JP2015199704A - oral composition - Google Patents
oral composition Download PDFInfo
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- JP2015199704A JP2015199704A JP2015051755A JP2015051755A JP2015199704A JP 2015199704 A JP2015199704 A JP 2015199704A JP 2015051755 A JP2015051755 A JP 2015051755A JP 2015051755 A JP2015051755 A JP 2015051755A JP 2015199704 A JP2015199704 A JP 2015199704A
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- ibuprofen
- mass
- oral
- oral composition
- carbocysteine
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- 239000000203 mixture Substances 0.000 title claims abstract description 34
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims abstract description 43
- 229960001680 ibuprofen Drugs 0.000 claims abstract description 43
- GBFLZEXEOZUWRN-VKHMYHEASA-N S-carboxymethyl-L-cysteine Chemical compound OC(=O)[C@@H](N)CSCC(O)=O GBFLZEXEOZUWRN-VKHMYHEASA-N 0.000 claims abstract description 20
- 229960004399 carbocisteine Drugs 0.000 claims abstract description 20
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 19
- 239000003765 sweetening agent Substances 0.000 claims abstract description 19
- 108010011485 Aspartame Proteins 0.000 claims description 16
- 239000000605 aspartame Substances 0.000 claims description 16
- 235000010357 aspartame Nutrition 0.000 claims description 16
- 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 claims description 16
- 229960003438 aspartame Drugs 0.000 claims description 16
- 239000004376 Sucralose Substances 0.000 claims description 9
- 235000019408 sucralose Nutrition 0.000 claims description 9
- BAQAVOSOZGMPRM-QBMZZYIRSA-N sucralose Chemical group O[C@@H]1[C@@H](O)[C@@H](Cl)[C@@H](CO)O[C@@H]1O[C@@]1(CCl)[C@@H](O)[C@H](O)[C@@H](CCl)O1 BAQAVOSOZGMPRM-QBMZZYIRSA-N 0.000 claims description 9
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 claims description 8
- 239000000619 acesulfame-K Substances 0.000 claims description 8
- HELXLJCILKEWJH-NCGAPWICSA-N rebaudioside A Chemical compound O([C@H]1[C@H](O)[C@@H](CO)O[C@H]([C@@H]1O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)O[C@]12C(=C)C[C@@]3(C1)CC[C@@H]1[C@@](C)(CCC[C@]1([C@@H]3CC2)C)C(=O)O[C@H]1[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O1)O)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O HELXLJCILKEWJH-NCGAPWICSA-N 0.000 claims description 8
- FTLYMKDSHNWQKD-UHFFFAOYSA-N (2,4,5-trichlorophenyl)boronic acid Chemical compound OB(O)C1=CC(Cl)=C(Cl)C=C1Cl FTLYMKDSHNWQKD-UHFFFAOYSA-N 0.000 claims description 7
- 229940085605 saccharin sodium Drugs 0.000 claims description 6
- 239000006188 syrup Substances 0.000 claims description 5
- 235000020357 syrup Nutrition 0.000 claims description 5
- 239000008187 granular material Substances 0.000 claims description 4
- 239000008123 high-intensity sweetener Substances 0.000 claims description 4
- 235000013615 non-nutritive sweetener Nutrition 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 239000007910 chewable tablet Substances 0.000 claims description 3
- 239000007788 liquid Substances 0.000 claims description 3
- 239000006191 orally-disintegrating tablet Substances 0.000 claims description 3
- 239000003826 tablet Substances 0.000 claims description 3
- 229940068682 chewable tablet Drugs 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 244000228451 Stevia rebaudiana Species 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 abstract description 4
- 230000000638 stimulation Effects 0.000 abstract description 4
- 239000004570 mortar (masonry) Substances 0.000 description 13
- 230000007794 irritation Effects 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 9
- 241000544066 Stevia Species 0.000 description 7
- 239000003795 chemical substances by application Substances 0.000 description 6
- 238000004519 manufacturing process Methods 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- -1 troche Substances 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 235000014486 Hydrangea macrophylla Nutrition 0.000 description 2
- 244000267823 Hydrangea macrophylla Species 0.000 description 2
- 239000004384 Neotame Substances 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 239000000284 extract Substances 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 235000019412 neotame Nutrition 0.000 description 2
- HLIAVLHNDJUHFG-HOTGVXAUSA-N neotame Chemical compound CC(C)(C)CCN[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 HLIAVLHNDJUHFG-HOTGVXAUSA-N 0.000 description 2
