CN101524353B - 口服抗过敏复方药物组合物 - Google Patents
口服抗过敏复方药物组合物 Download PDFInfo
- Publication number
- CN101524353B CN101524353B CN2008101012585A CN200810101258A CN101524353B CN 101524353 B CN101524353 B CN 101524353B CN 2008101012585 A CN2008101012585 A CN 2008101012585A CN 200810101258 A CN200810101258 A CN 200810101258A CN 101524353 B CN101524353 B CN 101524353B
- Authority
- CN
- China
- Prior art keywords
- levocetirizine
- pharmaceutical composition
- group
- compound recipe
- membrane stabilizer
- 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 - Fee Related
Links
- 150000001875 compounds Chemical class 0.000 title claims abstract description 26
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 12
- 230000003266 anti-allergic effect Effects 0.000 title claims abstract description 10
- 229960001508 levocetirizine Drugs 0.000 claims abstract description 147
- ZKLPARSLTMPFCP-OAQYLSRUSA-N 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid Chemical compound C1CN(CCOCC(=O)O)CCN1[C@@H](C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-OAQYLSRUSA-N 0.000 claims abstract description 106
- 239000003814 drug Substances 0.000 claims abstract description 32
- 239000008187 granular material Substances 0.000 claims abstract description 27
- 210000003630 histaminocyte Anatomy 0.000 claims abstract description 27
- 239000012528 membrane Substances 0.000 claims abstract description 22
- 239000003381 stabilizer Substances 0.000 claims abstract description 22
- 206010039085 Rhinitis allergic Diseases 0.000 claims abstract description 19
- 201000010105 allergic rhinitis Diseases 0.000 claims abstract description 18
- 239000002775 capsule Substances 0.000 claims abstract description 11
- 201000004624 Dermatitis Diseases 0.000 claims abstract description 9
- 239000002552 dosage form Substances 0.000 claims abstract description 3
- 239000003826 tablet Substances 0.000 claims abstract description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group 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 46
- 239000011734 sodium Substances 0.000 claims description 46
- 229910052708 sodium Inorganic materials 0.000 claims description 46
- 229950011082 suplatast tosilate Drugs 0.000 claims description 34
- 229950009147 repirinast Drugs 0.000 claims description 28
- 229960005342 tranilast Drugs 0.000 claims description 26
- RYVJQEZJUFRANT-UHFFFAOYSA-N [3-[4-(3-ethoxy-2-hydroxypropoxy)anilino]-3-oxopropyl]-dimethylsulfanium;4-methylbenzenesulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1.CCOCC(O)COC1=CC=C(NC(=O)CC[S+](C)C)C=C1 RYVJQEZJUFRANT-UHFFFAOYSA-N 0.000 claims description 25
- 229960003731 amlexanox Drugs 0.000 claims description 24
- 229950011558 tazanolast Drugs 0.000 claims description 23
- NZHGWWWHIYHZNX-CSKARUKUSA-N tranilast Chemical compound C1=C(OC)C(OC)=CC=C1\C=C\C(=O)NC1=CC=CC=C1C(O)=O NZHGWWWHIYHZNX-CSKARUKUSA-N 0.000 claims description 22
- SGRYPYWGNKJSDL-UHFFFAOYSA-N amlexanox Chemical compound NC1=C(C(O)=O)C=C2C(=O)C3=CC(C(C)C)=CC=C3OC2=N1 SGRYPYWGNKJSDL-UHFFFAOYSA-N 0.000 claims description 19
- NFQIAEMCQGTTIR-UHFFFAOYSA-N Repirinast Chemical group C12=CC=C(C)C(C)=C2NC(=O)C2=C1OC(C(=O)OCCC(C)C)=CC2=O NFQIAEMCQGTTIR-UHFFFAOYSA-N 0.000 claims description 17
- XQTARQNQIVVBRX-UHFFFAOYSA-N Tazanolast Chemical compound CCCCOC(=O)C(=O)NC1=CC=CC(C2=NNN=N2)=C1 XQTARQNQIVVBRX-UHFFFAOYSA-N 0.000 claims description 17
- 208000006673 asthma Diseases 0.000 claims description 13
- 229940079593 drug Drugs 0.000 claims description 12
- 239000000739 antihistaminic agent Substances 0.000 claims description 9
