JP6221644B2 - Oral composition - Google Patents
Oral composition Download PDFInfo
- Publication number
- JP6221644B2 JP6221644B2 JP2013227944A JP2013227944A JP6221644B2 JP 6221644 B2 JP6221644 B2 JP 6221644B2 JP 2013227944 A JP2013227944 A JP 2013227944A JP 2013227944 A JP2013227944 A JP 2013227944A JP 6221644 B2 JP6221644 B2 JP 6221644B2
- Authority
- JP
- Japan
- Prior art keywords
- ibuprofen
- oral
- oral composition
- sucralose
- tranexamic acid
- 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.)
- Active
Links
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、イブプロフェン、トラネキサム酸およびスクラロース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, tranexamic acid and sucralose, 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抑制効果は十分とはいえなかった。 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 the ibuprofen-derived oral irritation suppression effects were sufficient.
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、イブプロフェンにトラネキサム酸とスクラロース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、トラネキサム酸およびスクラロースを含有することを特徴とする経口用組成物、
(2)スクラロースの含有量が、イブプロフェンの1質量部に対して0.02〜0.8質量部である(1)に記載の経口用組成物、
(3)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)又は(2)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 tranexamic acid and sucralose with ibuprofen, and the present invention has been completed. That is, the present invention
(1) An oral composition comprising ibuprofen, tranexamic acid and sucralose,
(2) The oral composition according to (1), wherein the content of sucralose is 0.02 to 0.8 parts by mass with respect to 1 part by mass of ibuprofen,
(3) The oral composition according to (1) or (2), wherein the dosage form is a granule, powder, orally disintegrating tablet, fast dissolving tablet, chewable tablet, troche, drop, dry syrup or liquid object,
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5〜45質量%が好ましく、トラネキサム酸の含有量は、経口用組成物中5〜55質量%が好ましく、スクラロースの含有量は、経口用組成物中0.1〜5質量%が好ましい。 The content of ibuprofen of the present invention is preferably 5 to 45% by mass in the oral composition, the content of tranexamic acid is preferably 5 to 55% by mass in the oral composition, and the content of sucralose is oral. 0.1-5 mass% is preferable in a composition.
また、イブプロフェン由来の口腔刺激を抑制するという点から、スクラロースの含有量は、イブプロフェン1質量部に対して0.02〜0.8質量部配合するのが好ましい。 Moreover, it is preferable to mix | blend 0.02-0.8 mass part with respect to 1 mass part of ibuprofen from the point of suppressing the oral irritation | stimulation derived from ibuprofen.
本発明の経口用組成物としては、内服固形剤のみならず、内服液剤(懸濁剤含む)も含まれる。 The oral composition of the present invention includes not only a solid preparation for internal use but also a liquid preparation for internal use (including a suspension).
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、特に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、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 ibuprofen oral irritation even without coating with ibuprofen, and thus is usually difficult to perform coating, such as granules, powders, orally disintegrating tablets, and rapid oral dissolution. It is significant to implement as tablets, chewable tablets, troches, drops, especially powders and 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1−2及び比較例1−4の経口用組成物を調製した。
Production Example (1) Preparation of Each Composition The oral compositions of Example 1-2 and Comparative Example 1-4 shown below were prepared.
実施例1
イブプロフェン630mg、トラネキサム酸750mg、スクラロース45mg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
630 mg of ibuprofen, 750 mg of tranexamic acid, and 45 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630mg、トラネキサム酸750mg、スクラロース13mg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
630 mg of ibuprofen, 750 mg of tranexamic acid and 13 mg of sucralose were weighed, passed through a 30-mesh sieve and ground and mixed with a mortar.
比較例1
イブプロフェン630mg、スクラロース45mg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
630 mg of ibuprofen and 45 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630mg、トラネキサム酸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 2
630 mg of ibuprofen and 750 mg of tranexamic acid were weighed, passed through a 30 mesh sieve, ground in a mortar and mixed.
比較例3
イブプロフェン630mg、トラネキサム酸750mg、アスパルテーム45mg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
630 mg of ibuprofen, 750 mg of tranexamic acid, and 45 mg of aspartame were weighed, passed through a 30 mesh sieve, ground and mixed with a mortar.
比較例4
イブプロフェン630mg、トラネキサム酸750mg、ステビア45mg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 4
630 mg of ibuprofen, 750 mg of tranexamic acid and 45 mg of stevia were weighed, passed through a 30 mesh sieve, ground and mixed with a mortar.
(2)試験方法
上記実施例1〜2及び比較例1〜4の組成物各300mgずつを、3名のパネルが口に含み、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イブプロフェン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。
コントロール:
3名のパネルがイブプロフェン300mgを口に含み、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強度4とした。
(2) Test method 300 mg each of the compositions of Examples 1 and 2 and Comparative Examples 1 to 4 were included in the mouth of three persons, and after 5 seconds, further 20 mL of water was included in the mouth and after 5 seconds. The maximum value of oral irritation that was exhaled and felt was evaluated based on the evaluation criteria shown in Table 1 using ibuprofen as a control.
Control:
Three panelists included 300 mg of ibuprofen in the mouth, 5 seconds later, further 20 mL of water in the mouth, and discharged after 5 seconds.
結果を表2に示す。 The results are shown in Table 2.
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,ステビアを180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 with respect to sugar was calculated as the number of times the sweetness intensity felt compared to a sugar aqueous solution when compared with a sugar aqueous solution of the same concentration, with sucralose 600 times, aspartame 200 times, and stevia 180 times.
