CN102114020A - Pharmaceutical composition containing besivance or salts thereof and preparation method thereof - Google Patents
Pharmaceutical composition containing besivance or salts thereof and preparation method thereof Download PDFInfo
- Publication number
- CN102114020A CN102114020A CN2009102443817A CN200910244381A CN102114020A CN 102114020 A CN102114020 A CN 102114020A CN 2009102443817 A CN2009102443817 A CN 2009102443817A CN 200910244381 A CN200910244381 A CN 200910244381A CN 102114020 A CN102114020 A CN 102114020A
- Authority
- CN
- China
- Prior art keywords
- agent
- shellfish
- sodium
- water
- salt
- 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.)
- Granted
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 32
- 150000003839 salts Chemical class 0.000 title claims abstract description 18
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 6
- PMQBICKXAAKXAY-HNCPQSOCSA-N 7-[(3r)-3-aminoazepan-1-yl]-8-chloro-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid;hydrochloride Chemical compound Cl.C1[C@H](N)CCCCN1C1=C(F)C=C2C(=O)C(C(O)=O)=CN(C3CC3)C2=C1Cl PMQBICKXAAKXAY-HNCPQSOCSA-N 0.000 title abstract 2
- 229940021570 besivance Drugs 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 claims abstract description 24
- 239000007788 liquid Substances 0.000 claims abstract description 10
- 239000007787 solid Substances 0.000 claims abstract description 9
- 235000015170 shellfish Nutrition 0.000 claims description 34
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 21
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 20
- 239000000243 solution Substances 0.000 claims description 19
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 19
- 229920002472 Starch Polymers 0.000 claims description 15
- 239000008107 starch Substances 0.000 claims description 15
- 235000019698 starch Nutrition 0.000 claims description 15
- 239000003795 chemical substances by application Substances 0.000 claims description 12
- 235000019359 magnesium stearate Nutrition 0.000 claims description 10
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 9
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 8
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 8
- 229930195725 Mannitol Natural products 0.000 claims description 8
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 8
- 230000002421 anti-septic effect Effects 0.000 claims description 8
- 239000008187 granular material Substances 0.000 claims description 8
- 239000008101 lactose Substances 0.000 claims description 8
- 239000000594 mannitol Substances 0.000 claims description 8
- 235000010355 mannitol Nutrition 0.000 claims description 8
- 239000002245 particle Substances 0.000 claims description 8
- 239000003381 stabilizer Substances 0.000 claims description 8
- 239000002562 thickening agent Substances 0.000 claims description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 6
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 6
- 239000000853 adhesive Substances 0.000 claims description 6
- 230000001070 adhesive effect Effects 0.000 claims description 6
- 239000002775 capsule Substances 0.000 claims description 6
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 238000004132 cross linking Methods 0.000 claims description 6
- 239000000945 filler Substances 0.000 claims description 6
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims description 6
- 230000003204 osmotic effect Effects 0.000 claims description 6
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 6
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 6
- 239000003826 tablet Substances 0.000 claims description 6
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 5
- 239000003889 eye drop Substances 0.000 claims description 5
- 239000011734 sodium Substances 0.000 claims description 5
- 229910052708 sodium Inorganic materials 0.000 claims description 5
- 238000003756 stirring Methods 0.000 claims description 5
- 239000008215 water for injection Substances 0.000 claims description 5
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims description 4
- 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 claims description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 4
- 229960002233 benzalkonium bromide Drugs 0.000 claims description 4
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 4
- KHSLHYAUZSPBIU-UHFFFAOYSA-M benzododecinium bromide Chemical compound [Br-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 KHSLHYAUZSPBIU-UHFFFAOYSA-M 0.000 claims description 4
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 4
- 210000000481 breast Anatomy 0.000 claims description 4
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims description 4
- 235000019700 dicalcium phosphate Nutrition 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- 229960003943 hypromellose Drugs 0.000 claims description 4
- 239000000787 lecithin Substances 0.000 claims description 4
- 235000010445 lecithin Nutrition 0.000 claims description 4
