JPS5973600A - Ovulatory inducing agent - Google Patents
Ovulatory inducing agentInfo
- Publication number
- JPS5973600A JPS5973600A JP18212282A JP18212282A JPS5973600A JP S5973600 A JPS5973600 A JP S5973600A JP 18212282 A JP18212282 A JP 18212282A JP 18212282 A JP18212282 A JP 18212282A JP S5973600 A JPS5973600 A JP S5973600A
- Authority
- JP
- Japan
- Prior art keywords
- inducing agent
- ovulatory
- ovulation
- methylenecycloartanol
- starch
- 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
Abstract
Description
【発明の詳細な説明】
本発明は、***誘発剤に関する。更に詳しくは本発明は
、２４−メチレンシクロアルタノールを主成分として含
有することを特徴とする***誘発剤に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an ovulation-inducing agent. More specifically, the present invention relates to an ovulation-inducing agent characterized by containing 24-methylenecycloartanol as a main component.
従来２４−メチレンシクロアルタノールｌｄ、公知化合
物で、抗炎症剤（特公昭４８−１６６０４号）及び精神
安定剤（特開昭５４−６１２９９号）として知られて−
る。Conventionally, 24-methylenecycloartanol ld is a known compound, known as an anti-inflammatory agent (Japanese Patent Publication No. 16604/1982) and a tranquilizer (Japanese Patent Publication No. 61299/1989).
Ru.
本発ＦＩＪ者１ｒｉ、、２４−メチレンシクロアルタノ
ールの医薬用途につき鋭意研究を重ねた結果、従来の薬
理作用からは、予測困難な***誘発作用を有し***誘発
剤として有用であることを見 １−
い出し本発明を完成したものである。As a result of extensive research into the medicinal uses of 24-methylenecycloartanol, the FIJ researchers found that it has an ovulation-inducing effect that is difficult to predict based on conventional pharmacology, and that it is useful as an ovulation-inducing agent. 1- The present invention has been completed.
本発明の***誘発剤は、第１度無月経症等の無月経症、
月経困難症、***障害、月経周期の異常症等の治療薬と
して有用である。本発明の***誘発剤は、通常、２４−
メチレンシクロアルタノールと製剤的担体と共に、製剤
組成物の形態とされる。担体としては使用形態に応じた
薬剤を調製するのに通常使用される充填剤、増量剤、結
合剤、付湿剤、崩壊剤、表面活性剤、滑沢剤等の稀釈剤
あるいは賦形剤を例示できる。The ovulation-inducing agent of the present invention can treat amenorrhea such as first-degree amenorrhea,
It is useful as a therapeutic agent for dysmenorrhea, ovulation disorders, menstrual cycle abnormalities, etc. The ovulation-inducing agent of the present invention is usually 24-
Methylenecycloartanol and a pharmaceutical carrier are in the form of a pharmaceutical composition. As carriers, diluents or excipients such as fillers, fillers, binders, wetting agents, disintegrants, surfactants, lubricants, etc., which are commonly used to prepare drugs according to the usage form, can be used. I can give an example.
