JPS63198620A - Ibuprofen preparation - Google Patents
Ibuprofen preparationInfo
- Publication number
- JPS63198620A JPS63198620A JP3079887A JP3079887A JPS63198620A JP S63198620 A JPS63198620 A JP S63198620A JP 3079887 A JP3079887 A JP 3079887A JP 3079887 A JP3079887 A JP 3079887A JP S63198620 A JPS63198620 A JP S63198620A
- Authority
- JP
- Japan
- Prior art keywords
- ibuprofen
- antacid
- coating agent
- mucosa
- antipyretic
- 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
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 title claims abstract description 48
- 229960001680 ibuprofen Drugs 0.000 title claims abstract description 48
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims abstract description 11
- 229940069428 antacid Drugs 0.000 claims abstract description 11
- 239000003159 antacid agent Substances 0.000 claims abstract description 11
- 239000011248 coating agent Substances 0.000 claims abstract description 11
- 230000001458 anti-acid effect Effects 0.000 claims abstract description 9
- 239000002221 antipyretic Substances 0.000 abstract description 7
- 239000004480 active ingredient Substances 0.000 abstract description 6
- BWZOPYPOZJBVLQ-UHFFFAOYSA-K aluminium glycinate Chemical compound O[Al+]O.NCC([O-])=O BWZOPYPOZJBVLQ-UHFFFAOYSA-K 0.000 abstract description 6
- 230000001754 anti-pyretic effect Effects 0.000 abstract description 6
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 abstract description 4
- 238000000975 co-precipitation Methods 0.000 abstract description 3
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 abstract description 3
- 239000000347 magnesium hydroxide Substances 0.000 abstract description 3
- 229910001862 magnesium hydroxide Inorganic materials 0.000 abstract description 3
- 230000007721 medicinal effect Effects 0.000 abstract description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 abstract description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 abstract description 2
- 210000004877 mucosa Anatomy 0.000 abstract 4
- 230000000202 analgesic effect Effects 0.000 abstract 2
- WRCICOQZCXGSSW-UHFFFAOYSA-M C([Al](O)C)(=O)O Chemical compound C([Al](O)C)(=O)O WRCICOQZCXGSSW-UHFFFAOYSA-M 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 231100000957 no side effect Toxicity 0.000 abstract 1
- OTYBMLCTZGSZBG-UHFFFAOYSA-L potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 abstract 1
- 229910052939 potassium sulfate Inorganic materials 0.000 abstract 1
- 235000011151 potassium sulphates Nutrition 0.000 abstract 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 8
- 239000001095 magnesium carbonate Substances 0.000 description 8
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 8
- 208000018522 Gastrointestinal disease Diseases 0.000 description 6
- 238000007796 conventional method Methods 0.000 description 6
- 229920002261 Corn starch Polymers 0.000 description 5
- 239000008120 corn starch Substances 0.000 description 5
- 230000000694 effects Effects 0.000 description 5
- 230000002496 gastric effect Effects 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- 208000025865 Ulcer Diseases 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 239000008187 granular material Substances 0.000 description 4
- 239000000395 magnesium oxide Substances 0.000 description 4
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 4
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 4
- 241000700159 Rattus Species 0.000 description 3
- WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 3
- 229940024545 aluminum hydroxide Drugs 0.000 description 3
- 239000000730 antalgic agent Substances 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- 239000007903 gelatin capsule Substances 0.000 description 3
- 239000007902 hard capsule Substances 0.000 description 3
- 239000004615 ingredient Substances 0.000 description 3
- 231100000397 ulcer Toxicity 0.000 description 3
- 244000215068 Acacia senegal Species 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 229920000084 Gum arabic Polymers 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
- 239000000205 acacia gum Substances 0.000 description 2
- 235000010489 acacia gum Nutrition 0.000 description 2
- 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 2
- 239000002253 acid Substances 0.000 description 2
- WMGSQTMJHBYJMQ-UHFFFAOYSA-N aluminum;magnesium;silicate Chemical compound [Mg+2].[Al+3].[O-][Si]([O-])([O-])[O-] WMGSQTMJHBYJMQ-UHFFFAOYSA-N 0.000 description 2
- 229940035676 analgesics Drugs 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- PGZIKUPSQINGKT-UHFFFAOYSA-N dialuminum;dioxido(oxo)silane Chemical compound [Al+3].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O PGZIKUPSQINGKT-UHFFFAOYSA-N 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 229910052749 magnesium Inorganic materials 0.000 description 2
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 description 2
- 239000000391 magnesium silicate Substances 0.000 description 2
- 229910052919 magnesium silicate Inorganic materials 0.000 description 2
- 235000019792 magnesium silicate Nutrition 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229920002545 silicone oil Polymers 0.000 description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
- 239000007901 soft capsule Substances 0.000 description 2
- 206010000087 Abdominal pain upper Diseases 0.000 description 1
- -1 Fatty acid ester Chemical class 0.000 description 1
- 208000012895 Gastric disease Diseases 0.000 description 1
- 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 1
- 241001465754 Metazoa Species 0.000 description 1
- 206010053156 Musculoskeletal discomfort Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- BPQQTUXANYXVAA-UHFFFAOYSA-N Orthosilicate Chemical compound [O-][Si]([O-])([O-])[O-] BPQQTUXANYXVAA-UHFFFAOYSA-N 0.000 description 1
- 235000019485 Safflower oil Nutrition 0.000 description 1
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- DIZPMCHEQGEION-UHFFFAOYSA-H aluminium sulfate (anhydrous) Chemical compound [Al+3].[Al+3].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O DIZPMCHEQGEION-UHFFFAOYSA-H 0.000 description 1
- 229940008027 aluminum hydroxide / magnesium carbonate Drugs 0.000 description 1
- 229940024546 aluminum hydroxide gel Drugs 0.000 description 1
- SMYKVLBUSSNXMV-UHFFFAOYSA-K aluminum;trihydroxide;hydrate Chemical compound O.[OH-].[OH-].[OH-].[Al+3] SMYKVLBUSSNXMV-UHFFFAOYSA-K 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 125000002490 anilino group Chemical class [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 230000003217 anti-cancerogenic effect Effects 0.000 description 1
- 229940125716 antipyretic agent Drugs 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- SKKNACBBJGLYJD-UHFFFAOYSA-N bismuth magnesium Chemical compound [Mg].[Bi] SKKNACBBJGLYJD-UHFFFAOYSA-N 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- MKJXYGKVIBWPFZ-UHFFFAOYSA-L calcium lactate Chemical compound [Ca+2].CC(O)C([O-])=O.CC(O)C([O-])=O MKJXYGKVIBWPFZ-UHFFFAOYSA-L 0.000 description 1
- 239000001527 calcium lactate Substances 0.000 description 1
- 229960002401 calcium lactate Drugs 0.000 description 1
- 235000011086 calcium lactate Nutrition 0.000 description 1
- GDVKFRBCXAPAQJ-UHFFFAOYSA-A dialuminum;hexamagnesium;carbonate;hexadecahydroxide Chemical compound [OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-]C([O-])=O GDVKFRBCXAPAQJ-UHFFFAOYSA-A 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 229940015826 dihydroxyaluminum aminoacetate Drugs 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000004503 fine granule Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229960001545 hydrotalcite Drugs 0.000 description 1
- 229910001701 hydrotalcite Inorganic materials 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- TWNQGVIAIRXVLR-UHFFFAOYSA-N oxo(oxoalumanyloxy)alumane Chemical compound O=[Al]O[Al]=O TWNQGVIAIRXVLR-UHFFFAOYSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 229960005489 paracetamol Drugs 0.000 description 1
- GRLPQNLYRHEGIJ-UHFFFAOYSA-J potassium aluminium sulfate Chemical compound [Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRLPQNLYRHEGIJ-UHFFFAOYSA-J 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 235000005713 safflower oil Nutrition 0.000 description 1
- 239000003813 safflower oil Substances 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- VXYADVIJALMOEQ-UHFFFAOYSA-K tris(lactato)aluminium Chemical compound CC(O)C(=O)O[Al](OC(=O)C(C)O)OC(=O)C(C)O VXYADVIJALMOEQ-UHFFFAOYSA-K 0.000 description 1
- 230000036269 ulceration Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は、イブプロフェンの投与による消化管障害が生
じることが可及的に防止されたイブプロフェン製剤に関
する。DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to an ibuprofen preparation in which gastrointestinal disorders caused by administration of ibuprofen are prevented as much as possible.
