JPS6130567A - Method of stabilizing urea - Google Patents
Method of stabilizing ureaInfo
- Publication number
- JPS6130567A JPS6130567A JP15258284A JP15258284A JPS6130567A JP S6130567 A JPS6130567 A JP S6130567A JP 15258284 A JP15258284 A JP 15258284A JP 15258284 A JP15258284 A JP 15258284A JP S6130567 A JPS6130567 A JP S6130567A
- Authority
- JP
- Japan
- Prior art keywords
- urea
- amino acid
- basic amino
- aqueous solution
- acid salt
- 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
Landscapes
- Medicinal Preparation (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
【発明の詳細な説明】
[産業上の利用分野]
本発明は尿素水溶液配合製剤において長期間尿素の安定
性を保持させる方法に関するものである。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a method for maintaining the stability of urea for a long period of time in a preparation containing an aqueous urea solution.
[従来の技術]
尿素は皮膚の角層の吸湿性を高める作用や、角質熔解作
用があるので、魚鱗官、老人性乾皮症、アトピー性皮膚
炎等の疾患用の外用製剤中に配合されたり、保湿効果を
高めるために化粧料中に配合されてきた。また、単純水
溶液を利尿剤として内服する場合もある。[Prior art] Urea has the effect of increasing the hygroscopicity of the stratum corneum of the skin and has a keratin-dissolving effect, so it is often incorporated into external preparations for diseases such as ichthyosis, senile xeroderma, and atopic dermatitis. It has also been incorporated into cosmetics to enhance its moisturizing effect. In addition, a simple aqueous solution may be taken orally as a diuretic.
しかし、尿素は水の共存下で除々に分解することが知ら
れており、この分解は酸、アルカリの共存下ではさらに
促進される。尿素が分解するとアンモニアガスが発生し
、このものは、周知の通り、強い刺激臭を有するので、
大きな欠点となっていた。However, it is known that urea gradually decomposes in the coexistence of water, and this decomposition is further accelerated in the coexistence of acids and alkalis. When urea decomposes, ammonia gas is generated, and as is well known, this gas has a strong pungent odor.
This was a major drawback.
[発明が解決しようとする問題点コ
本発明者らはかかる事情に鑑み尿素の分解反応を抑制し
て安定な尿素水溶液配合製剤を開発すべく鋭意検討を重
ねた結果、本発明を完成した。[Problems to be Solved by the Invention] In view of the above circumstances, the present inventors have completed the present invention as a result of intensive studies to suppress the decomposition reaction of urea and develop a stable urea aqueous solution formulation.
[問題点を解決するための手段]
すなわち、本発明は、尿素水溶液に、塩基性アミノ酸塩
を配合することを特徴とする尿素の安定化法である。[Means for Solving the Problems] That is, the present invention is a method for stabilizing urea, which is characterized by blending a basic amino acid salt into an aqueous urea solution.
以下、本発明について詳述する。The present invention will be explained in detail below.
本発明において用いられる塩基性アミノ酸塩を構成する
塩基性アミノ酸としてはヒスチジン、リジン、オルニチ
ン、アルギニンなどがあり、塩としては塩酸塩、臭化水
素酸塩をはじめ、ピロリドンカルボン酸塩、ウロカニン
酸塩などの有機酸塩も用いることができる。The basic amino acids constituting the basic amino acid salt used in the present invention include histidine, lysine, ornithine, and arginine, and the salts include hydrochloride, hydrobromide, pyrrolidone carboxylate, and urocanate. Organic acid salts such as can also be used.
塩基性アミノ酸塩の添加量は、配合される尿素の量ある
いは保存される条件、期間などや希望する分解抑制の度
合によってそれぞれ適量を選ぶことができるが、尿素量
に対する塩基性アミノ酸塩量が増すほど抑制効果は大き
くなる。安定性を向上させる目的で配合される塩基性ア
ミノ酸塩の量は、尿素に対して重量で1/10倍以上、
3倍以下が望ましい。但し、過剰の塩基性アミノ酸塩の
添加は塩基性アミノ酸塩自身が変質し、変色、変臭など
を生じるために注意が必要である。また本発明で用いら
れる尿素水溶液の濃度は任意である。The amount of basic amino acid salt added can be selected appropriately depending on the amount of urea to be mixed, storage conditions, period, etc., and the desired degree of suppression of decomposition, but the amount of basic amino acid salt increases relative to the amount of urea. The greater the suppression effect. The amount of basic amino acid salt added for the purpose of improving stability is at least 1/10 times the weight of urea,
Desirably 3 times or less. However, care must be taken when adding an excessive amount of the basic amino acid salt, since the basic amino acid salt itself deteriorates, causing discoloration, odor, etc. Further, the concentration of the urea aqueous solution used in the present invention is arbitrary.