本発明の***誘発剤の投与単位形態としては各種の形態
を治療目的に応じて選択でき、その代表的なものとして
錠剤、丸剤、散剤、液剤、懸濁剤、乳剤、顆粒剤、カプ
セル剤、坐剤、注射剤等を例示できこれ等は、通常の方
法に従って容易に製造される。錠剤の形態に成形するに
際しては、担体として例えば乳糖、白糖、デンプン、カ
オリン、結晶セルロース、ケイ酸等ノ賦形剤、エタノー
ル、プロパツール、単シロップ、ブドウ糖、デンプン液
、ゼラチン溶、・液′、カルゼキシメチルセルロース、
セラック、メチルセルロース、リン酸カリウム、ポリビ
ニルピロリドン等の結合剤、乾燥デンプン、アルギン酸
ナトリウム、カンテン末、ラミナリア末、炭酸水素ナト
リウム、炭酸カルシウム、ツウイン、ラウリル硫酸ナト
リウム、ステアリン酸モノグリセリド、デンプン、乳糖
等の崩壊剤、白糖、ステアリン、カカオノ々タニ、水素
添加油−等の崩壊抑制剤、第四級アンモニウム塩基、ラ
ウリル硫酸ナトリウム等の吸収促進剤、グリセリン、デ
ンプン等の保湿剤、デンプン、・乳糖、カオリン、ベシ
トナイト、コロイド状ケイ酸等の吸着剤、精製タルク、
ステアリン酸塩、ホウ酸末、マクロゴール、固体ポリエ
チレングリコール等の滑沢剤等を使用できる。丸剤の形
態に成形するに際しては、担体として例えばブドウ糖、
乳糖、デンプン、カカオ脂、硬化植物油、カオリン、タ
ルク等の賦形剤、アラビアゴム末、トラガント末、ゼラ
チン、エタノール等の結合剤、ラミナリア、カンテン等
の崩壊剤等を使用できる。更に錠剤は必要に応じ通常の
剤皮を施した錠剤例えば糖衣錠、ゼラチン被包錠、腸溶
破錠、フィルムコーティング錠あるいは二重錠、多層錠
とすることができる。As the dosage unit form of the ovulation-inducing agent of the present invention, various forms can be selected depending on the therapeutic purpose, and representative examples include tablets, pills, powders, solutions, suspensions, emulsions, granules, and capsules. Examples include suppositories, injections, etc., which can be easily manufactured according to conventional methods. When forming into a tablet, carriers such as lactose, sucrose, starch, kaolin, crystalline cellulose, silicic acid, etc., ethanol, propatool, simple syrup, glucose, starch solution, gelatin solution, etc. , calxoxymethylcellulose,
Disintegration of binders such as shellac, methylcellulose, potassium phosphate, polyvinylpyrrolidone, dry starch, sodium alginate, agar powder, laminaria powder, sodium bicarbonate, calcium carbonate, Twin, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, etc. disintegration inhibitors such as white sugar, stearin, cocoa powder, hydrogenated oil, etc., absorption enhancers such as quaternary ammonium bases and sodium lauryl sulfate, humectants such as glycerin and starch, starch, lactose, kaolin, Adsorbents such as besitonite and colloidal silicic acid, purified talc,
Lubricants such as stearate, boric acid powder, macrogol, solid polyethylene glycol, etc. can be used. When forming into pill form, carriers such as glucose,
Excipients such as lactose, starch, cocoa butter, hydrogenated vegetable oil, kaolin and talc, binders such as gum arabic powder, tragacanth powder, gelatin and ethanol, and disintegrants such as laminaria and agar can be used. Furthermore, the tablets can be made into conventionally coated tablets, such as sugar-coated tablets, gelatin-encapsulated tablets, enteric-coated tablets, film-coated tablets, double tablets, or multilayer tablets, if necessary.
本発明の***誘発剤中に含有させるべき２４−メチレン
シクロアルタノールの量は、特に限定されず広範囲に適
宜選択されるが、通常全組成物中１〜７０重を気とする
のがよい。The amount of 24-methylenecycloartanol to be included in the ovulation-inducing agent of the present invention is not particularly limited and can be appropriately selected within a wide range, but it is usually 1 to 70 times the total composition.
また上記の***誘発剤は、その使用に際し特に制限はな
く各種形態に応じた方法で投与される。例えば錠剤、丸
剤、液剤、懸濁剤、乳剤、顆粒剤及びカプセル剤の場合
には経口投与され、注射剤の場合には単独であるいはブ
ドウ糖、アミノ酸等の通常の補液と混合して静脈内投与
され、さらに必要に応じて単独で筋肉内、皮肉、皮下若
しくは腹腔内投与され、坐剤の場合には直腸内投与され
る。Furthermore, the above-mentioned ovulation-inducing agent is not particularly limited in its use, and can be administered in a manner suitable for various forms. For example, in the case of tablets, pills, solutions, suspensions, emulsions, granules, and capsules, it is administered orally, and in the case of injections, it is administered intravenously alone or mixed with normal replenishing fluids such as glucose and amino acids. If necessary, it can be administered alone intramuscularly, subcutaneously, subcutaneously or intraperitoneally, and in the case of suppositories, it can be administered rectally.
