JPH02200633A - Vasodilator - Google Patents
VasodilatorInfo
- Publication number
- JPH02200633A JPH02200633A JP1873789A JP1873789A JPH02200633A JP H02200633 A JPH02200633 A JP H02200633A JP 1873789 A JP1873789 A JP 1873789A JP 1873789 A JP1873789 A JP 1873789A JP H02200633 A JPH02200633 A JP H02200633A
- Authority
- JP
- Japan
- Prior art keywords
- blood
- vasodilator
- hydrochloride
- nitro compound
- formula
- 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
- 229940124549 vasodilator Drugs 0.000 title claims abstract description 8
- 239000003071 vasodilator agent Substances 0.000 title claims abstract description 8
- 150000002828 nitro derivatives Chemical class 0.000 claims abstract description 14
- UOTMYNBWXDUBNX-UHFFFAOYSA-N 1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxyisoquinolin-2-ium;chloride Chemical compound Cl.C1=C(OC)C(OC)=CC=C1CC1=NC=CC2=CC(OC)=C(OC)C=C12 UOTMYNBWXDUBNX-UHFFFAOYSA-N 0.000 claims abstract description 12
- 229960003207 papaverine hydrochloride Drugs 0.000 claims abstract description 11
- 238000010521 absorption reaction Methods 0.000 claims abstract description 10
- 238000002156 mixing Methods 0.000 claims abstract description 5
- 210000004204 blood vessel Anatomy 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 7
- SNIOPGDIGTZGOP-UHFFFAOYSA-N Nitroglycerin Chemical compound [O-][N+](=O)OCC(O[N+]([O-])=O)CO[N+]([O-])=O SNIOPGDIGTZGOP-UHFFFAOYSA-N 0.000 abstract description 6
- 239000008280 blood Substances 0.000 abstract description 6
- 210000004369 blood Anatomy 0.000 abstract description 6
- 229960003711 glyceryl trinitrate Drugs 0.000 abstract description 5
- 210000003205 muscle Anatomy 0.000 abstract description 4
- 239000000006 Nitroglycerin Substances 0.000 abstract description 3
- 230000002195 synergetic effect Effects 0.000 abstract description 3
- YWXYYJSYQOXTPL-JGWLITMVSA-N [(3r,3ar,6s,6as)-3-hydroxy-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan-6-yl] nitrate Chemical compound [O-][N+](=O)O[C@H]1CO[C@@H]2[C@H](O)CO[C@@H]21 YWXYYJSYQOXTPL-JGWLITMVSA-N 0.000 abstract description 2
- 230000005856 abnormality Effects 0.000 abstract description 2
- 201000001881 impotence Diseases 0.000 abstract description 2
- -1 nitroglycerin or 1 Chemical class 0.000 abstract 1
- 230000001737 promoting effect Effects 0.000 abstract 1
- 230000002792 vascular Effects 0.000 description 6
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 4
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 4
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 4
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000004744 fabric Substances 0.000 description 3
- 210000002464 muscle smooth vascular Anatomy 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- ATHHXGZTWNVVOU-UHFFFAOYSA-N N-methylformamide Chemical compound CNC=O ATHHXGZTWNVVOU-UHFFFAOYSA-N 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 230000000916 dilatatory effect Effects 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000002107 myocardial effect Effects 0.000 description 2
- 210000004165 myocardium Anatomy 0.000 description 2
- 239000003883 ointment base Substances 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 230000036513 peripheral conductance Effects 0.000 description 2
- 239000004033 plastic Substances 0.000 description 2
- 229920003023 plastic Polymers 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 230000036316 preload Effects 0.000 description 2
- 210000002460 smooth muscle Anatomy 0.000 description 2
- 210000005166 vasculature Anatomy 0.000 description 2
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 208000015163 Biliary Tract disease Diseases 0.000 description 1
- 206010006784 Burning sensation Diseases 0.000 description 1
- 206010007556 Cardiac failure acute Diseases 0.000 description 1