- 229940067606 lecithin Drugs 0.000 claims description 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 4
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 4
- 239000000741 silica gel Substances 0.000 claims description 4
- 229910002027 silica gel Inorganic materials 0.000 claims description 4
- 239000011780 sodium chloride Substances 0.000 claims description 4
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims description 4
- 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 4
- 230000008961 swelling Effects 0.000 claims description 4
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 3
- -1 correctives Substances 0.000 claims description 3
- 239000007919 dispersible tablet Substances 0.000 claims description 3
- 239000000499 gel Substances 0.000 claims description 3
- 239000000314 lubricant Substances 0.000 claims description 3
- 210000000214 mouth Anatomy 0.000 claims description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 2
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims description 2
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 2
- 229920002125 Sokalan® Polymers 0.000 claims description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims description 2
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 claims description 2
- 229910021502 aluminium hydroxide Inorganic materials 0.000 claims description 2
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 230000003078 antioxidant effect Effects 0.000 claims description 2
- 229960001631 carbomer Drugs 0.000 claims description 2
- 239000007891 compressed tablet Substances 0.000 claims description 2
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 claims description 2
- 238000004090 dissolution Methods 0.000 claims description 2
- 235000019441 ethanol Nutrition 0.000 claims description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 2
- 238000000034 method Methods 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 2
- 238000010979 pH adjustment Methods 0.000 claims description 2
- 229960000502 poloxamer Drugs 0.000 claims description 2
- 229920001983 poloxamer Polymers 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 2
- 229920000053 polysorbate 80 Polymers 0.000 claims description 2
- 230000001105 regulatory effect Effects 0.000 claims description 2
- DCKVNWZUADLDEH-UHFFFAOYSA-N sec-butyl acetate Chemical compound CCC(C)OC(C)=O DCKVNWZUADLDEH-UHFFFAOYSA-N 0.000 claims description 2
- 239000000377 silicon dioxide Substances 0.000 claims description 2
- 235000012239 silicon dioxide Nutrition 0.000 claims description 2
- 239000001509 sodium citrate Substances 0.000 claims description 2
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims description 2
- 235000010265 sodium sulphite Nutrition 0.000 claims description 2
- 238000007614 solvation Methods 0.000 claims description 2
- 238000005303 weighing Methods 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 33
- 239000011230 binding agent Substances 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 206010042674 Swelling Diseases 0.000 description 3
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 239000003814 drug Substances 0.000 description 2
- 238000004945 emulsification Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 2
- 239000002002 slurry Substances 0.000 description 2
- 239000001488 sodium phosphate Substances 0.000 description 2
- 229910000162 sodium phosphate Inorganic materials 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 241000606161 Chlamydia Species 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 241000192125 Firmicutes Species 0.000 description 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
- 241000589248 Legionella Species 0.000 description 1
- 208000007764 Legionnaires' Disease Diseases 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 241000204031 Mycoplasma Species 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 239000003513 alkali Substances 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000000843 anti-fungal effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 210000001742 aqueous humor Anatomy 0.000 description 1
- 229940009098 aspartate Drugs 0.000 description 1
- 201000007032 bacterial conjunctivitis Diseases 0.000 description 1
- 239000011363 dried mixture Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229940124307 fluoroquinolone Drugs 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 238000011031 large-scale manufacturing process Methods 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 150000003891 oxalate salts Chemical class 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention provides a pharmaceutical composition containing besivance or salts thereof. The composition exists in a mode of a watery liquid preparation or a solid preparation, is convenient to operate, transmit and store and suitable for mass production and has wide range of applications.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to pharmaceutical preparation of shellfish Xisha star and preparation method thereof.