比較例1に示したとおり、イブプロフェンとスクラロースを組合せても、口腔刺激の強度はイブプロフェンのみの場合と同程度であり、スクラロースによる口腔刺激改善効果はみられなかった。同様に比較例2に示したとおり、イブプロフェンとトラネキサム酸を組み合わせても、口腔刺激の強度はイブプロフェンと同程度であった。
これに対し、実施例1、2に示したとおり、イブプロフェンとトラネキサム酸とスクラロースを組み合わせると、口腔刺激が大きく抑制されることがわかった。
比較例3、4に示したとおり、実施例1、2のスクラロースをアスパルテームやステビア等の甘味剤に置き換えた場合、口腔刺激は抑制されず、むしろ強くなることがわかった。
As shown in Comparative Example 1, even when ibuprofen and sucralose were combined, the intensity of oral irritation was similar to that of ibuprofen alone, and the effect of improving oral irritation by sucralose was not observed. Similarly, as shown in Comparative Example 2, even when ibuprofen and tranexamic acid were combined, the intensity of oral irritation was similar to that of ibuprofen.
In contrast, as shown in Examples 1 and 2, when ibuprofen, tranexamic acid, and sucralose were combined, oral irritation was greatly suppressed.
As shown in Comparative Examples 3 and 4, it was found that when the sucralose of Examples 1 and 2 was replaced with a sweetener such as aspartame or stevia, oral irritation was not suppressed but rather became stronger.
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, an oral composition containing ibuprofen can be provided without using conventional methods such as film coating and sugar coating. Now we can meet the needs more accurately.
Claims (3)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2013227944A JP6221644B2 (en) | 2012-11-09 | 2013-11-01 | Oral composition |
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2012247352 | 2012-11-09 | ||
JP2012247352 | 2012-11-09 | ||
JP2013227944A JP6221644B2 (en) | 2012-11-09 | 2013-11-01 | Oral composition |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2014111581A JP2014111581A (en) | 2014-06-19 |
JP6221644B2 true JP6221644B2 (en) | 2017-11-01 |
Family
ID=51169013
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013227944A Active JP6221644B2 (en) | 2012-11-09 | 2013-11-01 | Oral composition |
Country Status (1)
Country | Link |
---|---|
JP (1) | JP6221644B2 (en) |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP3070152B2 (en) * | 1991-06-25 | 2000-07-24 | ライオン株式会社 | Liquid oral composition |
JP3667381B2 (en) * | 1995-03-27 | 2005-07-06 | 株式会社資生堂 | Antipyretic analgesic |
JP2001342151A (en) * | 2000-03-31 | 2001-12-11 | Eisai Co Ltd | Pharmaceutical composition having sweet taste |
JP2003104881A (en) * | 2001-09-28 | 2003-04-09 | Taiho Yakuhin Kogyo Kk | Suspension for internal application |
JP4044748B2 (en) * | 2001-10-17 | 2008-02-06 | サンスター株式会社 | Oral liquid composition |
US20040258716A1 (en) * | 2002-06-17 | 2004-12-23 | Shen Gao | Ibuprofen suspension |
JP4814636B2 (en) * | 2004-01-29 | 2011-11-16 | 大日本住友製薬株式会社 | Biguanide drugs for internal use |
JP5249558B2 (en) * | 2007-11-08 | 2013-07-31 | 武田薬品工業株式会社 | Tranexamic acid-containing oral solution |
KR101683293B1 (en) * | 2009-06-29 | 2016-12-06 | 라이온 가부시키가이샤 | Composition for oral use |
-
2013
- 2013-11-01 JP JP2013227944A patent/JP6221644B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
JP2014111581A (en) | 2014-06-19 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5222841B2 (en) | Oseltamivir phosphate granule and preparation method thereof | |
TWI376243B (en) | Oral disintegrating tablet | |
WO2000078292A1 (en) | Quickly disintegrating solid preparations | |
JP2011502997A5 (en) | ||
JP5870690B2 (en) | Orally disintegrating tablet and method for producing the same | |
JP6133445B2 (en) | Oral rapidly disintegrating composition for solid preparation | |
CN102327244B (en) | Ambroxol hydrochloride orally disintegrating tablet and preparation method thereof | |
TWI314454B (en) | An oral liquid pharmaceutical composition of leukotriene antagonists | |
JP6204141B2 (en) | Oral rapidly disintegrating composition for solid preparation | |
JP6088151B2 (en) | Pharmaceutical composition | |
JP2014166994A (en) | Novel chinese medicine extract formulation | |
JP6221644B2 (en) | Oral composition | |
JP2010241760A (en) | Tablet quickly disintegrable in oral cavity that has unpleasant taste reduced, and method for preparing the same | |
JP6554839B2 (en) | Oral composition | |
JP6262490B2 (en) | Intraoral rapidly disintegrating tablet composition | |
HRP20220691T1 (en) | Improvements in and relating to compositions | |
JP6565334B2 (en) | Solid preparation | |
JP2018035132A (en) | Dry granule, and solid formulation containing dry granule and method for producing the same | |
JP2017137246A (en) | Chinese medicine jelly pharmaceutical composition | |
JP2001294524A (en) | Solid pharmaceutical preparation for internal use comprising acetaminophen formulated therein | |
TW201113051A (en) | Oral disintegrating tablet and manufacturing method thereof | |
KR100900915B1 (en) | Suspension formulation containing megestrol acetate and preparation method thereof | |
JP2015107951A (en) | Granules | |
JP2018177698A (en) | Solid composition | |
JP6946029B2 (en) | Oral pharmaceutical composition |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20161019 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20170620 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20170905 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20170918 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 6221644 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |