JPH02178226A - Remedy for disease accompanying raynaud's phenomenon - Google Patents
Remedy for disease accompanying raynaud's phenomenonInfo
- Publication number
- JPH02178226A JPH02178226A JP33173388A JP33173388A JPH02178226A JP H02178226 A JPH02178226 A JP H02178226A JP 33173388 A JP33173388 A JP 33173388A JP 33173388 A JP33173388 A JP 33173388A JP H02178226 A JPH02178226 A JP H02178226A
- Authority
- JP
- Japan
- Prior art keywords
- raynaud
- active ingredient
- prepared
- formula
- phenomenon
- 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
- 201000010099 disease Diseases 0.000 title claims abstract description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 10
- 208000012322 Raynaud phenomenon Diseases 0.000 title abstract description 12
- 239000004480 active ingredient Substances 0.000 claims abstract description 11
- 125000002947 alkylene group Chemical group 0.000 claims abstract description 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 4
- 239000000126 substance Substances 0.000 claims abstract 3
- 239000003814 drug Substances 0.000 claims description 9
- 229940124597 therapeutic agent Drugs 0.000 claims description 7
- 125000004106 butoxy group Chemical group [*]OC([H])([H])C([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 abstract description 18
- 238000002360 preparation method Methods 0.000 abstract description 11
- 239000002775 capsule Substances 0.000 abstract description 5
- 208000003782 Raynaud disease Diseases 0.000 abstract description 3
- 239000008187 granular material Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- RRGUKTPIGVIEKM-UHFFFAOYSA-N cilostazol Chemical compound C=1C=C2NC(=O)CCC2=CC=1OCCCCC1=NN=NN1C1CCCCC1 RRGUKTPIGVIEKM-UHFFFAOYSA-N 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 239000000829 suppository Substances 0.000 abstract 1
- 239000003826 tablet Substances 0.000 abstract 1
- 239000007788 liquid Substances 0.000 description 8
- 239000013078 crystal Substances 0.000 description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 239000001913 cellulose Substances 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000007796 conventional method Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 2
- 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 2
- 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 2
- 229930006000 Sucrose Natural products 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 229940099112 cornstarch Drugs 0.000 description 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000005720 sucrose Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 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
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 239000004278 EU approved seasoning Substances 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 239000000924 antiasthmatic agent Substances 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 229960004676 antithrombotic agent Drugs 0.000 description 1
- 239000003699 antiulcer agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000003899 bactericide agent Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000012059 conventional drug carrier Substances 0.000 description 1
- 238000005520 cutting process Methods 0.000 description 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 235000011194 food seasoning agent Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 239000000417 fungicide Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- 239000003589 local anesthetic agent Substances 0.000 description 1
- 229960005015 local anesthetics Drugs 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 206010025482 malaise Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- -1 methylene, ethylene, propylene, butylene Chemical group 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940124531 pharmaceutical excipient Drugs 0.000 description 1
- 239000008023 pharmaceutical filler Substances 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 239000002571 phosphodiesterase inhibitor Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical class C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 description 1
- RTKIYNMVFMVABJ-UHFFFAOYSA-L thimerosal Chemical compound [Na+].CC[Hg]SC1=CC=CC=C1C([O-])=O RTKIYNMVFMVABJ-UHFFFAOYSA-L 0.000 description 1
- 229940033663 thimerosal Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は例えば振動病、レイノー病などとして知られる
レイノー現象を伴う疾病の治療剤、さらに詳しくは、式
〔式中、Ｒはシクロアルキル基、Ａは低級アルキレン基
を示す〕
で表されるテトラゾリルアルコキシジヒドロカルボスチ
リル化合物を有効成分とするレイノー現象を伴う疾病の
治療剤。DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to therapeutic agents for diseases associated with Raynaud's phenomenon known as, for example, vibration disease and Raynaud's disease. represents a lower alkylene group] A therapeutic agent for diseases accompanied by Raynaud's phenomenon, which contains a tetrazolylalkoxydihydrocarbostyryl compound represented by the following as an active ingredient.
（２）該有効成分が６−（４−（１−シクロへキシルテ
トラゾール−５−イル）ブトキシ）−３，４＝ジヒドロ
カルボスチリルである請求項（１）に記載の治療剤。(2) The therapeutic agent according to claim (1), wherein the active ingredient is 6-(4-(1-cyclohexyltetrazol-5-yl)butoxy)-3,4=dihydrocarbostyryl.
