JP3141071B2 - Senso's side effect reducer - Google Patents
Senso's side effect reducerInfo
- Publication number
- JP3141071B2 JP3141071B2 JP03235685A JP23568591A JP3141071B2 JP 3141071 B2 JP3141071 B2 JP 3141071B2 JP 03235685 A JP03235685 A JP 03235685A JP 23568591 A JP23568591 A JP 23568591A JP 3141071 B2 JP3141071 B2 JP 3141071B2
- Authority
- JP
- Japan
- Prior art keywords
- senso
- epimedium
- extract
- side effects
- side effect
- 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
- 230000000694 effects Effects 0.000 title claims description 13
- 239000003638 chemical reducing agent Substances 0.000 title 1
- 241000893536 Epimedium Species 0.000 claims description 17
- 235000018905 epimedium Nutrition 0.000 claims description 17
- 239000000284 extract Substances 0.000 claims description 11
- 239000004480 active ingredient Substances 0.000 claims description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 239000003814 drug Substances 0.000 description 8
- 229940079593 drug Drugs 0.000 description 8
- 230000003177 cardiotonic effect Effects 0.000 description 6
- 150000003431 steroids Chemical class 0.000 description 6
- 239000000243 solution Substances 0.000 description 5
- 238000004128 high performance liquid chromatography Methods 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
- QEEBRPGZBVVINN-UHFFFAOYSA-N Desacetyl-bufotalin Natural products CC12CCC(C3(CCC(O)CC3CC3)C)C3C1(O)CCC2C=1C=CC(=O)OC=1 QEEBRPGZBVVINN-UHFFFAOYSA-N 0.000 description 3
- QEEBRPGZBVVINN-BMPKRDENSA-N bufalin Chemical group C=1([C@H]2CC[C@]3(O)[C@H]4[C@@H]([C@]5(CC[C@H](O)C[C@H]5CC4)C)CC[C@@]32C)C=CC(=O)OC=1 QEEBRPGZBVVINN-BMPKRDENSA-N 0.000 description 3
- 239000002775 capsule Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000029142 excretion Effects 0.000 description 3
- 230000004060 metabolic process Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 239000012044 organic layer Substances 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 238000011002 quantification Methods 0.000 description 2
- 239000012488 sample solution Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000012086 standard solution Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- 206010010904 Convulsion Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 230000036461 convulsion Effects 0.000 description 1
- 238000004821 distillation Methods 0.000 description 1
- 235000020696 epimedium extract Nutrition 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- ULULAZKOCFNOIM-UHFFFAOYSA-N hexyl 4-hydroxybenzoate Chemical compound CCCCCCOC(=O)C1=CC=C(O)C=C1 ULULAZKOCFNOIM-UHFFFAOYSA-N 0.000 description 1
- 230000000297 inotrophic effect Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 238000010298 pulverizing process Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Landscapes
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines Containing Plant Substances (AREA)
- Steroid Compounds (AREA)
Description
【0001】[0001]
【産業上の利用分野】本発明は、イカリソウ又はそのエ
キスを有効成分とするセンソの副作用低減剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an agent for reducing side effects of senso, comprising epimedium or its extract as an active ingredient.
【0002】[0002]
【従来の技術】イカリソウ(淫羊霍)は古来より強壮、
強精の目的で繁用されている生薬である。一方、センソ
(蟾酥)は強心の目的で繁用されてきた生薬であり、そ
の有効成分は強心ステロイドであって、且つその主成分
はブファリンである。又、本品は、優れた強心作用を示
すと共に不整脈、嘔吐、不快感、けいれん等の副作用も
比較的強く、該作用も前記強心ステロイドに基づくもの
である。本発明者等は、かかるセンソの副作用を低減す
る薬剤を見い出すべく鋭意検討した結果、本発明を完成
した。2. Description of the Related Art Epimedium has been strong since ancient times.
It is a crude drug that is used frequently for the purpose of strong energy. On the other hand, senso is a crude drug that has been used frequently for the purpose of instinct, its active ingredient is an inotropic steroid, and its main component is bufalin. In addition, the product exhibits excellent cardiotonic effects and relatively strong side effects such as arrhythmia, vomiting, discomfort, and convulsions, and these effects are also based on the cardiotonic steroids. The present inventors have conducted intensive studies to find a drug that reduces the side effects of Senso, and as a result, completed the present invention.
