JP2816500B2 - Anti-osteoporosis agent - Google Patents
Anti-osteoporosis agentInfo
- Publication number
- JP2816500B2 JP2816500B2 JP27997890A JP27997890A JP2816500B2 JP 2816500 B2 JP2816500 B2 JP 2816500B2 JP 27997890 A JP27997890 A JP 27997890A JP 27997890 A JP27997890 A JP 27997890A JP 2816500 B2 JP2816500 B2 JP 2816500B2
- Authority
- JP
- Japan
- Prior art keywords
- bucillamine
- bone
- agent
- osteoporosis
- disease
- 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.)
- Expired - Fee Related
Links
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
【発明の詳細な説明】 「産業上の利用分野」 本発明はブシラミンまたはその塩類を有効成分とする
抗骨粗鬆剤に関する。Description: TECHNICAL FIELD The present invention relates to an anti-osteoporotic agent containing bucillamine or a salt thereof as an active ingredient.
「従来技術、発明が解決しようとする課題及び課題を解
決するための手段」 ブシラミンは抗リウマチ剤として医薬品に用いられて
おり、他にも喀痰溶解剤、肝障害抑制剤、抗白内障剤と
して有用であることが報告されている（特公昭56−5388
号、特公昭60−11888号、特公昭62−13922号、特公昭63
−13964号）。"Prior art, problems to be solved by the invention and means for solving the problems" Bucillamine is used in pharmaceuticals as an antirheumatic agent, and is also useful as a sputum dissolving agent, a liver injury inhibitor, and an anticataract agent (Japanese Patent Publication No. 56-5388)
No., JP-B-60-11888, JP-B-62-13922, JP-B-63
No. 13964).
このように、ブシラミンは優れた薬効を有する化合物
であるが、骨に対する作用についてはまだ知られていな
かつた。As described above, bucillamine is a compound having excellent medicinal properties, but its action on bone has not been known yet.
骨粗鬆症は骨の生成と吸収のバランスが崩れ、骨の吸
収が異常に増加することにより骨の絶対量が減少する疾
患で、骨多孔症とも言われている。Osteoporosis is a disease in which the balance between bone formation and resorption is disrupted, and abnormal resorption of bone causes the absolute amount of bone to decrease, and is also called osteoporosis.
臨床的に最も問題となるのは老人性骨粗鬆症で、骨粗
鬆は加齢とともにその発症率が増大し、特に女性にその
傾向が顕著である。その症状は腰痛が主であり、また老
人の大腿骨骨折の原因のほとんどはこの骨粗鬆症による
ものである。これまで、骨粗鬆症の治療剤として使用さ
れているものにはカルシウム剤やビタミンＤ剤などがあ
るが、より効果の確実なものが求められていた。The most clinically problematic is senile osteoporosis, and the incidence of osteoporosis increases with age, especially in women. The symptoms are mainly low back pain, and most of the causes of femoral fractures in the elderly are due to this osteoporosis. Heretofore, there have been calcium preparations and vitamin D preparations used as therapeutic agents for osteoporosis, but more effective ones have been demanded.
そこで、本発明者等は、ブシラミンの新しい薬理作用
を見つけるべく種々検討した結果、抗骨粗鬆剤として有
用であることを見い出した。The present inventors have conducted various studies to find a new pharmacological action of busilamine, and as a result, have found that it is useful as an anti-osteoporotic agent.
「発明の構成」 本発明は下記式で示されるブシラミンまたはその塩類
（以下本化合物という）を有効成分とする抗骨粗鬆剤に
関する。"Constitution of the Invention" The present invention relates to an anti-osteoporotic agent comprising a bucillamine represented by the following formula or a salt thereof (hereinafter referred to as the present compound) as an active ingredient.
本発明における塩類とは、医薬として許容される塩で
あればよく、ナトリウム塩、カリウム塩等が例として挙
げられる。 The salt in the present invention may be a pharmaceutically acceptable salt, and examples thereof include a sodium salt and a potassium salt.
本化合物が抗リウマチ剤、喀痰溶解剤、肝障害抑制
剤、抗白内障剤として有用であることは知られている
が、骨に対する作用についてはまだ知られていなかつ
た。It is known that this compound is useful as an antirheumatic agent, sputum dissolving agent, liver injury inhibitor, and anticataract agent, but its effect on bone has not yet been known.
そこで、本発明者等は、本化合物の新しい薬理作用を
見つけるべく種々検討した結果、本化合物が骨吸収抑制
作用を有しており、抗骨粗鬆剤として有用であることを
見い出した。The present inventors have conducted various studies to find a new pharmacological action of the present compound, and as a result, have found that the present compound has a bone resorption inhibiting action and is useful as an antiosteoporotic agent.
骨粗鬆症に対する有用性を調べるため、老齢の雌マウ
スの加齢病変である線繊維骨疾患に対するブシラミンの
効果を検討した。In order to examine the usefulness for osteoporosis, the effect of bucillamine on fibrobone disease, an aging lesion in aged female mice, was examined.