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims description 9
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 8
- 239000000725 suspension Substances 0.000 claims description 6
- 239000007788 liquid Substances 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 3
- 229940124623 antihistamine drug Drugs 0.000 claims 2
- 239000000203 mixture Substances 0.000 abstract description 74
- -1 oral solution Substances 0.000 abstract description 50
- 210000003491 skin Anatomy 0.000 abstract description 15
- 208000010668 atopic eczema Diseases 0.000 abstract description 14
- 208000003251 Pruritus Diseases 0.000 abstract description 13
- 208000026935 allergic disease Diseases 0.000 abstract description 4
- 208000024780 Urticaria Diseases 0.000 abstract description 3
- 239000000375 suspending agent Substances 0.000 abstract 2
- 229940100688 oral solution Drugs 0.000 abstract 1
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 78
- 229920002472 Starch Polymers 0.000 description 39
- 235000019359 magnesium stearate Nutrition 0.000 description 39
- 239000008107 starch Substances 0.000 description 38
- 235000019698 starch Nutrition 0.000 description 38
- 238000002156 mixing Methods 0.000 description 33
- 241000700159 Rattus Species 0.000 description 32
- 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 description 31
- 239000008101 lactose Substances 0.000 description 31
- 238000012360 testing method Methods 0.000 description 26
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 24
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 24
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 24
- 229960003943 hypromellose Drugs 0.000 description 24
- 238000000034 method Methods 0.000 description 23
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 19
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 19
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 description 19
- 238000009775 high-speed stirring Methods 0.000 description 19
- 239000008108 microcrystalline cellulose Substances 0.000 description 19
- 229940016286 microcrystalline cellulose Drugs 0.000 description 19
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 19
- 239000000741 silica gel Substances 0.000 description 19
- 229910002027 silica gel Inorganic materials 0.000 description 19
- 230000000694 effects Effects 0.000 description 18
- 229960004958 ketotifen Drugs 0.000 description 18
- 238000002360 preparation method Methods 0.000 description 16
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N Ketotifene Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 ZCVMWBYGMWKGHF-UHFFFAOYSA-N 0.000 description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- 230000000172 allergic effect Effects 0.000 description 11
- 239000000243 solution Substances 0.000 description 11
- 235000000346 sugar Nutrition 0.000 description 11
- 208000024891 symptom Diseases 0.000 description 11
- 239000007864 aqueous solution Substances 0.000 description 10
- 239000000853 adhesive Substances 0.000 description 9
- 230000001070 adhesive effect Effects 0.000 description 9
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 9
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 9
- 206010070834 Sensitisation Diseases 0.000 description 8
- 210000000627 locus coeruleus Anatomy 0.000 description 8
- 230000008313 sensitization Effects 0.000 description 8
- 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 description 7
- 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 description 7
- 229920001353 Dextrin Polymers 0.000 description 7
