JPH01246224A - Remedy for dementia - Google Patents
Remedy for dementiaInfo
- Publication number
- JPH01246224A JPH01246224A JP63071992A JP7199288A JPH01246224A JP H01246224 A JPH01246224 A JP H01246224A JP 63071992 A JP63071992 A JP 63071992A JP 7199288 A JP7199288 A JP 7199288A JP H01246224 A JPH01246224 A JP H01246224A
- Authority
- JP
- Japan
- Prior art keywords
- dementia
- pts
- toki
- shakuyaku
- remedy
- 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
- 206010012289 Dementia Diseases 0.000 title abstract description 11
- 239000008704 toki-shakuyaku-san Substances 0.000 claims abstract description 5
- 239000002664 nootropic agent Substances 0.000 claims description 18
- 229940005524 anti-dementia drug Drugs 0.000 claims description 5
- 239000000284 extract Substances 0.000 abstract description 15
- 239000000843 powder Substances 0.000 abstract description 15
- 210000003710 cerebral cortex Anatomy 0.000 abstract description 6
- 239000003814 drug Substances 0.000 abstract description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 5
- 230000015572 biosynthetic process Effects 0.000 abstract description 4
- 201000010099 disease Diseases 0.000 abstract description 4
- 229940079593 drug Drugs 0.000 abstract description 4
- 238000002360 preparation method Methods 0.000 abstract description 4
- 238000003786 synthesis reaction Methods 0.000 abstract description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 4
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 abstract description 3
- 229960002748 norepinephrine Drugs 0.000 abstract description 3
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 abstract description 3
- 208000007502 anemia Diseases 0.000 abstract description 2
- 238000007796 conventional method Methods 0.000 abstract description 2
- 231100000053 low toxicity Toxicity 0.000 abstract description 2
- 230000001737 promoting effect Effects 0.000 abstract description 2
- 206010000087 Abdominal pain upper Diseases 0.000 abstract 1
- 235000013291 Alisma plantago aquatica Nutrition 0.000 abstract 1
- 240000004615 Alisma plantago-aquatica Species 0.000 abstract 1
- 241000544270 Angelica acutiloba Species 0.000 abstract 1
- 241000132011 Atractylodes lancea Species 0.000 abstract 1
- 241000533367 Cnidium officinale Species 0.000 abstract 1
- 244000236658 Paeonia lactiflora Species 0.000 abstract 1
- 235000008598 Paeonia lactiflora Nutrition 0.000 abstract 1
- 244000197580 Poria cocos Species 0.000 abstract 1
- 235000008599 Poria cocos Nutrition 0.000 abstract 1
- 241001558929 Sclerotium <basidiomycota> Species 0.000 abstract 1
- 238000001035 drying Methods 0.000 abstract 1
- 239000000706 filtrate Substances 0.000 abstract 1
- 238000001914 filtration Methods 0.000 abstract 1
- 239000007788 liquid Substances 0.000 abstract 1
- 229940125682 antidementia agent Drugs 0.000 description 13
- 241000411851 herbal medicine Species 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 241000700159 Rattus Species 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 239000002858 neurotransmitter agent Substances 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 108010009685 Cholinergic Receptors Proteins 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
- 102000034337 acetylcholine receptors Human genes 0.000 description 2
- 231100000215 acute (single dose) toxicity testing Toxicity 0.000 description 2
- 238000011047 acute toxicity test Methods 0.000 description 2
- 239000003651 drinking water Substances 0.000 description 2
- 235000020188 drinking water Nutrition 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- POPPVIRYGJQIOF-UHFFFAOYSA-N 2-acetyloxyethyl(trimethyl)azanium;3-(1-methylpyrrolidin-2-yl)pyridine Chemical compound CC(=O)OCC[N+](C)(C)C.CN1CCCC1C1=CC=CN=C1 POPPVIRYGJQIOF-UHFFFAOYSA-N 0.000 description 1
- 208000004998 Abdominal Pain Diseases 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products 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 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 230000002205 anti-dementic effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 210000005013 brain tissue Anatomy 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- JRFKIOFLCXKVOT-UHFFFAOYSA-N hydroxymethylnicotinamide Chemical compound OCNC(=O)C1=CC=CN=C1 JRFKIOFLCXKVOT-UHFFFAOYSA-N 0.000 description 1
- 229950005422 hydroxymethylnicotinamide Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
Landscapes
- Medicines Containing Plant Substances (AREA)
Abstract
Description
【発明の詳細な説明】 [産業上の利用分野] 本発明は抗痴呆症剤に関するものである。[Detailed description of the invention] [Industrial application field] The present invention relates to an anti-dementia agent.
