127 | 0.001 |
| Hydroxypropyl methylcellulose | 0.50 |
| Disodium edetate | 0.001 |
| Mannitol | 4.200 |
| Benzalkonium chloride | 0.006 |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| Pure water | Add to 100 grams |
Experimental example eight
Eight of the improved ciprofloxacin prescription of table 9
| Component | W/W％ |
| Ciprofloxacin | 0.35 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Hydroxypropyl methylcellulose | 1.000 |
| Disodium edetate | 0.001 |
| Mannitol | 3.00 |
| Benzalkonium chloride | 0.006 |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| Pure water | Add to 100 grams |
Experimental example nine
Nine of the improved ciprofloxacin prescription of table 10
| Component | W/W％ |
| Ciprofloxacin | 0.35 |
| Sodium acetate | 0.033 |
| Acetic acid | 0.042 |
| Polyvinyl alcohol | 1.000 |
| Disodium edetate | 0.001 |
| Mannitol | 3.00 |
| Benzalkonium chloride | 0.006 |
| Hydrochloric acid, 1N | The pH regulator agent adds in case of necessity |
| Sodium hydroxide, 1N | The pH regulator agent adds in case of necessity |
| Pure water | Add to 100 grams |
Claims (10)
1, a kind of ophthalmic preparation prescription that is applicable to ciprofloxacin is characterized in that: this prescription is mainly by pharmaceutically acceptable liquid carrier, the effectively medicine, buffer system of therapeutic dose and 0.001% to 25% different molecule co-polymer and/or form with the molecule co-polymer.
2, the prescription of stating according to claim 1 is characterized in that: ciprofloxacin is base or hydrochlorate or lactate.
3, prescription according to claim 1 is characterized in that: different molecule co-polymer and/or with the molecule co-polymer be poloxamer (poloxamers) or protect beautiful look bright (poloxmines) or hydroxypropyl methylcellulose or polyvinyl alcohol and/or hydrophile-lipophile balance value HLB from 5～35 other different molecule co-polymer and/or with the molecule co-polymer.
4, prescription according to claim 1 is characterized in that: different molecule copolymer is PluronicF-127.
5, prescription according to claim 1 is characterized in that: different molecule copolymer and/or with the molecule co-polymer for viscosity grade and/or different viscosities grade.
6, prescription according to claim 1 is characterized in that: pharmaceutically acceptable liquid carrier is for by weight or the liquid carrier formed of volume 75～100% water.
7, prescription according to claim 1 is characterized in that: buffer system be acetate buffer system or phosphoric acid buffer system or borate buffer system or citric acid buffer system or triple buffer system or mix buffer system and/or other biology buffer system.
8, prescription according to claim 1 is characterized in that: contain antiseptic in the prescription.
9, prescription according to claim 8 is characterized in that: antiseptic is benzalkonium chloride or benzalkonium bromide or disodium edetate (EDTA), or other ophthalmic preparation is used the combination of antiseptic with antiseptic or ophthalmic preparation.
10, a kind of using method that is applicable to the ophthalmic preparation prescription of ciprofloxacin is characterized in that: the ophthalmic preparation prescription is used as eye drop or aural preparations or nasal drop or nasal spray.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031528058A CN1488350A (en) | 2003-08-13 | 2003-08-13 | Eye preparation for mulating prescription suitable for ciprofloxacin and use method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031528058A CN1488350A (en) | 2003-08-13 | 2003-08-13 | Eye preparation for mulating prescription suitable for ciprofloxacin and use method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1488350A true CN1488350A (en) | 2004-04-14 |
Family
ID=34156576
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031528058A Pending CN1488350A (en) | 2003-08-13 | 2003-08-13 | Eye preparation for mulating prescription suitable for ciprofloxacin and use method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1488350A (en) |
-
2003
- 2003-08-13 CN CNA031528058A patent/CN1488350A/en active Pending
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