CN1539422A - Liquid preparation made from pazufloxacin leucinocaine fed through eye in application of curing ophthalmic diseases and producing method - Google Patents
Liquid preparation made from pazufloxacin leucinocaine fed through eye in application of curing ophthalmic diseases and producing method Download PDFInfo
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- CN1539422A CN1539422A CNA2003101058571A CN200310105857A CN1539422A CN 1539422 A CN1539422 A CN 1539422A CN A2003101058571 A CNA2003101058571 A CN A2003101058571A CN 200310105857 A CN200310105857 A CN 200310105857A CN 1539422 A CN1539422 A CN 1539422A
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- 239000007788 liquid Substances 0.000 title claims abstract description 18
- XAGMUUZPGZWTRP-ZETCQYMHSA-N LSM-5745 Chemical compound C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1C1(N)CC1 XAGMUUZPGZWTRP-ZETCQYMHSA-N 0.000 title claims description 34
- 229960002625 pazufloxacin Drugs 0.000 title claims description 34
- 238000002360 preparation method Methods 0.000 title claims description 27
- 201000010099 disease Diseases 0.000 title claims description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 13
- MLHBDHJHNDJBLI-UHFFFAOYSA-N leucinocaine Chemical compound CCN(CC)C(CC(C)C)COC(=O)C1=CC=C(N)C=C1 MLHBDHJHNDJBLI-UHFFFAOYSA-N 0.000 title 1
- 229950006997 leucinocaine Drugs 0.000 title 1
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims abstract description 42
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims abstract description 36
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims abstract description 28
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims abstract description 26
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims abstract description 13
- 235000019253 formic acid Nutrition 0.000 claims abstract description 13
- 229940098779 methanesulfonic acid Drugs 0.000 claims abstract description 13
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 39
- 238000003756 stirring Methods 0.000 claims description 35
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 32
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 31
- 238000007689 inspection Methods 0.000 claims description 23
- 239000008215 water for injection Substances 0.000 claims description 18
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 claims description 16
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 16
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 claims description 16
- 239000011780 sodium chloride Substances 0.000 claims description 16
- 239000000052 vinegar Substances 0.000 claims description 16
- 235000021419 vinegar Nutrition 0.000 claims description 16
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 15
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 15
- 235000019800 disodium phosphate Nutrition 0.000 claims description 15
- 239000007924 injection Substances 0.000 claims description 13
- 238000002347 injection Methods 0.000 claims description 13
- 229910000403 monosodium phosphate Inorganic materials 0.000 claims description 13
- 235000019799 monosodium phosphate Nutrition 0.000 claims description 13
- 238000012856 packing Methods 0.000 claims description 13
- AJPJDKMHJJGVTQ-UHFFFAOYSA-M sodium dihydrogen phosphate Chemical compound [Na+].OP(O)([O-])=O AJPJDKMHJJGVTQ-UHFFFAOYSA-M 0.000 claims description 13
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 claims description 13
- 238000011282 treatment Methods 0.000 claims description 13
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 12
- 230000001954 sterilising effect Effects 0.000 claims description 12
- 238000004659 sterilization and disinfection Methods 0.000 claims description 12
- 238000005303 weighing Methods 0.000 claims description 12
- 239000011265 semifinished product Substances 0.000 claims description 11
- 239000001632 sodium acetate Substances 0.000 claims description 8
- 235000017281 sodium acetate Nutrition 0.000 claims description 8
- 238000001914 filtration Methods 0.000 claims description 7
- 238000010438 heat treatment Methods 0.000 claims description 7
- 239000002671 adjuvant Substances 0.000 claims description 6
- 239000011521 glass Substances 0.000 claims description 6
- 239000012528 membrane Substances 0.000 claims description 6
- 235000002639 sodium chloride Nutrition 0.000 claims description 6
- 235000011091 sodium acetates Nutrition 0.000 claims description 4
- 239000003814 drug Substances 0.000 abstract description 21
- 230000008901 benefit Effects 0.000 abstract description 2
- 230000000694 effects Effects 0.000 abstract description 2
- 206010010741 Conjunctivitis Diseases 0.000 abstract 1
- 206010023332 keratitis Diseases 0.000 abstract 1
- 239000002994 raw material Substances 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 11
