KR20000025762A - Soluble composition of ivermectins - Google Patents
Soluble composition of ivermectins Download PDFInfo
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- KR20000025762A KR20000025762A KR1019980042961A KR19980042961A KR20000025762A KR 20000025762 A KR20000025762 A KR 20000025762A KR 1019980042961 A KR1019980042961 A KR 1019980042961A KR 19980042961 A KR19980042961 A KR 19980042961A KR 20000025762 A KR20000025762 A KR 20000025762A
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- oil
- ivermectins
- ivermectin
- glycofurol
- benzylbenzoate
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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
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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Abstract
Description
본 발명은 이버멕틴류의 가용화 조성물에 관한 것으로, 이버멕틴 B1a, 이버멕틴 Blb, 아버멕틴, 밀버마이신 및 그 유도체류에서 선택된 구충제를 사용하고 식물유에서 선택된 유지를 기제로 하고 여기에 벤질벤조에이트 및 글리코퓨롤에서 선택된 가용화제를 가하여 용해시켜서 제조된 조성물에 관한 것이다.The present invention relates to a solubilizing composition of ivermectin, comprising benzyl benzoate based on a fat or oil selected from vegetable oil, using an insect repellent selected from ivermectin B1a, ivermectin Blb, avermectin, milbamycin and derivatives thereof. And a solubilizer selected from glycofurol to dissolve.
이버멕틴은 아버멕틴(Avermectin)의 반합성 유도체로 두 개의 화합물(component Bla, component Blb)의 혼합체로 이루어진 광범위한 구충효과를 갖는 구충제이며 다음의 화학식 1을 가진다.Ivermectin is a semi-synthetic derivative of avermectin, an insect repellent having an extensive antiparasitic effect consisting of a mixture of two compounds (component Bla, component Blb) and has the following formula (1).
상기식에서 R은 메틸 또는 에틸기이다.( R이 메틸일때 Bla이고, 에틸일때 Blb이다.)Wherein R is a methyl or ethyl group (Bla when R is methyl, Blb when ethyl)
아버멕틴 및 밀버마이신 등도 이버멕틴과 유사물질로 이버멕틴과 같은 용도로 사용된다(이하 이버멕틴, 아버멕틴 및 밀버마이신을 총칭하여 "이버멕틴류"라 한다.). 이들 이버멕틴류는 가축, 예를들면, 양, 소, 말, 돼지, 개 등과 같은 동물에 사용되고 있을 뿐만아니라, 사람에 있어서는 사상충증의 치료에 사용된다. 본 발명은 포유류에 기생하는 기생충에 광범위한 활성을 나타내는 이버멕틴류의 가용화조성물에 관한 것이다.Avermectin and Milvermycin are also similar to ivermectin and are used for the same use as ivermectin (hereinafter referred to as ivermectin, collectively referred to as ivermectin). These ivermectins are used not only for livestock, for example animals such as sheep, cattle, horses, pigs, dogs, etc., but also for the treatment of filamentousworms in humans. The present invention relates to a solubilization composition of ivermectins that exhibits a wide range of activities against parasites parasitic in mammals.
이버멕틴류는 수성계에서는 매우 낮은 용해도를 가지고 있어 거의 녹지 않으며 일반적인 계면활성제 등을 사용하면 수용액으로 제조할 수 있다. 그러나, 이러한 제제는 불안정하고, 다른 공용매 및 안정화제를 필요로 하는 단점이 있다. 따라서, 공용매나 안정화제를 필요로 하지 않고 간단히 녹일 수 있는 가용화의 방법이 필요하다.Ivermectins have very low solubility in aqueous systems and are almost insoluble and can be prepared as aqueous solutions using common surfactants. However, these formulations are unstable and have the disadvantage of requiring other cosolvents and stabilizers. Therefore, there is a need for a solubilization method that can be simply dissolved without the need for a cosolvent or stabilizer.
