JPH04198135A - External preparation - Google Patents
External preparationInfo
- Publication number
- JPH04198135A JPH04198135A JP2326541A JP32654190A JPH04198135A JP H04198135 A JPH04198135 A JP H04198135A JP 2326541 A JP2326541 A JP 2326541A JP 32654190 A JP32654190 A JP 32654190A JP H04198135 A JPH04198135 A JP H04198135A
- Authority
- JP
- Japan
- Prior art keywords
- kallidinogenase
- external preparation
- active ingredient
- present
- pain
- 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.)
- Pending
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 13
- 102000001399 Kallikrein Human genes 0.000 claims abstract description 16
- 108060005987 Kallikrein Proteins 0.000 claims abstract description 16
- 229960003709 kallidinogenase Drugs 0.000 claims abstract description 16
- 239000004480 active ingredient Substances 0.000 claims abstract description 4
- 230000000699 topical effect Effects 0.000 claims 1
- 239000002674 ointment Substances 0.000 abstract description 7
- 208000006820 Arthralgia Diseases 0.000 abstract description 3
- 208000034656 Contusions Diseases 0.000 abstract description 3
- 102000004190 Enzymes Human genes 0.000 abstract description 3
- 108090000790 Enzymes Proteins 0.000 abstract description 3
- 208000000112 Myalgia Diseases 0.000 abstract description 3
- 208000002193 Pain Diseases 0.000 abstract description 3
- 229940088598 enzyme Drugs 0.000 abstract description 3
- 208000013465 muscle pain Diseases 0.000 abstract description 3
- 102000003886 Glycoproteins Human genes 0.000 abstract description 2
- 108090000288 Glycoproteins Proteins 0.000 abstract description 2
- 241000124008 Mammalia Species 0.000 abstract description 2
- 239000006071 cream Substances 0.000 abstract description 2
- 239000006210 lotion Substances 0.000 abstract description 2
- 239000000843 powder Substances 0.000 abstract description 2
- 239000007921 spray Substances 0.000 abstract description 2
- 239000000829 suppository Substances 0.000 abstract description 2
- -1 impregnated dressing Substances 0.000 abstract 2
- 241000282898 Sus scrofa Species 0.000 abstract 1
- 208000034526 bruise Diseases 0.000 abstract 1
- 239000002552 dosage form Substances 0.000 abstract 1
- 210000000952 spleen Anatomy 0.000 abstract 1
- 230000000694 effects Effects 0.000 description 9
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 206010061218 Inflammation Diseases 0.000 description 2
- 102000002397 Kinins Human genes 0.000 description 2
- 108010093008 Kinins Proteins 0.000 description 2
- 208000010040 Sprains and Strains Diseases 0.000 description 2
- 230000017531 blood circulation Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000002537 cosmetic Substances 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 208000014617 hemorrhoid Diseases 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 229940057995 liquid paraffin Drugs 0.000 description 2
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 2
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 229960002216 methylparaben Drugs 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 235000019271 petrolatum Nutrition 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 239000003826 tablet Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 239000003871 white petrolatum Substances 0.000 description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 1
- LEACJMVNYZDSKR-UHFFFAOYSA-N 2-octyldodecan-1-ol Chemical compound CCCCCCCCCCC(CO)CCCCCCCC LEACJMVNYZDSKR-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N 4-hydroxybenzoic acid Chemical compound OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 241000283153 Cetacea Species 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 208000010201 Exanthema Diseases 0.000 description 1
- 102000010631 Kininogens Human genes 0.000 description 1
- 108010077861 Kininogens Proteins 0.000 description 1
- 208000002720 Malnutrition Diseases 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
- 229940063655 aluminum stearate Drugs 0.000 description 1
- BTFJIXJJCSYFAL-UHFFFAOYSA-N arachidyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCO BTFJIXJJCSYFAL-UHFFFAOYSA-N 0.000 description 1
- 238000011888 autopsy Methods 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N beta-monoglyceryl stearate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000034994 death Effects 0.000 description 1
- 231100000517 death Toxicity 0.000 description 1
- 230000000916 dilatatory effect Effects 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
- 201000005884 exanthem Diseases 0.000 description 1
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000001071 malnutrition Effects 0.000 description 1
- 235000000824 malnutrition Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- 210000005036 nerve Anatomy 0.000 description 1
- 208000015380 nutritional deficiency disease Diseases 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 210000005259 peripheral blood Anatomy 0.000 description 1
- 239000011886 peripheral blood Substances 0.000 description 1
- 206010037844 rash Diseases 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
【発明の詳細な説明】 ［産業上の利用分野］ 本発明は、外用剤に関する。[Detailed description of the invention] [Industrial application field] The present invention relates to external preparations.
［従来の技術］
関節痛、筋肉痛、打撲、捻挫は、よく見られる症状であ
るが、その鎮痛・消炎には、外用剤としてサリチル酸メ
チルやメントールなどが使用されている。しかしながら
、その効果は、まだ十分といいがたい。[Prior Art] Arthralgia, muscle pain, bruises, and sprains are common symptoms, and methyl salicylate, menthol, and the like are used as external agents to relieve pain and eliminate inflammation. However, it is difficult to say that the effect is still sufficient.
［発明の概要］
本発明は、カリジノゲナーゼを有効成分とする外用剤に
関する。[Summary of the Invention] The present invention relates to an external preparation containing kallidinogenase as an active ingredient.
本発明に用いられるカリジノゲナーゼは、哺乳動物例え
ばブタの膵臓から抽出される酵素であって、白色又は淡
褐色の結晶性又は無品性の粉末であり、分子量的３００
００の糖蛋白である。この酵素は、血漿中のα、−グロ
ブリン分画中に存在するキニノーゲンからキニンを遊離
させる。この遊離したキニンが神経を介することなく血
管の平滑筋に直接作用して末梢血管を拡張させ、血管抵
抗を減少させ、脳、冠、四肢などの血液の流量を増加さ
せて、血行、血圧を調整する作用を有するとされる。こ
のため、カリジノゲナーゼは、初老性の循環障害、血行
障害に基づく組織の栄養障害などの治療に、錠剤、カプ
セル、注射の列形で用いられている。The kallidinogenase used in the present invention is an enzyme extracted from the pancreas of a mammal, such as a pig, and is a white or light brown crystalline or pure powder with a molecular weight of 300.
00 glycoprotein. This enzyme liberates kinin from kininogen, which is present in the α,-globulin fraction of plasma. This free kinin acts directly on the smooth muscles of blood vessels without going through nerves, dilating peripheral blood vessels, reducing vascular resistance, and increasing the flow of blood to the brain, coronary, limbs, etc., thereby improving blood circulation and blood pressure. It is said to have an adjusting effect. For this reason, kallidinogenase is used in the form of tablets, capsules, and injections to treat senile circulatory disorders, tissue malnutrition caused by blood circulation disorders, and the like.
本発明の外用剤の形態としては、従来用いられている外
用剤の形態があり、例えば軟膏、クリーム又はローショ
ン、含浸ドレッシング、ゲル・スティック、スプレィ、
座薬などが挙げられる。その製造に当たっては、従来か
ら行なわれている方法で行なうことができる。この際、
カリジノゲナーゼの含有量は、１ｇ当たり８０〜５００
０■Ｕ。The external preparation of the present invention may be in the form of conventionally used external preparations, such as ointments, creams or lotions, impregnated dressings, gel sticks, sprays, etc.
Examples include suppositories. Its manufacture can be carried out by conventional methods. On this occasion,
The content of kallidinogenase is 80-500 per gram.
0■U.
好ましくは１００〜３０００ＩＵである。この範囲より
少ない量では、目的とする効果を挙げることができない
。Preferably it is 100-3000 IU. If the amount is less than this range, the desired effect cannot be achieved.
本発明の外用剤は、関節痛、筋肉痛、打撲、捻挫の鎮痛
、消炎に極めて有効である。その外、内・外痔核の治療
などにも有効である。The external preparation of the present invention is extremely effective for relieving joint pain, muscle pain, bruises, sprains, and anti-inflammation. In addition, it is also effective in treating internal and external hemorrhoids.
本発明の外用剤は、症状により適量を１日１回以上使用
する。The external preparation of the present invention is used in an appropriate amount at least once a day depending on the symptoms.
本発明に使用される力・リジノゲナーゼの毒性は、極め
て低い０例えば、マウス及びラットに６７または３７５
１０／ｋｇを経口、静注、筋注投与し、１４日間観察す
ると、死亡例はなく、剖検によっても異常は認められな
かった。The toxicity of the lysinogenase used in the present invention is extremely low. For example, 67 or 375
When 10/kg was administered orally, intravenously, or intramuscularly and observed for 14 days, there were no deaths and no abnormalities were observed at autopsy.
カリジノゲナーゼは、従来、前述のように、錠剤、カプ
セル、注射剤の形態で使用されており、外用剤の形態で
は使用されていなかった。又、本発明が目的とする適応
には、用いられていなかった。As mentioned above, kallidinogenase has conventionally been used in the form of tablets, capsules, and injections, and has not been used in the form of external preparations. Moreover, it has not been used for the purpose of the present invention.
先に、本発明者は、カリジノゲナーゼを含有する化粧品
を発明した。化粧品のため、カリジノゲナーゼの使用量
が本発明の量の範囲より少なくても、その効果を挙げる
ことができた。しがし、その使用量では、本発明の目的
を達することができない。Previously, the present inventor invented a cosmetic product containing kallidinogenase. For cosmetics, even if the amount of kallidinogenase used was less than the range of the present invention, the effect could be achieved. However, the purpose of the present invention cannot be achieved with the amount used.
