KR100423486B1 - 알콜탐익을치료하기위한약제제조시의포스코린또는이를함유한추출물의용도 - Google Patents
알콜탐익을치료하기위한약제제조시의포스코린또는이를함유한추출물의용도 Download PDFInfo
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Abstract
본 발명은 알콜탐익(alcohol addiction)을 치료하기 위한 포스코린(forskolin) 및 그를 함유한 추출물의 용도에 관한 것이다.
Description
제1A도는 sP랫트(Sardinian alcohol-preferring rats)에서 알콜소비에 대한 포스코린 50mg/Kg를 반복경구투여시 효과를 나타낸 것이며,
제1B도는 sP랫트에서 물소비에 대한 포스코린 50mg/Kg을 반복경구투여시 효과를 나타낸 그라프이다.
본 발명은 알콜탐익(alcohol addiction)을 치료하기 위한 약제학적 조성물에 관한 것으로, 활성물질로 포스코린(forskolin) 또는 이를 함유한 추출물을 함유함을 특징으로 한다.
알콜남용 및 알콜탐익은 알콜중독에 의해 집학적으로 나타날 수 있는 현상으로, 현대사회 전반에 심각한 문제를 보인다(Gessa G.L., Bisogno compulsivo di bere e "principio del piacere" [The compulsive need to drink and the pleasure principle] in Medicina delle tossicodipendenze [Drug Addiction Medicine] II, 5(1994)).
예를들면, 이탈리아에는 인구의 9%이상(약 5백만명)이 대주가이며 이들중 1백만 이상이 알콜탐익을 보인다(Calamo-Specchia F.P.-Epidemiologia dell'alcolismo in Italia [Epidemiology of alcoholism in Italy] in Atti del VII Congresso Nazionale della S.I.A., [Records of the 7th National Congress of the S.I.A.] Mediserve, Rome, 295-301(1991)). 이와같은 현상은 1천 3백만명 이상의 알콜탐익환자가 있는 미국과 같은 나라들을 고려한다면 훨씬 높은 수치이다.
알콜남용과 알콜탐익은 공공자금의 막대한 지출을 갖어 오고(최근 1991년 이래, 미국은 한해에 약 2천억불을 소비하였다), 개인적으로 막대한 사회적 문제점과 정서적 문제점의 원인이 되었다.
현재의 알콜중독을 치료하는 방법이나 정서적본질(치료군, 등)을 치료하는 방법은 간성알데히드-데하이드로게나제(aldehyde-dehydrogenase)를 억제하면서 알콜대사에 작용하는 디설피람(disulfiram) 및 칼슘카바미드(calcium carbamide)와 같은 약물을 사용하는 것이나, 아세트알데히드(acetaldehyde)의 간수치를 높이며 그때마다 에탄올에 의해 일어나는 모든 바람직하지 못한 현상이 일어난다.
이와같은 실정에서 알콜중독의 치료를 위해 사용되어온 화합물 유도체를 함유한 유일한 식물은 칡(갈근)이며, 전통적인 중의약에서 폭넓게 사용되어 왔으며 특허출원 제WO93/00896호에 기재되어 있다.
이제, 탐익성을 유발하는 알콜 및 다른 약품의 자발적인 소비를 줄이기 위하여 포스코린(forskolin)이 성공적으로 사용될 수 있음이 놀라웁게도 발견되었다.
포스코린(forskolin)은, 17-β-아세톡시-8, 13-에폭시-1α,6β,9α-트리하이드록시라브드-14-엔-11-온(17-β-acetoxy-8,13-epoxy-1α,6β,9α-trihydroxylabd-14-en-11-one)으로 명명되고, 다음 구조식으로 표시되며;
아데닐에이트 사이클라제(adenylate cyclase)를 활성화시키는 능력이 있는, 인도산 식물인 콜리우스 포스콜리(Coleus forskohlii)에서 유도된 디텔페노이드(diterpenoid) 화합물이다.
그의 약리학적 작용은 De Souza and Shah in Economic and Medicinal Plant Research Vol.2, H.Wagner, H.Hihino and N.Farusuworth ed., Academic Press. 1988에 기재되어 있다.
심장순환계 및 호흡기계질환 그리고 녹내장 치료시의 포스코린(forskolin)의 용도는 알려져 있다; 참고적으로, 예를들면 상기 인용문헌; Seamon and Daly, Adv. Cyclic Nucleotide Res. 20, 1.을 참조한다. 알콜소비에 관한 억제작용의 확인을 "사디난 알콜-기호성"(Sardinian alcohol-preferring)(Sp)이라고 불리우는 속의 알콜소비성랫트를 사용하여 수행하였다(Fadda F., Mosca E., Colombo G., Gessa G.L., Alcohol-preferring rats; Genetic sensitivity to alcohol-induced stimulation of dopamine metabolism, in physiol. Behav. 47, 727(1990)).
