KR20010105771A - A tablet composition containing ibuprofen - Google Patents

A tablet composition containing ibuprofen Download PDF

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KR20010105771A
KR20010105771A KR1020000026677A KR20000026677A KR20010105771A KR 20010105771 A KR20010105771 A KR 20010105771A KR 1020000026677 A KR1020000026677 A KR 1020000026677A KR 20000026677 A KR20000026677 A KR 20000026677A KR 20010105771 A KR20010105771 A KR 20010105771A
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ibuprofen
water
tablet composition
soluble
organic compound
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KR100523242B1 (en
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주문기
우종수
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민경윤
한미약품공업 주식회사
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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
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Molecular Biology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

The invention relates to drylaid nonwoven materials comprising bicomponent fibres comprising a low melting polyolefin component and a high melting polyolefin component, the low melting polyolefin component constituting at least a part of the surface of the fibre and comprising a non-grafted polyolefin component and a grafted polyolefin component, wherein the grafted polyolefin component has been grafted with an unsaturated dicarboxylic acid or an anhydride thereof, e.g. with maleic acid or maleic anhydride. The bicomponent fibres have an excellent bonding affinity for natural fibres such as cellulose pulp fibres and allow the production of airlaid nonwovens with reduced generation of dust during the production process and with improved nonwoven strength properties.

Description

이부프로펜을 함유하는 정제 조성물{A tablet composition containing ibuprofen}A tablet composition containing ibuprofen

본 발명은 이부프로펜을 수용성 염기성 화합물을 혼합하여 직타하여 경구제형화시키거나, 수용성 고분자물질의 용액과 먼저 혼합하여 흡착시키는 습식공정으로 제제화함으로써 용출성이 향상된 이부프로펜 정제 조성물에 관한 것이다.The present invention relates to an ibuprofen tablet composition having improved elution by formulating ibuprofen by oral formulation by mixing a water-soluble basic compound or by direct wetting or adsorbing by mixing with a solution of a water-soluble polymer first.

2-(4-이소부틸페닐)프로피온산인 이부프로펜은 비스테로이드성, 진통성, 항염증성 및 항발열성을 지닌 잘 알려진 약제이다. 본 약제는 만성 관절류마티스, 관절통 및 관절염, 신경통 및 신경염, 상기도염, 월경곤란증, 홍반, 소염과 진통, 만성 기관지염, 하열, 강직성 적수염, 수술후 통증, 근육통, 쇠통 및 감기를 포함하는 열병 및 유행성 감기 증상에 통상적으로 일일량 600㎎을 3회에 나누어 복용한다. 소아의 경우, 5∼7세 200㎎, 8∼10세 300㎎~400㎎, 11∼15세 400㎎∼600㎎을 일일량으로 해서 2∼3회에 걸쳐 복용한다.Ibuprofen, a 2- (4-isobutylphenyl) propionic acid, is a well known drug with nonsteroidal, analgesic, anti-inflammatory and antipyretic properties. The drug is a fever and pandemic, including chronic arthritis, arthralgia and arthritis, neuralgia and neuritis, upper respiratory tract, dysmenorrhea, erythema, anti-inflammatory and analgesic, chronic bronchitis, fever, ankylosing erythritis, postoperative pain, myalgia, iron pain and cold Usually 600mg daily dose divided into three doses for cold symptoms. In children, 200 mg for 5-7 years old, 300 mg to 400 mg for 8-10 years old, and 400 mg to 600 mg for 11-15 years old are taken two to three times.

이부프로펜은 이러한 유용한 약리 효과를 가지지만 약물자체의 난용성으로 용출이 저조하므로 제제화에 많은 어려움이 있다. 그 예로, 대한민국 특허공개번호 제 99-87084호(99. 12. 15)에 이부프로펜이 산성 물질인 점을 고려하여 알카리성물질인 무기탄산염 또는 중탄산염등을 가해 신속히 붕괴되어 용출을 나타내는 제제화 방법이 개시되어 있다. 그러나, 이러한 탄산염을 함유하는 제제는 이부프로펜의 산성기와 반응하여 제제화 공정중 이산화탄소와 물이 발생되어 제제화가 어렵고, 또한 이로 인해 제제화 후에도 인습성, 부착성 등을 증가시키는 문제점을 가지고 있다.Ibuprofen has such a useful pharmacological effect, but there is a lot of difficulty in formulating because of poor dissolution due to poor solubility of the drug itself. For example, in consideration of the fact that ibuprofen is an acidic substance, Korean Patent Publication No. 99-87084 (99. 12. 15) discloses a formulation method which rapidly disintegrates by adding an inorganic carbonate or bicarbonate, which is an alkaline substance, to dissolve. have. However, such a carbonate-containing formulation reacts with an acidic group of ibuprofen to generate carbon dioxide and water during the formulation process, making it difficult to formulate, and thus, has a problem of increasing humidity and adhesion after formulation.

