JPH0344324A - Sexual function invigorator - Google Patents
Sexual function invigoratorInfo
- Publication number
- JPH0344324A JPH0344324A JP18086789A JP18086789A JPH0344324A JP H0344324 A JPH0344324 A JP H0344324A JP 18086789 A JP18086789 A JP 18086789A JP 18086789 A JP18086789 A JP 18086789A JP H0344324 A JPH0344324 A JP H0344324A
- Authority
- JP
- Japan
- Prior art keywords
- sexual function
- propentofylline
- invigorator
- active ingredient
- agent
- 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
- 230000036299 sexual function Effects 0.000 title claims abstract description 11
- 239000004480 active ingredient Substances 0.000 claims abstract description 10
- 239000002207 metabolite Substances 0.000 claims abstract description 6
- RBQOQRRFDPXAGN-UHFFFAOYSA-N Propentofylline Chemical compound CN1C(=O)N(CCCCC(C)=O)C(=O)C2=C1N=CN2CCC RBQOQRRFDPXAGN-UHFFFAOYSA-N 0.000 claims abstract 5
- 229960002934 propentofylline Drugs 0.000 claims abstract 5
- 239000012190 activator Substances 0.000 claims description 3
- -1 5- oxohexyl Chemical group 0.000 abstract description 8
- 210000003016 hypothalamus Anatomy 0.000 abstract description 5
- 210000003715 limbic system Anatomy 0.000 abstract description 5
- 235000013305 food Nutrition 0.000 abstract description 4
- 230000001256 tonic effect Effects 0.000 abstract description 4
- 229940079593 drug Drugs 0.000 abstract description 2
- 239000003814 drug Substances 0.000 abstract description 2
- 230000004936 stimulating effect Effects 0.000 abstract description 2
- 239000003795 chemical substances by application Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 description 7
- 238000002474 experimental method Methods 0.000 description 6
- 230000035946 sexual desire Effects 0.000 description 6
- 230000007423 decrease Effects 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- 241000700159 Rattus Species 0.000 description 3
- 210000004720 cerebrum Anatomy 0.000 description 3
- 235000012054 meals Nutrition 0.000 description 3
- 229930003231 vitamin Natural products 0.000 description 3
- 239000011782 vitamin Substances 0.000 description 3
- 235000013343 vitamin Nutrition 0.000 description 3
- 229940088594 vitamin Drugs 0.000 description 3
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical class O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 description 2
- 241000282472 Canis lupus familiaris Species 0.000 description 2
- 206010007269 Carcinogenicity Diseases 0.000 description 2
- 244000269722 Thea sinensis Species 0.000 description 2
- 230000009102 absorption Effects 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 238000009825 accumulation Methods 0.000 description 2
- 230000035508 accumulation Effects 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- CUFNKYGDVFVPHO-UHFFFAOYSA-N azulene Chemical compound C1=CC=CC2=CC=CC2=C1 CUFNKYGDVFVPHO-UHFFFAOYSA-N 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 230000007670 carcinogenicity Effects 0.000 description 2
- 231100000260 carcinogenicity Toxicity 0.000 description 2
- 230000029142 excretion Effects 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000001850 reproductive effect Effects 0.000 description 2
- 230000009329 sexual behaviour Effects 0.000 description 2
- 238000011282 treatment Methods 0.000 description 2
- 150000003722 vitamin derivatives Chemical class 0.000 description 2
- 241000237519 Bivalvia Species 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 description 1
- 101800003838 Epidermal growth factor Proteins 0.000 description 1
- 208000004930 Fatty Liver Diseases 0.000 description 1
- ZPACYDRSPFRDHO-ROBAGEODSA-N Gefarnate Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\CCC(=O)OC\C=C(/C)CCC=C(C)C ZPACYDRSPFRDHO-ROBAGEODSA-N 0.000 description 1
- 229920001386 Gefarnate Polymers 0.000 description 1
- 206010019708 Hepatic steatosis Diseases 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 1
- 229930182816 L-glutamine Natural products 0.000 description 1
- 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 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 244000131316 Panax pseudoginseng Species 0.000 description 1
- 235000005035 Panax pseudoginseng ssp. pseudoginseng Nutrition 0.000 description 1
