KR20020006555A - External gel preparation containing local anesthetics - Google Patents
External gel preparation containing local anesthetics Download PDFInfo
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- KR20020006555A KR20020006555A KR1020000037701A KR20000037701A KR20020006555A KR 20020006555 A KR20020006555 A KR 20020006555A KR 1020000037701 A KR1020000037701 A KR 1020000037701A KR 20000037701 A KR20000037701 A KR 20000037701A KR 20020006555 A KR20020006555 A KR 20020006555A
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- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- 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
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- 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
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
Abstract
Description
본 발명은 국소 마취제를 포함한 외용 겔제에 관한 것이다. 특히 본 발명은 피부를 통해 일정량의 약물을 전달시키는 약물전달시스템에 관한 것으로, 더욱 상세하게는, 활성성분으로 리도카인 및 그 염이 함유된 피부투과 촉진이 우수한 겔형의 외용제제에 관한 것이다. 전신 또는 국부에서 약효를 얻기 위해서 경피투과제제의 여러 가지 형태를 이용하여 약물을 피부를 통해 흡수시키는 것이 행하여 지고 있다.The present invention relates to an external gel preparation including a local anesthetic. In particular, the present invention relates to a drug delivery system for delivering a certain amount of drug through the skin, and more particularly, to a gel-type external preparation having excellent skin permeation promotion with lidocaine and its salt as an active ingredient. Absorption of the drug through the skin using various forms of transdermal preparations has been carried out in order to obtain the effect systemically or locally.
국소마취제의 제형으로는 주사제, 크림, 연고, 오일 및 겔제 등이 소개되고 있다. 미국 특허 제 4,562,060 호 및 제 4,529,601 호에 따르면 활성성분으로 프릴로카인과 리도카인을 일정 중량비로 녹인 후 그 혼합물로 하여 에멀젼화 하였고, 미국 특허 제 5,827,529 호에 따르면 위 제형들의 단점을 지적하고 있다. 그 단점의첫 번째로, 활성성분을 정량적으로 투여하기가 어렵다는 것과 국소 부위에 약물이 묻어나는 점, 그 두 번째로 물 및 용매의 사용으로 인한 증발로 약물의 흡수가 저하된다는 것이다. 그 세 번째로, 리도카인은 빠르게 대사되기 때문에 약물을 여러번 적용해야된다는 단점이 있다는 것을 지적하고 있다. 이를 개선하기 위해 겔기제로서 물에 녹는 고분자 물질, 예를 들면, 젤라틴, 전분, 아가, 아크릴산 폴리머 및 그 염, 메칠셀룰로오스, 또한 이들 물질의 공중합체를 사용하고 있다. 또한 글리콜류와 사카라이드류를 사용하여 물 및 용매의 증발을 방지하여 흡수를 촉진시키고 있다.Formulations of local anesthetics include injections, creams, ointments, oils and gels. According to U.S. Patent Nos. 4,562,060 and 4,529,601, the active ingredient was dissolved in a certain weight ratio of prilocaine and lidocaine and then emulsified into a mixture thereof, and U.S. Patent No. 5,827,529 points out the disadvantages of the above formulations. The first is the difficulty in quantitatively administering the active ingredient, the fact that the drug appears on the topical area, and secondly, the absorption of the drug is reduced by evaporation due to the use of water and solvents. Third, he points out that lidocaine is rapidly metabolized, requiring multiple applications of the drug. In order to improve this, water-soluble high molecular materials such as gelatin, starch, agar, acrylic acid polymers and salts thereof, methylcellulose, and copolymers of these materials are used. In addition, glycols and saccharides are used to prevent the evaporation of water and solvents to promote absorption.
본 발명에서는 국소마취제 약물의 부작용을 최소화하고, 흡수 효과가 우수하며, 지속적인 작용을 가지는 동시에 피부에 적용되었을 때 자극이 없고, 알러지 반응이 없는 안정한 외용 겔제를 제공함에 있다.The present invention provides a stable external gel that minimizes side effects of local anesthetic drugs, has an excellent absorption effect, has a continuous action, and has no irritation when applied to the skin and does not have an allergic reaction.