来の び ■が ゛ しようとする］北４区イブプ
ロフェンは、解熱鎮痛剤等として効果の高いことが従来
より知られているが、イブプロフェンを経口投与した場
合、背部不快感、胃痛、嘔気などが生じることがあり、
副作用として消化管障害を起こさせることが指摘されて
いる。Ibuprofen has long been known to be highly effective as an antipyretic analgesic, etc., but when ibuprofen is administered orally, it causes back discomfort, stomach pain, nausea, etc. may occur,
It has been pointed out that it causes gastrointestinal disorders as a side effect.
このために従来、イブプロフェンの経口投与による胃腸
障害を軽減させることを目的としてイブプロフェンをア
ニリン誘導体系解熱剤と併用したり（特開昭５６−９７
２２４号、恒７５６（５４４１６号公報）、アセトアミ
ノフェンと併用したり（特開昭５９−１０４３１５号公
＋ｉＩ） 、サリチル酸系薬物と併用したり（特開昭６
１−１３４３１５号公報）することが提案されている。For this reason, conventionally, ibuprofen was used in combination with an aniline derivative antipyretic agent for the purpose of alleviating gastrointestinal disorders caused by oral administration of ibuprofen (Japanese Patent Laid-Open No. 56-97
No. 224, Kou 756 (No. 54416), combined use with acetaminophen (JP-A-59-104315+iI), and salicylic acid drugs (JP-A No. 6-198).
1-134315).
しかしながら、これらは２種の解熱鎮痛剤を併用するも
のであり、有効成分としてイブプロフェンのみを用いた
場合にもその副作用を軽減させることが望まれる。However, these drugs use two types of antipyretic analgesics in combination, and it is desirable to reduce the side effects even when only ibuprofen is used as the active ingredient.
更に、イブプロフェンのみを用いる場合の胃障害軽減法
としては、固体脂肪と混合溶融し、得られた液を噴霧凝
固する方法（特開昭５７−１４５８０７号公報）がある
が、操作性に鷺があり、がつ表面が油性となるため、内
服した場合の有効性を低下させることが予想され、問題
がある。Furthermore, as a method for alleviating gastric disorders when only ibuprofen is used, there is a method in which it is mixed with solid fat and melted, and the resulting liquid is sprayed and solidified (Japanese Unexamined Patent Publication No. 145807/1983), but it is not easy to use. However, since the surface of the drug is oily, it is expected to reduce its effectiveness when taken internally, which is problematic.
本発明は上記事情に鑑みなされたもので、イブプロフェ
ンを投与した場合に生じる副作用、特に消化管障害が軽
減されたイブプロフェン製剤を提供することを目的とす
る。The present invention was made in view of the above circumstances, and an object of the present invention is to provide an ibuprofen preparation that reduces side effects, particularly gastrointestinal disorders, that occur when ibuprofen is administered.
ｒ□直 古を ゛するための− び。r □ - for straightening old things.
本発明者らは上記目的を達成するため鋭意検討を進めた
結果、炭酸マグネシウム、アルミニウムグリシネート等
の制酸剤や粘膜被膜剤をイブプロフェンと併用すると、
イブプロフェンの有する解熱鎮癌作用等の薬効を阻害す
ることなく、胃粘膜障′８を著しく改善し、消化管障害
を軽減することができ、このためイブプロフェンを有効
成分とする安全性の高い製剤が得られることを知見し１
本発明をなすに至った。The present inventors conducted intensive studies to achieve the above object, and found that when antacids and mucosal coating agents such as magnesium carbonate and aluminum glycinate are used in combination with ibuprofen,
It is possible to significantly improve gastric mucosal disorders'8 and alleviate gastrointestinal disorders without interfering with ibuprofen's medicinal effects such as its antipyretic and anticarcinogenic effects.Therefore, highly safe preparations containing ibuprofen as an active ingredient have been developed. Knowing what you can get 1
The present invention has been accomplished.
従って、本発明はイブプロフェンに制酸剤及び／又は粘
膜被膜剤を併用したイブプロフェン製剤を提供するもの
である。Therefore, the present invention provides an ibuprofen preparation containing ibuprofen in combination with an antacid and/or a mucosal coating agent.