- 235000003140 Panax quinquefolius Nutrition 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 241001061526 Pluteus cervinus Species 0.000 description 1
- 201000001880 Sexual dysfunction Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 206010043275 Teratogenicity Diseases 0.000 description 1
- 206010070863 Toxicity to various agents Diseases 0.000 description 1
- 229930003270 Vitamin B Natural products 0.000 description 1
- 229930003427 Vitamin E Natural products 0.000 description 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
- AMZWNNKNOQSBOP-UHFFFAOYSA-M [n'-(2,5-dioxoimidazolidin-4-yl)carbamimidoyl]oxyaluminum;dihydrate Chemical compound O.O.NC(=O)NC1N=C(O[Al])NC1=O AMZWNNKNOQSBOP-UHFFFAOYSA-M 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000037374 absorbed through the skin Effects 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 229940015825 aldioxa Drugs 0.000 description 1
- 210000004727 amygdala Anatomy 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 229940008396 carrot extract Drugs 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 235000020639 clam Nutrition 0.000 description 1
- 230000007012 clinical effect Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 230000000517 effect on sleep Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 208000010706 fatty liver disease Diseases 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 230000005176 gastrointestinal motility Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229960003779 gefarnate Drugs 0.000 description 1
- 235000008434 ginseng Nutrition 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 235000012907 honey Nutrition 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 208000013403 hyperactivity Diseases 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 229940069445 licorice extract Drugs 0.000 description 1
- 208000013433 lightheadedness Diseases 0.000 description 1
- 229940083747 low-ceiling diuretics xanthine derivative Drugs 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 239000004081 narcotic agent Substances 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 230000008285 neurophysiological mechanism Effects 0.000 description 1
- 231100001081 no carcinogenicity Toxicity 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 235000008935 nutritious Nutrition 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 210000004129 prosencephalon Anatomy 0.000 description 1
- 229940109850 royal jelly Drugs 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000035807 sensation Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 230000004617 sleep duration Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 231100000240 steatosis hepatitis Toxicity 0.000 description 1
- 229960004291 sucralfate Drugs 0.000 description 1
- MNQYNQBOVCBZIQ-JQOFMKNESA-A sucralfate Chemical compound O[Al](O)OS(=O)(=O)O[C@@H]1[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](COS(=O)(=O)O[Al](O)O)O[C@H]1O[C@@]1(COS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)O1 MNQYNQBOVCBZIQ-JQOFMKNESA-A 0.000 description 1
- 231100000211 teratogenicity Toxicity 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000820 toxicity test Toxicity 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 description 1
- 235000019156 vitamin B Nutrition 0.000 description 1
- 239000011720 vitamin B Substances 0.000 description 1
- 235000019165 vitamin E Nutrition 0.000 description 1
- 229940046009 vitamin E Drugs 0.000 description 1
- 239000011709 vitamin E Substances 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
- 235000016804 zinc Nutrition 0.000 description 1
- NWONKYPBYAMBJT-UHFFFAOYSA-L zinc sulfate Chemical compound [Zn+2].[O-]S([O-])(=O)=O NWONKYPBYAMBJT-UHFFFAOYSA-L 0.000 description 1
- 229960001763 zinc sulfate Drugs 0.000 description 1
- 229910000368 zinc sulfate Inorganic materials 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
（イ）産業上の利用分野
この発明は、ブａベントフィリンまたはその体内代謝産
物を有効成分として含有することからなる性機能賦活剤
に関する。DETAILED DESCRIPTION OF THE INVENTION (a) Field of Industrial Application This invention relates to a sexual function activator containing bubentophyllin or its in vivo metabolite as an active ingredient.