도 1은 본 발명의 실시예 1 내지 4와 비교예(실시예 6)의 외용 겔제의 피부투과율(%)을 나타낸 그래프이다.1 is a graph showing the skin transmittance (%) of the external gel preparation of Examples 1 to 4 and Comparative Example (Example 6) of the present invention.
상기와 같은 목적을 달성하기 위해 본 발명은 1) 활성성분으로 리도카인 및 그 염 2) 피부투과를 촉진시킬 수 있는 피부투과촉진제 3) 활성성분을 안정적으로 함유할 수 있는 겔화제, 및 4) 그 밖의 첨가제 등으로 구성된다.In order to achieve the above object, the present invention provides 1) lidocaine and its salt as active ingredients 2) a skin permeation accelerator capable of promoting skin permeation 3) a gelling agent which can stably contain an active ingredient, and 4) its Outside additives and the like.
본 발명에서 사용되는 국소마취제로서는 리도카인 및 그 염, 벤조카인, 프롤리카인 및 그 염 중에서 1 종 이상의 화합물을 사용한다.As the local anesthetic agent used in the present invention, at least one compound of lidocaine and salts thereof, benzocaine, prolycaine and salts thereof is used.
본 발명에서는 국소마취제 0.5-12.0 중량부, 단독 또는 2종 이상의 겔기제를 병용한 겔 기제 0.3-50 중량부, 피부투과촉진제 0.5-15 중량부, 유화제 1-15 중량부로 구성된다.In the present invention, 0.5-12.0 parts by weight of a local anesthetic agent, 0.3-50 parts by weight of a gel base used alone or in combination of two or more gel bases, 0.5-15 parts by weight of a skin permeation accelerator, and 1-15 parts by weight of an emulsifier.
여기에서 겔화제는 물과 알콜 접촉시 겔을 형성할 수 있는 첨가제는 어느것이든 사용가능하며, 일반적으로 하이드록시프로필메칠셀룰로오스, 하이드록시프로필셀룰로오스, 하이드록시에칠셀룰로오스 등과 같은 셀룰로오스 유도체, 카르복시비닐중합체, 폴리옥시에틸렌-폴리프로필렌 공중합체 (상품명 : Poloxamer) 등을 사용하며, 또한 이 들 중 두가지 정도를 혼합한 형태로 사용할 수 있다.Here, the gelling agent may be used any additive that can form a gel upon contact with water and alcohol, generally cellulose derivatives such as hydroxypropylmethyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, carboxyvinyl polymer , Polyoxyethylene-polypropylene copolymer (trade name: Poloxamer) may be used, and two or more of these may be used in a mixed form.
피부투과촉진제는 디에칠렌글리콜모노에칠에테르와 같은 에칠렌글리콜에테르계 와 라브라필 종류를 사용할 수 있다.Skin permeation accelerators may be used such as ethylene glycol ether type and Labrafil, such as die ethylene glycol monoethyl ether.
또한 겔을 제조하는 목적으로 적당 양의 아크릴레이트/C10-30 알킬아크릴레이트 공중합체(Pemulen)를 유화제로 사용할 수 있다.In addition, an appropriate amount of acrylate / C10-30 alkylacrylate copolymer (Pemulen) may be used as an emulsifier for the purpose of preparing the gel.
그 밖에 pH 조정제 및 보습제 등을 함유할 수 있다.In addition, a pH adjuster, a moisturizing agent, etc. can be contained.
본 발명에서는 겔화제를 단독 또는 2종 이상을 조합하여 사용할 수 있으나, 2종 이상을 조합하여 사용하는 것이 바람직하다.In the present invention, the gelling agent may be used alone or in combination of two or more thereof, but it is preferable to use two or more kinds in combination.
본 발명에서 사용되는 라브라필은 올레오일 마크로콜/6-글리세라이드이며, 라브라필은 상품명이다.Labrafil used in the present invention is oleoyl macrocol / 6-glyceride, and Labrafil is a trade name.
본 발명에서 사용되는 페뮤렌은 아크릴레이트/C10-30 알킬아크릴레이트 공중합체의 상품명이다.Femurene used in the present invention is a trade name of an acrylate / C10-30 alkylacrylate copolymer.
