JPH04149132A - Aqueous solution of danazol - Google Patents
Aqueous solution of danazolInfo
- Publication number
- JPH04149132A JPH04149132A JP27404190A JP27404190A JPH04149132A JP H04149132 A JPH04149132 A JP H04149132A JP 27404190 A JP27404190 A JP 27404190A JP 27404190 A JP27404190 A JP 27404190A JP H04149132 A JPH04149132 A JP H04149132A
- Authority
- JP
- Japan
- Prior art keywords
- danazol
- aqueous solution
- water
- solution
- dispersing
- 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
- POZRVZJJTULAOH-LHZXLZLDSA-N danazol Chemical compound C1[C@]2(C)[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=CC2=C1C=NO2 POZRVZJJTULAOH-LHZXLZLDSA-N 0.000 title claims abstract description 28
- 229960000766 danazol Drugs 0.000 title claims abstract description 28
- 239000007864 aqueous solution Substances 0.000 title claims abstract description 18
- 238000002360 preparation method Methods 0.000 claims abstract description 7
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract description 5
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 4
- 239000002736 nonionic surfactant Substances 0.000 claims abstract description 4
- 238000002347 injection Methods 0.000 claims abstract 3
- 239000007924 injection Substances 0.000 claims abstract 3
- 239000003755 preservative agent Substances 0.000 claims abstract 3
- 230000003381 solubilizing effect Effects 0.000 claims abstract 3
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000000243 solution Substances 0.000 abstract description 7
- 150000001875 compounds Chemical class 0.000 abstract description 4
- 230000003054 hormonal effect Effects 0.000 abstract description 2
- 230000028327 secretion Effects 0.000 abstract description 2
- 230000002335 preservative effect Effects 0.000 abstract 2
- 230000002054 antogonadotrophic effect Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 208000011099 endometrial disease Diseases 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 238000010521 absorption reaction Methods 0.000 description 3
- 238000010438 heat treatment Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 1
- 201000009273 Endometriosis Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 235000010469 Glycine max Nutrition 0.000 description 1
- 244000068988 Glycine max Species 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 description 1
- 229960001597 nifedipine Drugs 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
Abstract
Description
【発明の詳細な説明】 ＜Ａ）産業上の利用分野 本発明は、ダナゾールの水溶液に関するものである。[Detailed description of the invention] <A) Industrial application field The present invention relates to an aqueous solution of danazol.
（Ｂ）従来の技術
ダナゾールは、抗コナドトロビン作用によってＦ Ｓ
ＨやＬ）Ｉの分泌を抑制する一方で、性ホルモン作用を
有しないことから、子宮内膜症の治療に用いられる化合
物である。このダナゾールの優れた効果から、使用は年
々増加している９ダナゾールは現在ハードカプセルの形
で市販されており、１日あたり４００ｍｇ投与されてい
る。(B) Conventional technology Danazol has anti-conadotrobin effect that causes F S
It is a compound used in the treatment of endometriosis because it suppresses the secretion of H and L)I but does not have sex hormone effects. Due to the excellent effects of danazol, its use is increasing year by year.9 Danazol is currently commercially available in the form of hard capsules, and is administered at a dose of 400 mg per day.
このようにダナゾールの１日あたりの投与量か多いのは
、ダナゾールか水に難溶であるところから、製剤中に含
まれるダナゾールか消化管／（移行しないなめ、吸収さ
れないうちに体外へ排出されるためと考えられる。これ
らを解決するなめ、たとえば特開昭６１−１６１３号公
報にはダナゾールを微細に粉砕し、この粒子を胃腸管に
おけるｐ）Ｉて水または他の水溶性高分子、たとえはポ
リヒニルピロリドンなどて相互に結合させ、ヒース状に
する製剤か提示されている。しかし水沫はダナゾールの
溶解性を向上させたり、水溶液とすることは困難である
。The reason why the daily dose of danazol is so high is because danazol is poorly soluble in water, so the danazol contained in the preparation is absorbed into the gastrointestinal tract (it does not migrate and is excreted from the body before being absorbed). In order to solve these problems, for example, Japanese Patent Application Laid-open No. 1613/1983 has proposed finely pulverizing danazol and dispersing the particles into water or other water-soluble polymers, such as A preparation has been proposed in which the compounds are bonded together using polyhinylpyrrolidone to form a heath-like structure. However, it is difficult to improve the solubility of danazol or to form it into an aqueous solution using water droplets.