（ロ）従来の技術と解決されるべき課題従来より茶、コ
ーヒーなどが広く世界で嗜好されていることはよく知ら
れた事実であり、この根拠として以前よりこれらの中に
含まれるテオフィリンやカフェインが重要な生理活性物
質であることが判っている。また近年の研究により茶を
連用することにより脂肪肝の予防、癌の予防、糖尿病の
予防、高脂血症の予防など多方面にわたる効果のあるこ
とら知られている。(b) Conventional technologies and issues to be solved It is a well-known fact that tea, coffee, etc. have been widely enjoyed around the world. In is known to be an important physiologically active substance. In addition, recent research has shown that continuous use of tea has a wide range of effects, including the prevention of fatty liver, cancer, diabetes, and hyperlipidemia.
一方、性機能の賦活性を有する物質の出現が望まれてい
る。しかし、現在のところ性の機能的側面、即ち性欲の
発生、興奮の過程などについての神経生理的メカニズム
についての詳しい知見は得られていない。また人におい
ては大脳の役割の果たすところが多く、これを−層難し
くしている。On the other hand, the emergence of a substance that activates sexual function is desired. However, at present, detailed knowledge about the neurophysiological mechanisms of functional aspects of sexuality, such as the generation of sexual desire and the process of excitement, has not been obtained. Furthermore, in humans, the cerebrum plays many roles, making this even more difficult.
従来の研究によると思春期における性欲の発現状況から
性ホルモンの持つ神経や生殖器に対する影響は詳しく調
べられており、多くの結果が得られており、現在でもホ
ルモンの見地から性機能を見る学者が多いことは間違い
ない。According to previous research, the influence of sex hormones on the nerves and reproductive organs has been investigated in detail from the expression of sexual desire during adolescence, and many results have been obtained. There is no doubt that there are many.
しかしながら現実の性機能低下の治療の場では、中年以
降の人々における性の問題は大脳（特に大脳辺縁系ない
しは視床下部）における関与が大きくホルモン学説に基
づいた治療が効を奏することはないか、又はあっても−
時しのぎにすぎない。However, in the actual treatment of hyposexual function, sexual problems in middle-aged and older people involve the cerebrum (particularly the limbic system or hypothalamus), and treatments based on hormone theory are not effective. Or even if-
It's just a stopgap.
大脳における性欲又は性行動発現の中枢はサルの実験に
よると視床下部ないしは辺縁系であることが推定されて
おり、人もこれに準するものと考えられる。例えば前脳
中央部からその周囲の視床下部を刺激することによって
勃起や性行動をひき起こすことが知られている他、辺縁
系の一部である扁桃核を操作することによって性欲の異
常な亢進を惹起させることが出来るとの報告もある。Based on experiments on monkeys, it has been estimated that the center of the expression of sexual desire or sexual behavior in the cerebrum is the hypothalamus or limbic system, and it is thought that humans are similar to this. For example, it is known that stimulating the hypothalamus surrounding it from the central forebrain can induce erections and sexual behavior, and abnormal sexual desire can be induced by manipulating the amygdala nucleus, which is part of the limbic system. There are also reports that it can induce hyperactivity.
このようなことから大脳中枢部にターゲットをしぼった
活性物質、持に視床下部や辺縁系を刺激し性機能を賦活
させる物質の開発が望まれることとなる。これまでのと
ころこれに該当する薬物は一部の麻薬などを除いて一般
に使用されるものはなかった。For this reason, it is desired to develop active substances that target the central part of the brain, substances that stimulate the hypothalamus and limbic system and activate sexual function. So far, there have been no drugs in general use that fall under this category, with the exception of some narcotics.
（ハ）課題を解決しようとする手段
この発明によれば、プロベントフィリンまたはその体内
代謝産物を有効成分として含有することからなる性機能
賦活剤が提供される。(C) Means for Solving the Problems According to the present invention, there is provided a sexual function activator containing prevententphylline or its metabolite in the body as an active ingredient.
プロベントフィリンは、キサンチン誘導体で、３−メチ
ル−１−（３−オキソヘキシル）−７−ブロビルー７Ｈ
−プリン−２（３Ｈ） 、 ６ （ＬＨ）−ジオンであ
る。プロベントフィリンの体内代謝産物とは、プロベン
トフィリンの５−オキソヘキシル基（ＣＵＳ−Ｃ−（Ｃ
Ｈｔ）、 −）が５−ヒドロキシヘキシル基１
（ＣＨ３−Ｃ■−（ＣＨｔ）４） 、４−カルボキシブ
チルＨ
基（ＨＯＯＣ−（ＣＨｔ）４− ） 、３−カルボキシ
プロピル基（ＨＯＯＣ−（ＣＬ）ｓ −）に変化したも
のが含まれる。Proventophylline is a xanthine derivative, 3-methyl-1-(3-oxohexyl)-7-broby-7H
-purine-2(3H),6(LH)-dione. The in vivo metabolites of protectonphylline are the 5-oxohexyl group (CUS-C-(C
Ht), -) are 5-hydroxyhexyl group 1 (CH3-C■-(CHt)4), 4-carboxybutyl H group (HOOC-(CHt)4-), 3-carboxypropyl group (HOOC-(CL ) s −) is included.
この発明の活性成分は、現在のところ直接的な証拠は得
られていないが、大脳の上位中枢で作用を及ぼすものと
考えられ、性機能の賦活作用を有する。従って、強精剤
（もしくは強壮剤）として有用である。Although no direct evidence has been obtained at present, the active ingredient of this invention is thought to act on the upper cerebral center and has the effect of activating sexual function. Therefore, it is useful as a tonic (or tonic).
投与方法は、通常経口投与が好ましい。しかし、活性成
分を適当な媒体に懸濁又は溶解させて、非経口的（筋注
、静注など）に投与することもできる。また、活性成分
をテープに含有させ、皮膚外用剤として用いることもで
きる。経口投与量は、１日当りｌ０１１ｇ〜１８００ｍ
？、好ましくは、６０１１９〜６００Ｒｇを、１〜数回
に投与される。頓用で毎食後の連用も可能である。経口
投与剤として用いる場合、乳糖、デンプンなどを賦形剤
、胃への刺激性を軽くする為に、種々の胃粘膜保護剤（
例えばビタミンＵ１スクラルファート、Ｌ−グルタミン
、アズレン、ゲファルナート、ウロガストロン、アルジ
オキサ、甘草エキス、プロゲルミド、ソファルコン Ｆ
Ｍｌｏｏなど）と共に用いることができる。さらに、ビ
タミンＥやビタミンＢのようなビタミン類、亜鉛、人参
エキス、花粉、ローヤルゼリー、蜂蜜、鹿茸、淫羊蕾、
補骨脂、蛤創“、熟地黄、当帰などと共に用いることか
できる。As for the administration method, oral administration is usually preferred. However, the active ingredient can also be suspended or dissolved in a suitable vehicle and administered parenterally (intramuscularly, intravenously, etc.). Furthermore, the tape can contain the active ingredient and be used as an external skin preparation. Oral dosage is 1011g to 1800m per day
? , preferably 60119-600Rg, is administered in one to several doses. It can also be taken continuously after every meal. When used as an oral preparation, lactose, starch, etc. are used as excipients, and various gastric mucosal protectants (
For example, vitamin U1 sucralfate, L-glutamine, azulene, gefarnate, urogastrone, aldioxa, licorice extract, progelmide, sofalcon F
Mloo, etc.). In addition, vitamins such as vitamin E and vitamin B, zinc, carrot extract, pollen, royal jelly, honey, deer mushroom, sheep bud,
It can be used together with bone fat, clams, jukujiang, and dangki.
また、各種食品に添加して滋養強壮食品として用いるこ
ともできる。It can also be added to various foods and used as a nutritious and tonic food.
単独大量投与（例えば２００〜６００ｍｇ）の場合にｌ
〜８時間で性機能の賦活作用が発現し、ピークは約６時
間でみられる。In the case of single large doses (e.g. 200-600 mg)
The activation effect on sexual function appears in ~8 hours, and the peak is seen in about 6 hours.
この発明の代表的な活性成分であるプロベントフィリン
について、毒性、発癌性、吸収、排泄等などについて述
べると次の通りである。The toxicity, carcinogenicity, absorption, excretion, etc. of protectonphylline, which is a representative active ingredient of this invention, are as follows.
（以下余白） ｌ）毒性試験 （急性毒性 ＬＤ５゜。(Margin below) l) Toxicity test (acute toxicity LD5°.
ｍｙ／Ｋｇ）
この他ラットで５０ ｘ９／ Ｋｇ／ ｄａｙの３０日
間投与（経口）で何ら毒性症状は認められていない。my/Kg) No other toxic symptoms were observed in rats after 30 days of oral administration at 50 x 9/Kg/day.
また、イヌで２０ ｕ／Ｋｇ／ｄａｙの経口投与を６ケ
月にわたり行い特記すべき変化は認められなかった。In addition, no notable changes were observed after oral administration of 20 u/Kg/day to dogs for 6 months.
２）生殖ならびに発癌性試験
マウスの実験にて催奇形性は認められず、またラットの
実験で２年間の観察により発癌性も認められていない。2) Reproductive and carcinogenicity tests No teratogenicity was observed in mouse experiments, and no carcinogenicity was observed in rat experiments over a two-year period.
３）移行性、蓄積性、吸収ならびに排泄従来のキサンチ
ン誘導体に比し５〜７倍の脂溶性をもつため、細胞膜を
介しての吸収は良好で、皮膚や腸管から吸収される。ま
た、血液脳関門を通過することもできる。このため、脳
内での効果が高いものと考えられる。3) Transition, accumulation, absorption, and excretion Because it has 5 to 7 times more fat solubility than conventional xanthine derivatives, it is well absorbed through cell membranes and is absorbed through the skin and intestinal tract. It can also cross the blood-brain barrier. Therefore, it is thought to have a high effect in the brain.
ラットにおける反復投与実験から蓄積性は認められなか
った。No accumulation was observed in repeated administration experiments in rats.
イヌの経口投与実験で１０−１５分で血中に出現し、４
〜８時間でピークに達し、その後ｌＯ〜十数時間で血中
より消失する。In an oral administration experiment on dogs, it appeared in the blood within 10-15 minutes, and 4
It reaches its peak in ~8 hours and then disappears from the blood in ~10 hours.
投与後２４時間以内に約９０％が尿中排泄を受ける。Approximately 90% is excreted in the urine within 24 hours after administration.
４）また本物質はマウスの実験により、睡眠の導入時間
、睡眠時間に対して影響のないこと、消化管の運動や胃
液分泌に対しては影響のないことが確認されている。4) In addition, it has been confirmed through experiments on mice that this substance has no effect on sleep induction time or sleep duration, or on gastrointestinal motility or gastric juice secretion.
次にこの発明の活性成分の有効性を証すための臨床効果
を示す。Next, clinical effects will be shown to prove the effectiveness of the active ingredient of this invention.
試験例
１．３９才、男性
４〜５年前より性欲の低下があった。また、勃起時充分
な硬度が得られない。早朝勃起の頻度減少があったがプ
ロベントフィリン１００ｍ９を毎食後１日３回で内服し
たところ、約２週日より上記すべてにわたって改善の傾
向があった。しかしながら同時に硫酸亜鉛、花粉、ビタ
ミン８１人参末なども数カ月前より持続して内服してい
た為、本則のみの効果かどうかはっきりしなかった。Test Example 1. A 39-year-old male had a decrease in sexual desire from 4 to 5 years ago. Also, sufficient hardness cannot be obtained during erection. There was a decrease in the frequency of early morning erections, but when Proventophylline 100m9 was taken orally three times a day after each meal, all of the above tended to improve from about 2 weeks ago. However, at the same time, he had been taking zinc sulfate, pollen, and vitamin 81 ginseng powder for several months, so it was unclear whether the main effects alone were effective.