알콜과 물을 자유롭게 선택하여 투여된 이들 동물에게 매일 체중 kg당 알콜6 내지 7g을 투여하였으며(물과 알콜의 비율은 2:1이상임), 과거 수년간 알콜의 자발적 소비에 대한 여러 가지 물질의 효과를 측정시 성공적으로 사용되어온 동물이다; 예를들면, Balakeevsky A., Colombo G., Fadda F., Gessa G.L., Ro 19-463, a benzodiazepine receptor inverse agonist, attenuates voluntary ethanol consumption in rats selectively bred for high ethanol preference, in Alcohol Alcohol. 25, 449-452(1990); Fadda F., Garau B., Colombo G., Gessa G.L., Isradipine and other clacium channel antagonists attenuate ethanol consumption in ehanol-preferring rats, in Alcoholism: Clinical and Experimental Research 16(3), 449-552(1992).
정상적인 성장조건하에서 유지되어은 동물에게 물(통상의)과 알콜(10%용액 v/v)을 자유롭게 선택하여 1일 4시간동안 투여되었다(즉, 주/야 싸이클중 최초 어두운 4시간).
소비된 물과 알콜의 양을 매일 동시에 기록하였다. 알콜과 물의 안정한 소비가 이루어졌을때, 50mg/kg의 용량의 포스코린(forskolin)을 디메틸설폭사이드(dimethylsulfoxide)에 용해시키고, 7일간 연속하여 1일 1회 2ml/kg의 체적양을 경구투여하였다.
대조군으로서 담체의 동일체적이 사용되었다. 처치말기에 있어서, 알콜과 물소비를 처치전 기록된 수치에까지 기록하였다.
제IA도는 알콜소비에 대한 포스코린(forskolin) 50mg/kg을 반복투여시 효과를 나타낸 것이고, 제IB도는 물소비에 대한 효과를 나타낸 것이다.
제1도의 실험으로부터, 포스코린(forskolin)은 유의할만하게 알콜소비를 감소시켰다고 결론지을 수 있다. 알콜소비에 대한 감소는 7일째까지 유지되었고 현탁액 처치후 회귀하였다. 더욱이 이와같은 경향은, 마치 동물에 알콜 대신 대치된 것과 같이, 물소비를 점진적으로 증가시키는 추세를 동반하였다. 이와같은 후자의 관찰은 특히 중요한데, 이는 실험한 제품으로 처치를 수행할 때 완벽하게 좋은 내성을 보이며, 알콜 대신 물을 사용하여 많은 생리적 라이프 싸이클에 하등 어려움 없이 동물이 회복될 수 있음을 보여주는 것이기 때문이다.
그러므로 본 발명은 활성물질로 포스코린(forskolin)을 함유하고 경구적으로 투여될 수 있는 약제학적 조성물을 제공하는 것이다.
본 발명의 조성물은 활성물질 약 10mg 내지 약 500mg과 통상의 부형제 또는 담체가 부가적으로 포함될 수 있다.
실시예 1
샤켓제제(Sachet formulation)
매 2,300mg 샤켓당 함유량:
포스코린(forskolin) 100mg
샤카로스 2,000mg
말토덱스트린 110mg
구연산 30mg
오렌지향 40mg
수화된 식물유 20mg
실시예 2
정제제제(Tablet formulation)
매 100mg정당 함유량:
포스코린(forskolin) 25mg
미세결정셀룰로스 25mg
유당 37mg
콜로이드성 실리카 1mg
가교결합된 소디움카복시메틸셀룰로스 6mg
포리비닐피롤리돈 5mg
마그네슘 스테아레이트 1mg
Claims (3)
- 포스코린(forskolin)을 유효성분으로 함유하는 알콜탐익 치료제.
- 포스코린(forskolin)추출물을 유효성분으로 함유하는 알콜탐익 치료제.
