JPH01132524A - Remedy for climacteric disorder - Google Patents

Remedy for climacteric disorder

Info

Publication number
JPH01132524A
JPH01132524A JP28927887A JP28927887A JPH01132524A JP H01132524 A JPH01132524 A JP H01132524A JP 28927887 A JP28927887 A JP 28927887A JP 28927887 A JP28927887 A JP 28927887A JP H01132524 A JPH01132524 A JP H01132524A
Authority
JP
Japan
Prior art keywords
dihydroxyvitamin
1alpha
remedy
vitamin
bone
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.)
Granted
Application number
JP28927887A
Other languages
Japanese (ja)
Other versions
JPH07110809B2 (en
Inventor
Hideo Honjo
本庄 英雄
Kazuo Naito
内藤 和郎
Haruo Togawa
戸川 晴雄
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teijin Ltd
Original Assignee
Teijin Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Teijin Ltd filed Critical Teijin Ltd
Priority to JP62289278A priority Critical patent/JPH07110809B2/en
Publication of JPH01132524A publication Critical patent/JPH01132524A/en
Publication of JPH07110809B2 publication Critical patent/JPH07110809B2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Abstract

PURPOSE:To obtain a remedy for climacteric disorder, containing a vitamin D of active type. CONSTITUTION:A vitamin D of active type selected from 1alpha-hydroxyvitamin D, 1alpha, 24-dihydroxyvitamin D, 1alpha,25-dihydroxyvitamin D, 24,25-dihydroxyvitamin D, 1alpha,24,25-trihydroxyvitamin D, 24,25-F2-1 d,25-dihydroxyvitamin D and 26,26,26,27,27,27-F6-1alpha-25-dihydroxyvitamin is included as an active ingredient and pharmaceutically manufactured by a conventional procedure to give the aimed substance. The substance can be prepared into a dosage form such as soft or hard capsule, tablet, syrup or injection. A dose is 0.01-10mug/day. The titled remedy can be used with a hormone agent, automatic nerve controlling agent or antianxiety agent conventionally used as a remedy for climacteric disorder and especially preferably with estrogen.

Description

【発明の詳細な説明】 本発明は、活性型ビタミンDを有効成分として含有する
、更年期障害の治療薬に関する。
DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a therapeutic agent for menopausal disorders containing active vitamin D as an active ingredient.

閉経後の女性は、卵巣ホルモンであるエストロゲンの低
下を成因として骨減少を招くことが多く、特に60代以
降では、閉経後骨粗鬆症に高い頻度(約30%以上)で
罹患する。そして、この疾患に対しては、骨減少の進行
の防止、骨量の増加1骨折の危険の減少、骨減少に伴な
う腰背痛の防止を目的として、活性型ビタミンD、類が
治療薬として利用され、優れた効果をあげている。
Postmenopausal women often suffer from bone loss due to a decrease in the ovarian hormone estrogen, and especially those in their 60s and above suffer from postmenopausal osteoporosis at a high frequency (approximately 30% or more). Active vitamin D is used to treat this disease, with the aim of preventing the progression of bone loss, increasing bone mass, reducing the risk of fractures, and preventing lower back pain associated with bone loss. It is used as a medicine and has excellent effects.

ところで、閉経直後の40代から50代の女性では、更
年期障害に罹患することが多い、そこで本発明者らは、
更年期障害に罹患した患者では、閉経後骨粗鬆症の形の
骨萎縮が早期進行しているのではないかと予想し、更年
期障害患者に活性型ビタミンDの一つである1α−ヒド
ロキシビタミンD3(以下1α−0H−D3と略記する
)を投与し、その骨萎縮との関係を検討した。その結果
、驚くべきことに、更年期障害患者では骨萎縮又は骨含
量の減少はほとんど認められず、一方、1α−0H−D
、の投与によって患者の骨背痛や肩こりが非常に減少し
、かつ更年期障害の重症度を表わすKUDI]erla
n指数(J、^、I4.A、、 171.1627.1
959参照)も有意に減少していることを知見し、本発
明に到達した。
By the way, women in their 40s and 50s who have just gone through menopause often suffer from menopausal symptoms, so the present inventors
Anticipating that bone atrophy in the form of postmenopausal osteoporosis may progress early in patients suffering from menopausal disorders, 1α-hydroxyvitamin D3 (hereinafter referred to as 1α), an active form of vitamin D, is administered to menopausal patients. -0H-D3) was administered, and its relationship with bone atrophy was investigated. Surprisingly, there was little bone atrophy or bone content loss in menopausal patients, whereas 1α-0H-D
The patient's back pain and shoulder stiffness were greatly reduced by administration of KUDI]erla, which indicates the severity of menopausal disorder.
n index (J, ^, I4.A,, 171.1627.1
959) was also significantly reduced, leading to the present invention.