- 229940079593 drug Drugs 0.000 description 8
- 239000003889 eye drop Substances 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 5
- 239000003643 water by type Substances 0.000 description 5
- 206010059866 Drug resistance Diseases 0.000 description 4
- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 description 4
- 150000007660 quinolones Chemical class 0.000 description 4
- 210000004087 cornea Anatomy 0.000 description 3
- 239000010408 film Substances 0.000 description 3
- 210000003734 kidney Anatomy 0.000 description 3
- GSDSWSVVBLHKDQ-UHFFFAOYSA-N 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid Chemical compound FC1=CC(C(C(C(O)=O)=C2)=O)=C3N2C(C)COC3=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-UHFFFAOYSA-N 0.000 description 2
- GSDSWSVVBLHKDQ-JTQLQIEISA-N Levofloxacin Chemical compound C([C@@H](N1C2=C(C(C(C(O)=O)=C1)=O)C=C1F)C)OC2=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-JTQLQIEISA-N 0.000 description 2
- 230000003115 biocidal effect Effects 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 229960003405 ciprofloxacin Drugs 0.000 description 2
- 210000000795 conjunctiva Anatomy 0.000 description 2
- 229960003376 levofloxacin Drugs 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 229960001699 ofloxacin Drugs 0.000 description 2
- 239000010409 thin film Substances 0.000 description 2
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000009056 active transport Effects 0.000 description 1
- 230000036783 anaphylactic response Effects 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 230000001580 bacterial effect Effects 0.000 description 1
- 230000004397 blinking Effects 0.000 description 1
- 210000002164 blood-aqueous barrier Anatomy 0.000 description 1
- 230000004420 blood-aqueous barrier Effects 0.000 description 1
- 229960000484 ceftazidime Drugs 0.000 description 1
- NMVPEQXCMGEDNH-TZVUEUGBSA-N ceftazidime pentahydrate Chemical compound O.O.O.O.O.S([C@@H]1[C@@H](C(N1C=1C([O-])=O)=O)NC(=O)\C(=N/OC(C)(C)C(O)=O)C=2N=C(N)SC=2)CC=1C[N+]1=CC=CC=C1 NMVPEQXCMGEDNH-TZVUEUGBSA-N 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 239000003978 infusion fluid Substances 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 239000002997 ophthalmic solution Substances 0.000 description 1
- 229940054534 ophthalmic solution Drugs 0.000 description 1
- 229940041007 third-generation cephalosporins Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
A liquid medicine of Pazhushaxing methanesulfonate for treating conjunctivitis, keratitis and keratohelcosis by applying it in eyes is prepared from 12 raw materials including Pazhushaxing methanesulfonate, acetic acid, methanesulfonic acid, formic acid, sodium hydroxide, etc. Its preparing process is also disclosed. Its advantage is high curative effect.
Description
Technical field
The administration through eye that the present invention relates to contain Pazufloxacin Mesilate is used for the liquid preparation of ophthalmic diseases, comprises its preparation method.
Background technology
Because antibiotic extensive use and abuse, antibacterial constantly produces drug resistance to medicine, for head it off, new antibiotic constantly comes out, medicine for treatment for ophthalmic diseases, ophthalmology medicine commonly used is second filial generation quinolones ofloxacin eye drops, ciprofloxacin eye drop, levofloxacin eye drop at present, and along with the continuous generation of bacterial drug resistance, existing medicine is in the defective that exists cure rate to descend aspect the treatment oculopathy.
The Pazufloxacin Mesilate that present each family declares mostly is infusion solution or injection, also can treat ophthalmic diseases with it, but the relevant blood-aqueous barrier that exists between blood and eye that ocular tissue by blood vessel wall and all thickness constitutes with active transport, can stop before eyes section of some drugs to reach effective treatment concentration, just can reach valid density so ophthalmic diseases adopts the transfusion approach to treat the medicinal liquid that needs with hundreds of milliliters, its consumption is far longer than the consumption of administration through eye preparation.So the existing dosage form treatment ophthalmic diseases of Pazufloxacin Mesilate has three big unfavorable factors: 1. dosage is big, and behind the intravenously administrable, the medicine effective concentration of eye is very low, and diseased region is difficult to reach effective blood drug concentration.2. entering intravital most drug main will eliminate by kidney, increases patient's kidney burden, and renal function infull person can't use; 3. heavy dose of the use is easy to generate Drug resistance; Clinical use is inconvenience very.