본 발명은 상기와 같은 사실에 의거한 것으로서, 본 발명자들은 이러한 기존 제제화의 단점을 극복하고 동시에 용출율을 향상시킬 수 있는 이부프로펜 경구제형의 제조공정을 연구하던중, 이부프로펜을 수용성 염기성 화합물과 혼합하여 직타하여 경구제형화시키거나, 수용성 고분자물질의 용액과 먼저 혼합하여 흡착시키는 습식공정으로 제제화하는 경우 인습성등의 문제점없이 지속적이며 높은 용출율을 유지시키는 것을 발견하게 되어 본 발명을 완성하게 되었다.The present invention is based on the above facts, while the present inventors have studied the manufacturing process of ibuprofen oral formulation which can overcome the disadvantages of the existing formulation and at the same time improve the dissolution rate, by mixing ibuprofen with a water-soluble basic compound When formulated by oral formulation, or when formulated in a wet process of admixing with a solution of a water-soluble polymer first to adsorb, it has been found to maintain a continuous and high dissolution rate without problems such as humidity and to complete the present invention.

본 발명의 정제 조성물은 이부프로펜, 수용성 염기성 유기 화합물, 선택적으로 수용성 고분자 물질, 붕해제, 기타 약제학적 첨가제로 구성될 수 있다.The tablet composition of the present invention may consist of ibuprofen, a water soluble basic organic compound, optionally a water soluble high molecular material, a disintegrant, and other pharmaceutical additives.

이부프로펜은 광학적 이성체를 포함하는 모든 이부프로펜이 사용 가능하다. 이부프로펜의 입도는 크게 영향을 주지 않으나 주로 5 내지 100㎛, 바람직하게는 10 내지 50㎛이다. 또한, 통상적으로 이부프로펜은 제제중에서 20 내지 80%, 바람직하게는 40 내지 70%가 포함될 수 있다.Ibuprofen can be used with all ibuprofen including optical isomers. The particle size of ibuprofen does not significantly affect, but is mainly 5 to 100 µm, preferably 10 to 50 µm. In general, ibuprofen may also comprise 20 to 80%, preferably 40 to 70% in the formulation.

이부프로펜 제제에 첨가될 수 있는 수용성 염기성 유기 화합물은 이부프로펜의 용출율도 지속적으로 유지시키고 향상시키는데 필수적인 성분으로 무기탄산염의 단점을 보완할 수 있는 수용성 염기성 유기화합물은 모두 가능하다. 예를 들면, 아르기닌, 리신 히스티딘과 같은 수용성 염기성 아미노산이나, 메글루민, 에글루민, 그리고 유기성 아민염과 같은 염기성 화합물등을 들수 있다. 이 성분은 통상적으로 이부프로펜 1 에 대해 중량비로 0.1 내지 1.5, 바람직하게는 0.25 내지 1 포함될 수 있다.The water-soluble basic organic compound that can be added to the ibuprofen preparation is an essential ingredient for continuously maintaining and improving the dissolution rate of ibuprofen, and any water-soluble basic organic compound that can compensate for the disadvantages of the inorganic carbonate is possible. For example, water-soluble basic amino acids, such as arginine and lysine histidine, and basic compounds, such as meglumine, eglumine, and an organic amine salt, etc. are mentioned. This component may typically comprise 0.1 to 1.5, preferably 0.25 to 1, by weight relative to ibuprofen 1.