- 206010065559 Cerebral arteriosclerosis Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 208000007882 Gastritis Diseases 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 208000007101 Muscle Cramp Diseases 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 239000004264 Petrolatum Substances 0.000 description 1
- 208000034189 Sclerosis Diseases 0.000 description 1
- 208000005392 Spasm Diseases 0.000 description 1
- 239000002390 adhesive tape Substances 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 210000001367 artery Anatomy 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 230000004087 circulation Effects 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 201000005851 intracranial arteriosclerosis Diseases 0.000 description 1
- 230000000302 ischemic effect Effects 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 229940056211 paraffin Drugs 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 210000003899 penis Anatomy 0.000 description 1
- 230000003836 peripheral circulation Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 229940066842 petrolatum Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- CSIGAEASXSGNKS-UHFFFAOYSA-N propane-1,1,3-triol Chemical compound OCCC(O)O CSIGAEASXSGNKS-UHFFFAOYSA-N 0.000 description 1
- 210000001147 pulmonary artery Anatomy 0.000 description 1
- 230000002040 relaxant effect Effects 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 239000002195 soluble material Substances 0.000 description 1
- 239000006190 sub-lingual tablet Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 235000019605 sweet taste sensations Nutrition 0.000 description 1
- 230000024883 vasodilation Effects 0.000 description 1
- 230000002861 ventricular Effects 0.000 description 1
- 230000009278 visceral effect Effects 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
Landscapes
- Health & Medical Sciences (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
〈産業上の利用分野〉
本発明は、血管拡張剤に関し、特に経皮吸収型血管拡張
剤に係る。DETAILED DESCRIPTION OF THE INVENTION <Industrial Field of Application> The present invention relates to a vasodilator, and particularly to a transdermal vasodilator.
〈従来技術、〉 従来、各種の血管拡張剤が知られている。<Prior art> Conventionally, various vasodilators are known.
ここで、塩酸パパベリンとニトロ化合物について説明す
る。Here, papaverine hydrochloride and nitro compounds will be explained.
塩酸パパベリンは、一般に胃炎、胆道系疾患に伴う内臓
平滑筋のけいれん症状、脳動脈硬化症の随伴症状、末梢
循環障害、冠循環障害における血管拡張と症状の改善等
に使用されている。Papaverine hydrochloride is generally used for gastritis, visceral smooth muscle spasm symptoms associated with biliary tract diseases, accompanying symptoms of cerebral arteriosclerosis, vasodilation and symptom improvement in peripheral circulation disorders, coronary circulation disorders, and the like.
ニトロ化合物は、狭心症、心筋梗塞、起硬化症、急性心
不全等に使用されている。Nitro compounds are used for angina pectoris, myocardial infarction, sclerosis, acute heart failure, and the like.
〈 発明が解決しようとする課題 〉
上記のように、塩酸パパベリンおよびニトロ化合物には
、その効果には優れたものがある。しかし、塩酸パパベ
リンおよびニトロ化合物の注射剤は、いずれも長時間に
わたって点滴静注されるので、これを長期連用すること
は患者にとって負担となる場合がある。<Problems to be Solved by the Invention> As described above, papaverine hydrochloride and nitro compounds have excellent effects. However, since both papaverine hydrochloride and nitro compound injections are intravenously infused over a long period of time, long-term use may be burdensome for patients.
また、これらの内服剤を長期連用すると、耐薬性が生じ
投与量を増加しなければ効果を得ることができない場合
が生じる。特に、ニトログリセリンの舌下錠においては
、顕著に現われる。Furthermore, if these oral preparations are used continuously for a long period of time, drug resistance may develop and the effects may not be obtained unless the dosage is increased. This is particularly noticeable in sublingual nitroglycerin tablets.
さらに、その他種々問題点がある。Furthermore, there are various other problems.
そこで、本発明は、上記課題を解消することを目的とす
る。Therefore, an object of the present invention is to solve the above problems.
〈実施例〉
［発明の構成］
本発明は、塩酸パバベリンとニトロ化合物とを経皮吸収
基剤（軟膏基剤）により混合して成るものである。<Example> [Structure of the Invention] The present invention is made by mixing pavaberine hydrochloride and a nitro compound using a transdermal absorption base (ointment base).