さらに、尿素水溶液が油相等と乳化されて乳状製剤の形
等になっていても本発明の効果には全く差し支えない。Furthermore, even if the urea aqueous solution is emulsified with an oil phase or the like to form an emulsion preparation, the effects of the present invention will not be affected at all.
尿素の微量の分解を追跡するためにはpH変化を観察す
るのが簡便でしかも正確である。すなわち、尿素が分解
するとρIIが上昇する。以下に尿素と塩基性アミノ酸
塩を併用した場合の系のpl(変化などを示す。表1は
尿素および塩基性アミノ酸塩をそれぞれの量、精製水に
溶解し、全量を100とした水l/8液のpH値変比変
化ンモニア臭の評価結果である。塩基性アミノ酸塩を添
加しない尿素のみの水溶液の場合はρ11値が上昇し、
それに伴ってアンモニア臭が発生する。しかし本発明の
塩基性アミノ酸塩を添加したものについてはpl+変化
は若干あるもののかなり低くおさえられ、アンモニア臭
も認められない。In order to track the decomposition of minute amounts of urea, it is convenient and accurate to observe pH changes. That is, when urea decomposes, ρII increases. The pl (changes, etc.) of the system when urea and basic amino acid salts are used together are shown below. This is an evaluation result of pH value ratio change and ammonia odor of 8 liquids.In the case of an aqueous solution containing only urea without adding basic amino acid salt, the ρ11 value increases,
Along with this, an ammonia odor is generated. However, in the case where the basic amino acid salt of the present invention was added, although there was a slight change in pl+, it was suppressed to a fairly low level, and no ammonia odor was observed.
[実施例]
次に本発明を実施例および比較例によりさらに詳細に説
明するが、本発明はこれにより限定されるものではない
。[Examples] Next, the present invention will be explained in more detail with reference to Examples and Comparative Examples, but the present invention is not limited thereto.
実施例I
A、セタノール 3.0%固
型パラフィン 5.0ワセリン
15.0流動パラフイン
20.OB、尿素
2.0゛1ルギニン塩酸塩
5,0リジン酢酸塩 1.0精製
水 全体を100とする量Aに含まれる
成分を混合し70℃に加熱し、同様に加熱した■3の成
分中に加える。乳化処理後冷却処理を行い、外用尿素配
合剤を得た。Example I A, Setanol 3.0% Solid Paraffin 5.0 Vaseline
15.0 Liquid paraffin
20. OB, urea
2.0゛1 Luginine Hydrochloride
5,0 Lysine acetate 1.0 Purified water Quantity with the total as 100 Mix the components contained in A, heat to 70°C, and add to the similarly heated component (3). After the emulsification treatment, a cooling treatment was performed to obtain a urea formulation for external use.
比較例1
実施例1処方゛で塩基性アミノ酸塩を添加しない4)の
。Comparative Example 1 4) in which no basic amino acid salt was added to the recipe of Example 1.
実施例1および比較例1の試料を40℃にて2ケ月保存
した後、尿素の定量を行った結果、実施例1では96〜
99%の尿素が残存していたのに対し、比較例1では8
0〜85%に減少していた。After storing the samples of Example 1 and Comparative Example 1 for two months at 40°C, urea was quantitatively determined.
While 99% of urea remained, in Comparative Example 1, 8.
It decreased from 0 to 85%.
実施例2
尿素 5.0%精製糖
2,01、−オルニチン
塩酸塩 3.0精製水
90.0各成分を精製水に混合熔解し、内用
利尿剤とする。Example 2 Urea 5.0% Refined sugar 2,01,-ornithine hydrochloride 3.0 Purified water
90.0 Mix and dissolve each component in purified water to prepare an internal diuretic.
比較例2
実施例2処方で11.オルニチン塩酸塩を添加しないも
の。Comparative Example 2 11. Products without ornithine hydrochloride added.
実施例2および比較例2の試料を40℃にて2ケ月保存
したのち尿素の定量を行った結果、実施例2では97〜
99%の尿素が残存していたのに対し1、比較例2では
76〜83%に減少していた。After storing the samples of Example 2 and Comparative Example 2 for two months at 40°C, urea was quantitatively determined.