- 239000004375 Dextrin Substances 0.000 description 7
- 229930195725 Mannitol Natural products 0.000 description 7
- 241000699670 Mus sp. Species 0.000 description 7
- 230000001387 anti-histamine Effects 0.000 description 7
- 235000019425 dextrin Nutrition 0.000 description 7
- 229960001375 lactose Drugs 0.000 description 7
- 239000000594 mannitol Substances 0.000 description 7
- 235000010355 mannitol Nutrition 0.000 description 7
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 6
- 238000011534 incubation Methods 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 239000000047 product Substances 0.000 description 6
- 239000008213 purified water Substances 0.000 description 6
- 210000002784 stomach Anatomy 0.000 description 6
- NUKYPUAOHBNCPY-UHFFFAOYSA-N 4-aminopyridine Chemical compound NC1=CC=NC=C1 NUKYPUAOHBNCPY-UHFFFAOYSA-N 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 5
- 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 description 5
- 239000012153 distilled water Substances 0.000 description 5
- 229960004979 fampridine Drugs 0.000 description 5
- 229960001803 cetirizine Drugs 0.000 description 4
- IMZMKUWMOSJXDT-UHFFFAOYSA-N cromoglycic acid Chemical compound O1C(C(O)=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C(O)=O)O2 IMZMKUWMOSJXDT-UHFFFAOYSA-N 0.000 description 4
- 238000010998 test method Methods 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 230000000699 topical effect Effects 0.000 description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 108010058846 Ovalbumin Proteins 0.000 description 3
- 239000001768 carboxy methyl cellulose Substances 0.000 description 3
- 238000010835 comparative analysis Methods 0.000 description 3
- 229960000265 cromoglicic acid Drugs 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000008273 gelatin Substances 0.000 description 3
- 229920000159 gelatin Polymers 0.000 description 3
- 235000019322 gelatine Nutrition 0.000 description 3
- 235000011852 gelatine desserts Nutrition 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 210000001331 nose Anatomy 0.000 description 3
- 229940092253 ovalbumin Drugs 0.000 description 3
- 239000002243 precursor Substances 0.000 description 3
- 239000000376 reactant Substances 0.000 description 3
- 230000029058 respiratory gaseous exchange Effects 0.000 description 3
- 210000002966 serum Anatomy 0.000 description 3
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 3
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 235000010356 sorbitol Nutrition 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- MBUVEWMHONZEQD-UHFFFAOYSA-N Azeptin Chemical compound C1CN(C)CCCC1N1C(=O)C2=CC=CC=C2C(CC=2C=CC(Cl)=CC=2)=N1 MBUVEWMHONZEQD-UHFFFAOYSA-N 0.000 description 2
- ZKLPARSLTMPFCP-UHFFFAOYSA-N Cetirizine Chemical compound C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-UHFFFAOYSA-N 0.000 description 2
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- 206010020751 Hypersensitivity Diseases 0.000 description 2
- 206010039101 Rhinorrhoea Diseases 0.000 description 2
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 2
- 238000002835 absorbance Methods 0.000 description 2
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 2
- 230000002052 anaphylactic effect Effects 0.000 description 2
- 239000000427 antigen Substances 0.000 description 2
- 102000036639 antigens Human genes 0.000 description 2
- 108091007433 antigens Proteins 0.000 description 2
- 229960004574 azelastine Drugs 0.000 description 2