（１）塩酸パバベリン
（ａ）構造式および性状
組成式ＣｔｏＨ２＋ＮＯ＋ＩＨＣＩ（分子量・３７５８
５）、一般式
で示される１−（３，４−ジメトキシベンジル）６７−
シメトキシイソキノリンヒドロクロライドである。白色
の結晶または結晶性粉末で、臭いはなく、味は苦い。ク
ロロホルムにやや溶けやすく、水にやや溶けに＜＜、エ
タノールに溶けにくく、エーテルに殆ど溶けない。なお
、水溶液（ｌ→５０）のｐＨは３．０〜４０で、融点は
２２０〜２２５度である。(1) Pavaverine hydrochloride (a) Structural formula and properties Compositional formula CtoH2+NO+IHCI (molecular weight: 3758
5), 1-(3,4-dimethoxybenzyl)67- represented by the general formula
It is cymethoxyisoquinoline hydrochloride. White crystals or crystalline powder, odorless, bitter taste. Slightly soluble in chloroform, slightly soluble in water, slightly soluble in ethanol, almost insoluble in ether. In addition, the pH of the aqueous solution (l→50) is 3.0 to 40, and the melting point is 220 to 225 degrees.
（ｂ）薬効、薬理と特徴
各種の平滑筋、特に血管筋を弛緩させる。この作用は、
筋の緊張がすでに上昇しているときに著しく、緊張が正
常な場合には弛緩作用を現わさな張力の減少と心筋酸素
消費量の減少をもたらす。(b) Medicinal efficacy, pharmacology and characteristics Relaxes various smooth muscles, especially vascular muscles. This effect is
Significantly when the muscle tone is already elevated, it results in a decrease in tension and a decrease in myocardial oxygen consumption, which does not have a relaxing effect when the tone is normal.
また、直接血管平滑筋に作用し、低容量では静脈血管の
、高容量では静脈および動脈血管の拡張作用を示すとさ
れているが、この機序に関しては、細胞外へのＣａＩ排
出を促進し、細胞内Ｃａ”濃度を低くして血管平滑筋を
弛緩させるのが、その主な作用と考えられる。It also acts directly on vascular smooth muscle, and is said to dilate venous blood vessels at low volumes, and dilate venous and arterial blood vessels at high volumes. Its main action is thought to be to lower intracellular Ca'' concentration and relax vascular smooth muscle.
（Ｂ）硝酸イソソルビド
（ａ）構造式および性状
組成式Ｃ８Ｈｓ Ｎ ２０ ｓ （分子量；２３６．１
４）、般式
で示される１、４．３．６−ジアンヒドロ−Ｄ−グリチ
トールジニトレートである。白色の結晶また（２）ニト
ロ化合物
（Ａ）ニトログリセリン
（ａ）構造式および性状
組成式Ｃ３Ｈｓ Ｎ 、Ｏｓ （分子量；２２７．０９
）、般式
％式％
で示されるグリセリルトリニトレートまたは■２．３−
プロパントリオールトリニトレートである。常温で無色
透明の粘調性の液体で、味は甘く灼熱感があり、衝撃に
より爆発する。なお、沸点は１８０度以上（分解を伴う
）である。(B) Isosorbide nitrate (a) Structural formula and properties Compositional formula C8Hs N 20 s (molecular weight; 236.1
4), 1,4.3.6-dianhydro-D-glytitol dinitrate represented by the general formula. White crystals (2) Nitro compound (A) Nitroglycerin (a) Structural formula and properties Composition formula C3Hs N , Os (molecular weight; 227.09
), glyceryl trinitrate represented by the general formula % formula % or ■2.3-
Propanetriol trinitrate. It is a viscous liquid that is colorless and transparent at room temperature, has a sweet taste and a burning sensation, and explodes on impact. Note that the boiling point is 180 degrees or higher (accompanied by decomposition).
（ｂ）薬効、薬理と特徴
容量血管系および拡張血管系を拡張させ、静脈還流量と
末梢血管抵抗を減少させる。この作用は心室の前負荷と
後負荷を共に低下させるため心筋は結晶性粉末で臭いは
ないか、またわずかに硝酸臭がある。アセトンまたはン
メチルホルムアミドに極めて易溶、クロロホルムまたは
トルエンに易溶、メタノール、エタノールまたはエーテ
ルにやや易溶、水に殆ど不溶である。なお、融点は約７
０度である。(b) Drug efficacy, pharmacology and characteristics Dilates the capacitive vasculature and dilated vasculature, reducing venous return and peripheral vascular resistance. This action reduces both the preload and afterload of the ventricles, so the myocardium is a crystalline powder with no odor or a slight nitric acid odor. Very easily soluble in acetone or methylformamide, easily soluble in chloroform or toluene, slightly soluble in methanol, ethanol or ether, almost insoluble in water. In addition, the melting point is approximately 7
It is 0 degrees.