即ち、本発明は、活性型ビタミンDを有効成分とする更
年期障害の治療薬である。
That is, the present invention is a therapeutic agent for menopausal disorders containing active vitamin D as an active ingredient.

本発明における活性型ビタミンDとしては、例えば、1
α−ヒドロキシビタミンD、1α、24−ジヒドロキシ
ビタミンD、1α、25−ジヒドロキシビンタミンD、
24.25−ジヒドロキシビタミンD、1α、 24.
25− )ジヒドロキシビタミンD、24.25  F
2 1α、25−ジヒドロキシビンタミンD及び26,
26,26,27,27.27  Fs  1α−25
−ジヒドロキシビタミンDが挙げられる。好ましいのは
、それぞれの活性型ビタミンD3であり、特に好ましい
のは1α−ヒドロキシビタミンD3である。これらの有
効成分は公知の方法で、適当な賦型剤等を用いて軟カプ
セル剤、硬カプセル剤。
The active vitamin D in the present invention includes, for example, 1
α-hydroxyvitamin D, 1α,24-dihydroxyvitamin D, 1α,25-dihydroxyvintamine D,
24.25-dihydroxyvitamin D, 1α, 24.
25-) Dihydroxyvitamin D, 24.25 F
2 1α, 25-dihydroxyvintamine D and 26,
26, 26, 27, 27.27 Fs 1α-25
-dihydroxyvitamin D. Preferred are the respective active forms of vitamin D3, particularly preferred is 1α-hydroxyvitamin D3. These active ingredients can be formulated into soft capsules or hard capsules using appropriate excipients using known methods.

錠剤、シロップ等の経口剤あるいは注射剤にして使用で
きる。有効成分の投与量は、通常0.01〜10μg/
日/人程度であり、投与回数は、通常1〜3回/日であ
り、このような条件を満足するように製剤を調製するの
が好ましい。
It can be used in the form of oral preparations such as tablets and syrup, or injections. The dosage of the active ingredient is usually 0.01 to 10 μg/
The number of administrations is usually 1 to 3 times per day, and it is preferable to prepare a preparation to satisfy these conditions.

本発明の治療薬は、更年期障害の治療に従来用いられて
きたホルモン剤、自律神経調整剤、抗不安剤等と併用可
能であり、特にエストロゲンとの併用は好ましい。
The therapeutic agent of the present invention can be used in combination with hormones, autonomic nerve regulators, anxiolytics, etc. that have been conventionally used in the treatment of menopausal disorders, and combination with estrogen is particularly preferred.

以下、実施例により本発明を詳述する。Hereinafter, the present invention will be explained in detail with reference to Examples.

実施例1 11施設の病院産婦人科で、更年期障害と診断された症
例(、!に者)について、その年齢分布とMD法による
骨萎縮の調査を行なった。結果はそれぞれ第1表と第2
表に示した通りであった0年齢的には90%以上が60
才未満であり、また90%以上が骨は正常であることが
わかる(骨萎縮の結果が■度と1度の症例は、年齢的に
は60才以上の症例に対応していた)。
Example 1 In the obstetrics and gynecology departments of 11 hospitals, we investigated the age distribution and bone atrophy using the MD method for cases diagnosed with menopausal disorders. The results are shown in Tables 1 and 2, respectively.
As shown in the table, more than 90% of people were 60 years old.
It can be seen that more than 90% of the patients had normal bones (cases with bone atrophy results of grade 1 and grade 1 corresponded to cases aged 60 years or older).