- 108010070257 neotame Proteins 0.000 description 2
- 229920001542 oligosaccharide Polymers 0.000 description 2
- 150000002482 oligosaccharides Chemical class 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 229940081974 saccharin Drugs 0.000 description 2
- 235000019204 saccharin Nutrition 0.000 description 2
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 2
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000000892 thaumatin Substances 0.000 description 2
- 235000010436 thaumatin Nutrition 0.000 description 2
- HDTRYLNUVZCQOY-UHFFFAOYSA-N α-D-glucopyranosyl-α-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OC1C(O)C(O)C(O)C(CO)O1 HDTRYLNUVZCQOY-UHFFFAOYSA-N 0.000 description 1
- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 description 1
- PVXPPJIGRGXGCY-DJHAAKORSA-N 6-O-alpha-D-glucopyranosyl-alpha-D-fructofuranose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@](O)(CO)O1 PVXPPJIGRGXGCY-DJHAAKORSA-N 0.000 description 1
- 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 1
- 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 1
- 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 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
- 239000004386 Erythritol Substances 0.000 description 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 1
- 229930091371 Fructose Natural products 0.000 description 1
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 1
- 239000005715 Fructose Substances 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 244000068988 Glycine max Species 0.000 description 1
- 235000010469 Glycine max Nutrition 0.000 description 1
- 206010019233 Headaches 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
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- MUPFEKGTMRGPLJ-RMMQSMQOSA-N Raffinose Natural products O(C[C@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](O[C@@]2(CO)[C@H](O)[C@@H](O)[C@@H](CO)O2)O1)[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 MUPFEKGTMRGPLJ-RMMQSMQOSA-N 0.000 description 1
- WINXNKPZLFISPD-UHFFFAOYSA-M Saccharin sodium Chemical compound [Na+].C1=CC=C2C(=O)[N-]S(=O)(=O)C2=C1 WINXNKPZLFISPD-UHFFFAOYSA-M 0.000 description 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 description 1
- MUPFEKGTMRGPLJ-UHFFFAOYSA-N UNPD196149 Natural products OC1C(O)C(CO)OC1(CO)OC1C(O)C(O)C(O)C(COC2C(C(O)C(O)C(CO)O2)O)O1 MUPFEKGTMRGPLJ-UHFFFAOYSA-N 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 235000010358 acesulfame potassium Nutrition 0.000 description 1
- 229960004998 acesulfame potassium Drugs 0.000 description 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N alpha,alpha-trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QUYVBRFLSA-N beta-maltose Chemical compound OC[C@H]1O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@@H]1O GUBGYTABKSRVRQ-QUYVBRFLSA-N 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 229940124579 cold medicine Drugs 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- HEBKCHPVOIAQTA-NGQZWQHPSA-N d-xylitol Chemical compound OC[C@H](O)C(O)[C@H](O)CO HEBKCHPVOIAQTA-NGQZWQHPSA-N 0.000 description 1
- 235000013365 dairy product Nutrition 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 239000007888 film coating Substances 0.000 description 1
- 238000009501 film coating Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 235000021255 galacto-oligosaccharides Nutrition 0.000 description 1
- 150000003271 galactooligosaccharides Chemical class 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- DLRVVLDZNNYCBX-RTPHMHGBSA-N isomaltose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)C(O)O1 DLRVVLDZNNYCBX-RTPHMHGBSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- MUPFEKGTMRGPLJ-ZQSKZDJDSA-N raffinose 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[C@@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO)O2)O)O1 MUPFEKGTMRGPLJ-ZQSKZDJDSA-N 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
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- 238000010998 test method Methods 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
本発明は、イブプロフェン、カルボシステインを含有する組成物に関し、さらに詳しくは口腔刺激が抑制され、服用性が向上したイブプロフェン含有経口用組成物に関する。 The present invention relates to a composition containing ibuprofen and carbocysteine, and more particularly to an ibuprofen-containing oral composition in which oral irritation is suppressed and taking ability is improved.
頭痛薬や総合感冒薬の有効成分として汎用されているイブプロフェンは、苦味や口腔刺激等の不快感を有することからイブプロフェンを含む組成物において、不快感を抑制することは、組成物の服用性を向上させ、製品の差別化を図ることができるなど、大きなメリットがある。従って、イブプロフェンと甘味剤等を組み合わせた服用性向上に関する特許出願は複数存在する（特許文献１、特許文献２）。しかし、いずれもイブプロフェン由来の口腔刺激を十分抑制するものとはいえなかった。 Ibuprofen, which is widely used as an active ingredient in headache and general cold medicines, has discomfort such as bitterness and oral irritation, so in the composition containing ibuprofen, suppressing discomfort reduces the dose of the composition. There are significant advantages such as improvement and product differentiation. Therefore, there are a plurality of patent applications relating to improvement of taking ability by combining ibuprofen and sweeteners (Patent Documents 1 and 2). However, none of them could sufficiently suppress ibuprofen-derived oral irritation.
本発明はイブプロフェン由来の口腔刺激を抑制し、服用性良好な経口用組成物を提供することを課題とする。 An object of the present invention is to provide an oral composition that suppresses oral irritation derived from ibuprofen and has good dosing properties.
本発明者らは、上記課題を解決すべく鋭意検討した結果、イブプロフェンにカルボシステインと甘味剤を組み合わせることで、口腔刺激が大きく抑制されることを見出し、本発明を完成するに至った。すなわち、本発明は、
（１）イブプロフェン、カルボシステインおよび甘味剤を含有することを特徴とする経口用組成物、
（２）剤形が、顆粒剤、散剤、口腔内崩壊錠、口腔内速溶錠、チュアブル錠、トローチ剤、ドロップ剤、ドライシロップ剤または液剤である（１）に記載の経口用組成物、
（３）甘味剤が、高甘味度甘味剤である（１）に記載の経口用組成物、
（４）高甘味度甘味剤が、スクラロース、アスパルテーム、アセスルファムＫ、ステビア又はサッカリンナトリウムである（３）に記載の経口用組成物、
（５）甘味剤の含有量が、イブプロフェン１質量部に対して０．０２質量部以上である（１）に記載の経口用組成物、
である。
As a result of intensive studies to solve the above problems, the present inventors have found that oral stimulation is greatly suppressed by combining carbocysteine and a sweetener with ibuprofen, and have completed the present invention. That is, the present invention
(1) An oral composition comprising ibuprofen, carbocysteine and a sweetener,
(2) The oral composition according to (1), wherein the dosage form is a granule, powder, orally disintegrating tablet, fast-dissolving tablet in the oral cavity, chewable tablet, troche, drop agent, dry syrup agent, or liquid agent,
(3) The oral composition according to (1), wherein the sweetener is a high-intensity sweetener,
(4) The oral composition according to (3), wherein the high-intensity sweetener is sucralose, aspartame, acesulfame K, stevia or saccharin sodium,
(5) The composition for oral administration according to (1), wherein the content of the sweetener is 0.02 parts by mass or more with respect to 1 part by mass of ibuprofen,
It is.
本発明により、有効成分としてイブプロフェンを配合した服用性の良い製剤を提供することが可能となった。 According to the present invention, it is possible to provide a preparation with good dosing properties containing ibuprofen as an active ingredient.
本発明のイブプロフェンの含有量は、経口用組成物中５０質量％以下が好ましく、３質量％〜４４質量％が特に好ましい。５０質量％を超えるとイブプロフェンの口腔刺激を抑制できない場合があるからである。 The content of ibuprofen of the present invention is preferably 50% by mass or less, and particularly preferably 3% by mass to 44% by mass in the oral composition. This is because if it exceeds 50% by mass, oral stimulation of ibuprofen may not be suppressed.