While 99% of urea remained, in Comparative Example 2, it decreased to 76-83%.
Claims (1)
とする尿素の安定化法。A method for stabilizing urea, which comprises adding a basic amino acid salt to an aqueous urea solution.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15258284A JPS6130567A (en) | 1984-07-23 | 1984-07-23 | Method of stabilizing urea |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15258284A JPS6130567A (en) | 1984-07-23 | 1984-07-23 | Method of stabilizing urea |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS6130567A true JPS6130567A (en) | 1986-02-12 |
JPH0531540B2 JPH0531540B2 (en) | 1993-05-12 |
Family
ID=15543613
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP15258284A Granted JPS6130567A (en) | 1984-07-23 | 1984-07-23 | Method of stabilizing urea |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS6130567A (en) |
Cited By (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH067701U (en) * | 1992-07-02 | 1994-02-01 | 旭光学工業株式会社 | Endoscope air supply device |
WO1997005862A3 (en) * | 1995-08-03 | 1997-04-17 | Sigma Tau Ind Farmaceuti | Use of basic amino acids and derivatives for lowering ceramide levels |
JP2006524199A (en) * | 2003-04-24 | 2006-10-26 | ロレアル | Cosmetic peeling method |
US8440172B2 (en) | 2007-07-09 | 2013-05-14 | Symrise Ag | Stable soluble salts of phenylbenzimidazole sulfonic acid at PHS at or below 7.0 |
JP2014097934A (en) * | 2012-11-13 | 2014-05-29 | Ajinomoto Co Inc | Cosmetic composition containing acetate of amino acid compound |
US10004747B2 (en) | 2010-05-05 | 2018-06-26 | Boehringer Ingelheim International Gmbh | Combination therapy |
US10022379B2 (en) | 2008-04-03 | 2018-07-17 | Boehringer Ingelheim International Gmbh | DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation |
US10023574B2 (en) | 2002-08-21 | 2018-07-17 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
US10034877B2 (en) | 2008-08-06 | 2018-07-31 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients inappropriate for metformin therapy |
US10073104B2 (en) | 2013-03-14 | 2018-09-11 | Siemens Healthcare Diagnostics Inc. | Control of pH in aqueous urea-containing solutions utilizing amino acid-containing compositions |
US10080754B2 (en) | 2006-05-04 | 2018-09-25 | Boehringer Ingelheim International Gmbh | Uses of DPP IV inhibitors |
US10092571B2 (en) | 2009-11-27 | 2018-10-09 | Boehringer Ingelheim International Gmbh | Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin |
US10155000B2 (en) | 2016-06-10 | 2018-12-18 | Boehringer Ingelheim International Gmbh | Medical use of pharmaceutical combination or composition |
US10195203B2 (en) | 2012-05-14 | 2019-02-05 | Boehringr Ingelheim International GmbH | Use of a DPP-4 inhibitor in podocytes related disorders and/or nephrotic syndrome |
US10301313B2 (en) | 2006-05-04 | 2019-05-28 | Boehringer Ingelheim International Gmbh | Polymorphs |
US11033552B2 (en) | 2006-05-04 | 2021-06-15 | Boehringer Ingelheim International Gmbh | DPP IV inhibitor formulations |
US11911387B2 (en) | 2010-11-15 | 2024-02-27 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
US11911388B2 (en) | 2008-10-16 | 2024-02-27 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral or non-oral antidiabetic drug |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5550925A (en) * | 1978-10-09 | 1980-04-14 | Sakura Kogyo Kk | Muffler silencer producing device |
US4424232A (en) * | 1982-05-19 | 1984-01-03 | Parkinson Richard W | Treatment of herpes simplex |
JPS5920217A (en) * | 1982-07-27 | 1984-02-01 | Kawaken Fine Chem Co Ltd | Aqueous jellylike composition stably containing urea |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE1244762B (en) * | 1963-03-01 | 1967-07-20 | Heilmittelwerke Wien Ges Mit B | Stabilization of urea solutions |
-
1984
- 1984-07-23 JP JP15258284A patent/JPS6130567A/en active Granted
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5550925A (en) * | 1978-10-09 | 1980-04-14 | Sakura Kogyo Kk | Muffler silencer producing device |