し従来の技術および課題」
近年、わが国において人口構成の変化に伴い、老年考の
中貼神経障害、特に痴呆症が社会的に重要な問題となっ
ている。In recent years, with changes in the population composition of Japan, medial nerve disorders in the elderly, particularly dementia, have become a socially important problem.
最近では痴呆症に関して、大脳皮質内におけるレセプタ
ーおよび神経伝達物質の異常を指摘する報告がなされて
おり、それに対する様々な治療薬が検討、開発されてい
るが、優れた薬効を持つものは、未だに上申されていな
い。Recently, there have been reports pointing out abnormalities in receptors and neurotransmitters in the cerebral cortex regarding dementia, and various therapeutic drugs have been studied and developed for this disease, but there are still no drugs with excellent efficacy. It has not been escalated.
[課題を解決するための手段]
本発明者等は痴呆症を惹起する原因として、大脳皮質に
おけるニコヂンアセチルコリンレセプター等のレセプタ
ーおよびノルエピネフリン(norepinephri
ne)等の神経伝達物質の濃度の低下に着目し、大脳皮
質においてレセプターおよび神経伝達物質の合成を促進
すれば、痴呆症の治療ができるものと考え、種々の漢方
処方について鋭0研究を重ねた結果、勺薬、ノ几、沢瀉
、決苓、用荀、当帰からなる漢方処方、ずなわら当帰荀
藁散に抗痴呆効果のあることを見い出し、本発明を完成
するに至った。[Means for Solving the Problems] The present inventors believe that receptors such as nicodine acetylcholine receptors and norepinephrine in the cerebral cortex cause dementia.
Focusing on the decrease in the concentration of neurotransmitters such as ne), we believe that dementia can be treated by promoting the synthesis of receptors and neurotransmitters in the cerebral cortex, and have conducted intensive research on various Chinese herbal prescriptions. As a result, they discovered that Zunawara Tokishuonwara San, a Chinese herbal medicine prescription consisting of Tsunayaku, Norin, Sawatan, Kessei, Yoshuun, and Toki, has an anti-dementia effect, leading to the completion of the present invention. .
本発明はこの知見に括づくらので、当帰べ°j薬散上り
なる抗痴呆症剤(以下、本発明の坑痴呆症剤と称する。Since the present invention is based on this knowledge, we have developed an anti-dementia drug (hereinafter referred to as the anti-dementia drug of the present invention).
)である。).
本発明の抗痴呆症剤は漢方処方の古典である金ば要路に
その構成生薬、分量、抽出法等が記載されており、冷え
症、貧血、腹痛等の諸疾患に使用されているが、痴呆症
の治療効果のあることは従来全く知られていなかったこ
とである。The anti-dementia agent of the present invention has its component herbal medicines, dosage, extraction method, etc. described in the classic Chinese herbal prescription, Kinba Yoro, and is used for various diseases such as sensitivity to cold, anemia, and abdominal pain. It was completely unknown until now that it had a therapeutic effect on dementia.