Summary of the invention
Goal of the invention of the present invention provides a kind of ophtalmic treatments that is used for, toxic and side effects is little, the drug resistance occurrence probability is low, stable in aqueous solution, high temperature resistant, less generation anaphylaxis can effectively solve the application that liquid preparation that current resistance a new generation quinolones prepares administration through eye with Pazufloxacin Mesilate is used for the treatment of ophthalmic diseases.
Another goal of the invention of the present invention provides the liquid preparation preparation method of eye drop of pazufloxacin mesilate.
Realize that the goal of the invention technical scheme is to solve like this: the rich blood vessel of eyes own, medicine splash in the conjunctival sac and mainly absorb through cornea and two approach of binding film; Ophthalmic solution splashes into administration, and most of medicine is to reflect by capillary force, extension and the order that blinks in the following arched roof of conjunctiva, makes in the preceding thin film of medicine entering angle film, and penetrates in the cornea thus.Therefore, act on the medicine of eye, in most cases still with topical application for well.
Liquid preparation includes a kind of or several combination among 0.001～20 part of 2～10 parts of the Pazufloxacin Mesilates of parts by weight or volume parts and 0.01～100 part of acetic acid, 0.01～500 part of methanesulfonic acid, 2～80 parts in formic acid, 0.001～3 part of sodium hydroxide, 0.1～10 part of ethyl hydroxybenzoate, 1～10 part of sodium dihydrogen phosphate, 0.05～50 part of sodium hydrogen phosphate, 1～30 part of citric acid, 1～50 part of sodium acetate, 2～10 parts in sodium chloride, the hyaluronic acid sodium.Get the composition of above composition, use the water for injection heating for dissolving, stir, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir coarse filtration, fine straining, sterilization, packing, full inspection, packing promptly gets eye drop of pazufloxacin mesilate.Above-mentioned said component can be a kind of or two or more combination arbitrarily.
The liquid preparation preparation method, undertaken by following step:
1), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
2), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
3), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
4), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
5), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
6), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
The present invention compared with prior art, be directly drips of solution to be gone into the eye administration, most of medicine is in the following arched roof of conjunctiva, by capillary force, extension and the order reflection etc. of blinking, make in the preceding thin film of medicine entering angle film, and penetrate into thus in the cornea, therefore absorbing soon, action target spot is clear and definite, easy to use, reduce the burden of patient's kidney, and can overcome the problem that existing ophthalmic preparation treatment rate descends, market prospect and social benefit are preferably arranged.
The specific embodiment
Below in conjunction with embodiment content of the present invention is described further:
Embodiment 1
This drug prescription is drafted and is 2～10 parts of Pazufloxacin Mesilates, adds 2～10 parts of stirring and dissolving of spirit of vinegar, adds in 500 parts of 1～700 part of waters for injection, ethyl hydroxybenzoate dissolves the back with water for injection for 0.3～5 part and adds in the principal agent solution, with 1～30 part of citric acid, and 1～10 part of sodium hydrogen phosphate, 2～10 parts of addings of sodium chloride stir, and regulate pH value to 3.0～7.0, standardize solution stirs, and filters, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing promptly.
The liquid preparation preparation method, undertaken by following step:
1), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
2), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
3), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
4), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
5), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
6), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
Embodiment 2
This drug prescription is drafted and is 2～10 parts of Pazufloxacin Mesilates, add 2～10 parts of stirring and dissolving of spirit of vinegar, add in 500～700 parts of waters for injection, ethyl hydroxybenzoate dissolves the back with water for injection for 0.2～5 part and adds in the principal agent solution, with 5～15 parts of citric acid, and 0.5～30 part of sodium hydrogen phosphate, 3～7 parts in sodium chloride, 0.005～3 part of adding of hyaluronic acid sodium stirs, and regulates pH value to 3.0～7.0, standardize solution, stir, filter, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.Preparation method is with embodiment 1
Embodiment 3
This drug prescription is drafted and is 2～10 parts of Pazufloxacin Mesilates, adds 2～80 parts of stirring and dissolving of formic acid, adds in 500～700 parts of waters for injection, ethyl hydroxybenzoate dissolves the back with water for injection for 3 parts and adds in the principal agent solution, with 0.002～1 part of sodium hydroxide, and 10～40 parts of sodium acetates, 3～6 parts of addings of sodium chloride stir, and regulate pH value to 3.0～7.0, standardize solution stirs, and filters, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing promptly.Preparation method is with embodiment 1.
