JPS58134033A - Drug composition - Google Patents
Drug compositionInfo
- Publication number
- JPS58134033A JPS58134033A JP1606782A JP1606782A JPS58134033A JP S58134033 A JPS58134033 A JP S58134033A JP 1606782 A JP1606782 A JP 1606782A JP 1606782 A JP1606782 A JP 1606782A JP S58134033 A JPS58134033 A JP S58134033A
- Authority
- JP
- Japan
- Prior art keywords
- cinnarizine
- drug
- acidic substance
- stable
- drug composition
- 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.)
- Pending
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
この発明は溶解性の改善された経ロ投与用医薬イ：１１
成物に関するものであり、さらに詳しくはシンｐ ＩＪ
レジン酸性物質を添加してなる医薬組成物に関するもの
である。DETAILED DESCRIPTION OF THE INVENTION The present invention provides a pharmaceutical drug for oral administration with improved solubility.
For more details, refer to Symp IJ
The present invention relates to a pharmaceutical composition containing a resin acidic substance.
塩基性薬物であるシンナリジンが経［１投与された場合
、薬物の溶解度が個人の胃内ｐＨ値の変動により影響を
受け、したがって薬物の安定した吸収および薬効の発現
を期待し難いという問題がある。When cinnarizine, a basic drug, is administered orally, there is a problem in that the solubility of the drug is affected by fluctuations in the individual's gastric pH value, and therefore it is difficult to expect stable absorption of the drug and development of its medicinal efficacy. .
この発明の発明者らは、この問題を解決すべく鋭意研究
の結翠、シンナリジンに酸性物質を添加して得られる医
薬組成物は、胃内ｐＨ値が変動しても、薬物の溶解度が
安定していることを見出し、この発明を完成した。In order to solve this problem, the inventors of the present invention have conducted extensive research to develop a pharmaceutical composition obtained by adding an acidic substance to cinnarizine, which maintains stable drug solubility even when the pH value in the stomach fluctuates. discovered that this was the case, and completed this invention.
この発明の医薬組成物は、シンナリジンに酸性物質を添
加した組成物からなる。The pharmaceutical composition of this invention consists of a composition in which an acidic substance is added to cinnarizine.
シンナリジンは次の化学構造式で表わされる脳血管拡張
薬である。Cinnarizine is a cerebral vasodilator represented by the following chemical structure.
シンナリジンに添加される酸性物質は非毒性の固形物質
であればよく、具体的には酒石酸、クエン酸、サリチル
酸、フマル酸、リンゴ酸、コハク酸などの有機酸類、リ
ン酸−プトリウム、リン酸−カリウムなどの無機塩類、
トリプトファン、イソロイシンなどのアミノ酸およびそ
の塩類などが例示される。シンナリジンと酸性物質との
配合割合は、特に限定されるものでなく、酸性物質の種
類に応じて適宜定め得る。The acidic substance added to cinnarizine may be any non-toxic solid substance, and specifically includes organic acids such as tartaric acid, citric acid, salicylic acid, fumaric acid, malic acid, and succinic acid, phosphoric acid, putrium, and phosphoric acid. Inorganic salts such as potassium,
Examples include amino acids such as tryptophan and isoleucine, and salts thereof. The blending ratio of cinnarizine and acidic substance is not particularly limited, and can be determined as appropriate depending on the type of acidic substance.
両成分が配合されてなる医薬組成物は、通常のこの発明
の医薬組成物は、これを経口投与したときに、胃内ｐＨ
値の変動による影響を殆んど受けないため、消化管内で
安定した溶解度を示し、したがって体内への吸収および
賛助の発現も安定しているというすぐれた効果を奏する
。A pharmaceutical composition containing both components is a typical pharmaceutical composition of the present invention that, when administered orally, has a pH level in the stomach that is
Since it is almost unaffected by fluctuations in value, it exhibits stable solubility in the gastrointestinal tract, and therefore has the excellent effect of stable absorption into the body and stable expression of support.
次に、この発明を実施例によシ説明する。Next, the present invention will be explained using examples.