３、発明の詳細な説明
〔式中、Ｒはシクロアルキル基、Ａは低級アルキレン基
を示す〕
で表されるテトラゾリルアルコキシジヒドロカルボスチ
リル化合物を有効成分とするレイノー現象を伴う疾病の
治療剤に関する。3. Detailed description of the invention [In the formula, R is a cycloalkyl group and A is a lower alkylene group] A therapeutic agent for diseases accompanied by Raynaud's phenomenon, which contains a tetrazolylalkoxydihydrocarbostyryl compound represented by the following as an active ingredient: Regarding.
疋胆Δ遣４
上記式（Ｉ）で示されるテトラゾリルアルコキシジヒド
ロカルボスチリル化合物は特公昭６３−２０２３５号に
開示されており、その詳細な製造法のほか、これらの化
合物が抗血栓剤、脳循環改善剤、消炎剤、抗潰瘍剤、降
圧剤、抗喘息剤、ホスホジエステラーゼ阻害剤などとし
て有用なことがス己載されている。The tetrazolylalkoxydihydrocarbostyryl compound represented by the above formula (I) is disclosed in Japanese Patent Publication No. 63-20235, and in addition to its detailed production method, these compounds can also be used as antithrombotic agents, It has been reported that it is useful as a cerebral circulation improving agent, anti-inflammatory agent, anti-ulcer agent, antihypertensive agent, anti-asthma agent, phosphodiesterase inhibitor, etc.
発明が解決しようとする課題
本発明者らは前記一連のカルボスチリル化合物について
他の種々の薬効を研究した結果、特定の前記式（Ｉ）で
示される化合物が優れたレイノー現象を伴う疾病の治療
効果を有することを見い出した。Problems to be Solved by the Invention As a result of research into various other medicinal effects of the series of carbostyril compounds, the present inventors have found that a particular compound represented by formula (I) is excellent in the treatment of diseases accompanied by Raynaud's phenomenon. It was found that this method is effective.
課題を解決するための手段および発明の効果本発明は、
前記式（１）で示されるテトラゾリルアルコキンノヒド
ロカルボスチリル化合物を有効成分として含存するレイ
ノー現象を伴う疾病の治療剤を提供するものである。Means for Solving the Problems and Effects of the Invention The present invention has the following features:
The present invention provides a therapeutic agent for diseases accompanied by Raynaud's phenomenon, which contains a tetrazolylalkokinohydrocarbostyryl compound represented by the formula (1) as an active ingredient.
式（１）において、シクロアルキル基としてはシクロプ
ロピル、シクロブチル、シクロペンチル、シクロヘキシ
ル、シクロヘプチル、シクロオクチルなどが挙げられ、
とくにシクロブチルか好ましい。低級アルキレン基とし
ては、メチレン、エチレン、プロピレン、ブチレンなど
が挙げられ、と（にブチレンが好ましい。In formula (1), examples of the cycloalkyl group include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, etc.
Cyclobutyl is particularly preferred. Examples of the lower alkylene group include methylene, ethylene, propylene, butylene, and butylene is preferred.
特に好ましい化合物は、６−（４−（１−シクロへキシ
ルテトラゾール−５−イル）ブトキシ〕３４−ジヒドロ
カルボスチリルである。A particularly preferred compound is 6-(4-(1-cyclohexyltetrazol-5-yl)butoxy]34-dihydrocarbostyryl.
これらの化合物は、特公昭６３”−２０２３５号に記・
戟される方法により容易に製造される。These compounds are described in Japanese Patent Publication No. 63''-20235.
It is easily produced by a method that involves cutting.
本発明で用いられる式（Ｉ）の化合物はそのままである
いは慣用の製剤担体と共に投与することができる。投与
単位形態としては特に限定がなく、必要に応じ適宜選択
して使用される。かかる投与単位形態としては、錠剤、
カプセル剤、顆粒剤、各種経口用液剤などの経口剤、注
射剤、座刑などの非経口剤などを例示できる。投与され
るべき有効成分の量としては特に限定がなく広い範囲か
ら適宜選択されるが、所期の効果を発揮するためには大
人（体重５０ｋｇ）で１００〜４００ｍＳ＋／日の用量
にて１〜数回に分けて投与するのがよい。また、投与単
位形態中に有効成分を５０〜１００ｍｇ含有仕しめるの
がよい。The compound of formula (I) used in the present invention can be administered neat or with conventional pharmaceutical carriers. The dosage unit form is not particularly limited and may be appropriately selected and used as required. Such dosage unit forms include tablets,
Examples include oral preparations such as capsules, granules, and various oral liquid preparations, parenteral preparations such as injections, and oral preparations. The amount of the active ingredient to be administered is not particularly limited and is appropriately selected from a wide range, but in order to achieve the desired effect, an adult (body weight 50 kg) should be administered at a dose of 1 to 400 mS+/day. It is best to administer the drug in several doses. Further, it is preferable that the dosage unit form contains 50 to 100 mg of the active ingredient.