本発明の抗痴呆症剤は古典に則って、荀薬49、爪49
、沢瀉4g、決苓4g、用荀3g、当帰3gを220d
の水で煎じ、これを抗痴呆症剤として3回に分けて服用
することらできるが、服用のし易さ、携帯の便利さを考
慮して漢方薬エキス製剤としたものを抗痴呆症剤として
用いることもできる。The anti-dementia agent of the present invention is based on the classical medicine,
, 4g of sawa, 4g of katsurei, 3g of yosun, 3g of toki for 220d
It can be decoctioned with water and taken in three doses as an anti-dementia drug, but in order to make it easier to take and more convenient to carry, a herbal medicine extract preparation is used as an anti-dementia drug. It can also be used.
たとえば、荀薬3〜8重量部、JIt2〜6重量部、沢
瀉2〜8重量部、決苓2〜6重量部、用荀2〜5重重部
、当帰2〜5重量部をIO倍量程度の水で熱時抽出して
得た抽出液を濾過後、乾燥して抗痴呆症剤である当帰荀
薬散乾燥エキス粉末を得、これに通常の製剤に用いる適
当な賦形剤、補助剤等を加えて製剤製造の常法に従って
散剤、顆粒剤、錠剤、カプセル剤等の製剤にすることが
できる。For example, 3 to 8 parts by weight of Xunyaku, 2 to 6 parts by weight of JIt, 2 to 8 parts by weight of Zawatan, 2 to 6 parts by weight of Keili, 2 to 5 parts by weight of Yoxun, and 2 to 5 parts by weight of Danggui in IO times the amount. The extract obtained by hot extraction with a certain amount of water is filtered and dried to obtain a powder of Dangguixun medicinal powder, which is an anti-dementia agent. By adding adjuvants and the like, it can be made into preparations such as powders, granules, tablets, capsules, etc. according to conventional methods for manufacturing preparations.
本発明の抗痴呆症剤の製造の具体例を示すと次の如くで
ある。A specific example of the production of the anti-dementia agent of the present invention is as follows.
具体例
荀薬4g、蒼荒49、沢瀉49、決苓49、用チ39、
当帰3gの混合生薬に10倍量すなわち220ffi(
!の水を加えて1時間、100°cで加熱抽出して得た
抽出液を濾過後、スプレードライして3.89の乾燥エ
キス粉末を得た。Specific examples: Xun Yao 4g, Aoara 49, Zawatan 49, Kei Ling 49, Yochi 39,
Add 10 times the amount to 3g of mixed herbal medicine, or 220ffi (
! of water was added and extracted by heating at 100°C for 1 hour, and the resulting extract was filtered and spray-dried to obtain a dry extract powder with a weight of 3.89.
次に本発明の抗痴呆症剤が痴呆症の治療に有効であるこ
とについて実験例を挙げて説明する。Next, the effectiveness of the anti-dementia agent of the present invention in the treatment of dementia will be explained using experimental examples.
実験例1
SD系系外性ラット生後22日より、具体例で得た乾燥
エキス粉末を500〜/kqの割合で飲料水と共に1週
間投与した。コントロール群には飲料水のみを投与した
。1週間後、ラットを層殺し、脳を取り出し、大脳皮質
の部分をホモジナイズし、脳組織中のニコチンアセチル
コリンレセプター(以下、nAchRsと略する。)お
よびノルエピネフリン(以下、NEと略する。)の里を
測定した。その結果を第1表に示す。Experimental Example 1 From day 22 after birth, the dried extract powder obtained in the specific example was administered to SD rats at a rate of 500~/kq together with drinking water for one week. The control group received drinking water only. One week later, the rats were sacrificed, the brain was removed, and the cerebral cortex was homogenized to determine the concentration of nicotine acetylcholine receptors (hereinafter referred to as nAchRs) and norepinephrine (hereinafter referred to as NE) in the brain tissue. was measured. The results are shown in Table 1.
第1表
実験例2
生後22日より2週間投与する以外は、実験例1と同様
にしてnAchRs量を測定した結果、コントロール群
が182±22 fM/IIgであるのに対し、乾燥エ
キス粉末投与群では354±18 fM/149であっ
た。Table 1 Experimental Example 2 The nAchRs amount was measured in the same manner as in Experimental Example 1 except that the administration was carried out for 2 weeks from 22 days after birth. The result was 182 ± 22 fM/IIg in the control group, whereas the dry extract powder administration In the group, it was 354±18 fM/149.