本発明の***誘発剤としての投与針は使用目的、症状等
により適宜選択され、通常有効成分（２４−メチレンシ
クロアルタノール）を１日当り１〜ＩＯＱ／に９程度含
有する製剤組成物を１〜４回に分けて投与すればよ−。The administration needle for the ovulation-inducing agent of the present invention is appropriately selected depending on the purpose of use, symptoms, etc., and usually contains a pharmaceutical composition containing about 1 to 9 IOQ/day of the active ingredient (24-methylenecycloartanol). Just give it in 4 doses.
□以下に本発明を更に詳細に説明する為に臨床デー
ターを挙げるが本発明は、これ等に限定されるものでは
ない。□Clinical data will be listed below to explain the present invention in more detail, but the present invention is not limited thereto.
臨・法例
未婚第１度無月経婦人に対する、０Ｋ−０−０５（特開
昭５４−６１２９９号）の***誘発効果をみると共に、
血中ＬＨ，ＦＳＨ，Ｐｒｏｌａｃｔｌｎ（ＰＲＬ） 。In addition to looking at the ovulation-inducing effect of 0K-0-05 (Japanese Unexamined Patent Publication No. 1983-61299) on unmarried women with first-degree amenorrhea,
Blood LH, FSH, Prolactln (PRL).
、Ｄｏｐａｍｉｎｅ濃度の変化よりこの物質の***機構
に及ぼす影響を検討した。The effect of this substance on the ovulation mechanism was investigated by changing the concentration of Dopamine.
実験方法：実験対象は、ｎｏｒｍｏｐｒｏｌａｃＨｎａ
ｍｉｍを有する第１度無月経婦人（１８〜２２歳）とし
、心理テストで、神経症型、ＰＳＯ型、自律神経失、調
症を示さない正常型（現代産婦人科学大系第９巻、中白
書店Ｐ１８４（１９７０）参照）であることを確認し−
、ゲスタゲン（ｇ＠ｍｔａｇｅｎ ） Ｋよ消退出血後
５〜７日目より０Ｋ−０−０５：５０藁９Ｘ２Ｔ／ｄａ
ｙを、１４日間連日投与した。また、投与前後における
血中ＬＨ（黄体化ホルモン） ＦＳＩ（５−
（卵胞刺激ホルモン） ＰＲＬ （プロラクチン）、Ｄ
ｏｐａｍｌｎ・は前３者をＲＩＡ （谷沢修：講談社す
イエンテイフイク５ ： Ｐ２Ｏ３−１９０（１９７９
）’及び井上和子、榎本和子：講談社すイエンテイフイ
ク５ ： Ｐ２Ｏ３−２０６（１９７９）参照）で、Ｄ
ｏｐａｍｉｎｅはハイ・ノセーフオーマンス − リク
イラド・クロマトグラフィー（守和子：カテコールアミ
ンの高速液体クロマトグラフィーによる分析：産業医学
・１７ ： Ｐ１７０−１７１（１９７５）参照）を利
用して測定した。Experimental method: The experimental subject was normoprolacHna
A first-degree amenorrheic woman (18 to 22 years old) with MIM, and psychological tests showed that she was neurotic type, PSO type, autonomic nerve loss, and normal type without symptoms (Modern Obstetrics and Gynecology System Vol. 9, (See Chuhaku Shoten P184 (1970)).
, Gestagen (g@mtagen) 0K-0-05:50 9X2T/da from 5 to 7 days after withdrawal bleeding
y was administered daily for 14 days. In addition, blood LH (luteinizing hormone), FSI (5- (follicle stimulating hormone), PRL (prolactin), D
opamln is the former three RIA (Osamu Tanizawa: Kodansha University Book 5: P2O3-190 (1979)
)' and Kazuko Inoue, Kazuko Enomoto: Kodansha University Book 5: P2O3-206 (1979)), D.
Opamine was measured using high-no-safety-liquid chromatography (see Kazuko Mori: Analysis of catecholamines by high-performance liquid chromatography: Industrial Medicine 17: P170-171 (1975)).