２、この為、健康ではあるが精力の衰えを感する男性（
３５才〜５０才）１０人においてプロベントフィリンの
みの投与（１日３回、毎食後１ＯＯ１９づつ経口）を２
ケ月にわたり行った。試験の前後でアンケートを行った
ところ
ア、近年の性欲低下が改善した例 ７名イ９通常
に比し、性感覚がよくなった例 ３名つ、勃起の頻度や
硬度において改善の
みられた例 ２名この他、気
分の昂揚路、頭がさえる感じを訴えるものが各々１名あ
った。又、効果のみられた者のうち約６０％は比較的短
時間（１日〜１４日）で効果があったといっており、本
物質の即効性を示している。尚、副作用は１０名中目例
も認められなかった。2.For this reason, men who are healthy but feel a decline in energy (
In 10 patients (35 to 50 years old), Probentophylline alone was administered (orally, 100% after each meal, 3 times a day) for 2 days.
I went there for several months. Questionnaires were conducted before and after the test, and found that: (a) 7 cases showed improvement in recent decrease in sexual desire; (9) cases in which sexual sensation improved compared to normal; 3 cases showed improvement in the frequency and hardness of erections. In addition to the two patients, one patient each complained of high mood and a feeling of lightheadedness. Additionally, about 60% of those who saw the effect said that it was effective in a relatively short period of time (1 to 14 days), indicating the immediate effect of this substance. In addition, no side effects were observed among the 10 patients.
Claims (1)
成分として含有することからなる性機能賦活剤。1. A sexual function activator containing propentophylline or its internal metabolite as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18086789A JPH0344324A (en) | 1989-07-13 | 1989-07-13 | Sexual function invigorator |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18086789A JPH0344324A (en) | 1989-07-13 | 1989-07-13 | Sexual function invigorator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH0344324A true JPH0344324A (en) | 1991-02-26 |
Family
ID=16090740
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP18086789A Pending JPH0344324A (en) | 1989-07-13 | 1989-07-13 | Sexual function invigorator |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0344324A (en) |
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH05216816A (en) * | 1992-02-06 | 1993-08-27 | Pfu Ltd | Bus control circuit |
| US5981527A (en) * | 1995-07-14 | 1999-11-09 | Icos Corporation | Cyclic GMP-specific phosphodiesterase inhibitors |
| US6001847A (en) * | 1995-07-14 | 1999-12-14 | Icos Corporation | Chemical compounds |
| WO2000007541A3 (en) * | 1998-07-31 | 2000-05-04 | Aventis Pharma Gmbh | Use of xanthine derivatives for treating erectile disorder |
| US6117881A (en) * | 1996-05-10 | 2000-09-12 | Icos Corporation | N-cinnamoyl derivatives of (β) carbolines |
| US6140329A (en) * | 1995-07-14 | 2000-10-31 | Icos Corporation | Use of cGMP-phosphodiesterase inhibitors in methods and compositions to treat impotence |
| US6143746A (en) * | 1994-01-21 | 2000-11-07 | Icos Corporation | Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use |
| KR20010083203A (en) * | 2000-02-22 | 2001-08-31 | 나오야 하라노 | Method for transmitting image data and terminal for image processing and portable terminal |
| US6300335B1 (en) | 1994-11-26 | 2001-10-09 | Pfizer Inc. | 4-aminoquinazoline derivative cGMP-PDE inhibitors for the treatment of erectile dysfunction |
| EP1214938A2 (en) * | 1991-05-24 | 2002-06-19 | Fred Hutchinson Cancer Research Center | Modulation of cellular response to external stimuli |
| US6469012B1 (en) | 1993-06-09 | 2002-10-22 | Pfizer Inc | Pyrazolopyrimidinones for the treatment of impotence |