詳しくは薬理試験の項で記載するが、コントロールと
比較してブシラミン投与群では線繊維性骨疾患を抑制し
ており、ブシラミンが抗骨粗鬆剤として有用であること
が示された。As described in detail in the section of pharmacological test, the group treated with bucillamine suppressed the fibrotic bone disease as compared with the control, indicating that bucillamine is useful as an antiosteoporotic agent.
本化合物は経口投与、非経口投与のいずれでも投与す
ることができ、公知の製剤技術により錠剤、顆粒剤、散
剤、注射剤等の製剤とすることができる。The present compound can be administered either orally or parenterally, and can be made into tablets, granules, powders, injections and other preparations by known preparation techniques.
本化合物の投与量は病状、剤型、年令等によつて決め
られるが、経口投与の場合、通常１日10〜1000mgを１回
または数回にわけて投与すればよい。The dose of the present compound is determined according to the disease state, dosage form, age and the like. In the case of oral administration, it is usually sufficient to administer 10 to 1000 mg once or several times a day.
雌マウスの骨の加齢病変である線繊維骨疾患は骨髄腔
が線維芽細胞様細胞、骨芽細胞、破骨細胞および骨梁に
置換されていく病変であり、部位によつては既存の骨の
吸収や非薄化を伴うものである。Fibroblast disease, an age-related lesion in the bone of female mice, is a lesion in which the bone marrow cavity is replaced by fibroblast-like cells, osteoblasts, osteoclasts, and trabecular bone. It involves bone resorption and non-thinning.
そこで、本発明の有用性を調べるため、この雌マウス
の線維性骨疾患に対するブシラミンの効果を検討した。Therefore, in order to examine the usefulness of the present invention, the effect of bucillamine on fibrous bone disease of this female mouse was examined.
（実験方法） ブシラミンの投与量が2000mg/kgとなるように餌に混
ぜ、雌のCrj:B6C3F1マウス（１群54匹）に18ケ月投与し
１ケ月の休薬後、病理検査を行なつた。Mixed with food as the dose of (Experimental method) bucillamine is 2000 mg / kg, female Crj: B6C3F 1 mice (1 group 54 rats) to 18 months administered after 1 month washout, line summer the pathology Was.
（結果） 胸骨の病理検査の結果を表に示す。(Results) The results of pathological examination of the sternum are shown in the table.
表に示すように、ブシラミンを投与していないコント
ロール群では54例中53例のマウスで軽度異常の線繊維骨
疾患が生じているのに対し、ブシラミン投与群で線繊性
骨疾患が生じているのは54例中12例ににすぎなかつた。 As shown in the table, in the control group not receiving bucillamine, slightly abnormal fibrous bone disease occurred in 53 of 54 mice, whereas in the bucillamine administration group, fibrillar bone disease occurred. Only 12 of the 54 cases were present.
また、この傾向は腰椎の病理検査でも同様であつた。
以上のことから、ブシラミンを投与したものでは線維性
骨疾患が抑制されており、ブシラミンが抗骨粗鬆剤とし
て有用であることが示された。This tendency was also observed in the lumbar pathological examination.
From the above, it was shown that fibrous bone disease was suppressed by administration of bucillamine, and that bucillamine was useful as an antiosteoporotic agent.
「発明の効果」 薬理試験の結果で示されるように、ブシラミンは骨吸
収抑制作用を有しており、抗骨粗鬆剤として有用であ
る。[Effect of the Invention] As shown in the results of the pharmacological test, bucillamine has a bone resorption inhibiting effect and is useful as an anti-osteoporotic agent.
Claims (1)
る抗骨粗鬆剤。1. An anti-osteoporotic agent comprising bucillamine or a salt thereof as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27997890A JP2816500B2 (en) | 1990-10-17 | 1990-10-17 | Anti-osteoporosis agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP27997890A JP2816500B2 (en) | 1990-10-17 | 1990-10-17 | Anti-osteoporosis agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH04154722A JPH04154722A (en) | 1992-05-27 |
| JP2816500B2 true JP2816500B2 (en) | 1998-10-27 |
Family
ID=17618601
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP27997890A Expired - Fee Related JP2816500B2 (en) | 1990-10-17 | 1990-10-17 | Anti-osteoporosis agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2816500B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5670545A (en) * | 1996-02-09 | 1997-09-23 | Board Of Regents Of The University Of Colorado | Method for the treatment of ischemic disease and reperfusion injury and the prevention of the adverse effects of reactive oxygen species |
| CN1184965C (en) | 1999-06-21 | 2005-01-19 | 参天制药株式会社 | Remedies for arthrosis deformans |
-
1990
- 1990-10-17 JP JP27997890A patent/JP2816500B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH04154722A (en) | 1992-05-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |