JPS63104926A - Remedy or preventive agent against senile dementia - Google Patents
Remedy or preventive agent against senile dementiaInfo
- Publication number
- JPS63104926A JPS63104926A JP24837686A JP24837686A JPS63104926A JP S63104926 A JPS63104926 A JP S63104926A JP 24837686 A JP24837686 A JP 24837686A JP 24837686 A JP24837686 A JP 24837686A JP S63104926 A JPS63104926 A JP S63104926A
- Authority
- JP
- Japan
- Prior art keywords
- senile dementia
- vitamin
- active
- remedy
- agent
- 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
- 208000024827 Alzheimer disease Diseases 0.000 title claims abstract description 39
- 206010039966 Senile dementia Diseases 0.000 title claims abstract description 39
- 230000003449 preventive effect Effects 0.000 title abstract description 3
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 18
- 229940088594 vitamin Drugs 0.000 claims abstract description 14
- 229930003231 vitamin Natural products 0.000 claims abstract description 14
- 235000013343 vitamin Nutrition 0.000 claims abstract description 14
- 239000011782 vitamin Substances 0.000 claims abstract description 14
- 239000004480 active ingredient 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
- BJYLYJCXYAMOFT-RSFVBTMBSA-N tacalcitol Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CC[C@@H](O)C(C)C)=C\C=C1\C[C@@H](O)C[C@H](O)C1=C BJYLYJCXYAMOFT-RSFVBTMBSA-N 0.000 claims abstract 2
- 238000011282 treatment Methods 0.000 claims description 12
- 150000003722 vitamin derivatives Chemical class 0.000 claims description 9
- 230000002265 prevention Effects 0.000 claims description 8
- 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 abstract description 18
- 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 abstract description 15
- 235000005282 vitamin D3 Nutrition 0.000 abstract description 15
- 239000011647 vitamin D3 Substances 0.000 abstract description 15
- 229940021056 vitamin d3 Drugs 0.000 abstract description 15
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 abstract description 5
- 239000011575 calcium Substances 0.000 abstract description 5
- 229910052791 calcium Inorganic materials 0.000 abstract description 5
- 230000003913 calcium metabolism Effects 0.000 abstract description 5
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract description 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 abstract description 3
- 239000000203 mixture Substances 0.000 abstract description 3
- 239000003755 preservative agent Substances 0.000 abstract description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract description 2
- 229920002472 Starch Polymers 0.000 abstract description 2
- 239000003963 antioxidant agent Substances 0.000 abstract description 2
- 235000019359 magnesium stearate Nutrition 0.000 abstract description 2
- 239000002504 physiological saline solution Substances 0.000 abstract description 2
- 230000001737 promoting effect Effects 0.000 abstract description 2
- 239000008107 starch Substances 0.000 abstract description 2
- 235000019698 starch Nutrition 0.000 abstract description 2
- -1 succharides Chemical compound 0.000 abstract description 2
- 239000004094 surface-active agent Substances 0.000 abstract description 2
- 239000000454 talc Substances 0.000 abstract description 2
- 229910052623 talc Inorganic materials 0.000 abstract description 2
- 235000012222 talc Nutrition 0.000 abstract description 2
- 230000003078 antioxidant effect Effects 0.000 abstract 1
- 238000001179 sorption measurement Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 8
- 229940079593 drug Drugs 0.000 description 7
- 206010012289 Dementia Diseases 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 4
- 239000007901 soft capsule Substances 0.000 description 4
- 238000010521 absorption reaction Methods 0.000 description 3
- 229960005084 calcitriol Drugs 0.000 description 3
- 230000002490 cerebral effect Effects 0.000 description 3
- 210000001035 gastrointestinal tract Anatomy 0.000 description 3
- 208000020016 psychiatric disease Diseases 0.000 description 3
- JWUBBDSIWDLEOM-UHFFFAOYSA-N 25-Hydroxycholecalciferol Natural products C1CCC2(C)C(C(CCCC(C)(C)O)C)CCC2C1=CC=C1CC(O)CCC1=C JWUBBDSIWDLEOM-UHFFFAOYSA-N 0.000 description 2