선택적으로 사용될 수 있는 수용성 고분자 물질은 난용성인 이부프로펜에 흡착하여 용출률을 증가시킬 수 있는 것이면 어느것이나 가능하다. 예를 들면, 폴리비닐피롤리돈(포비돈), 폴리에틸렌글리콜류, 히드록시프로필셀룰로오스, 히드록시프로필메틸셀룰로오스, 아라비아 검류, 젤라틴, 히드록시에틸셀룰로오스, 폴록사머, 카르복시비닐 폴리머등이 사용될 수 있다. 이 성분은 통상적으로 이부프로펜 1에 대해 중량비로 0.001 내지 0.5, 바람직하게는 0.01 내지 0.2가 포함될 수 있다.The water-soluble polymer material which can be optionally used can be any so long as it can adsorb to poorly soluble ibuprofen to increase the dissolution rate. For example, polyvinylpyrrolidone (povidone), polyethylene glycols, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, gum arabic, gelatin, hydroxyethyl cellulose, poloxamer, carboxyvinyl polymer and the like can be used. This component may typically comprise 0.001 to 0.5, preferably 0.01 to 0.2, by weight relative to ibuprofen 1.

그리고, 첨가될 수 있는 붕해제로는 약제학적으로 일반적으로 사용되는 붕해제는 모두 사용될 수 있다. 예를 들면, 나트륨전분글리콜레이트, 저치환원히드록시프로필셀룰로오스, 알긴산, 가교결합된 폴리비닐피롤리돈, 마그네슘 알루미늄 실리케이트 및 크로스카멜로오스나트륨등을 들 수 있다. 바람직한 붕해제는 하나 이상의 크로스카멜로오스나트륨을 사용할 수 있다.In addition, as a disintegrant which may be added, all disintegrants which are generally used pharmaceutically may be used. For example, sodium starch glycolate, low-substituted hydroxypropyl cellulose, alginic acid, crosslinked polyvinylpyrrolidone, magnesium aluminum silicate, croscarmellose sodium, and the like. Preferred disintegrants may use one or more croscarmellose sodium.

이 성분은 통상적으로 이부프로펜 1에 대해 중량비로 0.01 내지 0.5, 바람직하게는 0.01 내지 0.3 포함될 수 있다.This component may typically be included in a weight ratio of 0.01 to 0.5, preferably 0.01 to 0.3, relative to ibuprofen 1.

기타 첨가될 수 있는 약제학제 첨가제로는 불활성희석제, 활택제 등이 사용될 수 있다. 불활성희석제로는 미결정셀룰로오스, 유당, 만니톨, 전분, 인산수소 칼슘, 황산칼슘등이 사용 가능하며, 활택제 성분으로는 스테아린산, 스테아린산 마그네슘, 스테아린산 아연, 탈크, 규산마그네슘, 규산알루미늄마그네슘, 메타규산알루미늄마그네슘, 경질무수규산, 수소화 식물성유등이 사용 가능하다.Inert diluents, lubricants and the like may be used as pharmaceutical additives that may be added. As an inert diluent, microcrystalline cellulose, lactose, mannitol, starch, calcium hydrogen phosphate, calcium sulfate, etc. can be used.Gluents include stearic acid, magnesium stearate, zinc stearate, talc, magnesium silicate, aluminum silicate silica, aluminum metasilicate. Magnesium, light anhydrous silicic acid and hydrogenated vegetable oils can be used.

이들 성분은 통상적으로 이부프로펜 1에 대하여 중량비로 0.01 내지 0.5, 바람직하게는 0.01 내지 0.3 포함될 수 있다.These components may typically be included from 0.01 to 0.5, preferably 0.01 to 0.3, by weight relative to ibuprofen 1.

따라서, 바람직한 이부프로펜 정제로 (a) 이부프로펜 1에 대해 중량비로 (b) 수용성 염기성 유기화합물 0.1 내지 1.5, (c) 선택적으로 수용성고분자 물질 0.001 내지 0.5, (d) 기타 약제학적 첨가제 0.001 내지 0.5를 포함한다. 또한, 바람직하게는 이부프로펜 1에 대해 중량비로 수용성 염기성 유기화합물 0.25 내지 1, 선택적으로 수용성 고분자물질 0.01 내지 0.2, 기타 약제학적 첨가제 0.01 내지 0.3을 포함한다.Thus, a preferred ibuprofen tablet comprises (a) 0.1 to 1.5 water soluble basic organic compounds (b) optionally from 0.001 to 0.5 water soluble polymer material, and (d) 0.001 to 0.5 other pharmaceutical additives in a weight ratio relative to ibuprofen 1 do. In addition, it preferably comprises from 0.25 to 1 of water-soluble basic organic compounds, optionally from 0.01 to 0.2 of water-soluble polymers, and from 0.01 to 0.3 of other pharmaceutical additives by weight relative to ibuprofen 1.