Background technology
Shellfish Xisha star be the 4th generation fluoroquinolone antibiotics, this novel quinolone medicine is except having has a broad antifungal spectrum, antibacterial activity height, the active characteristics of anti-gram negative bacteria, gram positive bacteria also there is strong antibacterial activity, particularly improved antibacterial activity, legionella, mycoplasma, chlamydia have all been had stronger effect anaerobe.Shellfish Xisha star has good aqueous humor permeability, and this medicine ratifies to be used for the treatment of bacterial conjunctivitis abroad at present.
Summary of the invention
The invention provides a kind of Pharmaceutical composition that contains shellfish Xisha star or its salt, its salt comprises for example acid-addition salts example hydrochloric acid salt, acetate, phosphate, sulfate, nitrate, hydrobromate, lactate, citrate, tartrate, oxalates, maleate, fumarate, malate, mesylate, aspartate etc., and with the salt of alkali such as sodium hydroxide, potassium hydroxide etc.
The Pharmaceutical composition of shellfish provided by the invention Xisha star or its salt exists with the form of aqueous liquid preparation or solid preparation, is convenient to operation, transportation and stores applied range, suitable large-scale production.
Described aqueous liquid preparation composed as follows:
1) the shellfish Xisha star that contains or its salt add with the micronization form, and its particle diameter is less than 10 μ m;
2) contain pharmaceutically available adjuvant, comprise one or more of thickening agent, antiseptic, osmotic pressure regulator, pH regulator agent, stabilizing agent and water;
3) thickening agent is selected from one or more mixture of hypromellose, hyaluronic acid sodium, carbomer, poloxamer;
4) antiseptic is selected from one or more mixture of benzalkonium chloride, benzalkonium bromide, Metagin, second, third, butyl ester;
5) osmotic pressure regulator is selected from one or more mixture of propylene glycol, glycerol, mannitol, sodium chloride, sodium bicarbonate, sodium citrate;
6) sodium hydroxide, potassium hydroxide, aluminium hydroxide, triethanolamine etc. are adopted in the pH regulator agent;
7) stabilizing agent adopts disodiumedetate, sodium sulfite, lecithin etc.
Described aqueous liquid preparation is prepared by following technology:
1) take by weighing 0.01～10% thickening agent and/or stabilizing agent and add the abundant swelling of suitable quantity of water, add 0.1%～20% shellfish Xisha star again or its salt fully grinds or stirs or the breast even or ultrasonic, solution I;
2) antiseptic, osmotic pressure regulator, stabilizing agent and/or thickening agent are added an amount of water dissolution, get solution II;
3) solution I and solution II are merged, even or stirring or ultransonic method mix homogeneously by breast, regulating pH value with pH adjustment agent is 5～7, adds water to total amount again.
Described aqueous liquid preparation is eye drop or gel for eye.
Described solid preparation composed as follows:
1) the shellfish Xisha star that contains or its salt add with micronization form or solvation form, and its particle diameter is less than 10 μ m;
2) acceptable accessories that contains comprises in filler, disintegrating agent, wet adhesive, lubricant, effervescent, correctives, antioxidant, the antiseptic one or more;
3) filler is selected from one or more in lactose, mannitol, starch, pre-paying starch, the calcium hydrogen phosphate;
4) disintegrating agent is selected from one or more in low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose, carboxymethylstach sodium, tween 80, the Polyethylene Glycol;
5) wet adhesive is selected from one or more in water, ethanol, starch, hydroxypropyl cellulose, polyvinylpyrrolidone, the methylcellulose;
6) lubricant is selected from one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, the silicon dioxide.The preparation technology of described solid preparation gets 0.1～20% shellfish Xisha star or its salt and 40%～80% filler, 3%～30% disintegrating agent mix homogeneously, adds suitable amount of adhesive and granulates, oven dry, granulate, add all the other adjuvants, mix homogeneously, compressed tablets or fill capsule.
Described solid preparation is tablet, dispersible tablet, oral cavity disintegration tablet or capsule.