以下、本発明につき更に詳しく説明する。The present invention will be explained in more detail below.
本発明に係るイブプロフェン製剤は、上述したようにイ
ブプロフェンに制酸剤及び／又は粘膜被膜剤を併用する
ものであるが、制酸剤や粘膜被膜剤としては、アルミニ
ウムグリシネート（ジヒドロキシアルミニウムアミノア
セテート）、炭酸水素ナトリウム、水酸化マグネシウム
、水酸化アルミナマグネシウム、炭酸マグネシウム、乳
酸アルミニウム、ケイ酸マグネシウム、ケイ酸アルミン
酸二マグネシウム、ケイ酸アルミン酸マグネシウムビス
マス、メタケイ酸アルミン酸マグネシウム。As mentioned above, the ibuprofen preparation according to the present invention uses ibuprofen in combination with an antacid and/or a mucosal coating agent, and the antacid and mucosal coating agent include aluminum glycinate (dihydroxyaluminum aminoacetate). , sodium bicarbonate, magnesium hydroxide, magnesium alumina hydroxide, magnesium carbonate, aluminum lactate, magnesium silicate, dimagnesium aluminate silicate, bismuth magnesium aluminate silicate, magnesium aluminate metasilicate.
乾燥水酸化アルミニラ１１ゲル、合成ケイ酸アルミニウ
ム、ショ糖硫酸エステルアルミニウム塩（アルサルミン
）、合成ヒドロタルサイト、酸化マグネシウム、ロート
エキス、乳酸カルシウム、アミノ酸酸、水酸化アルミニ
ウム・炭酸マグネシウム混合乾燥ゲル、水酸化アルミニ
ウム・炭酸水素ナトリウムの共沈生成物、水酸化アルミ
ニウム・炭酸カルシウム・炭酸マグネシウムの共沈生成
物。Dried aluminum hydroxide 11 gel, synthetic aluminum silicate, sucrose sulfate aluminum salt (arsalmin), synthetic hydrotalcite, magnesium oxide, funnel extract, calcium lactate, amino acid acid, aluminum hydroxide/magnesium carbonate mixed dry gel, water A coprecipitation product of aluminum oxide and sodium hydrogen carbonate, a coprecipitation product of aluminum hydroxide, calcium carbonate, and magnesium carbonate.
水酸化マグネシウム・硫酸アルミニウムカリウ１１の共
沈生成物などが挙げられる。本発明においてはこれらの
１種をイブプロフェンと併用するようにしてもよく、２
種以」―をイブプロフェンと併用するようにしてもよい
。Co-precipitated products of magnesium hydroxide and potassium aluminum sulfate 11 can be mentioned. In the present invention, one of these may be used in combination with ibuprofen, and two
It is also possible to use ibuprofen in combination with ibuprofen.
これらの制酸剤や粘膜被膜剤の配合量は特に制限されな
いが、イブプロフェン１００重量部に対し５〜５００重
量部の割合で使用することが好ましい。The amount of these antacids and mucosal membrane coating agents is not particularly limited, but it is preferable to use them in a proportion of 5 to 500 parts by weight per 100 parts by weight of ibuprofen.
本発明のイブプロフェン製剤において、イブプロフェン
の投与量は常用量（成人の場合１日６００ｍｇ程度）と
することができるが、この場合有効成分としてはイブプ
ロフェンを単独で使用してもよく、他の解熱鎮痛剤、そ
の他の有効成分と併用することもできる。ここで、他の
解熱鎮痛剤や有効成分を併用する場合は必要によりイブ
プロフェンの投与量を少なくすることができる。In the ibuprofen preparation of the present invention, the dose of ibuprofen can be the usual dose (about 600 mg per day for adults), but in this case, ibuprofen may be used alone as the active ingredient, or other antipyretic and analgesic agents can be used. It can also be used in combination with agents and other active ingredients. Here, if other antipyretic analgesics or active ingredients are used together, the dose of ibuprofen can be reduced if necessary.