- JWUBBDSIWDLEOM-DCHLRESJSA-N 25-Hydroxyvitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCCC(C)(C)O)C)=C/C=C1\C[C@@H](O)CCC1=C JWUBBDSIWDLEOM-DCHLRESJSA-N 0.000 description 2
- JWUBBDSIWDLEOM-NQZHSCJISA-N 25-hydroxy-3 epi cholecalciferol Chemical group C1([C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@@H](CCCC(C)(C)O)C)=CC=C1C[C@H](O)CCC1=C JWUBBDSIWDLEOM-NQZHSCJISA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 241000283986 Lepus Species 0.000 description 2
- 229910000323 aluminium silicate Inorganic materials 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- HNPSIPDUKPIQMN-UHFFFAOYSA-N dioxosilane;oxo(oxoalumanyloxy)alumane Chemical compound O=[Si]=O.O=[Al]O[Al]=O HNPSIPDUKPIQMN-UHFFFAOYSA-N 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- GMRQFYUYWCNGIN-UHFFFAOYSA-N 1,25-Dihydroxy-vitamin D3' Natural products C1CCC2(C)C(C(CCCC(C)(C)O)C)CCC2C1=CC=C1CC(O)CC(O)C1=C GMRQFYUYWCNGIN-UHFFFAOYSA-N 0.000 description 1
- 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 description 1
- 208000035473 Communicable disease Diseases 0.000 description 1
- 239000004129 EU approved improving agent Substances 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 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 description 1
- 235000020964 calcitriol Nutrition 0.000 description 1
- 239000011612 calcitriol Substances 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000003727 cerebral blood flow Effects 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 description 1
- 235000010228 ethyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004403 ethyl p-hydroxybenzoate Substances 0.000 description 1
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 230000037353 metabolic pathway Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 238000000554 physical therapy Methods 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000005544 vitamin D3 metabolite Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】 〈産業上の利用分野〉 本発明は新規の老年性痴呆症治療又は予防剤に関する。[Detailed description of the invention] <Industrial application field> The present invention relates to a novel agent for treating or preventing senile dementia.
更に詳しくは、活性型ビタミンＤ３類を有効成分とする
老年性痴呆症治療又は予防剤に関する。More specifically, the present invention relates to a treatment or prevention agent for senile dementia containing active vitamin D3 as an active ingredient.
〈従来技術とその問題点〉
医療技術の進歩は人間の寿命を延長した。各種の薬物の
開発、物理療法の進展、外科手法の進歩等により感染症
、＾血圧、癌等の治療法は確実に進歩してきた。そして
、人間の寿命は、今後も徐々にではあるが着実に延長し
つづけていくようである。<Prior art and its problems> Advances in medical technology have extended human lifespans. Treatment methods for infectious diseases, blood pressure, cancer, etc. have steadily progressed due to the development of various drugs, advances in physical therapy, advances in surgical techniques, etc. And it appears that human lifespans will continue to increase gradually but steadily.
しかるに、上記のような肉体的な疾患は克服されつつあ
る一方、精神的な疾患が社会問題化している。なかでも
社会が高齢化するに伴い、高齢者の精神疾患が増加して
いる。精神疾患の中でも老年性痴呆症は患者自身の人格
の喪失、家族の犠牲。However, while the physical illnesses mentioned above are being overcome, mental illnesses are becoming a social problem. In particular, as society ages, mental illnesses among the elderly are increasing. Among mental illnesses, senile dementia causes the patient to lose his or her own personality and sacrifices his or her family.
有効な治療法の欠如、病因の不明等の理由で重大な問題
といえよう。This is a serious problem due to the lack of effective treatments and the unknown etiology.
従来、老年性痴呆症の治療法としては脳血流循環改善剤
、脳代謝賦活剤等の薬物療法が試みられてきた。そして
老年性痴呆症の中でも脳血管型老年性痴呆症には、脳血
流循環改善剤と脳代謝賦活剤の併用により、症状の若干
の改善がみられるといわれている。Conventionally, drug treatments such as cerebral blood circulation improving agents and cerebral metabolism activating agents have been attempted as treatments for senile dementia. Among senile dementias, it is said that some improvement in the symptoms of cerebrovascular senile dementia can be seen by the combined use of a cerebral blood flow improving agent and a cerebral metabolism activator.
しかしながら老年性痴呆症の原因が明らかでないので、
実際には、十分に有効な薬物がないのが現状である。However, since the cause of senile dementia is not clear,
In reality, there are currently no sufficiently effective drugs.