Specific embodiment
1 one kinds of suspendible eye drop that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Hydrochloric acid shellfish Xisha star | 0.8 |
| Hypromellose | 0.5 |
| Benzalkonium chloride | 0.01 |
| Mannitol | 0.05 |
| Sodium chloride | 0.5 |
| Sodium hydroxide | In right amount |
| Disodiumedetate | 0.01 |
Preparation technology:
1, under aseptic condition, hypromellose and an amount of water for injection after 80～90 ℃ of abundant swellings, are cooled to room temperature, add hydrochloric acid shellfish Xisha star and grind evenly, solution I;
2, benzalkonium chloride, mannitol, sodium chloride, disodiumedetate are dissolved in an amount of water for injection successively, cross 0.2 μ m filter membrane, get solution II;
3, under aseptic condition, solution I and solution II are merged, by high speed dispersing emulsification machine mix homogeneously,, add the injection water again to total amount with 1M sodium hydroxide solution adjustment pH value to 5～7;
4, under aseptic condition, divide to be filled in the sterilized eye drop bottle.
2 one kinds of gel for eye that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Hydrochloric acid shellfish Xisha star | 0.6 |
| Hyaluronic acid sodium | 1.0 |
| Benzalkonium bromide | 0.01 |
| Dibastic sodium phosphate | 1 |
| Sodium hydroxide | In right amount |
| Lecithin | 0.01 |
Preparation method:
1, under aseptic condition, get segment glass acid sodium and an amount of abundant swelling of water for injection after, add hydrochloric acid shellfish Xisha star, lecithin stirs, solution I;
2, benzalkonium bromide, calcium hydrogen phosphate, residue hyaluronic acid sodium are dissolved in an amount of water for injection successively, cross 0.2 μ m filter membrane, get solution II;
3, under aseptic condition, solution I and solution II are merged, by high speed dispersing emulsification machine mix homogeneously,, add the injection water again to total amount with 1M sodium hydroxide solution adjustment pH value to 5～7;
4, under aseptic condition, divide to be filled in the sterilized eye drop bottle.
3 one kinds of tablets that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Hydrochloric acid shellfish Xisha star | 10 |
| Lactose | 60 |
| Dibastic sodium phosphate | 22 |
| Carboxymethylstach sodium | 5 |
| Starch | 2 |
| Magnesium stearate | 1 |
Preparation technology:
1, with hydrochloric acid shellfish Xisha star and lactose, calcium hydrogen phosphate and carboxymethylstach sodium mix homogeneously;
2, starch is made 10% starch slurry as binding agent, 18 mesh sieves are granulated;
3, particle drying is to moisture＜3.5%;
4,24 mesh sieve granulate add magnesium stearate, mix homogeneously;
5, compacting in flakes.
4 one kinds of dispersible tablets that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Shellfish Xisha star | 5 |
| Lactose | 58 |
| Starch | 30 |
| Cross-linking sodium carboxymethyl cellulose | 5 |
| Polyethylene glycol 6000 | 1 |
| Magnesium stearate | 1 |
Preparation technology:
1, shellfish Xisha star is added adequate amount of ethanol dissolving, and is scattered in the lactose, after to be dried mixture I;
2, with mixture I and starch, cross-linking sodium carboxymethyl cellulose mix homogeneously;
3, with water as wetting agent, 18 mesh sieves are granulated;
4, particle drying is to moisture＜3.5%;
5,24 mesh sieve granulate add polyethylene glycol 6000 and magnesium stearate, mix homogeneously;
6, compacting in flakes.
5 one kinds of oral cavity disintegration tablets that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Hydrochloric acid shellfish Xisha star | 6 |
| Mannitol | 50 |
| Microcrystalline Cellulose | 26 |
| Low-substituted hydroxypropyl cellulose (in add) | 8 |
| Polyvinylpyrrolidone | 1 |
| Low-substituted hydroxypropyl cellulose (adding) | 8 |
| Magnesium stearate | 1 |
Preparation technology:
1, with hydrochloric acid shellfish Xisha star and mannitol, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose (in add) mix homogeneously;
2, make binding agent with 3% polyvinylpyrrolidone alcoholic solution, 18 mesh sieves are granulated;
3, particle drying is to moisture＜3.5%;
4,24 mesh sieve granulate add low-substituted hydroxypropyl cellulose (adding) and magnesium stearate, mix homogeneously;
5, compacting in flakes.