본 발명의 이부프로펜 제제는 다음과 같은 방법으로 제조된다.The ibuprofen formulation of the present invention is prepared by the following method.

이부프로펜과 수용성 염기성 유기화합물을 잘 혼합한 후 붕해제 및 기타약제학적 첨가제를 섞어 직타하여 제조한다. 또는, 이부프로펜에 대하여 수용성 고분자 물질을 물 또는 에탄올, 이소프로필알콜등 유기용매에 녹여 이부프로펜과 연합, 건조한다. 여기에 수용성 염기성 유기화합물과 붕해제 및 기타약제학적 첨가제를 혼합하는 습식공정을 거친 후 타정하여 제조한다.It is prepared by mixing ibuprofen and a water-soluble basic organic compound well and then directly mixing a disintegrant and other pharmaceutical additives. Alternatively, with respect to ibuprofen, a water-soluble high molecular substance is dissolved in water or an organic solvent such as ethanol or isopropyl alcohol, and then combined with ibuprofen and dried. It is prepared by tableting after a wet process of mixing a water-soluble basic organic compound with a disintegrant and other pharmaceutical additives.

이하, 본 발명의 구체적인 구성과 작용을 실시예와 비교예를 통하여 구체적으로 설명하면 다음과 같으며, 본 발명이 이에 한정되는 것은 아니다.Hereinafter, the specific configuration and operation of the present invention will be described in detail with reference to Examples and Comparative Examples, but the present invention is not limited thereto.

실시예 1.Example 1.

이부프로펜 200 ㎎Ibuprofen 200 mg 포비돈 6 ㎎Povidone 6 mg 탈크 6 ㎎Talc 6 mg 미결정셀룰로오스 15 ㎎15 mg of microcrystalline cellulose 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 아르기닌 75 ㎎Arginine 75 mg 결정무수규산 7 ㎎Crystalline Anhydrous 7 mg 소디움라우릴 설페이트 2 ㎎Sodium Lauryl Sulfate 2 mg

이부프로펜에 대하여 수용성 고분자 물질인 포비돈을 물, 이소프로필알콜에 녹여 이부프로펜과 연합, 건조한다. 여기에, 수용성 염기성 유기화합물인 아르기닌과 나머지 성분인 붕해제 및 기타약제학적 첨가제를 혼합하여 타정하여 제조한다.About ibuprofen Povidone, a water-soluble polymer, is dissolved in water and isopropyl alcohol, and then combined with ibuprofen and dried. Herein, arginine, which is a water-soluble basic organic compound, and a disintegrating agent and other pharmaceutical additives, which are the remaining components, are mixed and prepared.

실시예 2.Example 2.

이부프로펜 200 ㎎Ibuprofen 200 mg 포비돈 6 ㎎Povidone 6 mg 탈크 6 ㎎Talc 6 mg 미결정셀룰로오스 15 ㎎15 mg of microcrystalline cellulose 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 아르기닌 80 ㎎Arginine 80 mg 결정무수규산 7 ㎎Crystalline Anhydrous 7 mg 소디움라우릴 설페이트 2 ㎎Sodium Lauryl Sulfate 2 mg

상기 실시예 1의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 1, followed by tableting.

실시예3.Example 3.

이부프로펜 200 ㎎Ibuprofen 200 mg 폴리에틸렌글리콜6000 10 ㎎Polyethylene glycol6000 10 mg 탈크 15 ㎎Talc 15 mg 미결정셀룰로오스 15 ㎎15 mg of microcrystalline cellulose 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 아르기닌 70 ㎎Arginine 70 mg 결정무수규산 7 ㎎Crystalline Anhydrous 7 mg 소디움라우릴 설페이트 2 ㎎Sodium Lauryl Sulfate 2 mg

상기 실시예 1의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 1, followed by tableting.

실시예 4.Example 4.

이부프로펜 200 ㎎Ibuprofen 200 mg 탈크 5 ㎎Talc 5 mg 미결정셀룰로오스 15 ㎎15 mg of microcrystalline cellulose 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 아르기닌 100 ㎎Arginine 100 mg 결정무수규산 7 ㎎Crystalline Anhydrous 7 mg 소디움라우릴 설페이트 2 ㎎Sodium Lauryl Sulfate 2 mg

이부프로펜 및 수용성 염기성 유기화합물 그리고, 붕해제 및 기타 약제학적 첨가제를 섞어 직타하여 제품을 얻는다.Ibuprofen and a water-soluble basic organic compound and a disintegrant and other pharmaceutical additives are mixed and fired to obtain a product.

실시예5.Example 5.

이부프로펜 400 ㎎Ibuprofen 400 mg 폴리에틸렌글리콜6000 20 ㎎Polyethylene Glycol6000 20 mg 탈크 20 ㎎Talc 20 mg 미결정셀룰로오스 40 ㎎40 mg of microcrystalline cellulose 크로스카멜로오스소디움 40 ㎎Croscarmellose sodium 40 mg 아르기닌 120 ㎎Arginine 120 mg 결정무수규산 6 ㎎Crystalline Anhydrous 6 mg 소디움라우릴 설페이트 4 ㎎Sodium Lauryl Sulfate 4 mg

상기 실시예 1의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 1, followed by tableting.

실시예6.Example 6.

이부프로펜 400 ㎎Ibuprofen 400 mg 탈크 12 ㎎Talc 12 mg 미결정셀룰로오스 40 ㎎40 mg of microcrystalline cellulose 크로스카멜로오스소디움 40 ㎎Croscarmellose sodium 40 mg 메글루민 120 ㎎Meglumine 120 mg 결정무수규산 6 ㎎Crystalline Anhydrous 6 mg 소디움라우릴 설페이트 5 ㎎Sodium Lauryl Sulfate 5 mg

상기 실시예 1의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 1, followed by tableting.

실시예7.Example 7.

이부프로펜 400 ㎎Ibuprofen 400 mg 포비돈 15 ㎎Povidone 15 mg 탈크 12 ㎎Talc 12 mg 미결정셀룰로오스 30 ㎎Microcrystalline cellulose 30 mg 크로스카멜로오스소디움 30 ㎎Croscarmellose sodium 30 mg 메글루민 150 ㎎Meglumine 150 mg 결정무수규산 8 ㎎Crystalline Anhydrous 8 mg 소디움라우릴 설페이트 5 ㎎Sodium Lauryl Sulfate 5 mg

상기 실시예 1의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 1, followed by tableting.

비교예 1.Comparative Example 1.

이부프로펜 200 ㎎Ibuprofen 200 mg 탈크 6 ㎎Talc 6 mg 미결정셀룰로오스 15 ㎎15 mg of microcrystalline cellulose 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 결정무수규산 7 ㎎Crystalline Anhydrous 7 mg 소디움라우릴 설페이트 2 ㎎Sodium Lauryl Sulfate 2 mg

상기 실시예 4의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 4, followed by tableting.

비교예 2.Comparative Example 2.

이부프로펜 200 ㎎Ibuprofen 200 mg 무수탄산나트륨 15 ㎎Anhydrous sodium carbonate 15 mg 미결정셀룰로오스 60 ㎎Microcrystalline Cellulose 60mg 크로스카멜로오스소디움 15 ㎎Croscarmellose sodium 15 mg 이산화규소 0.8 ㎎0.8 mg of silicon dioxide 스테아르산 3 ㎎Stearic acid 3 mg

상기 실시예 4의 제조방법과 동일하게 제조한 후 타정하여 제조한다.It is prepared in the same manner as in Preparation Example 4, followed by tableting.

실험예. 비교 용출 시험Experimental Example Comparative dissolution test

실시예 1 및 실시예 4에서 제조된 검체와 비교예 1 및 비교예 2의 검체를 약전 일반시험법중 용출시험법 제 2 법(패들법)에 따라 시험하고 10, 15, 30, 60분후 용출액을 취하여 용출된 양을 아래 분석법에 따라 시험하였다.The samples prepared in Examples 1 and 4 and the samples of Comparative Examples 1 and 2 were tested according to the Dissolution Test Method 2 (Paddle Method) of the Pharmacopoeia General Test Method, and the eluate after 10, 15, 30, and 60 minutes. The amount eluted was tested according to the assay below.