さらに、老年性痴呆症の別の型であるアルツハイマー型
老年性痴呆症は全く原因が不明であり、はとんど全く有
効な薬物がないといわれている。Furthermore, the cause of Alzheimer's senile dementia, which is another type of senile dementia, is completely unknown, and it is said that there are almost no effective drugs available.
したがって、老年性痴呆症に有効な薬剤、特にアルツハ
イマー型老年性痴呆症に有効な薬剤が望まれている。Therefore, there is a desire for a drug that is effective against senile dementia, especially a drug that is effective against senile dementia of the Alzheimer's type.
く問題点を解決するための手段〉
近年ＤｅｌｕｃａおよびＫＯｄｉＣｅｋらによってなさ
れたビタミンＤ３の代謝産物の分離・同定および代謝経
路の解明の結果、ビタミン０３は最初肝臓において２５
位が水酸化され２５−ヒドロキシビタミンＤ３に変換し
、次いで腎臓において更に２４位あるいは１α位の水酸
化が行なわれ２４．２５−ジヒドロキシビタミンＤ３や
ホルモン活性を有する１α。As a result of recent efforts by Deluca and KOdiCek et al. to isolate and identify the metabolites of vitamin D3 and to elucidate the metabolic pathway, vitamin 03 is initially produced in the liver at 25
It is hydroxylated at the 25-hydroxyvitamin D3 position and converted to 25-hydroxyvitamin D3, and then further hydroxylated at the 24th or 1α position in the kidney, resulting in 24.25-dihydroxyvitamin D3 and 1α, which has hormonal activity.
２５−ジヒドロキシビタミンＤ３および１α、２４゜２
５−トリヒドロキシビタミンＤ３に代謝されることが明
らかになった。そして、これらの代謝産物およびその合
成アナローブである１α−ヒドロキシビタミンＤ３等が
腸管からのカルシウム輸送能および骨塩動員能を促進し
種々のカルシウム代謝異常に基づく疾患の治療薬として
有用であることはよく知られている。25-dihydroxyvitamin D3 and 1α, 24°2
It has been revealed that it is metabolized to 5-trihydroxyvitamin D3. Furthermore, these metabolites and their synthetic analogues, such as 1α-hydroxyvitamin D3, promote the ability to transport calcium from the intestinal tract and the ability to mobilize bone minerals, and are useful as therapeutic agents for various diseases caused by abnormal calcium metabolism. well known.
本発明者らは、これらビタミンＤ３の代謝産物等の、す
なわち活性型ビタミンＤ３類の骨粗髭症への治療効果を
確認するための臨床試験を実施した際に、驚くべきこと
に、活性型ビタミンＤ３類が老年性痴呆症、特にアルツ
ハイマー型老年性痴呆症の治療に有効であることを知見
した。Surprisingly, when the present inventors conducted a clinical trial to confirm the therapeutic effects of these vitamin D3 metabolites, that is, active vitamin D3, on osteoporosis, we found that It has been found that vitamin D3 is effective in treating senile dementia, particularly senile dementia of the Alzheimer's type.
これらの活性型ビタミン０３類が、何故、老年性痴呆症
、特にアルツハイマー型老年性痴呆症に有効であるが、
現在のところ不明である。しかしながら、本発明者らは
アルツハイマー型老年性痴呆症の患者の脳内に、アルミ
ノケイ酸塩が異常に多く発見されること、カルシウムが
不足すると体内にアルミニウムがとり込まれやすくなる
こと、及び活性型ビタミンＤ３類が腸管からのカルシウ
ムの吸収を促進すること、等から考えて、活性型ビタミ
ンＤ３類がアルツハイマー型老年性痴呆症患者のカルシ
ウム代謝を正常化し、これによって脳内のアルミノケイ
酸塩を低減化するものと推定し、活性型ビタミンＤ３類
の老年性痴呆症への治療効果を調べたところ、これらが
、老年性痴呆症の治療又は予防剤として有効であること
を見い出したものである。しかして、本発明は活性型ビ
タミンＤ３類を有効成分とする老年性痴呆症治療又は予
防剤である。Why are these three active vitamins effective against senile dementia, especially Alzheimer's type senile dementia?
