JP2002308764A - Pharmaceutical composition for ophthalmic use - Google Patents
Pharmaceutical composition for ophthalmic useInfo
- Publication number
- JP2002308764A JP2002308764A JP2001298850A JP2001298850A JP2002308764A JP 2002308764 A JP2002308764 A JP 2002308764A JP 2001298850 A JP2001298850 A JP 2001298850A JP 2001298850 A JP2001298850 A JP 2001298850A JP 2002308764 A JP2002308764 A JP 2002308764A
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- bromfenac sodium
- vasoconstrictor
- ophthalmic pharmaceutical
- present
- 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.)
- Withdrawn
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 16
- 239000005526 vasoconstrictor agent Substances 0.000 claims abstract description 12
- 239000003889 eye drop Substances 0.000 claims abstract description 11
- 229960002716 bromfenac sodium Drugs 0.000 claims abstract description 9
- HZFGMQJYAFHESD-UHFFFAOYSA-M bromfenac sodium Chemical compound [Na+].NC1=C(CC([O-])=O)C=CC=C1C(=O)C1=CC=C(Br)C=C1 HZFGMQJYAFHESD-UHFFFAOYSA-M 0.000 claims abstract description 9
- 206010065334 Mucosal hyperaemia Diseases 0.000 claims description 5
- KWGRBVOPPLSCSI-WPRPVWTQSA-N (-)-ephedrine Chemical compound CN[C@@H](C)[C@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WPRPVWTQSA-N 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- BYJAVTDNIXVSPW-UHFFFAOYSA-N tetryzoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 claims description 4
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims description 3
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 claims description 3
- FMCGSUUBYTWNDP-ONGXEEELSA-N (1R,2S)-2-(dimethylamino)-1-phenyl-1-propanol Chemical compound CN(C)[C@@H](C)[C@H](O)C1=CC=CC=C1 FMCGSUUBYTWNDP-ONGXEEELSA-N 0.000 claims description 2
- 229930182837 (R)-adrenaline Natural products 0.000 claims description 2
- FMCGSUUBYTWNDP-UHFFFAOYSA-N N-Methylephedrine Natural products CN(C)C(C)C(O)C1=CC=CC=C1 FMCGSUUBYTWNDP-UHFFFAOYSA-N 0.000 claims description 2
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims description 2
- 229960002179 ephedrine Drugs 0.000 claims description 2
- 229960005139 epinephrine Drugs 0.000 claims description 2
- 229960002221 methylephedrine Drugs 0.000 claims description 2
- 229960005016 naphazoline Drugs 0.000 claims description 2
- 239000002674 ointment Substances 0.000 claims description 2
- 229960001802 phenylephrine Drugs 0.000 claims description 2
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 claims description 2
- 229960000337 tetryzoline Drugs 0.000 claims description 2
- 210000004877 mucosa Anatomy 0.000 abstract description 11
- 239000000203 mixture Substances 0.000 abstract description 6
- 208000024891 symptom Diseases 0.000 abstract description 4
- 239000003885 eye ointment Substances 0.000 abstract description 3
- 239000000243 solution Substances 0.000 abstract description 2
- 206010020565 Hyperaemia Diseases 0.000 description 8
- 239000000306 component Substances 0.000 description 7
- BIYQNLJPABKADF-UHFFFAOYSA-M sodium;2-[2-amino-3-(4-bromobenzoyl)phenyl]acetate;hydrate Chemical compound O.[Na+].NC1=C(CC([O-])=O)C=CC=C1C(=O)C1=CC=C(Br)C=C1 BIYQNLJPABKADF-UHFFFAOYSA-M 0.000 description 7
- 230000000694 effects Effects 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 239000008213 purified water Substances 0.000 description 4
- 238000011282 treatment Methods 0.000 description 4
- 206010010741 Conjunctivitis Diseases 0.000 description 3
- 206010020751 Hypersensitivity Diseases 0.000 description 3
- DJDFFEBSKJCGHC-UHFFFAOYSA-N Naphazoline Chemical compound Cl.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 DJDFFEBSKJCGHC-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000013566 allergen Substances 0.000 description 3
- 229940012356 eye drops Drugs 0.000 description 3