- 229960003291 chlorphenamine Drugs 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000006196 drop Substances 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 230000007803 itching Effects 0.000 description 2
- 238000011068 loading method Methods 0.000 description 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 2
- 208000010753 nasal discharge Diseases 0.000 description 2
- 229960004398 nedocromil Drugs 0.000 description 2
- RQTOOFIXOKYGAN-UHFFFAOYSA-N nedocromil Chemical compound CCN1C(C(O)=O)=CC(=O)C2=C1C(CCC)=C1OC(C(O)=O)=CC(=O)C1=C2 RQTOOFIXOKYGAN-UHFFFAOYSA-N 0.000 description 2
- 229960004114 olopatadine Drugs 0.000 description 2
- JBIMVDZLSHOPLA-LSCVHKIXSA-N olopatadine Chemical compound C1OC2=CC=C(CC(O)=O)C=C2C(=C/CCN(C)C)\C2=CC=CC=C21 JBIMVDZLSHOPLA-LSCVHKIXSA-N 0.000 description 2
- 229940126701 oral medication Drugs 0.000 description 2
- 230000035699 permeability Effects 0.000 description 2
- 238000003825 pressing Methods 0.000 description 2
- 229940083542 sodium Drugs 0.000 description 2
- 238000010254 subcutaneous injection Methods 0.000 description 2
- 239000007929 subcutaneous injection Substances 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
- 239000005526 vasoconstrictor agent Substances 0.000 description 2
- JJOFNSLZHKIJEV-UHFFFAOYSA-N 2-amino-2-(hydroxymethyl)propane-1,3-diol;2-[2-chloro-5-cyano-3-(oxaloamino)anilino]-2-oxoacetic acid Chemical compound OCC(N)(CO)CO.OCC(N)(CO)CO.OC(=O)C(=O)NC1=CC(C#N)=CC(NC(=O)C(O)=O)=C1Cl JJOFNSLZHKIJEV-UHFFFAOYSA-N 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 229920000178 Acrylic resin Polymers 0.000 description 1
- 235000019890 Amylum Nutrition 0.000 description 1
- 206010002198 Anaphylactic reaction Diseases 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- 241000195622 Astasia 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
- 206010010744 Conjunctivitis allergic Diseases 0.000 description 1
- 206010010947 Coordination abnormal Diseases 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 206010011703 Cyanosis Diseases 0.000 description 1
- 229920000858 Cyclodextrin Polymers 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 229940032024 DPT vaccine Drugs 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
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 241000581650 Ivesia Species 0.000 description 1
- HOKDBMAJZXIPGC-UHFFFAOYSA-N Mequitazine Chemical compound C12=CC=CC=C2SC2=CC=CC=C2N1CC1C(CC2)CCN2C1 HOKDBMAJZXIPGC-UHFFFAOYSA-N 0.000 description 1
- PVLJETXTTWAYEW-UHFFFAOYSA-N Mizolastine Chemical compound N=1C=CC(=O)NC=1N(C)C(CC1)CCN1C1=NC2=CC=CC=C2N1CC1=CC=C(F)C=C1 PVLJETXTTWAYEW-UHFFFAOYSA-N 0.000 description 1
- 208000007101 Muscle Cramp Diseases 0.000 description 1
- 229910002651 NO3 Inorganic materials 0.000 description 1
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical group Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 0.000 description 1
- JAUOIFJMECXRGI-UHFFFAOYSA-N Neoclaritin Chemical compound C=1C(Cl)=CC=C2C=1CCC1=CC=CN=C1C2=C1CCNCC1 JAUOIFJMECXRGI-UHFFFAOYSA-N 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
- ISFHAYSTHMVOJR-UHFFFAOYSA-N Phenindamine Chemical compound C1N(C)CCC(C2=CC=CC=C22)=C1C2C1=CC=CC=C1 ISFHAYSTHMVOJR-UHFFFAOYSA-N 0.000 description 1
- SSOXZAQUVINQSA-BTJKTKAUSA-N Pheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=CC=C1 SSOXZAQUVINQSA-BTJKTKAUSA-N 0.000 description 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 208000005392 Spasm Diseases 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 210000000683 abdominal cavity Anatomy 0.000 description 1