6 one kinds of capsules that contain hydrochloric acid shellfish Xisha star of embodiment
Prescription:
| Supplementary material | Percentage ratio (%) |
| Hydrochloric acid shellfish Xisha star | 10 |
| Lactose | 50 |
| Starch | 30 |
| Cross-linking sodium carboxymethyl cellulose | 5 |
| Starch (binding agent) | 2 |
| Micropowder silica gel | 2 |
| Magnesium stearate | 1 |
Preparation technology:
1, with hydrochloric acid shellfish Xisha star and lactose, starch, cross-linking sodium carboxymethyl cellulose mix homogeneously;
2, make binding agent with 10% starch slurry, 20 mesh sieves are granulated;
3, particle drying is to moisture＜3.5%;
4,30 mesh sieve granulate add micropowder silica gel and magnesium stearate, mix homogeneously;
5, fill capsule.
Claims (8)
1. Pharmaceutical composition that contains shellfish Xisha star or its salt and preparation method thereof is characterized in that shellfish Xisha star or its salt exist with aqueous liquid preparation or solid preparation.
2. aqueous liquid preparation according to claim 1 is characterized in that:
1) the shellfish Xisha star that contains or its salt add with the micronization form, and its particle diameter is less than 10 μ m;
2) contain pharmaceutically available adjuvant, comprise thickening agent, antiseptic, osmotic pressure regulator, pH regulator agent, stabilizing agent and water;
3) thickening agent is selected from one or more mixture of hypromellose, hyaluronic acid sodium, carbomer, poloxamer;
4) antiseptic is selected from one or more mixture of benzalkonium chloride, benzalkonium bromide, Metagin, second, third, butyl ester;
5) osmotic pressure regulator is selected from one or more mixture of propylene glycol, glycerol, mannitol, sodium chloride, sodium bicarbonate, sodium citrate;
6) sodium hydroxide, potassium hydroxide, aluminium hydroxide, triethanolamine etc. are adopted in the pH regulator agent;
7) stabilizing agent adopts disodiumedetate, sodium sulfite, lecithin etc.
3. the preparation technology of aqueous liquid preparation according to claim 2 is characterized in that:
1) take by weighing 0.01～10% thickening agent and/or stabilizing agent and add the abundant swelling of suitable quantity of water, add 0.1%～20% shellfish Xisha star again or its salt fully grinds or stirs or the breast even, solution I;
2) antiseptic, osmotic pressure regulator, stabilizing agent and/or thickening agent are added an amount of water dissolution, get solution II;
3) solution I and solution II are merged, the even or stirring method mix homogeneously by breast, regulating pH value with pH adjustment agent is 5～7, adds water to total amount again.
4. aqueous liquid preparation according to claim 2 is characterized in that water is water for injection.
5. exist with eye drop, gel for eye form according to the described aqueous liquid preparation of claim 2～4.
6. solid preparation according to claim 1 is characterized in that
1) the shellfish Xisha star that contains or its salt add with micronization form or solvation form, and its particle diameter is less than 10 μ m;
2) acceptable accessories that contains comprises in filler, disintegrating agent, wet adhesive, correctives, antioxidant, the antiseptic one or more;
3) filler is selected from one or more in lactose, mannitol, starch, pre-paying starch, the calcium hydrogen phosphate;
4) disintegrating agent is selected from one or more in low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, microcrystalline Cellulose, carboxymethylstach sodium, tween 80, the Polyethylene Glycol;
5) wet adhesive is selected from one or more in water, ethanol, starch, hydroxypropyl cellulose, polyvinylpyrrolidone, the methylcellulose;
6) lubricant is selected from one or more in magnesium stearate, Pulvis Talci, micropowder silica gel, the silicon dioxide.