以上の結果から、具体例で得た乾燥エキス粉末が、大脳
皮質におけるnAchRsの合成およびNEの合成を促
進することが確認され、抗痴呆症剤として有効であるこ
とが確認された。From the above results, it was confirmed that the dried extract powder obtained in the specific example promoted the synthesis of nAchRs and NE in the cerebral cortex, and was confirmed to be effective as an anti-dementia agent.
尚、本発明の抗痴呆症剤の経口投与での急性毒性試験を
ddY系雄性マウス、及びウィスター(Wistar)
系雄性ラットを用いて行ったところ、具体例で得た本発
明の抗痴呆症剤の乾燥エキス粉末は、15g/&9(投
与限界)の経口投与でも、死亡例を与えなかった。The acute toxicity test for oral administration of the anti-dementia agent of the present invention was conducted using ddY male mice and Wistar mice.
When the test was carried out using a strain of male rats, the dry extract powder of the anti-dementia agent of the present invention obtained in the specific example did not cause death even when administered orally at a dose of 15 g/&9 (dose limit).
このように、本発明の抗痴呆症剤は、極めて毒性が低く
安全性の高いものである。尚、当帰芍薬散は古来より現
在に至るまで奥方薬として用いられていることからみて
、副作用が少ないことが明らかである。上述の実験デー
タおよび急性毒性試験の結果から考えて、本発明の抗痴
呆症剤のa効投与量は、患者の年令、体重、疾患の程度
によっても異なるが、通常成人量で乾燥エキス粉末量と
して1日量1−toirを症状に合わせて、1日3回に
分けての服用が適当と認められる。Thus, the anti-dementia agent of the present invention has extremely low toxicity and high safety. Furthermore, considering that Tokishakuyakusan has been used as a medicinal medicine since ancient times up to the present, it is clear that it has few side effects. Considering the above experimental data and acute toxicity test results, the effective dose of the anti-dementia agent of the present invention varies depending on the age, weight, and severity of the disease of the patient, but is usually an adult dose of dry extract powder. It is considered appropriate to take 1-toir per day divided into 3 doses per day depending on the symptoms.
次に、実施例を示して更に具体的に説明するが、本発明
は、これより制限される乙のではない。Next, the present invention will be described in more detail by showing examples, but the present invention is not limited thereto.
実施例I
上記の具体例により製造した乾燥エキス粉末200gを
乳糖89g及びステアリン酸マグネシウム!9と混合し
、この混合物を単発弐打鍵機にて打錠して、直径20
my S重量約2.39のスラッグ錠を作りこれを、オ
ンレータ−にて粉砕し、整粒し、篩別して20〜50メ
ツシユの粒子の良好な顆粒剤を得た。Example I 200 g of dry extract powder produced according to the above specific example was combined with 89 g of lactose and magnesium stearate! 9 and press this mixture into tablets using a single-shot key press to form tablets with a diameter of 20 mm.
A slug tablet having a weight of about 2.39 myS was prepared, which was pulverized in an onrator, sized, and sieved to obtain good granules with particles of 20 to 50 mesh.
この顆粒剤は、症状に合わせて1同量0.5〜459(
本発明の抗痴呆症剤の乾燥エキス粉末重量として0.3
4〜3.10yに相当)を1日3回服用する。This granule is available in an equivalent amount of 0.5 to 459 (1) depending on the symptoms.
0.3 as dry extract powder weight of the anti-dementia agent of the present invention
(equivalent to 4 to 3.10 y) three times a day.