（ｂ）薬効、薬理と特徴
静脈系容量血管を拡張することにより、静脈環流の減少
、肺動脈楔入圧および左室拡張終期圧の低下（前負荷の
軽減）をもたらし、同時に末梢動脈を拡張して、総末梢
血管抵抗を減少（後負荷の軽減）させることにより心筋
の酸素需要を軽減させる。(b) Medicinal efficacy, pharmacology and characteristics By dilating the capacitance vessels of the venous system, it reduces venous return, reduces pulmonary artery wedge pressure and left ventricular end-diastolic pressure (reduces preload), and at the same time dilates peripheral arteries. This reduces myocardial oxygen demand by reducing total peripheral vascular resistance (reducing afterload).
また、血管平滑筋に直接作用して血管を拡張するが、比
較的太い冠動脈を拡張し、冠血管抵抗を減少させるとと
もに側副血管路も拡張し、虚血部心筋への酸素供給を増
加させる。その効果はニトログリセリンよりも弱いが、
持続は長い。It also dilates blood vessels by acting directly on vascular smooth muscles, dilating relatively large coronary arteries, reducing coronary vascular resistance, and expanding collateral vascular channels, increasing oxygen supply to ischemic myocardium. . Its effect is weaker than that of nitroglycerin, but
It lasts a long time.
（３）経皮吸収基剤（軟膏基剤）
基剤としては、一般に脂肪、脂肪酸、ラノリン、ワセリ
ン、パラフィン、ロウ、樹脂、プラスチック、グリコー
ル類、高級アルコール、グリセリン、水、名代剤、懸濁
剤が用いられており、本実施例では、ポリアクリル酸ナ
トリウム等を使用する。(3) Transdermal absorption base (ointment base) Bases generally include fats, fatty acids, lanolin, petrolatum, paraffin, wax, resins, plastics, glycols, higher alcohols, glycerin, water, generic agents, and suspensions. A clouding agent is used, and in this example, sodium polyacrylate or the like is used.
［製造方法コ
（第１法）
ロールミル、ニーダ、襠潰機、混合機等により塩酸パパ
ベリンおよびニトロ化合物を経皮吸収基剤（ポリアクリ
ル酸ナトリウム等）の一部と混合研和したのち、残りの
経皮吸収基剤を加えて全質均等として製する。[Manufacturing method 1 (method 1) After mixing papaverine hydrochloride and a nitro compound with a part of the transdermal absorption base (sodium polyacrylate, etc.) using a roll mill, kneader, crusher, mixer, etc., the remaining A transdermal absorption base is added to make the whole product homogeneous.
（第２法）
水溶材の襠潰機、混合機、三本ローラー等を利用して経
皮吸収基剤（ポリアクリル酸ナトリウム等）の成分のう
ち、溶けやすいものから順次溶かして塩酸パパベリンお
よびニトロ化合物と混和する。これを固まるまで混ぜて
製する。(Method 2) Using a water-soluble material crusher, mixer, triple roller, etc., dissolve papaverine hydrochloride and Miscible with nitro compounds. Mix this until it solidifies.
なお、塩酸パパベリン、ニトロ化合物および経皮吸収基
剤（ポリアクリル酸ナトリウム等）の混合率は、例えば
基剤１００ｍｇ中、塩酸パパベリン７５ ｍｇ、ニトロ
化合物にトログリセリン）２０ｍｇ。The mixing ratio of papaverine hydrochloride, the nitro compound, and the transdermal absorption base (sodium polyacrylate, etc.) is, for example, 75 mg of papaverine hydrochloride and 20 mg of the nitro compound and troglycerin in 100 mg of the base.
経皮吸収基剤（ポリアクリル酸ナトリウム等）５ｍｇに
て混合される。5 mg of a transdermal absorption base (sodium polyacrylate, etc.) is mixed.
［使用方法］
（１）目盛り付き測定用紙または、基布等に長さを測り
ながら押し出す。基剤（軟膏）を薄い均一な層になるよ
うに用紙または基布に広げ、腕や胸部のやわらかい皮膚
上に貼付し、絆創膏または、プラスチックラップで固定
する。[How to use] (1) Measure the length and extrude onto a calibrated measuring paper or base fabric. Spread the base (ointment) on paper or base cloth in a thin, even layer, apply it to the soft skin of the arm or chest, and secure with a bandage or plastic wrap.