本発明において錠剤、カプセル剤、経口用液剤などの経
口剤は常法に従って製造される。即ち錠剤は本発明化合
物をゼラチン、澱粉、乳糖、ステアリン酸マグネンウム
、滑石、アラビアゴムなどの製剤学的賦形剤と混合し、
賦形される。カプセル剤は、本発明化合物を不活性の製
剤充填剤もしくは希釈剤と混合し、硬質ゼラチンカプセ
ル、軟質カプセルなどに充填される。経「］用液剤のシ
ロップ剤およびエリキシル剤は本発明化合物をショ糖な
との甘味剤、メヂルーおよびプロピルパラベン類などの
防腐剤、着色剤、調味剤などと混合して製造される。ま
た非経口剤は常法にしたがって製造され、例えば、本発
明化合物を滅菌した液状担体に溶解して製造される。好
ましい担体は水または食塩水である。所望の透明度、安
定性および非経口使用の適応性を有する液剤は約５０〜
１００ｍｇの有効成分を、水および有機溶剤に溶解し、
さらに分子量２００〜５０００のポリエチレングリコー
ルに溶解して製造される。かかる液剤にはナトリウムカ
ルボキンメチルセルローズ、メチルセルローズ、ポリビ
ニルピロリドン、ポリビニルアルコールなどの潤滑剤が
配合されるのが好ましい。In the present invention, oral preparations such as tablets, capsules, and oral liquid preparations are manufactured according to conventional methods. That is, tablets are prepared by mixing the compound of the present invention with pharmaceutical excipients such as gelatin, starch, lactose, magnesium stearate, talc, gum arabic, etc.
Shaped. Capsules are prepared by mixing the compound of the present invention with an inert pharmaceutical filler or diluent, and filling the mixture into hard gelatin capsules, soft capsules, and the like. Liquid syrups and elixirs for oral administration are produced by mixing the compound of the present invention with sweeteners such as sucrose, preservatives such as medilu and propylparabens, coloring agents, seasonings, etc. Oral preparations are prepared according to conventional methods, for example, by dissolving the compound of the present invention in a sterile liquid carrier. Preferred carriers are water or saline. Desired clarity, stability and indications for parenteral use are provided. The liquid agent with the property is about 50~
100 mg of active ingredient is dissolved in water and organic solvent,
Furthermore, it is manufactured by dissolving it in polyethylene glycol having a molecular weight of 200 to 5,000. Preferably, such a liquid agent contains a lubricant such as sodium carboxyl methylcellulose, methylcellulose, polyvinylpyrrolidone, or polyvinyl alcohol.
さらには上記液剤中にベンジルアルコール、フェノール
、チメロサールなどの殺菌剤および防カビ剤、さらに必
要に応じ、ショ糖、塩化ナトリウムなどの等張剤、局所
麻酔剤、安定剤、緩衝剤などが含まれていてらよい。ま
た、非経口投与用薬剤は、その安定性の観点から、カプ
セルなどに充填後、冷凍し、通常の凍結乾燥技術により
水を除去し、使用直前に凍結乾燥粉末から液剤を再調製
することらできる。Furthermore, the above liquid preparation may contain bactericides and fungicides such as benzyl alcohol, phenol, and thimerosal, as well as isotonic agents such as sucrose and sodium chloride, local anesthetics, stabilizers, buffers, etc., as necessary. It's good to keep it. In addition, from the viewpoint of stability, drugs for parenteral administration must be filled into capsules, etc., frozen, water removed using normal freeze-drying techniques, and the liquid preparation prepared from the freeze-dried powder immediately before use. can.
臨床実験
本発明の化合物は振動器具を用いる作業に従事する作業
員などにしばしばみられる振動病や、レイノー病などの
レイノー現象を伴う疾病に対して有効である。それらの
効果について臨床実験結果を下記に示す。Clinical Experiment The compound of the present invention is effective against vibration sickness often seen in workers who use vibrating instruments, and diseases accompanied by Raynaud's phenomenon such as Raynaud's disease. The results of clinical experiments regarding these effects are shown below.
実験は、レイノー現象を示す６６歳の男性（！ｌ’。The experiment was conducted on a 66-year-old man who exhibits Raynaud's phenomenon (!l').