- 210000003489 abdominal muscle Anatomy 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 201000009961 allergic asthma Diseases 0.000 description 1
- 208000002205 allergic conjunctivitis Diseases 0.000 description 1
- 230000009285 allergic inflammation Effects 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 150000003927 aminopyridines Chemical class 0.000 description 1
- 208000003455 anaphylaxis Diseases 0.000 description 1
- 230000002804 anti-anaphylactic effect Effects 0.000 description 1
- 210000000709 aorta Anatomy 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- GXDALQBWZGODGZ-UHFFFAOYSA-N astemizole Chemical compound C1=CC(OC)=CC=C1CCN1CCC(NC=2N(C3=CC=CC=C3N=2)CC=2C=CC(F)=CC=2)CC1 GXDALQBWZGODGZ-UHFFFAOYSA-N 0.000 description 1
- 229940065779 atarax Drugs 0.000 description 1
- 208000024998 atopic conjunctivitis Diseases 0.000 description 1
- 229960000383 azatadine Drugs 0.000 description 1
- SEBMTIQKRHYNIT-UHFFFAOYSA-N azatadine Chemical compound C1CN(C)CCC1=C1C2=NC=CC=C2CCC2=CC=CC=C21 SEBMTIQKRHYNIT-UHFFFAOYSA-N 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 238000010241 blood sampling Methods 0.000 description 1
- 229960000725 brompheniramine Drugs 0.000 description 1
- ZDIGNSYAACHWNL-UHFFFAOYSA-N brompheniramine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Br)C=C1 ZDIGNSYAACHWNL-UHFFFAOYSA-N 0.000 description 1
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 229960002881 clemastine Drugs 0.000 description 1
- YNNUSGIPVFPVBX-NHCUHLMSSA-N clemastine Chemical compound CN1CCC[C@@H]1CCO[C@@](C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 YNNUSGIPVFPVBX-NHCUHLMSSA-N 0.000 description 1
- 229940109248 cromoglycate Drugs 0.000 description 1
- 229960001271 desloratadine Drugs 0.000 description 1
- ZDIGNSYAACHWNL-HNNXBMFYSA-N dexbrompheniramine Chemical compound C1([C@H](CCN(C)C)C=2N=CC=CC=2)=CC=C(Br)C=C1 ZDIGNSYAACHWNL-HNNXBMFYSA-N 0.000 description 1
- 229960002691 dexbrompheniramine Drugs 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 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 description 1
- 229960000520 diphenhydramine Drugs 0.000 description 1
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 1
- 238000007599 discharging Methods 0.000 description 1
- 229960005178 doxylamine Drugs 0.000 description 1
- HCFDWZZGGLSKEP-UHFFFAOYSA-N doxylamine Chemical compound C=1C=CC=NC=1C(C)(OCCN(C)C)C1=CC=CC=C1 HCFDWZZGGLSKEP-UHFFFAOYSA-N 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 229960001971 ebastine Drugs 0.000 description 1
- MJJALKDDGIKVBE-UHFFFAOYSA-N ebastine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(=O)CCCN1CCC(OC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 MJJALKDDGIKVBE-UHFFFAOYSA-N 0.000 description 1
- 229960000325 emedastine Drugs 0.000 description 1
- KBUZBQVCBVDWKX-UHFFFAOYSA-N emedastine Chemical compound N=1C2=CC=CC=C2N(CCOCC)C=1N1CCCN(C)CC1 KBUZBQVCBVDWKX-UHFFFAOYSA-N 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 229960003449 epinastine Drugs 0.000 description 1
- WHWZLSFABNNENI-UHFFFAOYSA-N epinastine Chemical compound C1C2=CC=CC=C2C2CN=C(N)N2C2=CC=CC=C21 WHWZLSFABNNENI-UHFFFAOYSA-N 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 229960003592 fexofenadine Drugs 0.000 description 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 210000003194 forelimb Anatomy 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 229960002897 heparin Drugs 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- ZQDWXGKKHFNSQK-UHFFFAOYSA-N hydroxyzine Chemical compound C1CN(CCOCCO)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZQDWXGKKHFNSQK-UHFFFAOYSA-N 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 239000003199 leukotriene receptor blocking agent Substances 0.000 description 1