（２）基剤（軟膏）を予め貼着テープ剤付きの用紙また
は基布に薄く均一に塗布し、やわらかい皮膚上に貼付し
て固定する。なお、前面被覆面は紙等により被覆する。(2) A base (ointment) is applied thinly and uniformly to paper or base cloth with an adhesive tape, and the base is pasted and fixed onto the soft skin. Note that the front surface is covered with paper or the like.
〈発明の効果〉
以上の説明から明らかな通り、本発明によると、特に心
臓疾患を有する患者に基剤を使用することにより、その
発作時等においてニトログリセリンの舌下錠の服用回数
、投与量を減少させ、かつ舌下錠服用時においてその効
果を少量の投与量によりその効果を助長することができ
る。<Effects of the Invention> As is clear from the above explanation, according to the present invention, by using a base material, the frequency and dosage of sublingual nitroglycerin tablets can be reduced during attacks, etc., especially for patients with heart disease. When taking sublingual tablets, the effect can be enhanced by a small dose.
＝７
また、基剤を経皮吸収型（軟膏）としているので、患者
の疾病の重篤塵に応じて投与量を簡単に調整できる。=7 Furthermore, since the base is a transdermal absorption type (ointment), the dosage can be easily adjusted depending on the severity of the patient's disease.
さらに、基剤は、血管筋を弛緩させる塩酸バパベリンと
、血管系を拡張させ血管抵抗を減少させるニトロ化合物
とが含有されているので、その相乗効果により血管内へ
の血液の流入を促進し、特に、陰茎の血管に異常がない
場合のインポテンスの治療に優れた効果がある。Furthermore, the base contains bapaverine hydrochloride, which relaxes vascular muscles, and a nitro compound, which dilates the vascular system and reduces vascular resistance, so their synergistic effect promotes the inflow of blood into the blood vessels. It is particularly effective in treating impotence when there is no abnormality in the blood vessels in the penis.
Claims (1)
混合して成る血管拡張剤。A vasodilator made by mixing papaverine hydrochloride and a nitro compound with a transdermal absorption base.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1873789A JPH02200633A (en) | 1989-01-27 | 1989-01-27 | Vasodilator |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1873789A JPH02200633A (en) | 1989-01-27 | 1989-01-27 | Vasodilator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH02200633A true JPH02200633A (en) | 1990-08-08 |
Family
ID=11979984
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1873789A Pending JPH02200633A (en) | 1989-01-27 | 1989-01-27 | Vasodilator |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH02200633A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0934744A1 (en) * | 1998-01-30 | 1999-08-11 | Futura Medical Limited | Nitroglycerin preparation for treatment of erectile dysfunction |
| WO1999059575A1 (en) * | 1998-05-18 | 1999-11-25 | Baker Norton Pharmaceuticals, Inc. | Compositions comprising organic mono- or dinitrate for treating impotence |
| FR2985907A1 (en) * | 2012-01-24 | 2013-07-26 | Assist Publ Hopitaux De Paris | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ERECTILE DYSFUNCTIONS |
-
1989
- 1989-01-27 JP JP1873789A patent/JPH02200633A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0934744A1 (en) * | 1998-01-30 | 1999-08-11 | Futura Medical Limited | Nitroglycerin preparation for treatment of erectile dysfunction |
| WO1999038506A3 (en) * | 1998-01-30 | 1999-09-30 | Futura Medical Limited | Use of topical preparations of glyceryl trinitrate and lanolin for the treatment of erectile dysfunction |
| AU747085B2 (en) * | 1998-01-30 | 2002-05-09 | Futura Medical Limited | Preparation for treatment of erectile dysfunction |
| WO1999059575A1 (en) * | 1998-05-18 | 1999-11-25 | Baker Norton Pharmaceuticals, Inc. | Compositions comprising organic mono- or dinitrate for treating impotence |
| US6056966A (en) * | 1998-05-18 | 2000-05-02 | Baker Norton Pharmaceuticals, Inc. | Method and compositions for treating impotence |
| FR2985907A1 (en) * | 2012-01-24 | 2013-07-26 | Assist Publ Hopitaux De Paris | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ERECTILE DYSFUNCTIONS |
| WO2013111085A1 (en) * | 2012-01-24 | 2013-08-01 | Assistance Publique - Hopitaux De Paris | Pharmaceutical composition for the treatment of erectile dysfunction |
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