第1表の患者のうち22人には、1α−0H−D、を1
日当り1.0μg投与し、別の5人には1α−0H−D
3以外に1日当り1.25■のエストロゲンを併用投与
した。そして、2ケ月経過後ににLIpp13rlan
指数を求め、その改善効果を改善点数側症例分布とし第
3表に示しな、85%以上で、にUpperlan指数
の改善効果が現われていることがわかる。また、エスト
ロゲンを併用すると、改善効果が増強される傾向にある
こともわかる。
Twenty-two of the patients in Table 1 received 1α-0H-D,
1.0 μg per day, and 1α-0H-D to another 5 patients.
In addition to 3, 1.25 μ of estrogen per day was administered in combination. Then, after 2 months, LIpp13rlan
The index is calculated and the improvement effect is shown in Table 3 as the case distribution on the improvement score side.It can be seen that the improvement effect of the Upperlan index appears in 85% or more. It can also be seen that when estrogen is used in combination, the improvement effect tends to be enhanced.

第3表 なおMD法とは、X線像の黒化度の基準として、アルミ
階段(Gray 5cale)とともに平部のX線像を
撮影し、第■中手骨の近位端と遠位端の中間点で、デン
シトメータを用いて、その黒化度を測定し、コンピュー
タを用いて、ピーク高さをアルミ階段の段数に換算し、
骨幅(D)、骨髄幅(d)。
Table 3 Note that the MD method involves taking an X-ray image of the flat part along with an aluminum staircase (Gray 5cale) as a standard for the degree of darkening of the X-ray image, and measuring the proximal and distal ends of the first metacarpal. At the midpoint, the degree of blackening is measured using a densitometer, and the peak height is converted to the number of steps of aluminum stairs using a computer.
Bone width (D), bone marrow width (d).

骨皮質幅指数[MDI= (D−d)/D)コ、骨皮質
の密度の指標(GSlax)、  (骨皮質+骨髄)の
密度の指標(GSlin ) 、単位長さ当りの骨密度
の指標(ΣF S/D )等を求め、これらの指標から
、骨萎縮(骨の@髭化)を判定する方法である(弁上、
串田、宮本、矢島、伊丹、山下、骨代謝、13巻、18
7〜195 (1980)) 。
Bone cortical width index [MDI = (D-d)/D), index of bone cortex density (GSlax), index of density of (bone cortex + bone marrow) (GSlin), index of bone density per unit length (ΣF S/D ), etc., and from these indicators, bone atrophy (bone formation) is determined (on the valve,
Kushida, Miyamoto, Yajima, Itami, Yamashita, Bone Metabolism, Volume 13, 18
7-195 (1980)).

実施例2 第1表の患者のうち29人に、1α−0H−D。Example 2 1α-0H-D in 29 of the patients in Table 1.

を1,0Hg/日ずつ2ケ月間投与し、腰背痛(疼痛指
数)の改善効果を調べた。うち5人には、実施例1の場
合と同様にエストロゲンも併用した。
was administered at a dose of 1.0 Hg/day for 2 months to examine its effect on improving lower back pain (pain index). Five of them also received estrogen as in Example 1.

結果を第4表に示した。The results are shown in Table 4.

第4表 第4表から、75%以上で疼痛指数が改善されているこ
とがわかる。
Table 4 Table 4 shows that the pain index was improved in 75% or more.

なお疼痛指数とは、下記のごとき7つの調査項目につい
て患者に評価してもらい、評点を合計したものを指数と
して定義したものである。
The pain index is defined as the sum of scores obtained by asking patients to evaluate the following seven survey items.