さらに投与前ＫＬＨ−ＲＨ（Ｌｕｔｅｌｎｉｚｉｎｇ
Ｈｏｒｍｏｎｅ−Ｒｅｌｅａｓｉｎｇ Ｉ（ｏｒｍｏｎ
ａ）テスト（五十嵐正雄：内分泌婦人科学：南山堂：
Ｐ２４９−２５１（１９７８）参照）を施行し、各症例
における下垂体機能の相違を検討した。In addition, KLH-RH (Lutelnizing
Hormone-Releasing I
a) Test (Masao Igarashi: Endocrinology and Gynecology: Nanzando:
P249-251 (1978)) was performed to examine differences in pituitary function in each case.
実験成績：***の有無の診断は、ＢＢＴ（基礎体温）（
飯塚埋入編集、鈴木雅洲、坂元正−監修：産婦人科シリ
ーズｖｏｌ１２不妊症診断のすべて（１９７５）参照）
血中エストラジオール、プロゲステロンの測定により行
ったが、０Ｋ−０−０５投与に ６−
より、２１１例中７に***を認め無***性周期に８例中
５例に***が認められた。周知の如く、***が起こり、
卵巣が黄体期になるとＢＢＴは高温期となり、血中エス
トラジオール、プロゲステロンが共に高値となることは
事実である（五十嵐正雄：内分泌婦人科学、ＲｏｓＩＩ
（ｅｔａｌ等）図Ｐ１２６（１９７Ｂ）。今回の我々の
データーでもＢＢＴは高温相を呈し血中エストラジオー
ル値は、３０〜１５０ｐ＃／ｍ！血中プロゲステロン値
は、９．６〜２２、０ ｒｄｊ／−の範囲にあり、上述
の如く黄体期になっていること、すなわち***が起った
ことをうらずけるものである。Experimental results: The presence or absence of ovulation can be diagnosed using BBT (basal body temperature) (
(Edited by Hiro Iizuka, Masasu Suzuki, Tadashi Sakamoto - supervised by: Obstetrics and Gynecology Series vol. 12: Everything about Infertility Diagnosis (1975))
Blood estradiol and progesterone were measured, and ovulation was observed in 7 out of 211 cases after administration of 0K-0-05, and ovulation was observed in 5 out of 8 cases during the anovulatory cycle. As we know, ovulation occurs,
It is true that when the ovary enters the luteal phase, BBT becomes high temperature, and blood estradiol and progesterone both become high (Masao Igarashi: Endocrinology and Gynecology, Ros II
(etal et al.) Figure P126 (197B). In our data, BBT exhibits a high temperature phase, and blood estradiol levels range from 30 to 150 p#/m! The blood progesterone level is in the range of 9.6 to 22.0 rdj/-, which indicates that the patient is in the luteal phase as described above, that is, that ovulation has occurred.
そこで、無***例を１群とし、その血中ホルモン動態を
検討すると、血中ＬＨは膜島前値の１９．３±８．１
ｍＩＵ／−から投与後は、３９．３±１７．４ｍＩＴＪ
／ｎ／と約２倍に増加し、血中ＦＳＨにも増加傾向を認
めたが、ＰＲＬ、Ｄｏｐａｍｌｎｅには変化がなかった
。Therefore, when anovulatory cases were considered as one group and their blood hormone dynamics were examined, blood LH was 19.3 ± 8.1 of the pre-island value.
After administration from mIU/-, 39.3±17.4 mITJ
/n/, and an increasing tendency was also observed in blood FSH, but there was no change in PRL and Dopamlne.
一方、***例におけるＬＨ，ＦＳＨは１群とは明らかに
異なり投与前に高値を示し、ＰＲＬ値は投与後低下する
のが認められた。ＬＨ−ＲＩＮに対する下垂体からのゴ
ナ−ビトロ２フ分泌パターンも１群とは異なり、殊にＬ
Ｈ分泌において***例では正常域をとるのに反し、１群
のそれは３０分以後過剰分泌型を呈した。一方ＦＳＨ分
ｍＡターンは両群における差が認められず下垂体機能が
正常に保たれている症例にのみ***が誘発された。On the other hand, LH and FSH in ovulatory cases were clearly different from those in group 1, showing high values before administration, and PRL values were observed to decrease after administration. The pattern of secretion of gona-vitro2 from the pituitary gland for LH-RIN is also different from that of group 1, especially for LH-RIN.