本発明のカルボシステインの含有量は、経口用組成物中９０質量％以下が好ましく、８質量％〜７６質量％がより好ましく、８質量％〜５５質量％が特に好ましい。また、イブプロフェン１質量部に対して０．８〜５ 質量部が好ましく、さらに好ましくは１．２５〜３．５質量部である。 90 mass% or less is preferable in an oral composition, as for content of the carbocysteine of this invention, 8 mass%-76 mass% are more preferable, and 8 mass%-55 mass% are especially preferable. Moreover, 0.8-5 mass parts is preferable with respect to 1 mass part of ibuprofen, More preferably, it is 1.25-3.5 mass parts.
本発明の甘味剤としては、例えばスクラロース、アスパルテーム、ステビア、グリチルチン、サッカリン、サッカリンナトリウム、アスパルテーム、アセスルファムＫ、ソーマチン、ネオテーム等の高甘味度甘味剤、アマチャ抽出物、砂糖、ブドウ糖、麦芽糖、果糖、水飴、異性化糖、イソマルトオリゴ糖、ガラクトオリゴ糖、キシロオリゴ糖、乳果オリゴ糖、大豆オリゴ糖、ラフィノース、トレハロース、乳糖、ソルビトール、マンニトール、マルチトール、還元水飴、還元パラチノース、キシリトール、エリスリトールが好ましい。このうち、特に好ましいのは、スクラロース、アスパルテーム、ステビア、グリチルチン、サッカリン、サッカリンナトリウム、アスパルテーム、アセスルファムＫ、アマチャ抽出物、ソーマチン、ネオテームであり、最も好ましのはスクラロース、アスパルテーム、アセスルファムＫ、ステビアまたはサッカリンナトリウムである。甘味剤の含有量は、経口用組成物中１質量％〜１０質量％が好ましく、４質量％〜８質量％がより好ましい。また、甘味剤の含有量は、イブプロフェン１質量部に対して０．０２質量部以上が好ましい。本発明の甘味剤としてスクラロースを配合する場合は、イブプロフェン１質量部に対して０．０３質量部以上が好ましく、０．０５質量部以上がさらに好ましい。アスパルテームを配合する場合は、０．０２質量部以上が好ましく、さらに好ましくは０．１７質量部以上である。アセスルファムＫを配合する場合は、イブプロフェン１質量部に対して０．０２質量部以上が好ましく、０．２質量部以上がさらに好ましい。ステビアを配合する場合は、イブプロフェン１質量部に対して０．００５質量部以上が好ましく、０．０２質量部以上がさらに好ましい。サッカリンナトリウムを配合する場合は、イブプロフェン１質量部に対して０．０２質量部以上が好ましく、０．２質量部以上がさらに好ましい。 Examples of the sweetening agent of the present invention include sucralose, aspartame, stevia, glycyrrhin, saccharin, saccharin sodium, aspartame, acesulfame K, thaumatin, neotame and other high-sweetness sweeteners, amacha extract, sugar, glucose, maltose, fructose, starch syrup Isomerized sugar, isomalto-oligosaccharide, galactooligosaccharide, xylo-oligosaccharide, dairy oligosaccharide, soybean oligosaccharide, raffinose, trehalose, lactose, sorbitol, mannitol, maltitol, reduced starch syrup, reduced palatinose, xylitol, erythritol. Of these, particularly preferred are sucralose, aspartame, stevia, glycyrrhin, saccharin, sodium saccharin, aspartame, acesulfame K, amacha extract, thaumatin, neotame, and most preferred are sucralose, aspartame, acesulfame K, stevia or sodium saccharin. It is. 1 mass%-10 mass% are preferable in an oral composition, and, as for content of a sweetener, 4 mass%-8 mass% are more preferable. Further, the content of the sweetener is preferably 0.02 parts by mass or more with respect to 1 part by mass of ibuprofen. When mix | blending sucralose as a sweetener of this invention, 0.03 mass part or more is preferable with respect to 1 mass part of ibuprofen, and 0.05 mass part or more is more preferable. When mix | blending aspartame, 0.02 mass part or more is preferable, More preferably, it is 0.17 mass part or more. When blending acesulfame K, 0.02 parts by mass or more is preferable with respect to 1 part by mass of ibuprofen, and 0.2 parts by mass or more is more preferable. When compounding stevia, 0.005 parts by mass or more is preferable with respect to 1 part by mass of ibuprofen, and 0.02 parts by mass or more is more preferable. When mix | blending saccharin sodium, 0.02 mass part or more is preferable with respect to 1 mass part of ibuprofen, and 0.2 mass part or more is more preferable.