実施例１ シンナリジン ２５η 酒石酸 ２００〜 両成分を混合粉砕してカプセルに充填する。Example 1 Cinnarizine 25η Tartaric acid 200~ Both ingredients are mixed and ground and filled into capsules.
これをイヌに経口投与したときのシンナリジンの作消中
濃度の経時的変化を、シンナリジンの水溶液及び現在実
用されているシンナリジンのカプセル剤と対比して第１
図に示す。The first study compared the time course of the concentration of cinnarizine during oral administration to dogs with an aqueous solution of cinnarizine and a capsule form of cinnarizine currently in practical use.
As shown in the figure.
実施例２ シンナリジン ２５■ クエン酸 ２００■ 両成分を混合粉砕してカプセルに充填する。Example 2 Cinnarizine 25■ Citric acid 200■ Both ingredients are mixed and ground and filled into capsules.
第１図は、実施例１で得られたカプセル剤をイヌに経口
投与したときの薬物の血清中濃度の経時的変化を、同一
薬物の水溶液および現在実用されている同一薬物含有カ
プセル剤と対比して示すものである。
○・・・・・シンナリジン２５■含有水溶液口・・・・
・実施例１のカプセル剤
△・・・・・現在実用されているシンナリジン２５ｍノ
含有カプセル剤
特許出願人 国立衛生試験所
藤沢薬品工業株式会社Figure 1 shows the change over time in the serum concentration of the drug when the capsule obtained in Example 1 was orally administered to dogs, and is compared with an aqueous solution of the same drug and capsules containing the same drug currently in practical use. This is shown below. ○・・・Aqueous solution containing cinnarizine 25■
・Capsules of Example 1 △・・・Cinnarizine 25m-containing capsules currently in practical use Patent applicant National Institutes of Health Fujisawa Pharmaceutical Co., Ltd.
Claims (1)
範囲第１項記載の医薬組成物(2) The pharmaceutical composition according to claim 1, wherein the acidic substance is tartaric acid or citric acid.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1606782A JPS58134033A (en) | 1982-02-02 | 1982-02-02 | Drug composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1606782A JPS58134033A (en) | 1982-02-02 | 1982-02-02 | Drug composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS58134033A true JPS58134033A (en) | 1983-08-10 |
Family
ID=11906219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1606782A Pending JPS58134033A (en) | 1982-02-02 | 1982-02-02 | Drug composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS58134033A (en) |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH03112928A (en) * | 1989-09-25 | 1991-05-14 | Otsuka Pharmaceut Co Ltd | Pharmaceutical composition improved in absorbability |
| WO2003074032A1 (en) * | 2002-03-07 | 2003-09-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Oral administration form for difficulty soluble basic active ingredients which are applied orally |
| US7932273B2 (en) | 2003-08-29 | 2011-04-26 | Boehringer Ingelheim International Gmbh | 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl) phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methansulfonate and its use as a medicament |
| EP1485094B1 (en) * | 2002-03-07 | 2012-07-04 | Boehringer Ingelheim International GmbH | Dosage form for oral administration of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazol-5-carbonyl)-pyridin-2-yl-amino] propionic acid ethyl ester or its salts |
| US9468639B2 (en) | 2001-10-20 | 2016-10-18 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| US9546141B2 (en) | 2008-12-15 | 2017-01-17 | Sprout Pharmaceuticals, Inc. | Salts |
| US9730927B2 (en) | 2005-08-03 | 2017-08-15 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
| US9763936B2 (en) | 2006-06-30 | 2017-09-19 | Sprout Pharmaceuticals, Inc. | Flibanserin for the treatment of urinary incontinence and related diseases |
| US9925174B2 (en) | 2002-03-07 | 2018-03-27 | Boehringer Ingelheim International Gmbh | Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonyl-amino-imino-methyl)-phenylamino]-methyl}-1-methyl-1 H-benzimidazol acid ethyl ester and the salts thereof |
| US10166230B2 (en) | 2007-09-12 | 2019-01-01 | Sprout Pharmaceuticals Inc. | Treatment of vasomotor symptoms |