It is currently unknown. However, the present inventors found that an abnormally large amount of aluminosilicate is found in the brains of patients with Alzheimer's type senile dementia, that a lack of calcium makes it easier for the body to take up aluminum, and that active Considering that vitamin D3 promotes the absorption of calcium from the intestinal tract, active vitamin D3 normalizes calcium metabolism in patients with Alzheimer's type senile dementia, thereby reducing aluminosilicate in the brain. When we investigated the therapeutic effects of active vitamin D3 on senile dementia, we found that these are effective as therapeutic or preventive agents for senile dementia. Therefore, the present invention is a senile dementia treatment or prevention agent containing active vitamin D3 as an active ingredient.
本発明の活性型ビタミン０３類を有効成分とする老年性
痴呆症治療又は予防剤は、老年性痴呆症のなかでも、特
にアルツハイマー型老年性痴呆症に著効がある。The senile dementia treatment or prevention agent containing active vitamin 03 as an active ingredient of the present invention is particularly effective against senile dementia of the Alzheimer's type among senile dementias.
本発明に用いられる活性型ビタミンＤ３類としては、カ
ルシウム代謝を正常化するものであれば何れでもよく、
例えば１α−ヒドロキシビタミンＤ１，１α、２５−ジ
ヒドロキシビタミン０３，１α、２４（Ｒ）−ジヒドロ
キシビタミンＤ３．１α。The active vitamin D3 used in the present invention may be any vitamin D3 that normalizes calcium metabolism.
For example, 1α-hydroxyvitamin D1,1α, 25-dihydroxyvitamin 03,1α, 24(R)-dihydroxyvitamin D3.1α.
２４（Ｓ）−ジヒドロキシビタミンＤ３，１α、２４゜
２５−トリヒドロキシビタミンＤ３．１α−ヒドロキシ
−２４−オキソビタミンＤ３．１α、２５−ジヒドロキ
シ−２６，２６，２６，２７，２７，２７−ヘキサフル
オロビタミンＤ３，１α、２５−ジヒドロキシ−２４゜
２４−ジフルオロビタミンＤ３１α、２５−ジヒドロキ
シビタミン［）３−２６．２３−ラクトン等の１α位に
水酸基を有する活性型ビタミンＤ３類：２４，２５−ジ
ヒドロキシビタミンＱ３，２４−ヒト０キシビタミンＤ
３，２５−ヒドロキシビタミン０３．ビタミンＤ３−２
６．２３−チクトン等の１α位に水酸基を有しない活性
型ビタミンＤ３類が挙げられる。24(S)-dihydroxyvitamin D3,1α, 24°25-trihydroxyvitamin D3.1α-hydroxy-24-oxovitamin D3.1α, 25-dihydroxy-26,26,26,27,27,27-hexafluoro Vitamin D3,1α, 25-dihydroxy-24゜24-difluorovitamin D31α, 25-dihydroxyvitamin [)3-26.Activated vitamin D3 types having a hydroxyl group at the 1α-position such as 23-lactone: 24,25-dihydroxyvitamin Q3,24-human oxyvitamin D
3,25-Hydroxyvitamin 03. Vitamin D3-2
Examples include active vitamin D3s that do not have a hydroxyl group at the 1α position, such as 6.23-tictone.
これらの活性型ビタミンＤ３類は公知の化合物であり、
公知の方法によって製造し得る［有機合成化学、第３７
巻、 ＮＱ９． ７５５（１９７９） ；有機合成化学
、第３７巻、社１０． ８０９（１９７９） ］ 。These active vitamin D3s are known compounds,
It can be produced by a known method [Organic Synthetic Chemistry, No. 37]
Volume, NQ9. 755 (1979); Organic Synthetic Chemistry, Volume 37, Sha 10. 809 (1979)].
上記活性型ビタミンＤ３類のなかでも、カルシウムの腸
管からの吸収促進により、カルシウム代謝を正常化する
能力の大きい１α−とドロキシビタミンＤ３，１α、２
４（Ｒ）−ジヒドロキシビタミンＤ３，１α、２５−ジ
ヒドロキシビタミンＤ３゜１α、２５−ジヒドロキシ−
２４，２４−ジフルオロビタミンＤ３，１α、２５−ジ
ヒドロキシ−２６，２６゜２６、２７．２７．２７−へ
キサフルオロビタミンＤ３が好ましく、特に１α−ヒド
ロキシビタミンＤ３゜１．２４（Ｒ）−ジヒドロキシビ
タミンＤ３が好ましい。Among the active vitamin D3 types mentioned above, 1α- and droxyvitamin D3, 1α, and 2 have the greatest ability to normalize calcium metabolism by promoting calcium absorption from the intestinal tract.
4(R)-dihydroxyvitamin D3,1α, 25-dihydroxyvitamin D3°1α, 25-dihydroxy-
24,24-difluorovitamin D3,1α, 25-dihydroxy-26,26°26,27.27.27-hexafluorovitamin D3 are preferred, especially 1α-hydroxyvitamin D3°1.24(R)-dihydroxyvitamin D3 is preferred.
本発明の老年性痴呆症治療又は予防剤は、上記活性型ビ
タミンＤ３類を含有し、下記に示す種々の製剤形態によ
って、経口、非経口のいずれでも投与され得る。非経口
投与は筋肉内、皮下、静脈内、直腸投与を含む。The senile dementia treatment or prevention agent of the present invention contains the above-mentioned active vitamin D3 and can be administered either orally or parenterally using various formulations shown below. Parenteral administration includes intramuscular, subcutaneous, intravenous, and rectal administration.
製剤形態としては、例えば、軟カプセル剤０錠剤゛、硬
カプセル剤、散剤、顆粒剤、液剤、注射剤。Examples of dosage forms include soft capsules, hard capsules, powders, granules, liquids, and injections.
外用剤半割等があげられる。その他の成分として、乳糖
、でんぷん、タルク、ステアリン酸マグネシウム、糖又
はその誘導体、アルコール、生理食塩水、界面活性剤、
抗酸化剤、防腐剤、吸収促進剤等を、本発明の活性型ビ
タミンＤ３類と併用し得る。Topical preparations can be given in half. Other ingredients include lactose, starch, talc, magnesium stearate, sugar or its derivatives, alcohol, physiological saline, surfactant,
Antioxidants, preservatives, absorption enhancers, etc. may be used in combination with the active vitamin D3s of the present invention.
本発明の老年性痴呆症治療又予防剤の有効成分である、
これらの活性型ビタミン０３類の投与量は、通常１人１
日当りＯ，ＯＳμｇ〜２０．０μ９．好ましくは１人１
日当り０．１μ９〜°５．０μ９である。The active ingredient of the senile dementia treatment or prevention agent of the present invention,
The dosage of these active vitamins 03 is usually 1 per person.
O,OSμg~20.0μ9 per day. Preferably 1 per person
It is 0.1 μ9 to °5.0 μ9 per day.
製剤中の活性型ビタミンＤ３類の含有値は、上記の投与
量から、用いる製剤の単位必要量に応じて適宜法められ
る。The content of active vitamin D3 in the preparation is determined as appropriate from the above-mentioned dosage depending on the required unit amount of the preparation used.
〈発明の効果〉
本発明によれば、活性型ビタミンＤ３類を有効成分とす
る老年性痴呆症治療又は予防剤が提供され、かかる治療
又は予防剤は、老年性痴呆症特にアルツハイマー型老年
性痴呆症の治療又は予防に有効である。<Effects of the Invention> According to the present invention, a treatment or prevention agent for senile dementia containing active vitamin D3 as an active ingredient is provided, and such treatment or prevention agent can be used to treat or prevent senile dementia, particularly senile dementia of the Alzheimer type. It is effective in treating or preventing diseases.
〈実施例〉 以下本発明を実施例により更に詳細に説明する。<Example> The present invention will be explained in more detail below with reference to Examples.
実施例１゜
１α−ごドロキシビタミンＤ３を含有する経口剤（ソフ
トカプセル剤）を、長谷用式簡易痴呆診査で痴呆と判定
された老年性痴呆症患者７人に、１日１人１μ９を長期
間投与して、投与前侵の痴呆診査の点数を比較し、１α
−ヒドロキシビタミンＤ３の治療効果を調べた。Example 1 An oral preparation (soft capsule) containing 1α-godroxyvitamin D3 was given to 7 senile dementia patients who were determined to have dementia using Hase's simple dementia test, at a dose of 1 μ9 per person per day. After administering the drug for a period of time, we compared the scores on the pre-administration dementia examination, and found that 1α
- The therapeutic effect of hydroxyvitamin D3 was investigated.