者Ａ）および６１歳の男性（患者Ｂ）に、それぞれ、６
−［４−（１−シクロへキシルテトラゾール−５イル）
ブトキシ］−３，４−ジヒドロカルボスチリル１００ｍ
ｇを含打する錠剤を朝夕２回４週間にわたって経口投与
し、種々の症状の改善度を調べた。その結果を第１表に
示す。patient A) and a 61-year-old man (patient B), respectively.
-[4-(1-cyclohexyltetrazol-5yl)
butoxy]-3,4-dihydrocarbostyryl 100m
Tablets impregnated with G were orally administered twice in the morning and evening for 4 weeks, and the degree of improvement in various symptoms was examined. The results are shown in Table 1.
第１表において症状の程度は下記基準にしたがって評価
した。In Table 1, the severity of symptoms was evaluated according to the following criteria.
０： 全くなし
ｌ： 軽度に認められた
２： 中程度認められた
３： 昔しい程度で認められた
製剤例
錠剤の調製
配 合 量（９）
６−（３−（１−シクロヘキシル
テトラゾール−５−イル）ブトキ
シ）−３，４−ノヒドロカルホス
チリル １００乳ｎ（日本
薬局方晶）４０
コーンスターチ（日本薬局方晶）２０
結晶セルローズ（日本薬局方晶）２０
ヒドロキノプロピルセルローズ
（日本薬局方晶） ４ステア
リン酸マグネシウム（日本
薬局方晶） ２上記本
発明の化合物、乳糖、コーンスターチおよび結晶セルロ
ーズを充分混合し、ヒドロキシプロピルセルローズの５
％水溶液で顆粒化し、２００メツシユの篩に通して注意
深く乾燥し、これを常法により打錠して錠剤ｉ ｏｏｏ
綻を調製する。0: None at all 1: Slightly observed 2: Moderately observed 3: Observed to an old degree Preparation example of tablets Amount (9)
6-(3-(1-Cyclohexyltetrazol-5-yl)butoxy)-3,4-nohydrocarfostyryl 100 Milk n (Japanese Pharmacopoeia Crystal) 40 Cornstarch (Japanese Pharmacopoeia Crystal) 20 Crystalline Cellulose (Japanese Pharmacopoeia Crystal) 20 Hydroquinopropyl cellulose (Japanese Pharmacopoeia crystal) 4 Magnesium stearate (Japanese Pharmacopoeia crystal) 2 The above compound of the present invention, lactose, cornstarch and crystalline cellulose are thoroughly mixed, and hydroxypropyl cellulose 5
% aqueous solution, carefully dried through a 200 mesh sieve, and compressed into tablets by a conventional method to form tablets i ooo
Prepare the solution.
Claims (2)
を示す〕 で表されるテトラゾリルアルコキシジヒドロカルボスチ
リル化合物を有効成分とするレイノー現象を伴う疾病の
治療剤。(1) Formula ▲ There are mathematical formulas, chemical formulas, tables, etc. ▼ [In the formula, R is a cycloalkyl group and A is a lower alkylene group] A therapeutic agent for diseases accompanied by this phenomenon.
トラゾール−５−イル）ブトキシ〕−３，４−ジヒドロ
カルボスチリルである請求項（１）に記載の治療剤。(2) The therapeutic agent according to claim (1), wherein the active ingredient is 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydrocarbostyryl.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP33173388A JPH02178226A (en) | 1988-12-28 | 1988-12-28 | Remedy for disease accompanying raynaud's phenomenon |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP33173388A JPH02178226A (en) | 1988-12-28 | 1988-12-28 | Remedy for disease accompanying raynaud's phenomenon |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH02178226A true JPH02178226A (en) | 1990-07-11 |
Family
ID=18246994
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP33173388A Pending JPH02178226A (en) | 1988-12-28 | 1988-12-28 | Remedy for disease accompanying raynaud's phenomenon |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH02178226A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7825251B2 (en) | 2001-05-02 | 2010-11-02 | Otsuka Pharmaceutical Co., Ltd. | Process for producing carbostyril derivatives |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5646810A (en) * | 1979-09-25 | 1981-04-28 | Otsuka Pharmaceut Co Ltd | Blood platelet coagulation inhibitor |
-
1988
- 1988-12-28 JP JP33173388A patent/JPH02178226A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5646810A (en) * | 1979-09-25 | 1981-04-28 | Otsuka Pharmaceut Co Ltd | Blood platelet coagulation inhibitor |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7825251B2 (en) | 2001-05-02 | 2010-11-02 | Otsuka Pharmaceutical Co., Ltd. | Process for producing carbostyril derivatives |
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