【0003】[0003]
【発明の構成】本発明はイカリソウ又はそのエキスを有
効成分とするセンソの副作用低減剤に関する。イカリソ
ウのエキスとしては、水、温湯、エタノール、含水エタ
ノール等通常生薬エキスの抽出に使用される溶媒を用い
て抽出し、次いで該溶媒を凍結乾燥、噴霧乾燥、減圧留
去等の方法で除去することにより得られる粉末をあげる
ことができる。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an agent for reducing side effects of senso, comprising epimedium or its extract as an active ingredient. As the extract of Epimedium, water, hot water, ethanol, aqueous ethanol and the like are used for extraction with a solvent usually used for extracting crude drug extracts, and then the solvent is removed by a method such as freeze-drying, spray-drying, and distillation under reduced pressure. The resulting powder can be used.
【0004】イカリソウ又はそのエキスは乾燥粉末とし
てそのまま使用可能であるが、通常この粉末を公知の製
剤化技術を用いて種々の製剤、例えば、錠剤、顆粒剤、
カプセル剤、液剤等に製剤化したものを経口投与すれば
よい。一方、センソは通常公知の製剤化技術を用いて種
々の製剤、例えば錠剤、カプセル剤、丸剤等に製剤化し
たものを経口投与すればよく、その投与量は0.5mg
〜5mgの範囲である。センソの副作用を低減する為の
イカリソウ又はそのエキスの投与量はセンソの投与量に
よって適宜決定され、センソの投与量が前記の場合には
イカリソウの投与量は1mg〜100mgの範囲、又イ
カリソウのエキスの場合は0.5mg〜50mgの範囲
である。イカリソウ又はそのエキスはセンソの投与時と
同時でもよく、又、それから2〜3時間後に投与しても
よいが、通常同時投与が簡便性の面から好ましく、その
場合にはそれぞれの製剤化したものを同時に投与しても
よく、又イカリソウ又はそのエキスとセンソを一緒に公
知の製剤化技術を用いて種々の製剤、例えば錠剤、カプ
セル剤、丸剤等に製剤化したものを投与してもよい。Epimedium or its extract can be used as a dry powder as it is, and this powder is usually used in various preparations such as tablets, granules,
What is formulated in a capsule, liquid or the like may be orally administered. Senso, on the other hand, may be orally administered to various formulations using known formulation techniques, for example, tablets, capsules, pills and the like, and the dosage is 0.5 mg.
In the range of 55 mg. The dose of Epimedium or its extract for reducing the side effects of Senso is appropriately determined according to the dose of Senso, and when the dose of Senso is as described above, the dose of Epimedium is in the range of 1 mg to 100 mg. Is in the range of 0.5 mg to 50 mg. Epimedium or its extract may be administered at the same time as the administration of Senso, or may be administered 2-3 hours after that, but usually simultaneous administration is preferred in terms of simplicity. May be administered simultaneously, or epidermal or its extract and senso may be administered together with various preparations using known preparation techniques, for example, tablets, capsules, pills and the like. .
【0005】[0005]
【発明の効果】センソの有効成分である強心ステロイド
は、安全域の狭い薬剤であり、センソの投与後速やかに
強心作用を示し、それに伴って副作用を示す。故に強心
ステロイドの吸収に影響を与えることなく、その排泄や
代謝を促進して体内中に残留しないようにすることが、
本ステロイドの副作用を低減する上で重要である。本発
明のかかわるイカリソウ及びそのエキスは、センソと同
時に経口投与すると、センソの副作用にかかわる強心ス
テロイドの代謝及び排泄を促進することができ、それに
伴いセンソの副作用も低減させることができた。従っ
て、本発明にかかわるイカリソウ及びそのエキスはセン
ソの副作用低減剤として優れたものである。以下、本発
明を更に実施例により説明するが、本発明はこれに限定
されるものではない。The cardiotonic steroid, which is an active ingredient of senso, is a drug with a narrow safety margin, shows a cardiotonic action immediately after administration of senso, and has side effects accompanying it. Therefore, without affecting the absorption of cardiotonic steroids, to promote its excretion and metabolism so that it does not remain in the body,
It is important in reducing the side effects of this steroid. Epimedium and its extract according to the present invention, when administered orally at the same time as Senso, were able to promote the metabolism and excretion of cardiotonic steroids related to the side effects of Senso, and also to reduce the side effects of Senso. Therefore, epimedium and its extract according to the present invention are excellent as agents for reducing side effects of senso. Hereinafter, the present invention will be further described with reference to Examples, but the present invention is not limited thereto.