本発明の経口用組成物としては、固形剤のみならず、液剤（懸濁剤含む）も含まれる。 The oral composition of the present invention includes not only solid agents but also liquid agents (including suspension agents).
本発明の経口用組成物は、イブプロフェンを被覆しなくてもイブプロフェンの口腔刺激を抑制することから、通常被覆を行うことが困難な、例えば顆粒剤、散剤、口腔内崩壊錠、口腔内速溶錠、チュアブル錠、トローチ剤、ドロップ剤等が好ましく、特に水や温湯に溶解または分散させて服用するタイプの散剤や顆粒剤（例えばドライシロップ剤）として実施する意義が大きい。本発明の経口用組成物の製造方法は、常法により製造することができ、その方法は特に限定されるものではない。 The oral composition of the present invention suppresses oral irritation of ibuprofen without coating with ibuprofen, so that it is usually difficult to perform coating, such as granules, powders, orally disintegrating tablets, orally dissolving tablets Chewable tablets, lozenges, drop agents and the like are preferable, and it is particularly significant to carry out as powders or granules (for example, dry syrup) of the type to be taken by dissolving or dispersing in water or hot water. The method for producing the oral composition of the present invention can be produced by a conventional method, and the method is not particularly limited.
以下に、製造例、実施例、比較例を挙げ、本説明をさらに詳細に説明するが、本発明はこれらの製造例等に何ら限定されるものではない。 Hereinafter, the present invention will be described in more detail with reference to production examples, examples and comparative examples, but the present invention is not limited to these production examples.
製造例
（１）各組成物の調製
下記に示す実施例１〜１０及び比較例１〜３の経口用組成物を調製した。
Production Example (1) Preparation of Each Composition The oral compositions of Examples 1 to 10 and Comparative Examples 1 to 3 shown below were prepared.
実施例１
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、スクラロース３０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 1
600 mg of ibuprofen, 750 mg of carbocysteine, and 30 mg of sucralose were weighed, passed through a 30-mesh sieve, ground in a mortar and mixed.
実施例２
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、アスパルテーム１２０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 2
600 mg of ibuprofen, 750 mg of carbocysteine, and 120 mg of aspartame were weighed, passed through a 30-mesh sieve, ground and mixed with a mortar.
実施例３
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、アスパルテーム１０４ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 3
600 mg of ibuprofen, 750 mg of carbocysteine, and 104 mg of aspartame were weighed, passed through a 30-mesh sieve, ground in a mortar and mixed.
実施例４
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、アスパルテーム５２ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 4
600 mg of ibuprofen, 750 mg of carbocysteine, and 52 mg of aspartame were weighed, passed through a 30-mesh sieve, ground and mixed with a mortar.
実施例５
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、アスパルテーム２６ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 5
600 mg of ibuprofen, 750 mg of carbocysteine, and 26 mg of aspartame were weighed, passed through a 30-mesh sieve, ground and mixed with a mortar.
実施例６
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、アセスルファムカリウム１２０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 6
600 mg of ibuprofen, 750 mg of carbocysteine, and 120 mg of acesulfame potassium were weighed, passed through a 30-mesh sieve, ground in a mortar and mixed.
実施例７
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、ステビア１５ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 7
600 mg of ibuprofen, 750 mg of carbocysteine, and 15 mg of stevia were weighed, passed through a 30-mesh sieve, ground and mixed with a mortar.
実施例８
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇ、サッカリンナトリウム１２０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 8
600 mg of ibuprofen, 750 mg of carbocysteine, and 120 mg of saccharin sodium were weighed, passed through a 30-mesh sieve, ground in a mortar and mixed.
実施例９
イブプロフェン４５０ｍｇ、カルボシステイン１５００ｍｇ、アスパルテーム１２０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 9
450 mg of ibuprofen, 1500 mg of carbocysteine and 120 mg of aspartame were weighed, passed through a 30-mesh sieve, ground and mixed with a mortar.