本発明のイブプロフェン製剤は１種々の形態、例えば錠
剤、顆粒剤、細粒剤、散剤、硬カプセル剤、軟カプセル
剤等として調製することができ、その形態に応じた通常
の用法に従って投与することができる。この場合、これ
らの製剤は常法に従って調製し得、この際上述した成分
に加えてその製剤に応じた通常の配合成分を配合して製
剤化することができる。The ibuprofen preparation of the present invention can be prepared in various forms, such as tablets, granules, fine granules, powders, hard capsules, soft capsules, etc., and can be administered according to the usual usage method depending on the form. Can be done. In this case, these preparations can be prepared according to conventional methods, and in addition to the above-mentioned ingredients, conventional ingredients depending on the preparation can be added to form the preparation.
３泄■す弧米
本発明のイブプロフェン製剤は、イブプロフェンに対し
制酸剤及び／又は粘膜被膜剤を併用したことにより、イ
ブプロフェンの副作用、特に消化管障害が軽減され、使
用上の安全性が高いものである。The ibuprofen preparation of the present invention uses ibuprofen in combination with an antacid and/or a mucosal coating agent, thereby reducing ibuprofen's side effects, particularly gastrointestinal disorders, and is highly safe in use. It is something.
次に実験例を示し、本発明の効果を具体的に示す。Next, experimental examples will be shown to concretely demonstrate the effects of the present invention.
シャーン（Ｊ ａｈｎ）らの方法によりラットの胃粘膜
障害を試験した。Gastric mucosal damage in rats was tested by the method of Jahn et al.
即ち、体重１３０ｇ前後の雄性ラッ１〜を１８時間絶食
させた後、１群７〜８匹を使用し、第１表に示す薬物を
１０％アラビアゴム水溶液に懸濁したものを投与した。Specifically, male rats weighing around 130 g were fasted for 18 hours, and then the drugs shown in Table 1 suspended in a 10% aqueous solution of gum arabic were administered to each group of 7 to 8 rats.
３．５時間後に動物を殺して胃を摘出し、火消に沿って
縦切し、肉１′＠的に胃粘膜障害の有無並びに程度を判
定した。この場合、潰瘍の程度はアダミ（Ａｄａｍｊ、
）らの方法（Ａｒｃｈ、ｉｎｔ。After 3.5 hours, the animals were sacrificed, the stomachs were removed, cut vertically along the fire line, and the presence and extent of gastric mucosal damage was determined visually. In this case, the degree of ulceration is determined by Adamj.
) et al.'s method (Arch, int.
Ｐｈａｒｍａｃｏｄｙｎ、１４７ 、１１３（１９６４
））により潰瘍係数（ｕｌｃｅｒ １ｎｄｅｘ）として
表わした。Pharmacodyn, 147, 113 (1964
)) was expressed as an ulcer index (ulcer index).
結果を第１表に示す。The results are shown in Table 1.
第 １ 表
第１表の結果に見られる通り、イブプロフェンＨｏｏｍ
ｇ／ｋｇ）の経口投与により潰瘍係数３．２程度の胃粘
膜障害が認められるが、炭酸マグネシウム又はこれとア
ルミニウムグリシネートを併用投与することによって胃
粘膜障害が著しく改善されることが認められた。Table 1 As seen in the results in Table 1, ibuprofen Hoom
Although gastric mucosal damage with an ulcer index of approximately 3.2 was observed with oral administration of 100 g/kg), it was observed that gastric mucosal damage was significantly improved by administering magnesium carbonate or a combination of magnesium carbonate and aluminum glycinate. .
以下、実施例（製剤例）を示し、本発明を具体的に示す
が、本発明は下記の例に制限されるものではない。Examples (formulation examples) are shown below to specifically illustrate the present invention, but the present invention is not limited to the following examples.
〔実施例１〕 錠 剤
イブプロフェン ７５ ｍｇ／
１錠炭酸マグネシウム １００ア
ルミニウムグリシネート ５０トウモロコ
シデンプン ５０結晶セルロース
５０ステアリン酸マグネシウム
２上記酸分を常法により打錠する。[Example 1] Tablet ibuprofen 75 mg/
1 tablet Magnesium Carbonate 100 Aluminum Glycinate 50 Corn Starch 50 Crystalline Cellulose
50 Magnesium stearate 2 The above acid content is compressed into tablets by a conventional method.
〔実施例２〕 錠 剤
イブプロフェン ７５■／１錠
酸化マグネシウム １０合成とド
ロサイト ２゜トウモロコシデ
ンプン ５０カルボキシメチルセルロ
ースナトリウム ３０硬化油 ３
上記成分を常法により打錠する。[Example 2] Tablets of Ibuprofen 75 μ/1 tablet Magnesium oxide 10 Synthesis and dolosite 2° Corn starch 50 Sodium carboxymethylcellulose 30 Hydrogenated oil 3 The above ingredients are compressed into tablets by a conventional method.