- 238000002636 symptomatic treatment Methods 0.000 description 3
- 230000001225 therapeutic effect Effects 0.000 description 3
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 2
- SQDAZGGFXASXDW-UHFFFAOYSA-N 5-bromo-2-(trifluoromethoxy)pyridine Chemical compound FC(F)(F)OC1=CC=C(Br)C=N1 SQDAZGGFXASXDW-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
- 229920001287 Chondroitin sulfate Polymers 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 208000026935 allergic disease Diseases 0.000 description 2
- 230000007815 allergy Effects 0.000 description 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 2
- 229940046978 chlorpheniramine maleate Drugs 0.000 description 2
- 229940059329 chondroitin sulfate Drugs 0.000 description 2
- RMRCNWBMXRMIRW-BYFNXCQMSA-M cyanocobalamin Chemical compound N#C[Co+]N([C@]1([H])[C@H](CC(N)=O)[C@]\2(CCC(=O)NC[C@H](C)OP(O)(=O)OC3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)C)C/2=C(C)\C([C@H](C/2(C)C)CCC(N)=O)=N\C\2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O RMRCNWBMXRMIRW-BYFNXCQMSA-M 0.000 description 2
- 229940041216 diphenhydramine hydrochloride 50 mg Drugs 0.000 description 2
- 239000006196 drop Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229960004760 naphazoline hydrochloride Drugs 0.000 description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- AEDORKVKMIVLBW-BLDDREHASA-N 3-oxo-3-[[(2r,3s,4s,5r,6r)-3,4,5-trihydroxy-6-[[5-hydroxy-4-(hydroxymethyl)-6-methylpyridin-3-yl]methoxy]oxan-2-yl]methoxy]propanoic acid Chemical compound OCC1=C(O)C(C)=NC=C1CO[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](COC(=O)CC(O)=O)O1 AEDORKVKMIVLBW-BLDDREHASA-N 0.000 description 1
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 description 1
- 208000035143 Bacterial infection Diseases 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- ZAKOWWREFLAJOT-CEFNRUSXSA-N D-alpha-tocopherylacetate Chemical compound CC(=O)OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C ZAKOWWREFLAJOT-CEFNRUSXSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- 206010015958 Eye pain Diseases 0.000 description 1
- 206010052140 Eye pruritus Diseases 0.000 description 1
- XLRHXNIVIZZOON-WFUPGROFSA-L Flavin adenine dinucleotide disodium Chemical compound [Na+].[Na+].C1=NC2=C(N)N=CN=C2N1[C@@H]([C@H](O)[C@@H]1O)O[C@@H]1COP([O-])(=O)OP([O-])(=O)OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C2=NC(=O)NC(=O)C2=NC2=C1C=C(C)C(C)=C2 XLRHXNIVIZZOON-WFUPGROFSA-L 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 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
- 208000003251 Pruritus Diseases 0.000 description 1
- 102100031083 Uteroglobin Human genes 0.000 description 1
- 108090000203 Uteroglobin Proteins 0.000 description 1
- NTCYWJCEOILKNG-ROLPUNSJSA-N [(1r,2s)-1-hydroxy-1-phenylpropan-2-yl]-dimethylazanium;chloride Chemical compound Cl.CN(C)[C@@H](C)[C@H](O)C1=CC=CC=C1 NTCYWJCEOILKNG-ROLPUNSJSA-N 0.000 description 1
- 208000030961 allergic reaction Diseases 0.000 description 1
- 229940124623 antihistamine drug Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 208000003464 asthenopia Diseases 0.000 description 1
- 208000022362 bacterial infectious disease Diseases 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 229960002504 capsaicin Drugs 0.000 description 1
- 235000017663 capsaicin Nutrition 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229960002104 cyanocobalamin Drugs 0.000 description 1
- 235000000639 cyanocobalamin Nutrition 0.000 description 1
- 239000011666 cyanocobalamin Substances 0.000 description 1
- 239000000850 decongestant Substances 0.000 description 1
- 238000000586 desensitisation Methods 0.000 description 1
- 229940057231 diphenhydramine hydrochloride 30 mg Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 229940073563 dl- methylephedrine hydrochloride Drugs 0.000 description 1