Embodiment 4
This drug prescription is drafted and is 2～10 parts of Pazufloxacin Mesilates, adds 0.01～300 part of stirring and dissolving of methanesulfonic acid, adds in 500～700 parts of waters for injection, ethyl hydroxybenzoate dissolves the back with water for injection for 0.3～5 part and adds in the principal agent solution, with 1～10 part of sodium dihydrogen phosphate, and 0.5～30 part of sodium hydrogen phosphate, 4～6 parts of addings of sodium chloride stir, and regulate pH value to 3.0～7.0, standardize solution stirs, and filters, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing promptly.Preparation method is with embodiment 1.
Embodiment 5
This drug prescription is drafted and is 3 parts of Pazufloxacin Mesilates, adds 10 parts of stirring and dissolving of spirit of vinegar, adds in 500 parts of waters for injection, ethyl hydroxybenzoate dissolves the back with water for injection for 3 parts and adds in the principal agent solution, with 4 parts of sodium dihydrogen phosphate, and 0.5 part of sodium hydrogen phosphate, 5 parts in sodium chloride, 2 parts of addings of hyaluronic acid sodium stir, regulate pH value to 3.0～7.0, standardize solution stirs, filter, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.Preparation method is with embodiment 1.
In sum, be the ophthalmic patient service in order to make Pazufloxacin Mesilate in scope the most safely and effectively, the invention provides liquid preparation-eye drop of pazufloxacin mesilate that a kind of Pazufloxacin Mesilate is used for ophthalmology.
Pazufloxacin Mesilate belongs to third generation quinolones, its clinical efficacy is better than second filial generation quinolones ofloxacin, ciprofloxacin, similar with levofloxacin, suitable with third generation cephalosporins medicine ceftazidime, have very important significance so develop the Pazufloxacin Mesilate tool.
Claims (6)
1, the liquid preparation for preparing administration through eye with Pazufloxacin Mesilate is used for the treatment of the application of ophthalmic diseases.
2, the liquid preparation for preparing administration through eye with Pazufloxacin Mesilate according to claim 1 is used for the treatment of the application of ophthalmic diseases, it is characterized in that liquid preparation includes 0.01～100 part of 2～10 parts of the Pazufloxacin Mesilates of parts by weight or volume parts and acetic acid, 0.01～500 part of methanesulfonic acid, 2～80 parts in formic acid, 0.001～3 part of sodium hydroxide, 0.1～10 part of ethyl hydroxybenzoate, 1～10 part of sodium dihydrogen phosphate, 0.05～50 part of sodium hydrogen phosphate, 1～30 part of citric acid, 1～50 part of sodium acetate, 2～10 parts in sodium chloride, 0.001～20 part of hyaluronic acid sodium, above-mentioned said component can be a kind of or two or more combination arbitrarily.
3, the liquid preparation for preparing administration through eye with Pazufloxacin Mesilate according to claim 1 is used for the treatment of the application of ophthalmic diseases, it is characterized in that including 0.1～90 part of 2～8 parts of the Pazufloxacin Mesilates of parts by weight or volume parts and acetic acid, 0.01～400 part of methanesulfonic acid, 10～70 parts in formic acid, 0.002～2 part of sodium hydroxide, 0.1～7 part of ethyl hydroxybenzoate, 2～8 parts of sodium dihydrogen phosphate, 0.1～40 part of sodium hydrogen phosphate, 5～25 parts of citric acid, 5～45 parts of sodium acetates, 3～8 parts in sodium chloride, 0.01～10 part of hyaluronic acid sodium, above-mentioned said component can be a kind of or two or more combination arbitrarily.
4, the liquid preparation for preparing administration through eye with Pazufloxacin Mesilate according to claim 1 and 2 is used for the treatment of the application of ophthalmic diseases, it is characterized in that including 0.5～80 part of 3～7 parts of the Pazufloxacin Mesilates of parts by weight or volume parts and acetic acid, 0.01～300 part of methanesulfonic acid, 20～60 parts in formic acid, 0.002～1 part of sodium hydroxide, 0.2～6 part of ethyl hydroxybenzoate, 3～7 parts of sodium dihydrogen phosphate, 0.5～30 part of sodium hydrogen phosphate, 10～20 parts of citric acid, 10～40 parts of sodium acetates, 4～7 parts in sodium chloride, 0.5～10 part of hyaluronic acid sodium, above-mentioned said component can be a kind of or two or more combination arbitrarily.
5, be used for the treatment of the application of ophthalmic diseases according to claim 1 or the 2 or 3 described liquid preparations that prepare administration through eye with Pazufloxacin Mesilate, it is characterized in that including 0.5～10 part of 3～5 parts of the Pazufloxacin Mesilates of parts by weight or volume parts and acetic acid, 0.01～300 part of methanesulfonic acid, 30～50 parts in formic acid, 0.002～0.01 part of sodium hydroxide, 0.2～5 part of ethyl hydroxybenzoate, 4～6 parts of sodium dihydrogen phosphate, 0.5～30 part of sodium hydrogen phosphate, 10～20 parts of citric acid, 15～30 parts of sodium acetates, 4～7 parts in sodium chloride, 0.5～8 part of hyaluronic acid sodium, above-mentioned said component can be a kind of or two or more combination arbitrarily.
6, realize the preparation method of the described liquid preparation of claim 1, it is characterized in that being undertaken by following step:
1), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
2), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
3), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
4), take by weighing Pazufloxacin Mesilate, add 0.01～100 part of spirit of vinegar (60ml acetic acid adds water to 1000ml) or 0.01～500 part of methanesulfonic acid or 2～80 parts of stirring and dissolving of formic acid, add in the water for injection of 1/2～2/3 recipe quantity;
5), take by weighing ethyl hydroxybenzoate, with water for injection heating (50 ℃～100 ℃) dissolving back adding (1);
6), getting all the other adjuvant sodium chloride, sodium dihydrogen phosphate, sodium hydrogen phosphate, hyaluronic acid sodium, citric acid, sodium acetate adds in (1) and stirs, regulate pH value to 3.50～4.50 with 0.1mol/L sodium hydroxide or spirit of vinegar, add injection water to 1000 part, stir, coarse filtration, reuse 0.45um microporous filter membrane or G
5The sintered glass funnel fine straining, after semi-finished product inspection is qualified, sterilization, aseptic subpackaged, full inspection, packing is promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310105857 CN1245981C (en) | 2003-10-27 | 2003-10-27 | Liquid preparation made from pazufloxacin leucinocaine fed through eye in application of curing ophthalmic diseases and producing method |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200310105857 CN1245981C (en) | 2003-10-27 | 2003-10-27 | Liquid preparation made from pazufloxacin leucinocaine fed through eye in application of curing ophthalmic diseases and producing method |
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| CN1539422A true CN1539422A (en) | 2004-10-27 |
| CN1245981C CN1245981C (en) | 2006-03-22 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115919761A (en) * | 2023-01-29 | 2023-04-07 | 浙江莎普爱思药业股份有限公司 | Pazufloxacin mesilate liquid preparation and preparation method thereof |
| CN116270448A (en) * | 2023-02-24 | 2023-06-23 | 浙江莎普爱思药业股份有限公司 | Preparation method of pazufloxacin mesylate liquid preparation |
-
2003
- 2003-10-27 CN CN 200310105857 patent/CN1245981C/en not_active Expired - Lifetime
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115919761A (en) * | 2023-01-29 | 2023-04-07 | 浙江莎普爱思药业股份有限公司 | Pazufloxacin mesilate liquid preparation and preparation method thereof |
| CN116270448A (en) * | 2023-02-24 | 2023-06-23 | 浙江莎普爱思药业股份有限公司 | Preparation method of pazufloxacin mesylate liquid preparation |
| CN116270448B (en) * | 2023-02-24 | 2024-01-30 | 浙江莎普爱思药业股份有限公司 | Preparation method of pazufloxacin mesylate liquid preparation |
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| Publication number | Publication date |
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| CN1245981C (en) | 2006-03-22 |
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