In contrast to the normal range of H secretion in the ovulatory cases, the H secretion in group 1 exhibited excessive secretion after 30 minutes. On the other hand, no difference was observed in the FSH minute mA turn between the two groups, and ovulation was induced only in cases in which pituitary function was maintained normally.
第１図〜第４図は、本発明の***誘発剤（前記の臨床例
）を投与した時の無***例及び***例のＬＨ，ＦＳＨ，
ＰＲＬ及び、Ｄｏｐａｍｌｎｅ値を各々示すものである
。Figures 1 to 4 show the LH, FSH, and
This shows the PRL and Dopamlne values, respectively.
Claims (1)
含有することを特徴とする***誘発剤。An ovulation-inducing agent characterized by containing 1,24-methylenecycloartanol as a main component.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18212282A JPS5973600A (en) | 1982-10-19 | 1982-10-19 | Ovulatory inducing agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18212282A JPS5973600A (en) | 1982-10-19 | 1982-10-19 | Ovulatory inducing agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS5973600A true JPS5973600A (en) | 1984-04-25 |
Family
ID=16112710
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP18212282A Pending JPS5973600A (en) | 1982-10-19 | 1982-10-19 | Ovulatory inducing agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5973600A (en) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000050012A1 (en) * | 1999-02-22 | 2000-08-31 | Elan Corporation, Plc | Solid oral dosage form containing an enhancer |
| US7658938B2 (en) | 1999-02-22 | 2010-02-09 | Merrion Reasearch III Limited | Solid oral dosage form containing an enhancer |
| US7674784B2 (en) | 2004-09-29 | 2010-03-09 | Morinaga Milk Industry Co., Ltd. | Drug and food or drink for improving hyperglycemia |
| US7704977B2 (en) | 2006-04-07 | 2010-04-27 | Merrion Research Iii Limited | Solid oral dosage form containing an enhancer |
| US7820722B2 (en) | 2001-05-11 | 2010-10-26 | Merrion Research Iii Limited | Permeation enhancers |
| US8999383B2 (en) | 2008-05-07 | 2015-04-07 | Merrion Research Iii Limited | Compositions of GnRH related compounds and processes of preparation |
| US10265384B2 (en) | 2015-01-29 | 2019-04-23 | Novo Nordisk A/S | Tablets comprising GLP-1 agonist and enteric coating |
| CN111050773A (en) * | 2017-08-30 | 2020-04-21 | 森永乳业株式会社 | Composition for increasing core body temperature |
-
1982
- 1982-10-19 JP JP18212282A patent/JPS5973600A/en active Pending
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000050012A1 (en) * | 1999-02-22 | 2000-08-31 | Elan Corporation, Plc | Solid oral dosage form containing an enhancer |
| US7658938B2 (en) | 1999-02-22 | 2010-02-09 | Merrion Reasearch III Limited | Solid oral dosage form containing an enhancer |
| US7820722B2 (en) | 2001-05-11 | 2010-10-26 | Merrion Research Iii Limited | Permeation enhancers |
| US7674784B2 (en) | 2004-09-29 | 2010-03-09 | Morinaga Milk Industry Co., Ltd. | Drug and food or drink for improving hyperglycemia |
| US7704977B2 (en) | 2006-04-07 | 2010-04-27 | Merrion Research Iii Limited | Solid oral dosage form containing an enhancer |
| US8883203B2 (en) | 2006-04-07 | 2014-11-11 | Merrion Research Iii Limited | Solid oral dosage form containing an enhancer |
| US8999383B2 (en) | 2008-05-07 | 2015-04-07 | Merrion Research Iii Limited | Compositions of GnRH related compounds and processes of preparation |
| US10265384B2 (en) | 2015-01-29 | 2019-04-23 | Novo Nordisk A/S | Tablets comprising GLP-1 agonist and enteric coating |
| CN111050773A (en) * | 2017-08-30 | 2020-04-21 | 森永乳业株式会社 | Composition for increasing core body temperature |
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