結果を第１表に示す。第１表より１α−ヒドロキシビタ
ミンＤ３の老年性痴呆症に対する良好な治療効果が明ら
かとなった。The results are shown in Table 1. Table 1 reveals that 1α-hydroxyvitamin D3 has a good therapeutic effect on senile dementia.
なお、長谷用式簡易診査は次のような質問が行われた。The following questions were asked in the Hase type simple examination.
質問内容 配点１、きようは何
日か？ 何月何日 何曜日
０，３２、ここはどこですか’ｉ’
０．２．５３、年齢は
？（３〜４年以内は正）０．２４、最近起こった出来事
から何年（何か月）位経ちましたか？あるいはいつごろ
でしたか７ ０．
２．５５、生まれたのはどこですか（出生地）０，２６
、大東亜戦争が終わった（または関東大震災があった）
のはいつですか？（３〜４年以内は正）
０．３．５７．１年
は何日ですか（または１時間は何分ですか）
０．２．５８、日本の総理大臣は？０．３
９．１００カら７を順に引イテ下サイ。１００−７−９
３ ９３−７−８６ ０．２，４１０、数の逆唱
（６−８−２，３−５−２−９）
０，２，４１１．５つの物品テスト５つの物品
を１ずつ言わせてそれらをかくして何があったかを問う
０，５
． １．５２．５． ３．５
所要時間１５分以内 満点３２．５点
合計点数 評価
＞３１ ｎｏｍａｌ （正常）
３０．５〜２２ ５ｕｂｎｏｕｌ （境界）２１．５〜
１０．５ ｐｒｅｄｅａｉｅｎｔｉａ （準痴呆）
１０＞ ｄｅＩｌｅｎｔｉａ（痴呆）第１表
実施例２゜
中鎖脂肪酸トリグリセライドエステル１ 、５ Ｋｇに
１α−とドロキシビタミンＤ３１０■を溶解し、１カプ
セル中に１α−ヒドロキシビタミンＤ３を１．０μ９含
有するように下記剤皮成分を加温溶解し、軟カプセル製
造機を用いて常法により軟カプセル剤を製造した。Question content Points: 1. What day is it today? What month, what day, what day of the week?
0,32, where is this 'i'
0.2.53, how old are you? (Correct within 3-4 years) 0.24 How many years (months) have passed since the recent event? Or when was it?7 0.
2.55, where were you born? (place of birth) 0,26
, the Greater East Asia War ended (or the Great Kanto Earthquake occurred)
When is it? (Correct within 3-4 years)
0.3.57. How many days in a year (or how many minutes in an hour)
0.2.58, Who is the Prime Minister of Japan? 0.3 9. Draw 7 from 100 in order. 100-7-9
3 93-7-86 0.2,410, reciting numbers backwards (6-8-2, 3-5-2-9)
0, 2, 411. 5 Objects Test Ask students to name 5 objects one by one and ask them what happened. 0, 5
．． 1.52.5. 3.5 Required time within 15 minutes Total score of 32.5 points Evaluation > 31 normal (normal) 30.5 ~ 22 5ubnoul (border) 21.5 ~
10.5 predeaientia (semi-dementia)
10> deIlentia (dementia) Table 1 Example 2 Medium chain fatty acid triglyceride ester 1.1α- and droxyvitamin D310■ are dissolved in 5 kg, and 1 capsule contains 1.0μ9 of 1α-hydroxyvitamin D3. The following shell components were dissolved by heating, and soft capsules were produced in a conventional manner using a soft capsule making machine.
剤皮処方例
ゼラチン １０ 重量部製グリセ
リン ２
防腐剤（エチルパラベン＋プロピルパラベン）０．０５
Ｎ
水 ０．
２ 〃（最終形態に於ける重量部）Shell formulation example Gelatin 10 parts by weight Glycerin 2 Preservatives (ethylparaben + propylparaben) 0.05
N water 0.