- 239000000428 dust Substances 0.000 description 1
- 229960003072 epinephrine hydrochloride Drugs 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 235000012041 food component Nutrition 0.000 description 1
- 239000005428 food component Substances 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 229960003630 ketotifen fumarate Drugs 0.000 description 1
- YNQQEYBLVYAWNX-WLHGVMLRSA-N ketotifen fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 YNQQEYBLVYAWNX-WLHGVMLRSA-N 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 229940080927 menthol 10 mg Drugs 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 230000004089 microcirculation Effects 0.000 description 1
- OSZNNLWOYWAHSS-UHFFFAOYSA-M neostigmine methyl sulfate Chemical compound COS([O-])(=O)=O.CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 OSZNNLWOYWAHSS-UHFFFAOYSA-M 0.000 description 1
- 229960002253 neostigmine methylsulfate Drugs 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 239000003883 ointment base Substances 0.000 description 1
- 239000002997 ophthalmic solution Substances 0.000 description 1
- 229940054534 ophthalmic solution Drugs 0.000 description 1
- 229960003733 phenylephrine hydrochloride Drugs 0.000 description 1
- OCYSGIYOVXAGKQ-FVGYRXGTSA-N phenylephrine hydrochloride Chemical compound [H+].[Cl-].CNC[C@H](O)C1=CC=CC(O)=C1 OCYSGIYOVXAGKQ-FVGYRXGTSA-N 0.000 description 1
- 229940068988 potassium aspartate Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229940053679 pyridoxine hydrochloride 50 mg Drugs 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 229960005404 sulfamethoxazole Drugs 0.000 description 1
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- XOAAWQZATWQOTB-UHFFFAOYSA-N taurine Chemical compound NCCS(O)(=O)=O XOAAWQZATWQOTB-UHFFFAOYSA-N 0.000 description 1
- 229940021790 tetrahydrozoline hydrochloride Drugs 0.000 description 1
- BJORNXNYWNIWEY-UHFFFAOYSA-N tetrahydrozoline hydrochloride Chemical compound Cl.N1CCN=C1C1C2=CC=CC=C2CCC1 BJORNXNYWNIWEY-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229940042585 tocopherol acetate Drugs 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、眼科用医薬組成物
に関する。さらに詳しくは、眼粘膜の充血症状の軽減・
除去に有効な眼科用医薬組成物に関する。TECHNICAL FIELD The present invention relates to an ophthalmic pharmaceutical composition. For more details, reduce the hyperemia of the ocular mucosa
The present invention relates to an ophthalmic pharmaceutical composition effective for removal.
【０００２】[0002]
【従来の技術】眼粘膜の充血症状を示す疾患、例えば結
膜炎は眼粘膜の炎症性疾患である。結膜炎の原因は多岐
にわたり、従来は主として細菌感染に基づく症状とされ
ていたが、近年は病因の一つとしてアレルギーが注目さ
れている。アレルギーの原因物質（アレルゲン）は種々
あるが、花粉、ハウスダスト、排気ガス中の微粒子、食
物成分等がアレルゲンになるとされている。2. Description of the Related Art Diseases showing hyperemia of the ocular mucosa, such as conjunctivitis, are inflammatory diseases of the ocular mucosa. The causes of conjunctivitis vary widely and have been previously mainly associated with bacterial infections, but in recent years allergy has been attracting attention as one of the etiologies. Although there are various allergen-causing substances (allergens), pollen, house dust, fine particles in exhaust gas, food components, and the like are considered to be allergens.
【０００３】一般に、アレルギーはアレルゲンを除去す
ることにより原因療法がなされると考えられ、減感作療
法も行われているが、治療期間が長くなり、通院頻度が
増すという欠点を有する。そのため、患者の負担が比較
的大きく、日常生活の中で治療を継続していくことが困
難であり、なかなか原因療法として定着しないというの
が実状である。よって、自ずと対症療法が中心とならざ
るをえない。[0003] In general, it is considered that allergy is treated by removing allergens, and desensitization therapy is also performed. However, there is a drawback that the treatment period is prolonged and the frequency of hospital visits is increased. For this reason, the burden on the patient is relatively large, and it is difficult to continue the treatment in daily life. Therefore, the symptomatic treatment must be the center.
【０００４】種々の眼粘膜充血に対する対症療法として
は、血管収縮薬による赤目の除去・軽減、局所麻酔薬に
よる眼痛、眼掻痒感及び眼不快感の除去・軽減等が一般
的であるが他に、抗ヒスタミン薬による花粉症に代表さ
れるアレルギー反応の抑制または眼掻痒感の除去・軽
減、ビタミン類による微小循環の改善及び眼精疲労の改
善等も知られている。[0004] As symptomatic treatments for various ocular mucosal hyperemias, removal and alleviation of red eyes with a vasoconstrictor, removal and reduction of eye pain, pruritus and discomfort with a local anesthetic are common. In addition, it is also known that an antihistamine drug suppresses allergic reaction typified by hay fever or removes / alleviates eye pruritus, improves microcirculation with vitamins, and improves eyestrain.
【０００５】特に結膜炎等の治療においては、眼粘膜の
充血等の諸症状をいかに早く除去・軽減するかが治療上
の重要な要素とされている。中でも、眼粘膜の腫脹をは
じめとする充血症状は、ＱＯＬの観点から、また重篤な
症状への移行を未然に防止するという観点からも早期に
改善することが求められ、一般用医薬品の分野において
もこのような治療効果を発揮することは重要なことであ
る。[0005] In the treatment of conjunctivitis and the like in particular, it is an important element in the treatment how quickly various symptoms such as hyperemia of the ocular mucosa are reduced or alleviated. Above all, hyperemia, including swelling of the ocular mucosa, is required to be improved promptly from the viewpoint of QOL and from the viewpoint of preventing the transition to serious symptoms beforehand. In such cases, it is important to exhibit such a therapeutic effect.
【０００６】しかしながら、上述のような対症療法では
充分な治療効果が得られず、作用も一過性であるた投薬
の回数も必然的に多くなる。そのため、従来の対症療法
薬にはない充分な治療効果を発揮する点眼剤または眼軟
膏剤を開発することが望まれていた。[0006] However, the above-mentioned symptomatic treatment does not provide a sufficient therapeutic effect, and the number of times of administration, which has a temporary effect, is inevitably increased. Therefore, it has been desired to develop eye drops or eye ointments that exhibit a sufficient therapeutic effect not found in conventional symptomatic drugs.
【０００７】[0007]
【発明が解決しようとする課題】本発明は、眼粘膜の充
血症状を軽減・除去するのに有効な眼科用医薬組成物を
提供することを課題とする。SUMMARY OF THE INVENTION An object of the present invention is to provide an ophthalmic pharmaceutical composition which is effective for reducing or eliminating hyperemia of the ocular mucosa.
【０００８】[0008]
【課題を解決するための手段】本発明者らは、前記課題
を解決すべく鋭意研究した結果、非ステロイド性抗炎症
薬の１種であるブロムフェナクナトリウムと血管収縮薬
を共に配合した組成物が眼粘膜の充血による諸症状の軽
減・除去に極めて効果的に作用することを見いだし、本
発明を完成するに至った。Means for Solving the Problems The present inventors have made intensive studies to solve the above-mentioned problems, and as a result, have found that a composition comprising both bromfenac sodium, one of non-steroidal anti-inflammatory drugs, and a vasoconstrictor. The present inventors have found that a substance extremely effectively acts to reduce or eliminate various symptoms due to hyperemia of the ocular mucosa, and have completed the present invention.
【０００９】すなわち、本発明は、ブロムフェナクナト
リウム及び血管収縮薬を含有することを特徴とする眼科
用医薬組成物である。[0009] That is, the present invention is an ophthalmic pharmaceutical composition containing bromfenac sodium and a vasoconstrictor.
【００１０】本発明におけるブロムフェナクナトリウム
は非ステロイド性抗炎症薬として知られ、これは塩また
は水和物であってもよい。[0010] Bromfenac sodium in the present invention is known as a nonsteroidal anti-inflammatory drug, which may be a salt or a hydrate.
【００１１】本発明の血管収縮薬としては、テトラヒド
ロゾリン、ナファゾリン、フェニレフリン、エフェドリ
ン、メチルエフェドリン、エピネフリンが好ましく、こ
れらは塩であってもよい。塩としては、塩酸塩、硝酸塩
等を挙げることができる。また、これら血管収縮薬は、
いずれか１種だけでなく、２種以上を組み合わせて配合
することもできる。The vasoconstrictor of the present invention is preferably tetrahydrozoline, naphazoline, phenylephrine, ephedrine, methylephedrine or epinephrine, and these may be salts. Examples of the salt include hydrochloride and nitrate. Also, these vasoconstrictors
Not only one kind but also two or more kinds can be combined and compounded.
【００１２】本発明の眼科用医薬組成物におけるブロム
フェナクナトリウム及び血管収縮薬の配合量は次のよう
になる。ブロムフェナクナトリウムでは、１日当たり
０．１〜０．５ｍｇ、１回当たり０．０２〜０．１５ｍ
ｇになるように配合する。１回当たり０．０２ｍｇ未満
では充分な効果が得られず、１回当たり０．１５ｍｇを
超えると眼粘膜に対する刺激を生じることがあるからで
ある。血管収縮薬では、１日当たり０．００４〜４ｍ
ｇ、１回当たり０．００１〜１．５ｍｇになるように配
合する。１回当たり０．００１ｍｇ未満では充分な充血
除去効果が得られず、１．５ｍｇを超えると耐性を生じ
ることがあり、好ましくないからである。The amounts of bromfenac sodium and vasoconstrictor in the ophthalmic pharmaceutical composition of the present invention are as follows. In bromfenac sodium, 0.1 to 0.5 mg per day, 0.02 to 0.15 m per time
g. If the dose is less than 0.02 mg at a time, a sufficient effect cannot be obtained. If the dose exceeds 0.15 mg at a time, irritation to the ocular mucosa may occur. For vasoconstrictors, 0.004-4m per day
g, blended in an amount of 0.001 to 1.5 mg each time. If the amount is less than 0.001 mg per time, a sufficient decongestion-removing effect cannot be obtained, and if it exceeds 1.5 mg, resistance may be generated, which is not preferable.
【００１３】[0013]
【発明の実施の形態】本発明における眼科用医薬組成物
には、上記成分に加え、必要により他の成分を適宜に配
合することができる。BEST MODE FOR CARRYING OUT THE INVENTION In the ophthalmic pharmaceutical composition of the present invention, in addition to the above components, other components can be appropriately compounded as required.
【００１４】本発明の眼科用医薬組成物は、常法により
調製することができる。例えば、ブロムフェナクナトリ
ウム及び血管収縮薬を添加剤等とともに滅菌精製水に溶
解させることにより調製することができる。製剤の調製
に使用できる添加剤としては、界面活性剤、溶解補助
剤、緩衝剤等、保存剤、香料・清涼化剤（メントール、
カンフル等）、色素、防腐剤等が挙げられる。[0014] The ophthalmic pharmaceutical composition of the present invention can be prepared by a conventional method. For example, it can be prepared by dissolving bromfenac sodium and a vasoconstrictor together with additives and the like in sterile purified water. Additives that can be used in the preparation of formulations include surfactants, solubilizers, buffers, preservatives, fragrances / fresheners (menthol,
Camphor etc.), coloring matter, preservatives and the like.
【００１５】本発明の眼科用医薬組成物は、点眼剤とし
て適量を眼に滴下したり、軟膏剤として適量を塗布する
ことにより投与することができる。The ophthalmic pharmaceutical composition of the present invention can be administered by dropping an appropriate amount of eye drops as an eye drop or applying an appropriate amount of an ointment.
【００１６】[0016]
【実施例】以下に、実施例及び試験例を挙げて本発明を
更に詳細に説明するが、本発明はこれらに限定されるも
のではない。The present invention will be described in more detail with reference to the following examples and test examples, but the present invention is not limited to these examples.
【００１７】 （実施例１） ブロムフェナクナトリウム水和物 ５０ｍｇ 塩酸ナファゾリン ２ｍｇ 塩酸ジフェンヒドラミン ３０ｍｇ 上記の各成分を秤量し、精製水に溶解させ、全量を１０
０ｍＬにした。これを１５ｍＬずつ容器に充填して点眼
薬を製した。Example 1 Bromfenac sodium hydrate 50 mg Naphazoline hydrochloride 2 mg Diphenhydramine hydrochloride 30 mg The above components were weighed and dissolved in purified water, and the total amount was 10%.
Brought to 0 mL. This was filled into a container by 15 mL each to prepare an eye drop.
【００１８】 （実施例２） ブロムフェナクナトリウム水和物 １００ｍｇ ＤＬ−塩酸メチルエフェドリン ７５ｍｇ 塩酸ジフェンヒドラミン ５０ｍｇ シアノコバラミン ２０ｍｇ 上記の各成分を秤量し、精製水に溶解させ、全量を１０
０ｍＬにした。これを１５ｍＬずつ容器に充填して点眼
薬を製した。(Example 2) Bromfenac sodium hydrate 100 mg DL-methylephedrine hydrochloride 75 mg Diphenhydramine hydrochloride 50 mg Cyanocobalamin 20 mg The above components were weighed and dissolved in purified water, and the total amount was 10%.
Brought to 0 mL. This was filled into a container by 15 mL each to prepare an eye drop.
【００１９】 （実施例３） ブロムフェナクナトリウム水和物 １００ｍｇ 塩酸テトラヒドロゾリン ５０ｍｇ マレイン酸クロルフェニラミン ３０ｍｇ Ｌ−アスパラギン酸カリウム １ｇ 上記の各成分を秤量し、精製水に溶解させ、全量を１０
０ｍＬにした。これを１５ｍＬずつ容器に充填して点眼
薬を製した。Example 3 Bromfenac sodium hydrate 100 mg Tetrahydrozoline hydrochloride 50 mg Chlorpheniramine maleate 30 mg L-potassium aspartate 1 g The above components were weighed and dissolved in purified water, and the total amount was 10%.
Brought to 0 mL. This was filled into a container by 15 mL each to prepare an eye drop.
【００２０】 （実施例４） ブロムフェナクナトリウム水和物 １００ｍｇ 塩酸エピネフリン ３ｍｇ マレイン酸クロルフェニラミン ３００ｍｇ コンドロイチン硫酸ナトリウム ５００ｍｇ 塩酸ピリドキシン ５０ｍｇ 上記の各成分を秤量し、精製水に溶解させ、全量を１０
０ｍＬにした。これを１５ｍＬずつ容器に充填して点眼
薬を製した。Example 4 Bromfenac Sodium Hydrate 100 mg Epinephrine Hydrochloride 3 mg Chlorpheniramine Maleate 300 mg Chondroitin Sulfate 500 mg Pyridoxine Hydrochloride 50 mg
Brought to 0 mL. This was filled into a container by 15 mL each to prepare an eye drop.
【００２１】 （実施例５） スルファメトキサゾール ３ｇ ブロムフェナクナトリウム水和物 １００ｍｇ 塩酸フェニレフリン １００ｍｇ フマル酸ケトチフェン ２５ｍｇ フラビンアデニンジヌクレオチドナトリウム ５０ｍｇ アミノエチルスルホン酸 １ｇ 上記の各成分を秤量し、精製水に溶解させ、全量を１０
０ｍＬにした。これを１５ｍＬずつ容器に充填して点眼
薬を製した。Example 5 Sulfamethoxazole 3 g Bromfenac sodium hydrate 100 mg Phenylephrine hydrochloride 100 mg Ketotifen fumarate 25 mg Flavin adenine dinucleotide sodium 50 mg Aminoethylsulfonic acid 1 g The above components were weighed, and purified water was purified. And the total amount is 10
Brought to 0 mL. This was filled into a container by 15 mL each to prepare an eye drop.
【００２２】 （実施例６） ブロムフェナクナトリウム水和物 １００ｍｇ 塩酸ナファゾリン ３ｍｇ メチル硫酸ネオスチグミン ３ｍｇ 塩酸ジフェンヒドラミン ５０ｍｇ コンドロイチン硫酸ナトリウム ３００ｍｇ 酢酸トコフェロール ５０ｍｇ Ｌ−メントール １０ｍｇ プロピレングリコール ５００ｍｇ パラオキシ安息香酸メチル ３０ｍｇ 上記の各成分を秤量し均一に混合した後、軟膏基剤（プ
ラスベチベース）に分散・懸濁させて全量を１００ｇと
した。これを容器に充填し、眼軟膏を製した。Example 6 Bromfenac sodium hydrate 100 mg Naphazoline hydrochloride 3 mg Neostigmine methyl sulfate 3 mg Diphenhydramine hydrochloride 50 mg Chondroitin sulfate 300 mg Tocopherol acetate 50 mg L-menthol 10 mg Propylene glycol 500 mg Methyl paraoxybenzoate 30 mg Each of the above components After weighing and mixing uniformly, the mixture was dispersed and suspended in an ointment base (plus betty base) to make the total amount 100 g. This was filled in a container to produce an eye ointment.