- 유효성분인 포스코린(forskolin)또는 포스코린 추출물과 부형제 또는 담체로 구성된 알콜탐익 치료용 약제조성물.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI951023A IT1275436B (it) | 1995-05-19 | 1995-05-19 | Uso della forskolina e di estratti che la contengono per il trattamento della alcol-dipendenza |
| ITMI95A001023 | 1995-05-19 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR19990014876A KR19990014876A (ko) | 1999-02-25 |
| KR100423486B1 true KR100423486B1 (ko) | 2004-06-05 |
Family
ID=11371634
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019970708221A KR100423486B1 (ko) | 1995-05-19 | 1996-05-09 | 알콜탐익을치료하기위한약제제조시의포스코린또는이를함유한추출물의용도 |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US5902823A (ko) |
| EP (1) | EP0825859B1 (ko) |
| JP (1) | JP3001641B2 (ko) |
| KR (1) | KR100423486B1 (ko) |
| CN (1) | CN1099286C (ko) |
| AT (1) | ATE215368T1 (ko) |
| AU (1) | AU697449B2 (ko) |
| CA (1) | CA2221592C (ko) |
| DE (1) | DE69620394T2 (ko) |
| DK (1) | DK0825859T3 (ko) |
| ES (1) | ES2175099T3 (ko) |
| HK (1) | HK1005651A1 (ko) |
| HU (1) | HU223474B1 (ko) |
| IT (1) | IT1275436B (ko) |
| NO (1) | NO316054B1 (ko) |
| PT (1) | PT825859E (ko) |
| RU (1) | RU2183455C2 (ko) |
| WO (1) | WO1996036332A1 (ko) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2298142C (en) | 1997-07-30 | 2005-07-12 | Indena S.P.A. | Soya extract, process for its preparation and pharmaceutical composition |
| EP1645272A3 (en) * | 1998-05-12 | 2008-11-05 | The Endowment For Research In Human Biology, Inc. | Daidzin derivatives for the treatment of alcohol dependence or alcohol abuse |
| US20060122261A1 (en) * | 2003-11-20 | 2006-06-08 | Muhammed Majeed | [method of preparing labdane diterpene composition, preferably isoforskolin and deacetylforskolin from forskolin extract and their use for promoting lean body mass and other applications] |
| US20100144885A1 (en) * | 2006-09-29 | 2010-06-10 | The Board Of Trustees Of The University Of Illinois | Histone acetyl transferase activators and histone deacetylase inhibitors in the treatment of alcoholism |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4120975A (en) * | 1976-08-26 | 1978-10-17 | Fisons Limited | Method of psychiatric conditions |
| US4782082A (en) * | 1982-12-27 | 1988-11-01 | Schering Corporation | Method for treating allergic reactions with Forskolin |
| IL89530A0 (en) * | 1989-03-08 | 1989-09-10 | Jeffrey J Feigenbaum | Compositions containing forskolin |
| US5366990A (en) * | 1991-11-14 | 1994-11-22 | Reid Larry D | Method for treating alcohol abuse and alcoholism |
-
1995
- 1995-05-19 IT ITMI951023A patent/IT1275436B/it active IP Right Grant
-
1996
- 1996-05-09 AT AT96919731T patent/ATE215368T1/de not_active IP Right Cessation
- 1996-05-09 WO PCT/EP1996/001952 patent/WO1996036332A1/en active Search and Examination
- 1996-05-09 RU RU97120756/14A patent/RU2183455C2/ru active
- 1996-05-09 DK DK96919731T patent/DK0825859T3/da active
- 1996-05-09 US US08/952,472 patent/US5902823A/en not_active Expired - Fee Related
- 1996-05-09 KR KR1019970708221A patent/KR100423486B1/ko not_active IP Right Cessation
- 1996-05-09 AU AU58163/96A patent/AU697449B2/en not_active Ceased
- 1996-05-09 CA CA002221592A patent/CA2221592C/en not_active Expired - Fee Related
- 1996-05-09 HU HU9801236A patent/HU223474B1/hu not_active IP Right Cessation
- 1996-05-09 ES ES96919731T patent/ES2175099T3/es not_active Expired - Lifetime
- 1996-05-09 EP EP96919731A patent/EP0825859B1/en not_active Expired - Lifetime
- 1996-05-09 JP JP8534525A patent/JP3001641B2/ja not_active Expired - Fee Related
- 1996-05-09 PT PT96919731T patent/PT825859E/pt unknown
- 1996-05-09 DE DE69620394T patent/DE69620394T2/de not_active Expired - Fee Related
- 1996-05-09 CN CN96194036A patent/CN1099286C/zh not_active Expired - Fee Related
-
1997
- 1997-11-10 NO NO19975155A patent/NO316054B1/no not_active IP Right Cessation
-
1998
- 1998-06-03 HK HK98104794A patent/HK1005651A1/xx not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2221592C (en) | 2002-07-09 |
| CN1184422A (zh) | 1998-06-10 |
| ES2175099T3 (es) | 2002-11-16 |
| JP3001641B2 (ja) | 2000-01-24 |
| KR19990014876A (ko) | 1999-02-25 |
| NO316054B1 (no) | 2003-12-08 |
| CN1099286C (zh) | 2003-01-22 |
| IT1275436B (it) | 1997-08-07 |
| JPH11500738A (ja) | 1999-01-19 |
| ITMI951023A0 (it) | 1995-05-19 |
| EP0825859A1 (en) | 1998-03-04 |
| DE69620394T2 (de) | 2002-10-02 |
| ITMI951023A1 (it) | 1996-11-19 |
| NO975155D0 (no) | 1997-11-10 |
| WO1996036332A1 (en) | 1996-11-21 |
| HK1005651A1 (en) | 1999-01-22 |
| US5902823A (en) | 1999-05-11 |
| AU5816396A (en) | 1996-11-29 |
| HUP9801236A3 (en) | 2001-09-28 |
| HUP9801236A2 (hu) | 2000-06-28 |
| NO975155L (no) | 1997-11-10 |
| HU223474B1 (hu) | 2004-07-28 |
| DK0825859T3 (da) | 2002-07-29 |
| PT825859E (pt) | 2002-08-30 |
| RU2183455C2 (ru) | 2002-06-20 |
| DE69620394D1 (de) | 2002-05-08 |
| AU697449B2 (en) | 1998-10-08 |
| CA2221592A1 (en) | 1996-11-21 |
| ATE215368T1 (de) | 2002-04-15 |
| EP0825859B1 (en) | 2002-04-03 |
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