- 229960001120 levocabastine Drugs 0.000 description 1
- ZCGOMHNNNFPNMX-KYTRFIICSA-N levocabastine Chemical compound C1([C@@]2(C(O)=O)CCN(C[C@H]2C)[C@@H]2CC[C@@](CC2)(C#N)C=2C=CC(F)=CC=2)=CC=CC=C1 ZCGOMHNNNFPNMX-KYTRFIICSA-N 0.000 description 1
- 229960004305 lodoxamide Drugs 0.000 description 1
- RVGLGHVJXCETIO-UHFFFAOYSA-N lodoxamide Chemical compound OC(=O)C(=O)NC1=CC(C#N)=CC(NC(=O)C(O)=O)=C1Cl RVGLGHVJXCETIO-UHFFFAOYSA-N 0.000 description 1
- 229960000558 lodoxamide tromethamine Drugs 0.000 description 1
- 229960003088 loratadine Drugs 0.000 description 1
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 229960000582 mepyramine Drugs 0.000 description 1
- YECBIJXISLIIDS-UHFFFAOYSA-N mepyramine Chemical compound C1=CC(OC)=CC=C1CN(CCN(C)C)C1=CC=CC=N1 YECBIJXISLIIDS-UHFFFAOYSA-N 0.000 description 1
- 229960005042 mequitazine Drugs 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 229960001144 mizolastine Drugs 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 229960004760 naphazoline hydrochloride Drugs 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 208000037916 non-allergic rhinitis Diseases 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 229960002698 oxatomide Drugs 0.000 description 1
- BAINIUMDFURPJM-UHFFFAOYSA-N oxatomide Chemical compound O=C1NC2=CC=CC=C2N1CCCN(CC1)CCN1C(C=1C=CC=CC=1)C1=CC=CC=C1 BAINIUMDFURPJM-UHFFFAOYSA-N 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- HIANJWSAHKJQTH-UHFFFAOYSA-N pemirolast Chemical compound CC1=CC=CN(C2=O)C1=NC=C2C=1N=NNN=1 HIANJWSAHKJQTH-UHFFFAOYSA-N 0.000 description 1
- 229960004439 pemirolast Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229960003534 phenindamine Drugs 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
- 239000002571 phosphodiesterase inhibitor Substances 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 230000007015 preclinical effect Effects 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
- 238000006748 scratching Methods 0.000 description 1
- 230000002393 scratching effect Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 231100000245 skin permeability Toxicity 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229910052567 struvite Inorganic materials 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 229960000351 terfenadine Drugs 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 229960001128 triprolidine Drugs 0.000 description 1
- CBEQULMOCCWAQT-WOJGMQOQSA-N triprolidine Chemical compound C1=CC(C)=CC=C1C(\C=1N=CC=CC=1)=C/CN1CCCC1 CBEQULMOCCWAQT-WOJGMQOQSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
组别 | 剂量(mg/kg) | 10min内舔体次数 |
模型组左西替利嗪组甲磺司特组曲尼司特组左西替利嗪甲磺司特复方组左西替利嗪曲尼司特复方组 | -0.6412.938.70.64+12.90.64+38.7 | 51.9±10.0529.3±11.0**30.4±12.63**39.2±9.58*16.8±9.49**#△19.6±10.23**#△ |
组别 | 剂量(mg/kg) | 引喘潜伏期(s) |
模型组左西替利嗪组酮替芬组瑞吡司特组 | -0.450.094.5 | 78.4±16.180.2±15.793.3±13.7*97.6±14.2* |
氨米占司组 | 4.5 | 94.1±16.8* |
左西替利嗪酮替芬复方组 | 0.45+0.09 | 108.4±15.9**##△ |
左西替利嗪瑞吡司特复方组 | 0.45+4.5 | 116.8±13.2**##△△ |
左西替利嗪氨米占司复方组 | 0.45+4.5 | 109.8±14.9**##△ |
组别 | 剂量(mg/kg) | 过敏症状评分 |
正常组模型组左西替利嗪组甲磺司特组色羟丙钠组左西替利嗪甲磺司特复方组左西替利嗪色羟丙钠复方组 | --0.459.09.00.45+9.00.45+9.0 | 1.00±0.826.50±1.354.37±1.56**4.62±1.25**3.88±1.03**2.00±1.41**##△△1.89±1.54**##△△ |
组别 | 剂量(mg/kg) | 1∶5抗血清 | 1∶10抗血清 | ||
蓝斑面积(cm2) | Evan’s OD值 | 蓝斑面积(cm2) | Evan’s OD值 | ||