【００２３】（試験例） ［配合製剤のウサギ眼粘膜充
血反応に対する緩解作用］ １２週齢の日本白色雄性兎を各群３匹用い、予め３．０
％カプサイシン液を２滴点眼して眼粘膜の充血症状を惹
起させた。これに表１記載の処方（１００ｍＬ中）に従
い、それぞれ２滴の薬剤を点眼し、点眼後１時間経過後
における充血除去効果を比較した。評価は下記の３段階
の基準を指標にして目視にて行った。結果を表２に示
す。 評価基準 真っ赤に充血している ＋＋ 充血している ＋ ほとんど充血していない ±(Test Example) [Relieving Effect of Combination Preparation on Rabbit Eye Mucosal Hyperemia] Three 12-week-old Japanese white male rabbits were used in each group, and 3.0 in advance.
Two drops of% capsaicin solution were instilled to induce hyperemia of the ocular mucosa. In accordance with the formulation (in 100 mL) shown in Table 1, 2 drops of each drug were instilled, and the decongestant effect 1 hour after the instillation was compared. The evaluation was visually performed using the following three-step criteria as indices. Table 2 shows the results. Evaluation criteria Reddish red ++ Reddish + Almost reddish ±
【００２４】[0024]
【表１】 [Table 1]
【表２】 [Table 2]
【００２５】表２から、眼粘膜充血反応に対する緩解作
用は、Ａ、Ｂ群が他の対照群より著しく優っており、本
発明にかかる点眼薬が、ブロムフェナクナトリウム水和
物及び血管収縮薬を単独で使用した場合と比較して、眼
粘膜充血症状の軽減・除去作用において顕著な作用を奏
することがわかる。From Table 2, it can be seen that the remission effect on ocular mucosal hyperemia was markedly superior in the groups A and B than in the other control groups, and the eye drops according to the present invention were treated with bromfenac sodium hydrate and It can be seen that as compared with the case of using alone, a remarkable action is exhibited in the action of reducing and eliminating ocular mucosal hyperemia.
【００２６】[0026]
【発明の効果】本発明により、眼粘膜の充血症状の軽減
・除去に有効な眼科用医薬組成物及び該組成物よりなる
点眼剤等を提供することが可能となった。Industrial Applicability According to the present invention, it has become possible to provide an ophthalmic pharmaceutical composition effective for reducing and eliminating hyperemia of the ocular mucosa and an ophthalmic solution comprising the composition.
───────────────────────────────────────────────────── フロントページの続き (72)発明者 中神 浄二 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 (72)発明者 相川 勝義 東京都豊島区高田３丁目24番１号 大正製 薬株式会社内 Ｆターム(参考） 4C076 AA06 AA12 BB24 CC10 DD37 DD38 DD45 DD49 DD51 DD59 EE37 4C084 AA19 MA02 MA58 NA05 ZA33 ZC75 4C206 AA01 AA02 FA31 KA01 MA01 MA02 MA03 MA04 MA05 MA37 MA48 MA78 NA05 ZA33 ──────────────────────────────────────────────────続 き Continuing on the front page (72) Inventor Joji Nakagami 3- 24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (72) Inventor Katsuyoshi Aikawa 3- 24-1, Takada, Toshima-ku, Tokyo No. Taisho Seiyaku Co., Ltd. F-term (reference) 4C076 AA06 AA12 BB24 CC10 DD37 DD38 DD45 DD49 DD51 DD59 EE37 4C084 AA19 MA02 MA58 NA05 ZA33 ZC75 4C206 AA01 AA02 FA31 KA01 MA01 MA02 MA03 MA04 MA05 MA37 MA48 MA78 NA05 ZA33
Claims (4)
薬を含有することを特徴とする眼科用医薬組成物。1. An ophthalmic pharmaceutical composition comprising bromfenac sodium and a vasoconstrictor.