7. the preparation technology of solid preparation according to claim 6, it is characterized in that getting 0.1～20% shellfish Xisha star or its salt and 40%～80% filler, 3%～30% disintegrating agent mix homogeneously, adding suitable amount of adhesive granulates, oven dry, granulate, add all the other adjuvants, mix homogeneously, compressed tablets or fill capsule.
8. exist with the form of tablet, dispersible tablet, oral cavity disintegration tablet, capsule according to claim 6,7 described solid preparations.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910244381.7A CN102114020B (en) | 2009-12-30 | 2009-12-30 | A kind of Pharmaceutical composition containing besifloxacin or its salt and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200910244381.7A CN102114020B (en) | 2009-12-30 | 2009-12-30 | A kind of Pharmaceutical composition containing besifloxacin or its salt and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102114020A true CN102114020A (en) | 2011-07-06 |
| CN102114020B CN102114020B (en) | 2016-04-20 |
Family
ID=44213020
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200910244381.7A Active CN102114020B (en) | 2009-12-30 | 2009-12-30 | A kind of Pharmaceutical composition containing besifloxacin or its salt and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102114020B (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102908323A (en) * | 2012-10-30 | 2013-02-06 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN103565742A (en) * | 2012-07-25 | 2014-02-12 | 天津金耀集团有限公司 | Fluorometholone eye drops |
| CN108815119A (en) * | 2018-08-10 | 2018-11-16 | 亚邦医药股份有限公司 | A kind of pharmaceutical composition and preparation method thereof containing besifloxacin hydrochloride |
| CN115708805A (en) * | 2022-11-21 | 2023-02-24 | 山东诺明康药物研究院有限公司 | Bexifloxacin hydrochloride in-situ gel eye drops and preparation method thereof |
| CN115919758A (en) * | 2022-11-21 | 2023-04-07 | 山东诺明康药物研究院有限公司 | Bexifloxacin hydrochloride ion sensitive in-situ gel eye drops and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101278905A (en) * | 2008-05-13 | 2008-10-08 | 山东博士伦福瑞达制药有限公司 | Ophthalmic composition containing natamycin, use and preparation method thereof |
| WO2008154136A1 (en) * | 2007-06-11 | 2008-12-18 | Bausch & Lomb Incorporated | Compositions and methods for modulating inflammation using fluoroquinolones |
-
2009
- 2009-12-30 CN CN200910244381.7A patent/CN102114020B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008154136A1 (en) * | 2007-06-11 | 2008-12-18 | Bausch & Lomb Incorporated | Compositions and methods for modulating inflammation using fluoroquinolones |
| CN101278905A (en) * | 2008-05-13 | 2008-10-08 | 山东博士伦福瑞达制药有限公司 | Ophthalmic composition containing natamycin, use and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| TIMOTHY L.等: "Efficacy and Safety of Besifloxacin Ophthalmic Suspension 0.6% in Pediatric Patients With Bacterial Conjunctivitis", 《OPTOMETRY》 * |
| 杨桂明主编: "《中药药剂学》", 30 June 2005, 人民卫生出版社 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103565742A (en) * | 2012-07-25 | 2014-02-12 | 天津金耀集团有限公司 | Fluorometholone eye drops |
| CN102908323A (en) * | 2012-10-30 | 2013-02-06 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN102908323B (en) * | 2012-10-30 | 2015-03-04 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN108815119A (en) * | 2018-08-10 | 2018-11-16 | 亚邦医药股份有限公司 | A kind of pharmaceutical composition and preparation method thereof containing besifloxacin hydrochloride |
| CN115708805A (en) * | 2022-11-21 | 2023-02-24 | 山东诺明康药物研究院有限公司 | Bexifloxacin hydrochloride in-situ gel eye drops and preparation method thereof |