Claims (1)

【特許請求の範囲】 1、活性型ビタミンDを有効成分とする更年期障害の治
療薬。 2、活性型ビタミンDが、1α−ヒドロキシビタミンD
、1α,24−ジヒドロキシビタミンD、1α,25−
ジヒドロキシビンタミンD、24,25−ジヒドロキシ
ビタミンD、1α,24,25−トリヒドロキシビタミ
ンD、24,25−F_2−1α,25−ジヒドロキシ
ビンタミンD及び26,26,26,27,27,27
−F_6−1α−25−ジヒドロキシビタミンDからな
る群から選ばれたものである、特許請求の範囲第1項記
載の更年期障害の治療薬。 3、活性型ビタミンDが1α−ヒドロキシビタミンD_
3である特許請求の範囲第1項記載の更年期障害の治療
薬。 4、活性型ビタミンDの他に有効成分としてエストロゲ
ンを含む、特許請求の範囲第1項記載の更年期障害の治
療薬。
[Claims] 1. A therapeutic agent for menopausal disorders containing active vitamin D as an active ingredient. 2. Active vitamin D is 1α-hydroxyvitamin D
, 1α,24-dihydroxyvitamin D, 1α,25-
Dihydroxyvintamine D, 24,25-dihydroxyvitamin D, 1α,24,25-trihydroxyvitamin D, 24,25-F_2-1α,25-dihydroxyvintamine D and 26,26,26,27,27,27
-F_6-1α-25-dihydroxyvitamin D. 3. The active form of vitamin D is 1α-hydroxyvitamin D_
3. The therapeutic agent for menopausal disorder according to claim 1, which is No. 3. 4. The therapeutic agent for menopausal disorders according to claim 1, which contains estrogen as an active ingredient in addition to active vitamin D.
JP62289278A 1987-11-18 1987-11-18 Remedies for menopause Expired - Fee Related JPH07110809B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP62289278A JPH07110809B2 (en) 1987-11-18 1987-11-18 Remedies for menopause

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP62289278A JPH07110809B2 (en) 1987-11-18 1987-11-18 Remedies for menopause

Publications (2)

Publication Number Publication Date
JPH01132524A true JPH01132524A (en) 1989-05-25
JPH07110809B2 JPH07110809B2 (en) 1995-11-29

Family

ID=17741100

Family Applications (1)

Application Number Title Priority Date Filing Date
JP62289278A Expired - Fee Related JPH07110809B2 (en) 1987-11-18 1987-11-18 Remedies for menopause

Country Status (1)

Country Link
JP (1) JPH07110809B2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19916419A1 (en) * 1999-04-08 2000-10-19 Schering Ag Combination preparation of vitamin D metabolites or vitamin D analogues and an estrogenic component for the treatment of osteoporosis

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60120812A (en) * 1983-12-02 1985-06-28 Teijin Ltd Remedy for diabetic osteopenia
JPS61130225A (en) * 1984-11-29 1986-06-18 Kureha Chem Ind Co Ltd Pain mitigating agent for renal osteodystrophy
JPS6233A (en) * 1985-04-04 1987-01-06 ザ、ゼネラル、ホスピタル、コ−ポレ−シヨン Medicine compound for increasing bone mass

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS60120812A (en) * 1983-12-02 1985-06-28 Teijin Ltd Remedy for diabetic osteopenia
JPS61130225A (en) * 1984-11-29 1986-06-18 Kureha Chem Ind Co Ltd Pain mitigating agent for renal osteodystrophy
JPS6233A (en) * 1985-04-04 1987-01-06 ザ、ゼネラル、ホスピタル、コ−ポレ−シヨン Medicine compound for increasing bone mass

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19916419A1 (en) * 1999-04-08 2000-10-19 Schering Ag Combination preparation of vitamin D metabolites or vitamin D analogues and an estrogenic component for the treatment of osteoporosis
WO2000061123A3 (en) * 1999-04-08 2000-12-28 Schering Ag Compound preparation made of vitamin d metabolites or vitamin d analogues and an oestrogenic component for treating osteoporosis
JP2002541188A (en) * 1999-04-08 2002-12-03 シエーリング アクチエンゲゼルシャフト Composite preparation comprising vitamin-D-metabolite or vitamin D-analog and estrogen component for treating osteoporosis
DE19916419B4 (en) * 1999-04-08 2005-06-16 Schering Ag Combination preparation of vitamin D metabolites or vitamin D analogues and an estrogen partial agonist for the treatment of osteoporosis

Also Published As

Publication number Publication date
JPH07110809B2 (en) 1995-11-29

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