본 발명은 이하의 실시 예에서 더욱 상세히 설명하지만 본 발명이 다음의 실시 예로 한정하려는 것은 아니다.The present invention is described in more detail in the following examples, but the present invention is not intended to be limited to the following embodiments.
실시 예 1.Example 1.
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
폴록사머 F127 20.0Poloxamer F127 20.0
디에칠렌글리콜모노에칠에테르 5.0Diethylene glycol monoethyl ether 5.0
라브라필 1.0Labrador 1.0
페뮤렌 0.2Pemureen 0.2
에탄올 29.8Ethanol 29.8
정제수 34.2Purified water 34.2
트리에탄올아민 적량Triethanolamine appropriate amount
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
실시 예2Example 2
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
폴록사머F127 20.0Poloxamer F127 20.0
디에칠렌글리콜모노에칠에테르 5.0Diethylene glycol monoethyl ether 5.0
라브라필 1.0Labrador 1.0
프로필렌글리콜 6.0Propylene Glycol 6.0
글리세린 4.4Glycerin 4.4
폴리에칠렌글리콜4000 16.5Polyethylene Glycol 4000 16.5
정제수 적량Purified water
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
실시 예 3Example 3
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
카보폴940 1.0Cabopol940 1.0
디에칠렌글리콜모노에칠에테르 5.5Diethylene glycol monoethyl ether 5.5
라브라필 1.0Labrador 1.0
에탄올 38.5Ethanol 38.5
정제수 38.0Purified water 38.0
프로필렌글리콜 5.0Propylene Glycol 5.0
트리에탄올아민 적량Triethanolamine appropriate amount
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
실시예 4Example 4
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
페뮤렌 1.5Pemuren 1.5
디에칠렌글리콜모노에칠에테르 5.0Diethylene glycol monoethyl ether 5.0
라브라필 1.0Labrador 1.0
에탄올 38.1Ethanol 38.1
정제수 38.0Purified water 38.0
프로필렌글리콜 5.0Propylene Glycol 5.0
트리에탄올아민 적량Triethanolamine appropriate amount
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
실시예 5Example 5
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
하이드록시에칠셀룰로오스 3.0Hydroxyethyl Cellulose 3.0
페뮤렌 1.0Pemuren 1.0
디에칠렌글리콜모노에칠에테르 5.0Diethylene glycol monoethyl ether 5.0
라브라필 1.0Labrador 1.0
프로필렌글리콜 5.0Propylene Glycol 5.0
에탄올 40.0Ethanol 40.0
정제수 적량Purified water
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
실시예 6 (비교 제제)Example 6 (Comparative Formulation)
중량부Parts by weight
리도카인 9.6Lidocaine 9.6
카보풀940 1.1Carbopool940 1.1
에탄올 43.0Ethanol 43.0
트리에탄올아민 1.3Triethanolamine 1.3
정제수 적량Purified water
위의 물질들을 호모믹서하여 전질이 고른 겔을 조제하였다.The above materials were homomixed to prepare gels of homogeneous quality.
위의 실시 예들에서 조제된 외용 국소마취제를 가지고 피부투과실험을 행하였다.A skin permeation experiment was performed with an external topical anesthetic prepared in the above examples.
실험예 1Experimental Example 1
무모 마우스를 이용한 경피투과실험Percutaneous Permeation Experiment using Hairless Mouse
본 발명의 실시예들의 겔제와 비교제제의 피부투과도를 측정하기 위해 무모마우스(Hairless mouse)의 피부를 적출한 다음 프란츠타잎 셀(Franz diffusion cell)을 이용하여 시간대별로 수용기(receptor))액 중에서 리도카인 농도를 측정하였다.In order to measure the skin permeability of the gel and the comparative agent of the embodiments of the present invention, skin of a hairless mouse was extracted, and then lidocaine in a receptor solution at a time period using a Franz diffusion cell. The concentration was measured.
