KR19990022143A - Hydrogels containing sorbic acid - Google Patents

Hydrogels containing sorbic acid Download PDF

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Publication number
KR19990022143A
KR19990022143A KR1019970708622A KR19970708622A KR19990022143A KR 19990022143 A KR19990022143 A KR 19990022143A KR 1019970708622 A KR1019970708622 A KR 1019970708622A KR 19970708622 A KR19970708622 A KR 19970708622A KR 19990022143 A KR19990022143 A KR 19990022143A
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sorbic acid
polyhydric
hydrogels
ethers
hydrogels containing
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KR1019970708622A
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Korean (ko)
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카린 호프만
유타 리들
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에바-마리아 시마-메이어, 얼설라 멜져
쉐링 악티엔게젤샤프트
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Publication of KR19990022143A publication Critical patent/KR19990022143A/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

유일한 활성 성분으로서 소르빈산 및 임의로 다가 알콜 및(또는) 다가 에테르를 함유하는 것을 특징으로 하는 하이드로겔 형태의 제약 제제가 제공된다.Pharmaceutical formulations in the form of hydrogels are provided which contain as the only active ingredient sorbic acid and optionally polyhydric alcohols and / or polyhydric ethers.

Description

소르빈산을 함유하는 하이드로겔Hydrogels containing sorbic acid

본 발명은 유일한 활성 성분으로서 소르빈산 및 임의로 다가 알콜 및(또는) 다가 에테르를 함유하는 것을 특징으로하는 하이드로겔 형태의 제약 제제에 관한 것이다.The present invention relates to pharmaceutical preparations in the form of hydrogels which contain sorbic acid and optionally polyhydric alcohols and / or polyhydric ethers as the only active ingredient.

국부 도포용으로 사용되는, 예를 들면 연고 또는 크림과 같은 하이드로겔 형태의 제약 제제가 하기 화학식 I의 소르빈산 (2,4-헥사디엔산)을 함유할 수 있음은 공지되어 있다.It is known that pharmaceutical formulations used for topical application, for example in the form of hydrogels such as ointments or creams, may contain sorbic acid (2,4-hexadienoic acid) of the formula (I).

CH3-CH=CH-CH=CH-COOHCH 3 -CH = CH-CH = CH-COOH

상기 소르빈산은 제약 제제의 보존에 사용된다 (Ullmann's Encyclopedia of Industrial Chemistry, 5판, VCH Verlagsgesellschaft mbH D-69451 Weinheim (DE), 1993, A24권, 507쪽 ff).The sorbic acid is used for the preservation of pharmaceutical formulations (Ullmann's Encyclopedia of Industrial Chemistry, 5th edition, VCH Verlagsgesellschaft mbH D-69451 Weinheim (DE), 1993, vol. 24, 507 ff).

이러한 제형이 피부의 건조 방지를 돕고 피부를 유연하게 하는 다가 알콜 및(또는) 다가 에테르, 예를 들면 에틸렌 글리콜, 프로필렌 글리콜, 글리세롤 또는 폴리옥시알킬렌(보습제, 유연화제 및 연화제)을 함유할 수 있음도 공지되어 있다 (Ullmann's Encyclopedia of Industrial Chemistry, 5판, VCH Verlagsgesellschaft mbH D-69451 Weinheim (DE), 1993, A10권, 101쪽 ff, A21권 579쪽 ff 및 A22권, 163쪽). 활성 성분-함유 제제의 경우에 이러한 첨가제들이 활성 성분의 침투도를 증진시키기 위한 제제 (증진제)로서 사용될 수도 있다.Such formulations may contain polyhydric alcohols and / or polyhydric ethers, such as ethylene glycol, propylene glycol, glycerol or polyoxyalkylenes (humidants, softeners and emollients) that help prevent skin dryness and soften the skin. Also known is Ullmann's Encyclopedia of Industrial Chemistry, 5th edition, VCH Verlagsgesellschaft mbH D-69451 Weinheim (DE), 1993, vol. 10, pp. 101, ff. A21, pp. 579, ff and A22, 163. In the case of active ingredient-containing preparations such additives may also be used as preparations (enhancers) to enhance the penetration of the active ingredient.

이제 유일한 활성 성분으로서 소르빈산, 바람직하게는 다가 알콜 및(또는) 다가 에테르와 함께 소르빈산을 함유하는 하이드로겔 형태의 제약 제제가 국부 도포 시에 아주 충분히, 좌창 환자의 염증 발진에 대한 아주 현저한 치료 효과를 나타냄이 밝혀졌으며, 이는 하기 실시예에 보다 상세히 설명될 것이다.Pharmaceutical formulations in the form of hydrogels containing sorbic acid, together with sorbic acid, preferably polyhydric alcohols and / or polyhydric ethers, as the only active ingredient now have a very significant therapeutic effect on inflammatory rashes in acne patients, when applied topically. It was found that this will be explained in more detail in the examples below.