〔実施例３〕 顆 粒 剤
イブプロフェン １５Ｑｒｎｇ／ｌ
包ケイ酸マグネシウＡｓ ２００カ
ルボキシメチルセルロースナ１−リウム ５０シ：ＩＮ
脂肪酸エステル １５ヒドロキシプロ
ピルセルロース ５〔実施例４〕 顆 粒
剤
イブプロフェン ２００ｆｆ１ｇ
／ｌ包炭酸マグネシウム １５０メ
タケイ酸アルミン酸マグネシウム １００結晶セルロ
ース ５０ヒドロキシプロピル
セルロース １０〔実施例Ｓ〕細粒剤
イブプロフェン １５０■／１包
酸化マグネシウム ６０炭酸マグ
ネシウム ６５アラビアゴム
５乳 糖
２０〔実施例６〕 散 剤
細粒酸化マグネシウム ５０■／１包
イブプロフエン １３０トウモロ
コシデンプン ２０〔実施例７〕 硬
カプセル剤
水酸化アルミニウ！、ゲル １００■／１カプセ
ルイブプロフェン ８０トウモロコシ
デンプン １０シリコーン油
２常法によりゼラチン硬カプセルに充填する。[Example 3] Ibuprofen granule 15Qrng/l
Magnesium encapsulated silicate As 200 Sodium carboxymethyl cellulose 50: IN
Fatty acid ester 15-hydroxypropylcellulose 5 [Example 4] Granules
Agent ibuprofen 200ff1g
/l pack magnesium carbonate 150 magnesium aluminate metasilicate 100 crystalline cellulose 50 hydroxypropyl cellulose 10 [Example S] fine granule ibuprofen 150 / pack magnesium oxide 60 magnesium carbonate 65 gum arabic
5 Lactose
20 [Example 6] Powder Fine Magnesium Oxide 50 ■/1 package Ibuprofen 130 Corn Starch 20 [Example 7] Hard Capsule Aluminum Hydroxide! , Gel 100 ■/1 Capsule Ibuprofen 80 Corn Starch 10 Silicone Oil
2. Fill into hard gelatin capsules using a conventional method.
〔実施例８〕 硬カプセル
イブプロフェン １００■／１カプセル
ケイ酸マグネシウム １００トウモロコシデ
ンプン １００シリコーン油
５常法によりゼラチン硬カプセルに充填する。[Example 8] Hard capsule ibuprofen 100 ■/1 capsule Magnesium silicate 100 Corn starch 100 Silicone oil
5. Fill into hard gelatin capsules using a conventional method.
〔実施例９〕 軟カプセル
イブプロフェン ７５ｍｇ／ｌカプセ
ル水酸化アルミニウムゲル １００Ｎ−アシルア
ミノ酸 ２サフラワー油
２００常法によりゼラチン軟カプセルに充填する。[Example 9] Soft capsule ibuprofen 75mg/l capsule aluminum hydroxide gel 100N-acyl amino acid 2 safflower oil