【0006】[0006]
1)実験材料 1.被験薬物 センソ(中国山東省産)は乾燥塊状の物を粉砕して用い
た。イカリソウ(黄花イカリソウ 富山産)は乾燥品の
葉部を粉砕し、55%エタノール(100℃、5時間)
で抽出した物を用いた。またセンソ粉砕品は充分水に膨
潤させ超音波処理した均質な液性とした物を投与薬液と
した。投与薬液はセンソとして4mg/mlに調製し
た。センソおよびイカリソウの混合薬液は、センソ薬液
にてイカリソウ抽出物を溶解し調製した。(センソとし
て4mg/ml、イカリソウとして8mg/ml)1) Experimental materials Test drug Senso (produced in Shandong, China) was used by pulverizing a dry mass. Epimedium (Yellow-flowered Epimedium Toyama) crushes the leaves of the dried product and 55% ethanol (100 ° C, 5 hours)
The material extracted in step was used. The pulverized product of Senso was sufficiently swelled in water and ultrasonically treated to obtain a homogeneous liquid, which was used as a drug solution for administration. The drug solution for administration was prepared as 4 mg / ml as Senso. The mixed chemical solution of Senso and Epimedium was prepared by dissolving Epimedium extract with Senso chemical solution. (4 mg / ml as Senso and 8 mg / ml as Epimedium)
【0007】2.実験動物 Wistar系の雄性ラット(体重160〜180g)
を三協ラボサービス(株)より購入し予備飼育した後実
験に使用した。[0007] 2. Experimental animal Wistar male rat (weight 160-180g)
Was purchased from Sankyo Lab Service Co., Ltd., and preliminarily reared before use in experiments.
【0008】2)実験方法 血中ブフォステロイドの定量 ラット血清1mlに、ヘキサンとクロロホルムの混液
(4:1)4mlを加え10分間振とうした後、3,0
00rpmにて遠心分離し有機層3.6mlを正確に分
取する。得られた有機層を減圧留去し残渣を得る。これ
を内部標準溶液*100μlで溶解し試料溶液とした。
この試料溶液40μlにつき高速液体クロマトグラフ
(以下HPLC)にて定量を行なった。尚、HPLC条
件を下記に示した。 HPLC条件 移動相;水:アセトニトリル(1:1) 流 量;1ml/分 カラム;Wakosil 5C18N 4.6mm ×15cm 5μm 40
℃ 検出器;UV 300nm *内部標準溶液 p−ヒドロキシ安息香酸n−ヘキシル
の50%エタノール液2) Experimental method Quantification of bufosteroid in blood To 1 ml of rat serum, 4 ml of a mixture of hexane and chloroform (4: 1) was added and shaken for 10 minutes.
Centrifuge at 00 rpm and accurately collect 3.6 ml of the organic layer. The obtained organic layer is distilled off under reduced pressure to obtain a residue. This was dissolved in 100 μl of an internal standard solution * to obtain a sample solution.
Quantification was performed on 40 μl of this sample solution by high performance liquid chromatography (hereinafter, HPLC). The HPLC conditions are shown below. HPLC conditions Mobile phase; water: acetonitrile (1: 1) Flow rate: 1 ml / min Column: Wakosil 5C18N 4.6 mm × 15 cm 5 μm 40
C Detector: UV 300 nm * Internal standard solution 50% ethanol solution of n-hexyl p-hydroxybenzoate
【0009】3)実験結果3) Experimental results
【表1】 [Table 1]
【0010】上記の結果からすると、センソ投与群での
ブファリンの血中での半減期は1.3時間であり、一
方、〔センソ+イカリソウ〕投与群でのそれは0.91
時間であった。従って、イカリソウはセンソ中のブファ
リンについて優れた代謝・排泄促進効果を有することが
確認された。From the above results, the half-life of bufalin in blood in the group receiving senso was 1.3 hours, whereas that in the group receiving [senso + epimedium] was 0.91.
It was time. Therefore, it was confirmed that Epimedium has an excellent metabolism and excretion promoting effect on bufalin in Senso.
Claims (1)
するセンソの副作用低減剤。1. An agent for reducing side effects of senso, comprising epimedium or its extract as an active ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP03235685A JP3141071B2 (en) | 1991-08-23 | 1991-08-23 | Senso's side effect reducer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP03235685A JP3141071B2 (en) | 1991-08-23 | 1991-08-23 | Senso's side effect reducer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH06256206A JPH06256206A (en) | 1994-09-13 |
| JP3141071B2 true JP3141071B2 (en) | 2001-03-05 |
Family
ID=16989697
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP03235685A Expired - Fee Related JP3141071B2 (en) | 1991-08-23 | 1991-08-23 | Senso's side effect reducer |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3141071B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100342440B1 (en) * | 1999-12-24 | 2002-07-04 | 손 경 식 | Pharmaceutical composition for preventing and treating erecile impoterice using purified Sumsoo extract and method of preparation thereof |
| CN105125592A (en) * | 2015-10-12 | 2015-12-09 | 北京诺康达医药科技有限公司 | Medicine containing toad venom lipid-soluble substances and preparation method thereof |
-
1991
- 1991-08-23 JP JP03235685A patent/JP3141071B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH06256206A (en) | 1994-09-13 |
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| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
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