JPH01132524A - Remedy for climacteric disorder - Google Patents
Remedy for climacteric disorderInfo
- 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
Links
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims abstract description 12
- 229930003316 Vitamin D Natural products 0.000 claims abstract description 11
- 235000019166 vitamin D Nutrition 0.000 claims abstract description 11
- 239000011710 vitamin D Substances 0.000 claims abstract description 11
- 150000003710 vitamin D derivatives Chemical class 0.000 claims abstract description 11
- 229940046008 vitamin d Drugs 0.000 claims abstract description 11
- 239000004480 active ingredient Substances 0.000 claims abstract description 7
- 229940011871 estrogen Drugs 0.000 claims abstract description 7
- 239000000262 estrogen Substances 0.000 claims abstract description 7
- OFHCOWSQAMBJIW-AVJTYSNKSA-N alfacalcidol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C OFHCOWSQAMBJIW-AVJTYSNKSA-N 0.000 claims abstract description 6
- FCKJYANJHNLEEP-OIMXRAFZSA-N 24,25-Dihydroxyvitamin D Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCC(O)C(C)(C)O)C)=C\C=C1\C[C@H](O)CCC1=C FCKJYANJHNLEEP-OIMXRAFZSA-N 0.000 claims abstract 2
- 208000017657 Menopausal disease Diseases 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 7
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 238000000034 method Methods 0.000 abstract description 4
- 239000005556 hormone Substances 0.000 abstract description 3
- 229940088597 hormone Drugs 0.000 abstract description 3
- 239000002249 anxiolytic agent Substances 0.000 abstract description 2
- 239000007902 hard capsule Substances 0.000 abstract description 2
- 238000002347 injection Methods 0.000 abstract description 2
- 239000007924 injection Substances 0.000 abstract description 2
- 239000007901 soft capsule Substances 0.000 abstract description 2
- 239000006188 syrup Substances 0.000 abstract description 2
- 235000020357 syrup Nutrition 0.000 abstract description 2
- 239000003826 tablet Substances 0.000 abstract description 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- GMRQFYUYWCNGIN-NKMMMXOESA-N calcitriol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCCC(C)(C)O)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C GMRQFYUYWCNGIN-NKMMMXOESA-N 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 210000005036 nerve Anatomy 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 description 7
- 206010068975 Bone atrophy Diseases 0.000 description 6
- 230000000694 effects Effects 0.000 description 5
- 206010065687 Bone loss Diseases 0.000 description 3
- 208000002193 Pain Diseases 0.000 description 3
- 208000008930 Low Back Pain Diseases 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 210000001185 bone marrow Anatomy 0.000 description 2
- 208000001685 postmenopausal osteoporosis Diseases 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 208000008035 Back Pain Diseases 0.000 description 1
- 206010017076 Fracture Diseases 0.000 description 1
- 206010027304 Menopausal symptoms Diseases 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 229940005530 anxiolytics Drugs 0.000 description 1
- 210000000467 autonomic pathway Anatomy 0.000 description 1
- 230000037182 bone density Effects 0.000 description 1
- 230000004097 bone metabolism Effects 0.000 description 1
- 230000001054 cortical effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000009245 menopause Effects 0.000 description 1
- 230000011164 ossification Effects 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 235000005282 vitamin D3 Nutrition 0.000 description 1
- 239000011647 vitamin D3 Substances 0.000 description 1
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 description 1
- 229940021056 vitamin d3 Drugs 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
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)
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.
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)
| 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)
| 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 |
-
1987
- 1987-11-18 JP JP62289278A patent/JPH07110809B2/en not_active Expired - Fee Related
Patent Citations (3)
| 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)
| 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| LAPS | Cancellation because of no payment of annual fees |