実施例2
上記の具体例により製造した乾燥エキス粉末200gを
微結晶セルロース209およびステアリン酸マグネノウ
ム5gと混合し、この混合物を単発式打錠機にて打錠し
て直径7朋、重量225〜の錠剤を製造した。本錠剤1
錠中には本発明の抗痴呆症剤の乾燥エキス粉末を200
〜含有する。Example 2 200 g of the dry extract powder produced according to the above specific example was mixed with 209 microcrystalline cellulose and 5 g of magnesium stearate, and this mixture was compressed using a single-shot tablet machine to form tablets with a diameter of 7 mm and a weight of 225 ~. Tablets were manufactured. This tablet 1
The tablet contains 200% dry extract powder of the anti-dementia agent of the present invention.
~contains.
本錠剤は、症状に合わせて1同量2〜16錠を1日3回
服用する。Take 2 to 16 tablets of the same amount three times a day depending on your symptoms.
実施例3
上記の具体例により製造した乾燥エキス粉末5007f
i9を硬カプセルに充填した。本カプセルは、症状に合
わせて2〜20カプセルを1日3回に分けて服用する。Example 3 Dry extract powder 5007f produced according to the above specific example
i9 was filled into hard capsules. This capsule is taken in 2 to 20 capsules three times a day, depending on the symptoms.
Claims (1)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP63071992A JP2629251B2 (en) | 1988-03-28 | 1988-03-28 | Anti-dementia agent |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP63071992A JP2629251B2 (en) | 1988-03-28 | 1988-03-28 | Anti-dementia agent |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH01246224A true JPH01246224A (en) | 1989-10-02 |
JP2629251B2 JP2629251B2 (en) | 1997-07-09 |
Family
ID=13476470
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP63071992A Expired - Lifetime JP2629251B2 (en) | 1988-03-28 | 1988-03-28 | Anti-dementia agent |
Country Status (1)
Country | Link |
---|---|
JP (1) | JP2629251B2 (en) |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04275224A (en) * | 1991-03-02 | 1992-09-30 | Kissei Pharmaceut Co Ltd | Therapeutic agent for dementia |
JPH0987187A (en) * | 1995-07-13 | 1997-03-31 | Hagino Nobuyoshi | Apoptosis inhibitor |
KR20000002474A (en) * | 1998-06-20 | 2000-01-15 | 신민규 | Preventive and therapeutic agent for degenerative cerebrum neurological disease |
KR20000002473A (en) * | 1998-06-20 | 2000-01-15 | 신민규 | Medication for preventing and curing degenerative cerebral neural disease |
KR100336182B1 (en) * | 1999-04-13 | 2002-05-10 | 이희설 | Composition for preventing or treating dementia comprising a hydroxycinnamic acid derivative or an extract of a plant of genus angelicae comprising same |
KR100413963B1 (en) * | 2000-12-06 | 2004-01-07 | 주식회사 엘컴사이언스 | Use of coumarin derivatives as anti-alzheimer's disease drugs and pharmaceutical preparations containing them as active ingredients |
-
1988
- 1988-03-28 JP JP63071992A patent/JP2629251B2/en not_active Expired - Lifetime
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04275224A (en) * | 1991-03-02 | 1992-09-30 | Kissei Pharmaceut Co Ltd | Therapeutic agent for dementia |
JPH0987187A (en) * | 1995-07-13 | 1997-03-31 | Hagino Nobuyoshi | Apoptosis inhibitor |
KR20000002474A (en) * | 1998-06-20 | 2000-01-15 | 신민규 | Preventive and therapeutic agent for degenerative cerebrum neurological disease |
KR20000002473A (en) * | 1998-06-20 | 2000-01-15 | 신민규 | Medication for preventing and curing degenerative cerebral neural disease |
KR100336182B1 (en) * | 1999-04-13 | 2002-05-10 | 이희설 | Composition for preventing or treating dementia comprising a hydroxycinnamic acid derivative or an extract of a plant of genus angelicae comprising same |
KR100413963B1 (en) * | 2000-12-06 | 2004-01-07 | 주식회사 엘컴사이언스 | Use of coumarin derivatives as anti-alzheimer's disease drugs and pharmaceutical preparations containing them as active ingredients |
Also Published As
Publication number | Publication date |
---|---|
JP2629251B2 (en) | 1997-07-09 |
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