2 (Weight part in final form)
Claims (1)
呆症治療又は予防剤。 ２、活性型ビタミンＤ＿３類が１α−ヒドロキシビタミ
ンＤ＿３であることを特徴とする特許請求の範囲第１項
記載の老年性痴呆症治療又は予防剤。 ３、活性型ビタミンＤ＿３類が１α，２４（Ｒ）−ジヒ
ドロキシビタミンＤ＿３であることを特徴とする特許請
求の範囲第１項記載の老年性痴呆症治療又は予防剤。 ４、老年性痴呆症がアルツハイマー型老年性痴呆症であ
る特許請求の範囲第１項ないし第３項のいずれか１項に
記載の老年性痴呆症治療又は予防剤。[Scope of Claims] 1. A senile dementia treatment or prevention agent containing active vitamin D_3 as an active ingredient. 2. The agent for treating or preventing senile dementia according to claim 1, wherein the active vitamin D_3 is 1α-hydroxyvitamin D_3. 3. The agent for treating or preventing senile dementia according to claim 1, wherein the active vitamin D_3 is 1α,24(R)-dihydroxyvitamin D_3. 4. The agent for treating or preventing senile dementia according to any one of claims 1 to 3, wherein the senile dementia is Alzheimer's type senile dementia.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP24837686A JPS63104926A (en) | 1986-10-21 | 1986-10-21 | Remedy or preventive agent against senile dementia |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP24837686A JPS63104926A (en) | 1986-10-21 | 1986-10-21 | Remedy or preventive agent against senile dementia |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS63104926A true JPS63104926A (en) | 1988-05-10 |
| JPH0443886B2 JPH0443886B2 (en) | 1992-07-20 |
Family
ID=17177180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP24837686A Granted JPS63104926A (en) | 1986-10-21 | 1986-10-21 | Remedy or preventive agent against senile dementia |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS63104926A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995002409A3 (en) * | 1993-07-15 | 1995-04-27 | Univ Pennsylvania | Use of vitamin d and derivatives thereof for the manufacture of a medicament for protection against neuron loss |
| WO1997029740A1 (en) * | 1996-02-13 | 1997-08-21 | Wisconsin Alumni Research Foundation | Multiple sclerosis treatment |
| US6479474B2 (en) | 1999-07-08 | 2002-11-12 | Wisconsin Alumni Research Foundation | Dietary calcium as a supplement to vitamin D compound treatment of multiple sclerosis |
| JP5789339B2 (en) * | 2013-01-21 | 2015-10-07 | レジリオ株式会社 | Therapeutic drugs and therapeutic methods involving 1,25D3-MARRS for neurological diseases including Alzheimer's disease, etc. |
| US10232008B1 (en) * | 2015-10-05 | 2019-03-19 | Michael P. Moran | Multi-purpose nutritional supplement composition |
-
1986
- 1986-10-21 JP JP24837686A patent/JPS63104926A/en active Granted
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995002409A3 (en) * | 1993-07-15 | 1995-04-27 | Univ Pennsylvania | Use of vitamin d and derivatives thereof for the manufacture of a medicament for protection against neuron loss |
| US5939407A (en) * | 1993-07-15 | 1999-08-17 | University Of Kentucky Research Foundation | Method of protecting against neuron loss |
| WO1997029740A1 (en) * | 1996-02-13 | 1997-08-21 | Wisconsin Alumni Research Foundation | Multiple sclerosis treatment |
| US5716946A (en) * | 1996-02-13 | 1998-02-10 | Wisconsin Alumni Research Foundation | Multiple sclerosis treatment |
| US6479474B2 (en) | 1999-07-08 | 2002-11-12 | Wisconsin Alumni Research Foundation | Dietary calcium as a supplement to vitamin D compound treatment of multiple sclerosis |
| JP5789339B2 (en) * | 2013-01-21 | 2015-10-07 | レジリオ株式会社 | Therapeutic drugs and therapeutic methods involving 1,25D3-MARRS for neurological diseases including Alzheimer's disease, etc. |
| EP2946792A4 (en) * | 2013-01-21 | 2016-09-28 | Resilio Company Ltd | THERAPEUTIC AGENT AND THERAPEUTIC METHOD RELATING TO 1,25D3-MARRS FOR NEUROLOGICAL DISEASE SUCH AS ALZHEIMER'S DISEASE& xA; |
| US10232008B1 (en) * | 2015-10-05 | 2019-03-19 | Michael P. Moran | Multi-purpose nutritional supplement composition |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0443886B2 (en) | 1992-07-20 |
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| LAPS | Cancellation because of no payment of annual fees |