模型组左西替利嗪组瑞吡司特组他扎司特组左西替利嗪瑞吡司特复方组左西替利嗪他扎司特复方组 | -0.454.56.70.45+4.50.45+6.7 | 4.772±1.8202.019±0.993**2.183±1.257**1.954±1.108**0.921±0.368**##△△0.822±0.276**##△△ | 0.153±0.0280.115±0.037*0.116±0.025**0.097±0.021**0.078±0.032**#△△0.069±0.034**##△ | 5.522±1.7463.128±0.715**3.350±0.726**2.825±0.803**1.008±0.429**##△△0.945±0.197**##△△ | 0.161±0.0210.125±0.024**0.131±0.017**0.106±0.020**0.081±0.016**## △△0.074±0.022**##△△ |
Claims (8)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2008101012585A CN101524353B (zh) | 2008-03-03 | 2008-03-03 | 口服抗过敏复方药物组合物 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2008101012585A CN101524353B (zh) | 2008-03-03 | 2008-03-03 | 口服抗过敏复方药物组合物 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101524353A CN101524353A (zh) | 2009-09-09 |
CN101524353B true CN101524353B (zh) | 2012-02-22 |
Family
ID=41092529
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2008101012585A Expired - Fee Related CN101524353B (zh) | 2008-03-03 | 2008-03-03 | 口服抗过敏复方药物组合物 |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN101524353B (zh) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103463089B (zh) * | 2013-08-26 | 2016-03-02 | 王大光 | 一种盐酸西替利嗪口服溶液组合物 |
CN103690555B (zh) * | 2014-01-02 | 2015-06-24 | 王雪雁 | 一种治疗乙酰胆碱性荨麻疹的药物组合物 |
CN109589317A (zh) * | 2018-12-10 | 2019-04-09 | 中国海洋大学 | 一种兼具抑制组胺释放与组胺受体拮抗功能的纳米颗粒的制备方法 |
-
2008
- 2008-03-03 CN CN2008101012585A patent/CN101524353B/zh not_active Expired - Fee Related
Non-Patent Citations (2)
Title |
---|
李明华.抗过敏药物的种类、药理学和临床应用.《中国临床医生》.2003,第31卷(第9期),15-18. * |
梁斌慧.酮替芬联合盐酸西替利嗪治疗慢性荨麻疹34例.《实用临床医学》.2007,第8卷(第1期),38. * |
Also Published As
Publication number | Publication date |
---|---|
CN101524353A (zh) | 2009-09-09 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP6294476B2 (ja) | 血球減少を予防又は治療するための薬物の製造におけるアンヒドロイカリチンの使用 | |
CN101069675A (zh) | 用于减轻痉挛状态的体征和症状的方法 | |
CN104367765A (zh) | 一种用于治疗抑郁症的中药组合物及其制备方法和应用 | |
CN101524353B (zh) | 口服抗过敏复方药物组合物 | |
CN106309388A (zh) | 一种用于心衰治疗的药物组合物及其制备方法 | |
CN101103960A (zh) | 一种含有消旋卡多曲的干混悬剂及其制备方法 | |
CN104000789A (zh) | 一种阿德福韦酯分散片及其制备方法 | |
CN102267959B (zh) | 一种瑞格列奈晶体、其制备方法及含有该晶体的固体口服制剂 | |
CN104688760B (zh) | 一种由柴胡皂苷a和牛磺酸组成的药物组合物及其用途 | |
CN109988104B (zh) | 山奈酚与异烟酰胺共晶物及制备方法和其药物组合物与用途 | |
CN101120943A (zh) | 一种治疗脑胶质瘤的药物组合物、其制备方法及制剂 | |
CN101461832A (zh) | 治疗口腔溃疡的生物粘附贴片 | |
CN1312157C (zh) | 卤代二氢青蒿素及其制备方法以及用途 | |
CN103271907B (zh) | 一种小檗碱和二甲双胍的口服药物组合物及其制备方法 | |
CN105147709B (zh) | 一种替诺福韦二吡呋酯或其药用盐的用途 | |
CN100509017C (zh) | 治疗胆道感染的药物及其制备方法 | |
CN103222966A (zh) | 一种含有盐酸芬戈莫德的固体药物组合物及其制备方法 | |
CN103284953A (zh) | 一种双环醇固体制剂及其制备方法 | |
CN101797253B (zh) | 一种岩白菜素、盐酸西替利嗪复方口服剂型 | |
CN101579342A (zh) | 一种含有地氯雷他定的感冒药组合物 | |
CN101940619A (zh) | 一种治疗格林-巴利综合征疾病的中药制剂及制备方法 | |
CN109260217A (zh) | 3`-脱氧次黄嘌呤核苷在制备用于多种疾病药品、食品或保健品中的应用 | |
CN105078994B (zh) | 吡嗪衍生物的用途、药物组合物、保健食品 | |
CN115702898B (zh) | 一种btk抑制剂固体制剂及其制备方法 | |
CN107669700A (zh) | 一种治疗溃疡性结肠炎的药物及其制备方法 |
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 | ||
ASS | Succession or assignment of patent right |
Owner name: CHONGQING HUAPONT PHARMACEUTICAL CO., LTD. Free format text: FORMER OWNER: HUABANG PHARMACEUTICAL CO., LTD., CHONGQING Effective date: 20130217 |
|
C41 | Transfer of patent application or patent right or utility model | ||
TR01 | Transfer of patent right |
Effective date of registration: 20130217 Address after: 401121 Chongqing, Yubei District and the number of stars Avenue, No. 69 Patentee after: CHONGQING HUAPONT PHARM. Co.,Ltd. Address before: 401121 Chongqing, Yubei District and the number of stars Avenue, No. 69 Patentee before: CHONGQING HUAPONT PHARM. Co.,Ltd. |
|
CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20120222 |
|
CF01 | Termination of patent right due to non-payment of annual fee |