본 발명에 따른 제약 제제에 있어, 다가 알콜 및(또는) 다가 에테르로서는 바람직하게는 약리학적으로 무해한, 이러한 제약 제제에 통상 사용되는 물질군 중의 액상 물질이면 적당하다. 이러한 화합물은 예를 들면, 하기 화학식 II의 화합물이다.In the pharmaceutical preparations according to the invention, the polyhydric alcohols and / or polyhydric ethers are preferably liquid substances in the group of substances normally used in such pharmaceutical preparations, which are preferably pharmacologically harmless. Such compounds are, for example, compounds of formula II.

H-(O-CHR-CH2)n-OHH- (O-CHR-CH 2 ) n-OH

식 중,In the formula,

n은 1 내지 12 (바람직하게는 1 내지 8)이고,n is 1 to 12 (preferably 1 to 8),

R은 수소 원자, 메틸기를 나타내거나, 또는 n이 1인 경우에 히드록시메틸기를 나타낸다.R represents a hydrogen atom, a methyl group, or represents a hydroxymethyl group when n is 1.

화학식 I의 적당한 알콜 또는 에테르로는, 예를 들면 에틸렌 글리콜, 프로필렌 글리콜, 글리세롤, 디에틸렌 글리콜, 트리에틸렌 글리콜, 디프로필렌 글리콜 또는 트리프로필렌 글리콜이 있다. 이 화합물들은 국부 도포용 제약 제제에 그 제약 제제에 사용된 활성 성분에 대한 증진제로서도 사용되는 물질이다 (예를 들면, EP-A 0 165 696, WO88/01496 및 DE-A 2 515 594 참조).Suitable alcohols or ethers of formula (I) are, for example, ethylene glycol, propylene glycol, glycerol, diethylene glycol, triethylene glycol, dipropylene glycol or tripropylene glycol. These compounds are substances which are also used in topical pharmaceutical formulations as enhancers for the active ingredients used in the pharmaceutical formulations (see eg EP-A 0 165 696, WO88 / 01496 and DE-A 2 515 594).

또한, 본 발명에 따른 제약 제제 조성물은 다가 알콜 또는 다가 에테르로서는 시클릭 폴리올 또는 폴리에테르, 예를 들면 디메틸이소소르비드, 또는 글리콜 에테르, 예를 들면 디글리콜 디메틸 에테르도 함유할 수 있다. 현재까지 이루어진 연구로는 프로필렌 글리콜이 특히 적당함이 밝혀졌다.The pharmaceutical formulation compositions according to the invention may also contain cyclic polyols or polyethers, for example dimethylisosorbide, or glycol ethers, for example diglycol dimethyl ether, as polyhydric alcohols or polyhydric ethers. Research to date has shown that propylene glycol is particularly suitable.

본 발명에 따른 하이드로겔 형태의 제약 제제는, 예를 들면 소르빈산을 0.05 내지 2.5 중량%, 바람직하게는 0.1 내지 1.0 중량%, 및 다가 알콜 및(또는) 다가 에테르를 0 내지 30 중량%, 바람직하게는 5 내지 20 중량% 포함할 수 있다.Pharmaceutical formulations in the form of hydrogels according to the invention are for example 0.05 to 2.5% by weight of sorbic acid, preferably 0.1 to 1.0% by weight, and 0 to 30% by weight of polyhydric alcohols and / or polyhydric ethers, preferably May comprise 5 to 20% by weight.

하이드로겔을 제조하기 위하여서는 종래 사용되는 증점제를 사용할 수 있다 (Ullmann's Encyclopedia of Industrial Chemistry, 5판, A24권 220쪽 ff.). 적당한 증점제로서는 겔-형성 다당류 및 단백질, 예를 들면 젤라틴, 한천-한천, 펙틴 및 덱스트린 또는 특히 폴리아크릴레이트, 예를 들면 카르보폴(Carbopol)(등록상표) 형(Goodrich Chem.사 제품, 미국 클리블랜드 소재)의 폴리아크릴레이트가 있다.Conventional thickeners can be used to prepare hydrogels (Ullmann's Encyclopedia of Industrial Chemistry, 5th edition, A24, p. Ff.). Suitable thickeners include gel-forming polysaccharides and proteins, for example gelatin, agar-agar, pectin and dextrins or in particular polyacrylates, for example Carbopol® type from Goodrich Chem., Cleveland, USA Material).

하이드로겔의 적당한 제형은 예를 들면 본 발명에 따른 하기 조성을 가질 수 있다.Suitable formulations of the hydrogel may have the following composition according to the invention, for example.

소르빈산 0.15 내지 0.50 중량%Sorbic acid 0.15 to 0.50 wt%

프로필렌 글리콜 10.0 내지 15.0 중량%Propylene glycol 10.0-15.0 wt%

카르보폴(등록상표) 980 0.5 내지 2.0 중량%Carbopol® 980 0.5 to 2.0 wt%

수산화나트륨 02 내지 0.5 중량%Sodium hydroxide 02-0.5 wt%

정제수 100중량% 까지Up to 100% by weight of purified water

하기의 실시예를 본 발명을 보다 상세히 설명하기 위한 것이다.The following examples are intended to illustrate the invention in more detail.