人体Ｉ＼の吸収性の向上を目的とした他の方法としては
、離水溶液の化合物であるニフェジピンの吸収性を向上
させるなめ、ニフェジピンとポリエチレンクリコールと
ポリオギンエチレンンルヒタンモノ第１・−トの特定配
合からなる製剤か特公昭６１−４０６４７号公報に記載
されているほか、特開平２−４２ Ｑ ２０には、ダナ
ゾール０，５〜５重量０゜をＨＬ Ｂ値か１２以上の界
面活性剤を選択し、１〜５０重量％および多価アルコー
ル４５〜９８．５重量を配合してダナゾール水溶液解し
た安定性の高い澄明な消か得ちれたと記されている。Another method aimed at improving the absorption of the human body is to improve the absorption of nifedipine, which is a compound in a synergic solution. In addition, Japanese Patent Publication No. 61-40647 describes a preparation consisting of a specific combination of It is reported that a highly stable and clear solution was obtained by dissolving danazol in an aqueous solution by blending 1 to 50% by weight of a danazol agent and 45 to 98.5% by weight of a polyhydric alcohol.
−かし、これらの技術は屯に製剤からの溶出性を向上し
、消化管からの体内への吸収性を向上させようというも
のである。このことは、ダナゾールか溶解していれは更
に速やかに吸収されることを表わしている。そこで本発
明者らは、ダナゾールの水溶液を得ることを鋭意検討し
、非イオン性界面活性剤と水溶性ポリマーを禽む水溶イ
ａ中に分散したのち、７０°へ８０ ”て力旧品ン容解
さぜる事により長期間安定なダナゾール水溶液を得る二
とかできた。However, these techniques are primarily aimed at improving dissolution from the preparation and absorption into the body from the gastrointestinal tract. This indicates that when danazol is dissolved, it is absorbed more rapidly. Therefore, the present inventors made extensive studies to obtain an aqueous solution of danazol, and after dispersing a nonionic surfactant and a water-soluble polymer in a water-soluble aqueous solution, the old product was By dissolving and stirring, it was possible to obtain a long-term stable danazol aqueous solution.
以下に実施例を示す９
実施例１
ダナゾール
緩衝液（ｐＨ７，８）
ポリビニルピロリドン
ンイーン−８０
ｇ
００ｍ１
Ｑ ｇ
ｍｌ
」二記組成の液を８０°て３０分加温溶解させたのち、
室温まで冷却し、水を加えて１０００ｍ ｌとし、透明
なダナソールＯ，ｉ’ｏ水溶液を得た。Examples are shown below. Example 1 Danazol buffer (pH 7, 8) Polyvinylpyrrolidone-80 g 00 ml Q g ml After dissolving the solution by heating at 80° for 30 minutes,
The mixture was cooled to room temperature, and water was added to make a total volume of 1000 ml to obtain a transparent Danasol O, i'o aqueous solution.
実方醒例 ２
ダナゾール
緩衝液（ｐｉ−（７，Ｓ ）
ポリヒニルアルコール
ソイーン２０
ｇ
００ｍ１
０ｇ
５ｍ１
一ト記組成の液を８０°て］時間加温溶解させたのち、
室温まで冷却し、水を加疋て１０１００Ｏとし、透明な
ダナゾール０．１°。水溶液を得た。Example 2 Danazol buffer (pi-(7,S) polyhinyl alcohol soybean 20 g 00 ml 0 g 5 ml After dissolving the solution by heating at 80° for an hour,
Cool to room temperature, add water to 10100O, and clear danazol 0.1°. An aqueous solution was obtained.