実施例１０
イブプロフェン４５０ｍｇ、カルボシステイン１５００ｍｇ、アスパルテーム２６ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Example 10
450 mg of ibuprofen, 1500 mg of carbocysteine and 26 mg of aspartame were weighed, passed through a 30-mesh sieve, ground in a mortar and mixed.
比較例１
イブプロフェン６００ｍｇ、スクラロース３０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Comparative Example 1
600 mg of ibuprofen and 30 mg of sucralose were weighed, passed through a 30 mesh sieve, ground and mixed in a mortar.
比較例２
イブプロフェン６００ｍｇ、アスパルテーム１０４ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Comparative Example 2
600 mg of ibuprofen and 104 mg of aspartame were weighed, passed through a 30 mesh sieve, ground and mixed with a mortar.
比較例３
イブプロフェン６００ｍｇ、カルボシステイン７５０ｍｇを量り、３０メッシュの篩を通し、乳鉢ですりつぶして混合した。
Comparative Example 3
600 mg of ibuprofen and 750 mg of carbocysteine were weighed, passed through a 30 mesh sieve, ground and mixed with a mortar.
（２）試験方法
上記実施例１〜５及び比較例１〜３の組成物を表２に示した一回服用量をパネルが口に含み、５秒後、さらに２０ｍLの水を口に含み、５秒後に吐き出し、感じた口腔刺激の最大値を、比較例１をコントロールとして表１の評価基準に基づき評価した。上記実施例６〜１０の組成物についても、同様の方法で試験を行い、比較例１をコントロールとして表１の評価基準に基づき評価した。
(2) Test method The panel contains the doses of the compositions of Examples 1 to 5 and Comparative Examples 1 to 3 shown in Table 2, and after 5 seconds, further contains 20 mL of water in the mouth. The maximum value of oral irritation that was discharged and felt after 5 seconds was evaluated based on the evaluation criteria shown in Table 1 using Comparative Example 1 as a control. The compositions of Examples 6 to 10 were also tested in the same manner and evaluated based on the evaluation criteria shown in Table 1 using Comparative Example 1 as a control.
結果を表２〜３に示す。 The results are shown in Tables 2-3.
ここで、甘味度とは甘味剤の対砂糖甘味度に処方中の高甘味度甘味剤の重量比をかけた値と定義した。対砂糖甘味度は同じ濃度の砂糖水溶液と比較した際に、甘味強度を砂糖水溶液の何倍感じるかであり、スクラロースを６００倍、アスパルテームを２００倍、アセスルファムＫを２００倍、ステビアを１８０倍、サッカリンナトリウムを４５０倍として計算した。 Here, the sweetness level was defined as a value obtained by multiplying the sweetness level of the sweetener with respect to the sugar sweetness by the weight ratio of the high sweetness level sweetener in the formulation. The sweetness to sugar is the number of times the sweetness intensity is felt when compared with a sugar aqueous solution of the same concentration, sucralose 600 times, aspartame 200 times, acesulfame K 200 times, stevia 180 times, The saccharin sodium was calculated as 450 times.
比較例１、２、３に示したとおり、イブプロフェンと甘味剤、イブプロフェンとカルボシステインを用いた場合に口腔刺激に大きな変化はなく、口腔刺激は甘味度や一回服用量による口腔刺激改善効果はみられなかった。これに対し、イブプロフェン、カルボシステイン、及び甘味剤を組み合わせた実施例１〜１０の組成物は、口腔刺激が大きく抑制されることがわかった。 As shown in Comparative Examples 1, 2, and 3, when ibuprofen and a sweetener, ibuprofen and carbocysteine were used, there was no significant change in oral irritation, and oral irritation was the effect of improving oral irritation by sweetness and single dose It was not seen. In contrast, it was found that oral irritation was greatly suppressed in the compositions of Examples 1 to 10 in which ibuprofen, carbocysteine, and a sweetener were combined.
本発明により、従来のフィルムコーティングや糖衣といった方法を用いないでも、イブプロフェンを含有した服用性が良好な経口用組成物を提供することが可能となったので、剤形のバリエーションが広がり、消費者のニーズに、より的確に対応できるようになった。 According to the present invention, it is possible to provide a composition for oral administration containing ibuprofen with good dosage without using conventional methods such as film coating and sugar coating. To meet the needs of customers more accurately.
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