소르빈산 0.2 g, 프로필렌 글리콜 12.0 g 및 정제수 76.55 g을 혼합하고 35 ℃로 가열하고 교반하면서 소르빈산을 용해시켰다. 그 다음, 이 용액을 20 ℃로 식히고, 카르보폴(등록상표) 1.0 g과 혼합하고 균질화시켰다. 이어서, 정제수 10.25 g 중의 수산화 나트륨 10.0 g 용액을 이 혼합물에 첨가하고, 겔 골격이 완전히 형성될 때까지 이 혼합물을 균질화시켰다.0.2 g of sorbic acid, 12.0 g of propylene glycol and 76.55 g of purified water were mixed, heated to 35 ° C., and the sorbic acid was dissolved while stirring. The solution was then cooled to 20 ° C., mixed with 1.0 g of Carbopol® and homogenized. A 10.0 g solution of sodium hydroxide in 10.25 g of purified water was then added to this mixture and the mixture was homogenized until the gel skeleton was fully formed.

10개 시험 센터로부터의 최종적인 의학적 의견은 소르빈산을 갖는 하이드로겔 베이스가 적당히 심각한 좌창의 치료에 평균적으로 우수 내지 매우 우수의 적합성을 갖는다고 평가했다.Final medical comments from the ten test centers evaluated that hydrogel bases with sorbic acid had a good to very good suitability on average for the treatment of moderately severe acne.

따라서, 소르빈산을 갖는 하이드로겔 베이스는 또한 하이드로겔 베이스의 예측되는 부형제 효과를 훨씬 넘어서서 강한 항미생물 효과와 좌창에서의 염증 진전에 대한 명백한 효과를 나타낸다.Thus, hydrogel bases with sorbic acid also exhibit strong antimicrobial effects and apparent effects on inflammatory development in acne far beyond the expected excipient effects of hydrogel bases.

Claims (2)

유일한 활성 성분으로서 소르빈산, 및 임의로 다가 알콜 및(또는) 다가 에테르를 함유하는 것을 특징으로 하는 하이드로겔 형태의 제약 제제.A pharmaceutical formulation in the form of a hydrogel, characterized in that it contains sorbic acid as the only active ingredient, and optionally a polyhydric alcohol and / or a polyhydric ether. 제1항에 있어서,The method of claim 1, 소르빈산 0.15 내지 0.50 중량%Sorbic acid 0.15 to 0.50 wt% 프로필렌 글리콜 10.0 내지 15.0 중량%Propylene glycol 10.0-15.0 wt% 카르보폴(등록상표) 980 0.5 내지 2.0 중량%Carbopol® 980 0.5 to 2.0 wt% 수산화나트륨 0.2 내지 0.5 중량%Sodium hydroxide 0.2-0.5 wt% 를 함유하는 하이드로겔 형태의 제약 제제.Pharmaceutical formulations in the form of a hydrogel containing.
KR1019970708622A 1995-05-31 1996-05-30 Hydrogels containing sorbic acid KR19990022143A (en)

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DE19520838 1995-05-31
DE19520838.2 1995-05-31

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EP (1) EP0831803A1 (en)
JP (1) JPH11506441A (en)
KR (1) KR19990022143A (en)
CN (1) CN1185735A (en)
AU (1) AU6002796A (en)
CA (1) CA2222566A1 (en)
CZ (1) CZ374797A3 (en)
HU (1) HUP9801745A3 (en)
IS (1) IS4606A (en)
PL (1) PL323598A1 (en)
TR (1) TR199701463T1 (en)
WO (1) WO1996038135A1 (en)

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GB9826656D0 (en) 1998-12-03 1999-01-27 Novartis Ag Organic compounds
BE1023757B1 (en) * 2016-06-30 2017-07-12 Yun NV STORAGE OF MICRO-ORGANISMS

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JPS6333314A (en) * 1986-07-29 1988-02-13 Sansho Seiyaku Kk External preparation
US5013769A (en) * 1988-08-22 1991-05-07 Medipro Sciences Limited Method of making a hydrogel-forming wound dressing or skin coating material

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HUP9801745A3 (en) 2000-04-28
CN1185735A (en) 1998-06-24
HUP9801745A2 (en) 1998-12-28
CA2222566A1 (en) 1996-12-05
JPH11506441A (en) 1999-06-08
AU6002796A (en) 1996-12-18
CZ374797A3 (en) 1998-04-15
WO1996038135A1 (en) 1996-12-05
PL323598A1 (en) 1998-04-14
EP0831803A1 (en) 1998-04-01
IS4606A (en) 1997-10-31
TR199701463T1 (en) 1998-02-21

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