［実施例コ 実施例 １ 以下の処方を用いて、軟膏を常法により製造した。[Example code] Example 1 Ointments were prepared in a conventional manner using the following formulation.
プロピレングリコール １０（ｇ）ステアリ
ン酸モノグリセライド ３白色ワセリン
２゜ステアリルアルコール
８流動パラフイン ２゜プロピルパ
ラベン ０．０３イソプロピルミリス
テート ３ラウリル硫酸ナトリウム
２メチルパラベン ０．０５
カリジノゲナーゼ ０． ２精製水
３３．７２ ＯＯ
カリジノゲナーゼの活性は、５００’ＩＯ／ｇであった
。Propylene glycol 10 (g) Stearic acid monoglyceride 3 White petrolatum
2゜stearyl alcohol
8 Liquid paraffin 2゜Propyl paraben 0.03 Isopropyl myristate 3 Sodium lauryl sulfate
2 Methylparaben 0.05
Kallidinogenase 0. 2 Purified water
33.72 OO The activity of kallidinogenase was 500'IO/g.
実施例 ２ 以下の処方を用いて、軟膏を常法により製造した。Example 2 Ointments were prepared in a conventional manner using the following formulation.
ステアリル酸アルミニウム １．２（ｇ）オクチ
ルドデカノール ５流動パラフイン
３２固形パラフイン
ｌ白色ワセリン ７クジラ
ロウ ４ステアリルアルコー
ル ２セタノール
３晒しミツロウ ８メチル
パラベン ０．１８エチルパラベン
０．０７プロビルバラベン
０．０５ソルビタンモノステアレート
５カリジノゲナーゼ ０．
２７０％ソルビトール ３精製水
２８．５カリジノゲナーゼ
の活性は、１０００ＩＯ／ｇであった。Aluminum stearate 1.2 (g) Octyldodecanol 5 Liquid paraffin
32 solid paraffin
1 White petrolatum 7 Whale wax 4 Stearyl alcohol 2 Cetanol
3 Bleached beeswax 8 Methylparaben 0.18 Ethylparaben 0.07 Probylparaben
0.05 sorbitan monostearate 5 kallidinogenase 0.
270% sorbitol 3 purified water
The activity of 28.5 kallidinogenase was 1000 IO/g.
［効果コ 実施例１の軟膏を使用して、その効果を確かめた。[Effect Co. The ointment of Example 1 was used to confirm its effectiveness.
肩こりのひどい患者１０名の患部に１日章４ｇを１日２
回塗布した。５日間の使用で、肩こりの痛みが８名で消
滅し、２名で軽減した。この際、発赤、発疹などは生じ
ながった。10 patients with severe shoulder stiffness were given 4g of soap twice a day on the affected areas.
Applied twice. After using the product for 5 days, the pain from stiff shoulders disappeared in 8 patients and was alleviated in 2 patients. At this time, no redness or rash occurred.
一方、実施例１の軟膏の処方において、カリジノゲナー
ゼの活性を６０ＩＵ／ｇとしたものを製造し、これを用
いた。１０日間使用しても効果がなかった。On the other hand, in the ointment formulation of Example 1, an ointment with a kallidinogenase activity of 60 IU/g was manufactured and used. There was no effect even after using it for 10 days.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2326541A JPH04198135A (en) | 1990-11-28 | 1990-11-28 | External preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2326541A JPH04198135A (en) | 1990-11-28 | 1990-11-28 | External preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04198135A true JPH04198135A (en) | 1992-07-17 |
Family
ID=18188986
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2326541A Pending JPH04198135A (en) | 1990-11-28 | 1990-11-28 | External preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04198135A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006047948A1 (en) * | 2004-11-03 | 2006-05-11 | Techpool Bio-Pharma Co., Ltd. | The use of human urinary kallidinogenase for the manufacture of a medicine for the treatment of sepsis |
| US20080103102A1 (en) * | 2006-10-27 | 2008-05-01 | Bmb Patent Holding Corporation | Therapeutic compositions and methods of treatment with capsianoside-type compounds |
-
1990
- 1990-11-28 JP JP2326541A patent/JPH04198135A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006047948A1 (en) * | 2004-11-03 | 2006-05-11 | Techpool Bio-Pharma Co., Ltd. | The use of human urinary kallidinogenase for the manufacture of a medicine for the treatment of sepsis |
| US20080103102A1 (en) * | 2006-10-27 | 2008-05-01 | Bmb Patent Holding Corporation | Therapeutic compositions and methods of treatment with capsianoside-type compounds |
| US10195224B2 (en) | 2006-10-27 | 2019-02-05 | Bmb Patent Holding Corporation | Therapeutic compositions and methods of treatment with capsianoside-type compounds |
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