実方色Ｍ３
ダナゾール
緩衝液＜ Ｔ） ｔＩ２． 、０ ）
ポリビニルピロリドン
ノイーン８０
塩化ヘンザルコニウム
ｇ
７００ｒｒｉ１
０ ｇ
５ｍ１
０．１ｇ
上記組成の液を８０°で１時間加温溶解させたのち、室
温まで冷却し、水を加えて１０１００Ｏとし、透明なり
ナソール０．１°。水溶液を得た。Solid color M3 Danazol buffer < T) tI2. , 0) Polyvinylpyrrolidone noine 80 Henzalkonium chloride g 700rri10 g 5ml1 0.1g After heating and dissolving the liquid with the above composition at 80° for 1 hour, it was cooled to room temperature, water was added to make it 10100O, and it became transparent. 0.1°. An aqueous solution was obtained.
特１〒巳伸ベ ハイロシ貿易株式会社Special 1〒Minobu Hiroshi Trading Co., Ltd.
Claims (2)
２・３−α］イソキサゾール−１７オル（以下ダナゾー
ル）を有効成分として含むことを特徴とする水溶液。(1) 17α-pregnar 2,4 diene-20-ino[
An aqueous solution containing 2,3-α]isoxazol-17ol (hereinafter referred to as danazol) as an active ingredient.
性ポリマーを含む水溶液中に分散、可溶化させたのち、
等張化剤、防腐剤等を添加し、外用剤および注射剤とし
て調製されたダナゾール水溶液。(2) After dispersing and solubilizing danazol in an aqueous solution containing a nonionic surfactant and a water-soluble polymer,
Danazol aqueous solution prepared as external preparations and injections by adding tonicity agents, preservatives, etc.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27404190A JPH04149132A (en) | 1990-10-13 | 1990-10-13 | Aqueous solution of danazol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27404190A JPH04149132A (en) | 1990-10-13 | 1990-10-13 | Aqueous solution of danazol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04149132A true JPH04149132A (en) | 1992-05-22 |
Family
ID=17536144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP27404190A Pending JPH04149132A (en) | 1990-10-13 | 1990-10-13 | Aqueous solution of danazol |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04149132A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8227457B2 (en) | 2009-06-22 | 2012-07-24 | Dmi Acquisition Corp. | Method for treatment of diseases |
| US8586568B2 (en) | 2005-07-12 | 2013-11-19 | Ampio Pharmaceuticals, Inc. | Methods and products for treatment of diseases |
| US9351979B2 (en) | 2012-12-19 | 2016-05-31 | Ampio Pharmaceuticals, Inc. | Methods of treatment of diseases |
-
1990
- 1990-10-13 JP JP27404190A patent/JPH04149132A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8586568B2 (en) | 2005-07-12 | 2013-11-19 | Ampio Pharmaceuticals, Inc. | Methods and products for treatment of diseases |
| US8722651B2 (en) | 2005-07-12 | 2014-05-13 | Ampio Pharmaceuticals, Inc. | Methods and products for treatment of diseases |
| US8227457B2 (en) | 2009-06-22 | 2012-07-24 | Dmi Acquisition Corp. | Method for treatment of diseases |
| US9233113B2 (en) | 2009-06-22 | 2016-01-12 | Ampio Pharmaceuticals, Inc. | Method for treatment of diseases |
| US9987292B2 (en) | 2009-06-22 | 2018-06-05 | Ampio Pharmaceuticals, Inc. | Method for treatment of diseases |
| US9351979B2 (en) | 2012-12-19 | 2016-05-31 | Ampio Pharmaceuticals, Inc. | Methods of treatment of diseases |
| US10058562B2 (en) | 2012-12-19 | 2018-08-28 | Ampio Pharmaceuticals, Inc. | Methods of treatment of diseases |
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