ァゾリン、フェニレフリン、エフェドリン、メチルエフ
ェドリン、エピネフリン及びこれらの塩からなる群より
選ばれる１種または２種以上である請求項１記載の眼科
用医薬組成物。2. The ophthalmic pharmaceutical composition according to claim 1, wherein the vasoconstrictor is one or more selected from the group consisting of tetrahydrozoline, naphazoline, phenylephrine, ephedrine, methylephedrine, epinephrine and salts thereof.
載の眼科用医薬組成物。3. The ophthalmic pharmaceutical composition according to claim 1, which is an eye drop or an ointment.
薬を含有することを特徴とする眼科用医薬組成物を用い
た眼粘膜充血症状の治療方法。4. A method for treating ocular mucosal hyperemia using an ophthalmic pharmaceutical composition comprising bromfenac sodium and a vasoconstrictor.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001298850A JP2002308764A (en) | 2001-02-09 | 2001-09-28 | Pharmaceutical composition for ophthalmic use |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2001-33009 | 2001-02-09 | ||
| JP2001033009 | 2001-02-09 | ||
| JP2001298850A JP2002308764A (en) | 2001-02-09 | 2001-09-28 | Pharmaceutical composition for ophthalmic use |
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| Publication Number | Publication Date |
|---|---|
| JP2002308764A true JP2002308764A (en) | 2002-10-23 |
Family
ID=26609166
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001298850A Withdrawn JP2002308764A (en) | 2001-02-09 | 2001-09-28 | Pharmaceutical composition for ophthalmic use |
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| JP2006528703A (en) * | 2003-05-20 | 2006-12-21 | アラーガン、インコーポレイテッド | Methods and compositions for treating ocular disorders |
| JP2010502564A (en) * | 2006-08-28 | 2010-01-28 | 千寿製薬株式会社 | Ophthalmic transdermal preparation |
| US20120115957A1 (en) * | 2003-01-21 | 2012-05-10 | Shirou Sawa | Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid |
| JP2012224628A (en) * | 2011-04-08 | 2012-11-15 | Rohto Pharmaceutical Co Ltd | Bromfenac-containing composition |
| WO2013147000A1 (en) * | 2012-03-28 | 2013-10-03 | 参天製薬株式会社 | Aqueous composition containing 2-amino-3-(4-bromobenzoyl)- phenylacetic acid |
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| JP2016117737A (en) * | 2009-10-15 | 2016-06-30 | ジョンソン、マッセイ、パブリック、リミテッド、カンパニーＪｏｈｎｓｏｎ Ｍａｔｔｈｅｙ Ｐｕｂｌｉｃ Ｌｉｍｉｔｅｄ Ｃｏｍｐａｎｙ | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
-
2001
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| JP2006528703A (en) * | 2003-05-20 | 2006-12-21 | アラーガン、インコーポレイテッド | Methods and compositions for treating ocular disorders |
| JP2010502564A (en) * | 2006-08-28 | 2010-01-28 | 千寿製薬株式会社 | Ophthalmic transdermal preparation |
| JP2016117737A (en) * | 2009-10-15 | 2016-06-30 | ジョンソン、マッセイ、パブリック、リミテッド、カンパニーＪｏｈｎｓｏｎ Ｍａｔｔｈｅｙ Ｐｕｂｌｉｃ Ｌｉｍｉｔｅｄ Ｃｏｍｐａｎｙ | Polymorphs of bromfenac sodium and methods for preparing bromfenac sodium polymorphs |
| JP2012224628A (en) * | 2011-04-08 | 2012-11-15 | Rohto Pharmaceutical Co Ltd | Bromfenac-containing composition |
| JP2014521606A (en) * | 2011-07-22 | 2014-08-28 | インサイト・ビジョン・インコーポレイテッド | Compositions and methods for the treatment of ocular surface allergies |
| WO2013147000A1 (en) * | 2012-03-28 | 2013-10-03 | 参天製薬株式会社 | Aqueous composition containing 2-amino-3-(4-bromobenzoyl)- phenylacetic acid |
| JP2014088379A (en) * | 2012-10-05 | 2014-05-15 | Rohto Pharmaceut Co Ltd | Composition comprising bromfenac |
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