US4424232A (en) * | 1982-05-19 | 1984-01-03 | Parkinson Richard W | Treatment of herpes simplex |
JPS5920217A (en) * | 1982-07-27 | 1984-02-01 | Kawaken Fine Chem Co Ltd | Aqueous jellylike composition stably containing urea |
Cited By (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH067701U (en) * | 1992-07-02 | 1994-02-01 | 旭光学工業株式会社 | Endoscope air supply device |
JP2558172Y2 (en) * | 1992-07-02 | 1997-12-17 | 旭光学工業株式会社 | Endoscope air supply device |
WO1997005862A3 (en) * | 1995-08-03 | 1997-04-17 | Sigma Tau Ind Farmaceuti | Use of basic amino acids and derivatives for lowering ceramide levels |
US10023574B2 (en) | 2002-08-21 | 2018-07-17 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
US10202383B2 (en) | 2002-08-21 | 2019-02-12 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
JP2006524199A (en) * | 2003-04-24 | 2006-10-26 | ロレアル | Cosmetic peeling method |
US11084819B2 (en) | 2006-05-04 | 2021-08-10 | Boehringer Ingelheim International Gmbh | Polymorphs |
US11291668B2 (en) | 2006-05-04 | 2022-04-05 | Boehringer Ingelheim International Gmbh | Uses of DPP IV inhibitors |
US10080754B2 (en) | 2006-05-04 | 2018-09-25 | Boehringer Ingelheim International Gmbh | Uses of DPP IV inhibitors |
US11033552B2 (en) | 2006-05-04 | 2021-06-15 | Boehringer Ingelheim International Gmbh | DPP IV inhibitor formulations |
US11919903B2 (en) | 2006-05-04 | 2024-03-05 | Boehringer Ingelheim International Gmbh | Polymorphs |
US10301313B2 (en) | 2006-05-04 | 2019-05-28 | Boehringer Ingelheim International Gmbh | Polymorphs |
US8440172B2 (en) | 2007-07-09 | 2013-05-14 | Symrise Ag | Stable soluble salts of phenylbenzimidazole sulfonic acid at PHS at or below 7.0 |
US10022379B2 (en) | 2008-04-03 | 2018-07-17 | Boehringer Ingelheim International Gmbh | DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation |
US10973827B2 (en) | 2008-04-03 | 2021-04-13 | Boehringer Ingelheim International Gmbh | DPP-IV inhibitor combined with a further antidiabetic agent, tablets comprising such formulations, their use and process for their preparation |
US10034877B2 (en) | 2008-08-06 | 2018-07-31 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients inappropriate for metformin therapy |
US11911388B2 (en) | 2008-10-16 | 2024-02-27 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral or non-oral antidiabetic drug |
US10092571B2 (en) | 2009-11-27 | 2018-10-09 | Boehringer Ingelheim International Gmbh | Treatment of genotyped diabetic patients with DPP-IV inhibitors such as linagliptin |
US10004747B2 (en) | 2010-05-05 | 2018-06-26 | Boehringer Ingelheim International Gmbh | Combination therapy |
US11911387B2 (en) | 2010-11-15 | 2024-02-27 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
US10195203B2 (en) | 2012-05-14 | 2019-02-05 | Boehringr Ingelheim International GmbH | Use of a DPP-4 inhibitor in podocytes related disorders and/or nephrotic syndrome |
JP2014097934A (en) * | 2012-11-13 | 2014-05-29 | Ajinomoto Co Inc | Cosmetic composition containing acetate of amino acid compound |
US10921333B2 (en) | 2013-03-14 | 2021-02-16 | Siemens Healthcare Diagnostics Inc. | Control of pH in aqueous urea-containing solutions utilizing amino acid-containing compositions |
US10073104B2 (en) | 2013-03-14 | 2018-09-11 | Siemens Healthcare Diagnostics Inc. | Control of pH in aqueous urea-containing solutions utilizing amino acid-containing compositions |
US11921124B2 (en) | 2013-03-14 | 2024-03-05 | Siemens Healthcare Diagnostics Inc. | Control of pH in aqueous urea-containing solutions utilizing amino acid-containing compositions |
US10155000B2 (en) | 2016-06-10 | 2018-12-18 | Boehringer Ingelheim International Gmbh | Medical use of pharmaceutical combination or composition |
Also Published As
Publication number | Publication date |
---|---|
JPH0531540B2 (en) | 1993-05-12 |
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