| CN115919758A (en) * | 2022-11-21 | 2023-04-07 | 山东诺明康药物研究院有限公司 | Bexifloxacin hydrochloride ion sensitive in-situ gel eye drops and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102114020B (en) | 2016-04-20 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN102470133B (en) | Quinoline derivative-containing pharmaceutical composition | |
| CN102114020B (en) | A kind of Pharmaceutical composition containing besifloxacin or its salt and preparation method thereof | |
| CN101390837B (en) | Amoxicillin granule and production method thereof | |
| CN101594865A (en) | The pharmaceutical composition that contains the low hydroxy propyl cellulose that replaces | |
| JP6399115B2 (en) | Solid pharmaceutical composition containing a compound having angiotensin II antagonistic activity | |
| CN101822674B (en) | Iloperidone drug composition and preparation method thereof | |
| CN105213333A (en) | A kind of tadanafil pharmaceutical composition and preparation method thereof | |
| AU2007330605A1 (en) | New crystalline forms | |
| CN103301080B (en) | Moxifloxacin hydrochloride-containing pharmaceutical composition and preparation method thereof | |
| CN102526748B (en) | Oral tablet containing Valsartan, Hydrochioro and Amlodipine Besylate Tablet | |
| WO2007102082A1 (en) | High oxazolidinone content solid dosage forms | |
| CN103142506B (en) | Cefpodoxime proxetil granules and preparation method thereof | |
| CN110075079A (en) | A kind of appropriate logical sequence pivoxil plain piece of spore, the appropriate logical sequence pivoxil piece of spore and preparation method | |
| JP4774739B2 (en) | Kampo extract-containing tablet composition and method for producing the same | |
| CN101711753B (en) | Preparation method of lansoprazole solid preparation | |
| CZ301299B6 (en) | Solid pharmaceutical composition with atorvastatin and telmisartan active ingredients | |
| CN111377947B (en) | Amoxicillin trihydrate pharmaceutical composition with low water activity and preparation method thereof | |
| CN104721827A (en) | Insoluble antifungal medicament solid dispersion and preparation method thereof | |
| CN102552170A (en) | Solid preparation taking prasugrel benzene sulfonate as active component | |
| CN103006614B (en) | Cefuroxime axetil capsule in non-gel state in water and preparation method of cefuroxime axetil capsule | |
| CN108938576A (en) | A kind of Voriconazole Dispersible Tablets and preparation method thereof | |
| CN107296800A (en) | A kind of Loratadine effervescent tablet and preparation method thereof | |
| CN102335151B (en) | Clindamycin phosphate vaginal mucosa tablet and preparation method thereof | |
| CN110787155A (en) | Itopride hydrochloride pharmaceutical composition and preparation method thereof | |
| CN110075078A (en) | A kind of Cefditoren pivoxil Cephalosporins composition and Cefditoren pivoxil Cephalosporins piece |
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 | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20201202 Address after: No. 279 Nanhai Road, Xiuying District 570314 Hainan city of Haikou Province Patentee after: AVENTIS PHARMA (HAINAN) Co.,Ltd. Address before: 100097, Wanquan mansion, 3 Jin Zhuang, Haidian District, Beijing, Sijiqing Patentee before: BEIJING D-VENTURE PHARMACEUTICAL TECHNOLOGY Corp. |
|
| TR01 | Transfer of patent right | ||
| DD01 | Delivery of document by public notice |
Addressee: Song Xuemei Document name: Notice of conformity |
|
| DD01 | Delivery of document by public notice | ||
| PE01 | Entry into force of the registration of the contract for pledge of patent right |
Denomination of invention: A medicinal composition containing berxifloxacin or its salt and its preparation method Granted publication date: 20160420 Pledgee: Sanya Rural Commercial Bank Co.,Ltd. Pledgor: AVENTIS PHARMA (HAINAN) Co.,Ltd. Registration number: Y2024980014810 |