무모마우스는 여성의 4-6 주령, 등쪽을 샘플로 하였으며, 프란츠타잎 셀의 면적은 1.77Cm 용적은 13 밀리리터를 사용하였다. 수용기의 용액은 인산염 완충액(pH 6.8)을 사용하였다.The hairless mice were sampled at 4-6 weeks old, dorsal side of the female, and the area of the Franz-Tipar cell was 1.77 cm in 13 milliliters. Phosphate buffer (pH 6.8) was used as the solution in the receiver.
본 발명의 약물과 대조약간의 비교 실험에 의해 측정된 결과는 도 1 에 나타내었다. 이 도면에 의하면, 비교예(실시예 6)의 경우는 투여후 120시간에 투과율이 10%에도 미치지 못하는 반면, 본 발명의 실시예에서는 그 피부투과율이 투여후 120분에서 17% 이상이며, 특히 실시예 2에서는 33% 이상임이 확인된다.The results measured by the comparative experiment between the drug of the present invention and the reference drug are shown in FIG. 1. According to this figure, in the case of the comparative example (Example 6), the transmittance was less than 10% at 120 hours after administration, whereas in the example of the present invention, the skin transmittance was at least 17% at 120 minutes after administration. In Example 2, it is confirmed that 33% or more.
상기 실험결과는 본 발명의 외용약제가 피부투과도면에서 우수함을 보여주고 있으며 또한 지속적임을 나타내고 있다. 또한 겔화제를 단독으로 사용하는 것보다는, 2종 이상을 병용하여 사용하는 것이 더욱 효과적임이 확인되었다.The experimental results show that the external medicine of the present invention is excellent in terms of skin permeability and also shows that it is persistent. Moreover, it was confirmed that it is more effective to use 2 or more types together rather than using a gelling agent alone.
본 발명의 리도카인 국소마취제는 국소부위에 작용하여 투과가 뛰어나며, 지속적으로 작용하면서 부작용이 없는 탁월한 외용 겔제제이며, 피부투과촉진제를 사용하면 그 효과가 더욱 우수하며, 겔화제를 2종 이상 사용하면, 그 효과가 가장 우수함이 확인되었다.Lidocaine local anesthetic of the present invention acts on the topical area and has excellent permeability, and is an excellent external gel preparation that does not have side effects while continuously acting. The use of a skin permeation accelerator is more effective, and when two or more gelling agents are used, The effect was confirmed to be the best.
Claims (5)
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2013027840A1 (en) * | 2011-08-25 | 2015-03-23 | ニプロパッチ株式会社 | Water-containing patch |
| KR102419076B1 (en) * | 2022-01-17 | 2022-07-08 | 장보경 | Anesthetic composition and method for preparing same |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61254519A (en) * | 1985-05-07 | 1986-11-12 | Nitto Electric Ind Co Ltd | Gelatinous medicinal pharmaceutical |
| JPH09255565A (en) * | 1996-03-26 | 1997-09-30 | Daikyo Yakuhin Kogyo Kk | Hydrogel patch for dermal local anesthesia |
| KR19980054302A (en) * | 1996-12-27 | 1998-09-25 | 김상웅 | Novel gels containing local anesthetics |
| KR20000017706A (en) * | 1999-07-08 | 2000-04-06 | 이승하 | New pharmaceutical composition of gel preparation containing local anaesthetic agents |
-
2000
- 2000-07-03 KR KR1020000037701A patent/KR20020006555A/en not_active Application Discontinuation
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61254519A (en) * | 1985-05-07 | 1986-11-12 | Nitto Electric Ind Co Ltd | Gelatinous medicinal pharmaceutical |
| JPH09255565A (en) * | 1996-03-26 | 1997-09-30 | Daikyo Yakuhin Kogyo Kk | Hydrogel patch for dermal local anesthesia |
| KR19980054302A (en) * | 1996-12-27 | 1998-09-25 | 김상웅 | Novel gels containing local anesthetics |
| KR20000017706A (en) * | 1999-07-08 | 2000-04-06 | 이승하 | New pharmaceutical composition of gel preparation containing local anaesthetic agents |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2013027840A1 (en) * | 2011-08-25 | 2015-03-23 | ニプロパッチ株式会社 | Water-containing patch |
| KR102419076B1 (en) * | 2022-01-17 | 2022-07-08 | 장보경 | Anesthetic composition and method for preparing same |
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