또한 이버맥틴류는 비수성계에서 대부분의 유기용매에는 녹는 성질을 가지고 있으나, n-헥산 또는 이소옥탄과 같은 유기용매에는 거의 녹지 않을 뿐 아니라 다른 용제에 녹여 비수성계에서 사용할 때에는 높은 점도로 인하여 주사제로의 적용이 어려운 경향이 있다. 이러한 이버멕틴류의 수성계와 비수성계에서의 복잡한 용해도는 가용화에 의한 실제적인 이버멕틴류의 제제화를 어럽게 만들고 있다.In addition, ivermactin is soluble in most organic solvents in non-aqueous systems, but it is hardly soluble in organic solvents such as n-hexane or isooctane, and is dissolved in other solvents. It tends to be difficult to apply. The complex solubility of these ivermectins in the aqueous and non-aqueous systems makes it difficult to formulate the actual ivermectins by solubilization.
따라서, 본 발명의 목적은 특별한 계면활성제나 안정화제를 사용하지 않고 간단하게 이버멕틴류를 용해함으로써 우수한 구충효과를 가지는 조성물을 제공하는 것이다.Accordingly, it is an object of the present invention to provide a composition having excellent antiparasitic effect by simply dissolving ivermectins without using a special surfactant or stabilizer.
이버멕틴류는 앞서 언급한 바와 같이 포유류에 내,외부 기생충에 광범위한 구충작용을 나타내어 널리 쓰이고 있으나 이러한 구충작용은 수성계보다 비수성계에서 활성이 증가 된다고 알려져 있다. 따라서, 비수성계에서의 제제화가 더욱 유용하고 이러한 비수성계에서 가용화를 위해서는 앞서 언급한 다량의 유기용매나 기타 다른 용제의 종류, 사용량, 물리적인 성질 등에 있어 많은 제약이 있다는 점에서 현실적인 제제화가 어려운 실정이다.Ivermectins, as mentioned above, are widely used in mammals because they exhibit a wide range of antiparasitic effects on internal and external parasites, but these parasites are known to increase their activity in non-aqueous systems rather than in aqueous systems. Therefore, the formulation in the non-aqueous system is more useful, and in the case of solubilization in the non-aqueous system, there are many limitations in the type, amount, physical properties, etc. of the aforementioned large amount of organic solvents or other solvents. to be.
본 발명자들은 이러한 이버멕틴류의 용해성 및 그 제제화에 대하여 오랜 연구를 행한 결과, 참기름, 면실유, 낙화생유, 콩기름, 옥수수기름, 채종유등과 같은 식물유가 이버멕틴류를 잘 용해시킬 뿐만아니라, 이러한 식물유를 용해기제로 사용하면, 피하나 근육주사시에 주성분의 효과를 오래 유지시키는 작용이 있는 것으로알려져 있어 이버멕틴류와 같은 구충제에 있어서는 더욱 효과적인 사실을 발견하여 본 발명을 완성하였다. 더욱이 이버멕틴류의 가용화제로 안식향산 벤젠(Benzyl benzoate)이나 글리코퓨롤(Glycofurol)등을 사용하면, 식물유의 점도를 저하시켜줌으로서 주사제로의 적용을 용이하게 만들어준다.The present inventors have conducted a long study on the solubility and formulation of such ivermectins, and as a result, vegetable oils such as sesame oil, cottonseed oil, peanut oil, soybean oil, corn oil, rapeseed oil and the like dissolve ivermectin well, When used as a dissolving agent, it has been known to have an effect of maintaining the long-term effect of the main component during the intramuscular injection, and found a more effective in the insect repellents such as ivermectins, completed the present invention. Furthermore, the use of benzoic acid benzoate or glycofurol as a solubilizing agent for ivermectins reduces the viscosity of vegetable oils, making it easier to apply to injections.
벤질벤조에이트나 글리코퓨롤은 전체 조성물에 대하여 5.0 내지 30.0Wt%를 함유하는 것이 바람직하다.It is preferable that benzyl benzoate and glycofurol contain 5.0-30.0 Wt% with respect to the whole composition.
나머지는 식물유이다.The rest is vegetable oil.
다음의 실시예는 본 발명의 내용을 더욱 이해하기 쉽게 하기 위한 것으로 본 발명을 이에 제한하는 것으로 간주되어서는 안된다.The following examples are provided to make the contents of the present invention easier to understand and should not be construed as limiting the present invention thereto.
실시예 1.Example 1.
이버멕틴 1.0gIvermectin 1.0g
벤질벤조에이트 20.0gBenzylbenzoate 20.0 g
참기름 적당량가하여 전체 100.0g100.0g total by adding an appropriate amount of sesame oil
이버멕틴을 벤질벤조에이트에 용해시킨 후 참기름을 첨가하여 전체를 100.0g으로 제조한다.Ivermectin is dissolved in benzylbenzoate and sesame oil is added to make 100.0 g of the whole.
실시예 2.Example 2.
이버멕틴 1.0gIvermectin 1.0g
글리코퓨롤 20.0gGlycopurol 20.0g
참기름 적당량 가하여 전체 100.0gAdd 10ml of sesame oil
이버멕틴을 글리코퓨롤에 용해시킨 후 참기름을 첨가하여 전체를 100.0g으로 제조한다.Ivermectin is dissolved in glycofurol and sesame oil is added to make 100.0 g of the whole.
실시예 3.Example 3.
이버멕틴 1.0gIvermectin 1.0g
아버멕틴 1.0gAvermectin 1.0g
벤질벤조에이트 10.0gBenzylbenzoate 10.0 g
글리코퓨롤 10.0gGlycopurol 10.0g
콩기름 적당량 가하여 전체 100.0gAdd 100.0g of soybean oil
이버멕틴과 아버멕틴을 벤질벤조에이트와 글리코퓨롤에 용해시킨 후 콩기름을 첨가하여 전체를 100.0g으로 제조한다.Ivermectin and avermectin are dissolved in benzylbenzoate and glycofurol, and soybean oil is added to prepare a total of 100.0 g.
실시예 4Example 4
아버멕틴 0.5gAvermectin 0.5g
밀버마이신 0.5gMilvermycin 0.5g
벤질벤조에이트 20.0gBenzylbenzoate 20.0 g
참기름 적당량 가하여 전체 100.0gAdd 10ml of sesame oil
아버멕틴과 밀버마이신을 벤질벤조에이트에 용해시키고 참기름을 가하여 전체를 100.0g으로 제조한다.Avermectin and Milmycin are dissolved in benzylbenzoate and sesame oil is added to make 100.0 g in total.
실시예 5Example 5
이버멕틴 0.1gIvermectin 0.1g
밀버마이신 0.2gMilvermycin 0.2 g
벤질벤조에이트 5.0gBenzylbenzoate 5.0 g
글리코퓨롤 5.0gGlycofurol 5.0g
낙화생유 적당량 가하여 전체 100.0g100.0g total amount of peanut oil
이버멕틴과 밀버마이신을 벤질벤조에이트 및 글리코퓨롤에 용해시키고 낙화생유를 가하여 전체를 100.0g으로 제조한다.Ivermectin and Milmycin are dissolved in benzylbenzoate and glycofurol and peanut oil is added to make 100.0 g of the whole.
실시예 6Example 6
아버멕틴 0.5gAvermectin 0.5g
밀버마이신 0.1gMilvermycin 0.1g
글리코퓨롤 5.0gGlycofurol 5.0g
벤질벤조에이트 5.0gBenzylbenzoate 5.0 g
면실유 적당량 가하여 전체 100.0gAdd 100.0 g of cottonseed oil
아버멕틴과 밀버마이신을 글리코퓨롤과 벤질벤조에이트에 용해시키고 여기에 면실유를 가하여 전체를 100.0g으로 제조한다.Avermectin and Milmycin are dissolved in glycofurol and benzylbenzoate, and cottonseed oil is added thereto to make 100.0 g of the whole.
본 발명은 수성계와 비수성계에서의 복잡한 용해도를 갖는 이버멕틴류를 특별한 계면활성제나 안정화제를 사용하지 않고 식물유를 이용하여 간단하게 용해함으로써 우수한 구충효과를 가지는 제제를 만들 수 있다.The present invention can prepare a formulation having excellent antiparasitic effect by simply dissolving ivermectins having complex solubility in aqueous and non-aqueous systems using vegetable oil without using a special surfactant or stabilizer.
Claims (2)
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1019980042961A KR20000025762A (en) | 1998-10-14 | 1998-10-14 | Soluble composition of ivermectins |
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| Application Number | Priority Date | Filing Date | Title |
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| KR1019980042961A KR20000025762A (en) | 1998-10-14 | 1998-10-14 | Soluble composition of ivermectins |
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| KR20000025762A true KR20000025762A (en) | 2000-05-06 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20020067781A (en) * | 2001-02-19 | 2002-08-24 | 주식회사 엘지씨아이 | Anthelmintic injectable composition containing ivermectin and process for preparation thereof |
| KR100600406B1 (en) * | 2002-07-22 | 2006-07-14 | 주식회사 엘지생명과학 | Ivermectin Composition for Injection and Method for Preparing the Same |
| JP2012517994A (en) * | 2009-02-16 | 2012-08-09 | ファイザー・インク | High dose doramectin formulation |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4096271A (en) * | 1977-08-03 | 1978-06-20 | American Cyanamid Company | Slow release injectable formulations of tetramisole and derivatives in benzyl benzoate |
| EP0393890A1 (en) * | 1989-04-11 | 1990-10-24 | Pfizer Limited | Injectable compositions containing 25-cyclohexyl-avermectin B1 |
| US5045536A (en) * | 1986-06-07 | 1991-09-03 | Baker Ivor P | Liquid formulations |
| WO1997011709A1 (en) * | 1995-09-25 | 1997-04-03 | Ashmont Holdings Limited | Anthelmintic macrocyclic lactone compositions |
| WO1998011902A1 (en) * | 1996-09-18 | 1998-03-26 | Bayer Aktiengesellschaft | Injectable formulations of avermectins and milbemycins |
| US5756474A (en) * | 1996-04-17 | 1998-05-26 | Pfizer, Inc. | Non-aqueous oral-drench compositions containing avermectin compounds |
-
1998
- 1998-10-14 KR KR1019980042961A patent/KR20000025762A/en not_active Application Discontinuation
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4096271A (en) * | 1977-08-03 | 1978-06-20 | American Cyanamid Company | Slow release injectable formulations of tetramisole and derivatives in benzyl benzoate |
| US5045536A (en) * | 1986-06-07 | 1991-09-03 | Baker Ivor P | Liquid formulations |
| EP0393890A1 (en) * | 1989-04-11 | 1990-10-24 | Pfizer Limited | Injectable compositions containing 25-cyclohexyl-avermectin B1 |
| WO1997011709A1 (en) * | 1995-09-25 | 1997-04-03 | Ashmont Holdings Limited | Anthelmintic macrocyclic lactone compositions |
| US5756474A (en) * | 1996-04-17 | 1998-05-26 | Pfizer, Inc. | Non-aqueous oral-drench compositions containing avermectin compounds |
| WO1998011902A1 (en) * | 1996-09-18 | 1998-03-26 | Bayer Aktiengesellschaft | Injectable formulations of avermectins and milbemycins |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20020067781A (en) * | 2001-02-19 | 2002-08-24 | 주식회사 엘지씨아이 | Anthelmintic injectable composition containing ivermectin and process for preparation thereof |
| KR100600406B1 (en) * | 2002-07-22 | 2006-07-14 | 주식회사 엘지생명과학 | Ivermectin Composition for Injection and Method for Preparing the Same |
| JP2012517994A (en) * | 2009-02-16 | 2012-08-09 | ファイザー・インク | High dose doramectin formulation |
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