| US6534511B1 (en) | 1994-11-26 | 2003-03-18 | Pfizer Inc. | Bicyclic heterocyclic compounds for the treatment of impotence |
| JP2015183003A (en) * | 2014-03-25 | 2015-10-22 | クワン ドン ファーマシューティカル カンパニー，リミテッド | Male sterility preventive and therapeutic pharmaceutical composition containing mixtures of rehmannia glutinosa liboschitz var.purpurae makino, lycium chinense miller, aquillaria agallocha roxburgh, poria cocos wolf, panax ginseng ca meyer and honey as active ingredients |
-
1989
- 1989-07-13 JP JP18086789A patent/JPH0344324A/en active Pending
Cited By (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1214938A2 (en) * | 1991-05-24 | 2002-06-19 | Fred Hutchinson Cancer Research Center | Modulation of cellular response to external stimuli |
| EP1214938A3 (en) * | 1991-05-24 | 2003-08-06 | Fred Hutchinson Cancer Research Center | Modulation of cellular response to external stimuli |
| JPH05216816A (en) * | 1992-02-06 | 1993-08-27 | Pfu Ltd | Bus control circuit |
| US6469012B1 (en) | 1993-06-09 | 2002-10-22 | Pfizer Inc | Pyrazolopyrimidinones for the treatment of impotence |
| US6143746A (en) * | 1994-01-21 | 2000-11-07 | Icos Corporation | Tetracyclic cyclic GMP-specific phosphodiesterase inhibitors, process of preparation and use |
| US6656945B2 (en) | 1994-11-26 | 2003-12-02 | Pfizer Inc | 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-one cGMP-PDE inhibitors for the treatment of erectile dysfunction |
| US6300335B1 (en) | 1994-11-26 | 2001-10-09 | Pfizer Inc. | 4-aminoquinazoline derivative cGMP-PDE inhibitors for the treatment of erectile dysfunction |
| US6534511B1 (en) | 1994-11-26 | 2003-03-18 | Pfizer Inc. | Bicyclic heterocyclic compounds for the treatment of impotence |
| US6140329A (en) * | 1995-07-14 | 2000-10-31 | Icos Corporation | Use of cGMP-phosphodiesterase inhibitors in methods and compositions to treat impotence |
| US6218400B1 (en) | 1995-07-14 | 2001-04-17 | Icos Corporation | Treatment method using a cGMP-Specific PDE inhibitor |
| US6608065B1 (en) | 1995-07-14 | 2003-08-19 | Icos Corporation | Use of cGMP phosphodiesterase inhibitors in methods to treat female sexual dysfunction |
| US6001847A (en) * | 1995-07-14 | 1999-12-14 | Icos Corporation | Chemical compounds |
| US5981527A (en) * | 1995-07-14 | 1999-11-09 | Icos Corporation | Cyclic GMP-specific phosphodiesterase inhibitors |
| US6117881A (en) * | 1996-05-10 | 2000-09-12 | Icos Corporation | N-cinnamoyl derivatives of (β) carbolines |
| US6306870B1 (en) | 1996-05-10 | 2001-10-23 | Icos Corporation | N-cinnamoyl derivatives of beta-carboline |
| WO2000007541A3 (en) * | 1998-07-31 | 2000-05-04 | Aventis Pharma Gmbh | Use of xanthine derivatives for treating erectile disorder |
| KR20010083203A (en) * | 2000-02-22 | 2001-08-31 | 나오야 하라노 | Method for transmitting image data and terminal for image processing and portable terminal |
| JP2015183003A (en) * | 2014-03-25 | 2015-10-22 | クワン ドン ファーマシューティカル カンパニー，リミテッド | Male sterility preventive and therapeutic pharmaceutical composition containing mixtures of rehmannia glutinosa liboschitz var.purpurae makino, lycium chinense miller, aquillaria agallocha roxburgh, poria cocos wolf, panax ginseng ca meyer and honey as active ingredients |
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