200 Filled into soft gelatin capsules by a conventional method.
Claims (1)
用したことを特徴とするイブプロフェン製剤。1. An ibuprofen preparation characterized by using ibuprofen in combination with an antacid and/or a mucosal coating agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3079887A JP2704721B2 (en) | 1987-02-12 | 1987-02-12 | Ibuprofen formulation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP3079887A JP2704721B2 (en) | 1987-02-12 | 1987-02-12 | Ibuprofen formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS63198620A true JPS63198620A (en) | 1988-08-17 |
| JP2704721B2 JP2704721B2 (en) | 1998-01-26 |
Family
ID=12313699
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3079887A Expired - Lifetime JP2704721B2 (en) | 1987-02-12 | 1987-02-12 | Ibuprofen formulation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2704721B2 (en) |
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05148139A (en) * | 1991-11-29 | 1993-06-15 | Lion Corp | Antipyretic analgesic agent containing ibuprofen |
| US5262179A (en) * | 1989-09-13 | 1993-11-16 | Nicholas Kiwi Pty Ltd. | Non-effervescent ibuprofen compositions |
| US5288507A (en) * | 1992-07-29 | 1994-02-22 | Merck & Co., Inc. | Ibuprofen antacid combinations |
| US5409709A (en) * | 1991-11-29 | 1995-04-25 | Lion Corporation | Antipyretic analgesic preparation containing ibuprofen |
| JP2005035995A (en) * | 2003-07-01 | 2005-02-10 | Sankyo Co Ltd | Ibuprofen-containing oral composition |
| JP2009242360A (en) * | 2008-03-31 | 2009-10-22 | Kobayashi Pharmaceut Co Ltd | Orally administrable chronic pain preventing or treating agent |
| JP2009242365A (en) * | 2008-03-31 | 2009-10-22 | Kobayashi Pharmaceut Co Ltd | Oral pharmaceutical composition |
| JP2014070024A (en) * | 2012-09-27 | 2014-04-21 | Kobayashi Pharmaceutical Co Ltd | Pharmaceutical composition containing phenylpropionic acid-based anti-inflammatory analgesic agent |
| JP2014098036A (en) * | 2004-07-13 | 2014-05-29 | Daiichi Sankyo Co Ltd | Loxoprofen-containing oral composition 4 |
| JP2014159406A (en) * | 2013-01-28 | 2014-09-04 | Taisho Pharmaceutical Co Ltd | Solid formulation |
| WO2018117249A1 (en) * | 2016-12-22 | 2018-06-28 | エスエス製薬株式会社 | Oral ibuprofen preparation |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5296968B2 (en) * | 2005-06-17 | 2013-09-25 | 第一三共ヘルスケア株式会社 | Oral pharmaceutical composition containing ibuprofen |
-
1987
- 1987-02-12 JP JP3079887A patent/JP2704721B2/en not_active Expired - Lifetime
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5262179A (en) * | 1989-09-13 | 1993-11-16 | Nicholas Kiwi Pty Ltd. | Non-effervescent ibuprofen compositions |
| JPH05148139A (en) * | 1991-11-29 | 1993-06-15 | Lion Corp | Antipyretic analgesic agent containing ibuprofen |
| US5409709A (en) * | 1991-11-29 | 1995-04-25 | Lion Corporation | Antipyretic analgesic preparation containing ibuprofen |
| US5288507A (en) * | 1992-07-29 | 1994-02-22 | Merck & Co., Inc. | Ibuprofen antacid combinations |
| JP2005035995A (en) * | 2003-07-01 | 2005-02-10 | Sankyo Co Ltd | Ibuprofen-containing oral composition |
| JP2014098036A (en) * | 2004-07-13 | 2014-05-29 | Daiichi Sankyo Co Ltd | Loxoprofen-containing oral composition 4 |
| JP2009242365A (en) * | 2008-03-31 | 2009-10-22 | Kobayashi Pharmaceut Co Ltd | Oral pharmaceutical composition |
| JP2009242360A (en) * | 2008-03-31 | 2009-10-22 | Kobayashi Pharmaceut Co Ltd | Orally administrable chronic pain preventing or treating agent |
| JP2014070024A (en) * | 2012-09-27 | 2014-04-21 | Kobayashi Pharmaceutical Co Ltd | Pharmaceutical composition containing phenylpropionic acid-based anti-inflammatory analgesic agent |
| JP2014159406A (en) * | 2013-01-28 | 2014-09-04 | Taisho Pharmaceutical Co Ltd | Solid formulation |
| WO2018117249A1 (en) * | 2016-12-22 | 2018-06-28 | エスエス製薬株式会社 | Oral ibuprofen preparation |
| JP2018104299A (en) * | 2016-12-22 | 2018-07-05 | エスエス製薬株式会社 | Oral ibuprofen preparation |
| AU2017384442B2 (en) * | 2016-12-22 | 2022-12-08 | SSP Co., Ltd. Japan | Oral ibuprofen preparation |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2704721B2 (en) | 1998-01-26 |
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| EXPY | Cancellation because of completion of term |