| WO2020045607A1 (en) | 2018-08-31 | 2020-03-05 | アステラス製薬株式会社 | Pharmaceutical composition for oral administration |
| US10675280B2 (en) | 2001-10-20 | 2020-06-09 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
-
1982
- 1982-02-02 JP JP1606782A patent/JPS58134033A/en active Pending
Cited By (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH03112928A (en) * | 1989-09-25 | 1991-05-14 | Otsuka Pharmaceut Co Ltd | Pharmaceutical composition improved in absorbability |
| US9782403B2 (en) | 2001-10-20 | 2017-10-10 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| US9468639B2 (en) | 2001-10-20 | 2016-10-18 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| US10675280B2 (en) | 2001-10-20 | 2020-06-09 | Sprout Pharmaceuticals, Inc. | Treating sexual desire disorders with flibanserin |
| WO2003074032A1 (en) * | 2002-03-07 | 2003-09-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Oral administration form for difficulty soluble basic active ingredients which are applied orally |
| JP2005526738A (en) * | 2002-03-07 | 2005-09-08 | ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト | Dosage form for oral administration of drugs with low solubility |
| EP1818047A2 (en) * | 2002-03-07 | 2007-08-15 | Boehringer Ingelheim Pharma GmbH & Co. KG | Oral administration form for difficulty soluble basic active ingredients |
| EP1818047A3 (en) * | 2002-03-07 | 2008-08-06 | Boehringer Ingelheim Pharma GmbH & Co. KG | Oral administration form for difficulty soluble basic active ingredients |
| EP1485094B1 (en) * | 2002-03-07 | 2012-07-04 | Boehringer Ingelheim International GmbH | Dosage form for oral administration of 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazol-5-carbonyl)-pyridin-2-yl-amino] propionic acid ethyl ester or its salts |
| HRP20040807B1 (en) * | 2002-03-07 | 2014-11-21 | Boehringer Ingelheim International Gmbh | Oblik etil estera form of presentation for 3-[(2-{[4-(hexyloxycarbonylamino-imino-methyl)-phenylamino]-methyl}-1-methyl-1h-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionic acid ethyl ester to be administered orally |
| US9925174B2 (en) | 2002-03-07 | 2018-03-27 | Boehringer Ingelheim International Gmbh | Administration form for the oral application of 3-[(2-{[4-(hexyloxycarbonyl-amino-imino-methyl)-phenylamino]-methyl}-1-methyl-1 H-benzimidazol acid ethyl ester and the salts thereof |
| US7932273B2 (en) | 2003-08-29 | 2011-04-26 | Boehringer Ingelheim International Gmbh | 3-[(2-{[4-(hexyloxycarbonylaminoiminomethyl) phenylamino]methyl}-1-methyl-1H-benzimidazol-5-carbonyl)pyridin-2-ylamino]propionic acid ethylester methansulfonate and its use as a medicament |
| US9730927B2 (en) | 2005-08-03 | 2017-08-15 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
| US10335407B2 (en) | 2005-08-03 | 2019-07-02 | Sprout Pharmaceuticals, Inc. | Use of flibanserin in the treatment of obesity |
| US10874668B2 (en) | 2005-08-03 | 2020-12-29 | Sprout Pharmaceuticals, Inc. | Use of Flibanserin in the treatment of obesity |
| US9763936B2 (en) | 2006-06-30 | 2017-09-19 | Sprout Pharmaceuticals, Inc. | Flibanserin for the treatment of urinary incontinence and related diseases |
| US10004731B2 (en) | 2006-06-30 | 2018-06-26 | Sprout Pharmaceuticals, Inc. | Flibanserin for the treatment of urinary incontinence and related diseases |
| US10166230B2 (en) | 2007-09-12 | 2019-01-01 | Sprout Pharmaceuticals Inc. | Treatment of vasomotor symptoms |
| US9546141B2 (en) | 2008-12-15 | 2017-01-17 | Sprout Pharmaceuticals, Inc. | Salts |
| WO2020045607A1 (en) | 2018-08-31 | 2020-03-05 | アステラス製薬株式会社 | Pharmaceutical composition for oral administration |
| KR20210052495A (en) | 2018-08-31 | 2021-05-10 | 아스텔라스세이야쿠 가부시키가이샤 | Pharmaceutical composition for oral administration |
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