용출실험장치 : Erweka DT 80Dissolution Test Equipment: Erweka DT 80

용출액 : 물 900mlEluent: 900 ml of water

용출액의 온도 : 37±0.5℃Eluent temperature: 37 ± 0.5 ℃

회전속도 : 50 rpmRotational Speed: 50 rpm

분석법 : 액체크로마토그라피법Assay: Liquid Chromatography

칼 럼 : Cosmosil C18(150㎜×4.6㎜)Column: Cosmosil C 18 (150㎜ × 4.6㎜)

이동상 : 아세토니트릴 : 1% 염화 초산 (pH3.0) (65 : 35)Mobile phase: Acetonitrile: 1% chloride acetic acid (pH 3.0) (65: 35)

유 속 : 1.2 ㎖/minFlow rate: 1.2 ml / min

검출기 : UV 254㎚Detector: UV 254 nm

주입량 : 20㎕Injection amount: 20µl

하기 표 1에 나타낸 결과로부터 알 수 있는 바와 같이, 수용성 고분자 물질과 수용성 염기성 유기 화합물의 첨가에 의한 본 발명에 따르는 실시예 1 제제는 비교예 1에 비해 용출을 현저히 증가시켜 난용성 이부프로펜의 용해성 증가를 확인할 수 있었고, 기존의 공지문헌보다 제조공정이 용이하므로 당해 기술 분야에서 명백한 진보성을 제공한다.As can be seen from the results shown in Table 1, the formulation of Example 1 according to the present invention by the addition of a water-soluble high molecular substance and a water-soluble basic organic compound significantly increased dissolution compared to Comparative Example 1, thereby increasing the solubility of poorly soluble ibuprofen. It could be confirmed, and since the manufacturing process is easier than the existing known literature provides a clear advance in the art.

비교용출시험 결과 (단위 : 용출율%)Comparative Dissolution Test Result (Unit: Dissolution Rate%) 검체 시간Sample time 10분10 minutes 15분15 minutes 30분30 minutes 60분60 minutes 120분120 minutes 실시예 1Example 1 32%32% 50%50% 62%62% 76%76% 84%84% 실시예 4Example 4 35%35% 52%52% 64%64% 78%78% 85%85% 비교예 1Comparative Example 1 7%7% 10%10% 13%13% 18%18% 24%24% 비교예 2Comparative Example 2 25%25% 45%45% 62%62% 75%75% 83%83%

이상 설명하고 실시예를 통하여 알 수 있는 바와 같이, 본 발명의 정제 조성물은 이부프로펜을 수용성 염기성 화합물을 혼합하여 직타하여 경구제형화시키거나, 수용성 고분자물질의 용액과 먼저 혼합하여 흡착시키는 습식공정으로 제제화함으로써 용출성이 향상된 이부프로펜 정제 조성물에 관한 것으로, 제제화시 인습성등의 문제점이 없으며, 지속적이며 높은 용출율을 유지할 수 있는 효과가 있다.As described above and as can be seen through the examples, the tablet composition of the present invention is formulated by oral formulation of ibuprofen by mixing a water-soluble basic compound with orthogonal or by first mixing with a solution of a water-soluble polymer to adsorb it. The present invention relates to an ibuprofen tablet composition having improved dissolution properties, and does not have a problem such as humidity during formulation, and has an effect of maintaining a continuous and high dissolution rate.

Claims (6)

이부프로펜을 아르기닌, 리신, 히스티딘, 메글루민, 에글루민에서 선택된 1종 이상의 수용성 염기성 유기화합물과 혼합하여 타정한 이부프로펜 정제 조성물.An ibuprofen tablet composition obtained by mixing ibuprofen with at least one water-soluble basic organic compound selected from arginine, lysine, histidine, meglumine, and eglumine. 이부프로펜을 폴리비닐피롤리돈(포비돈), 폴리에틸렌글리콜류, 히드록시프로필 셀룰로오스, 히드록시프로필메틸셀루로오스, 아라비아검류, 젤라틴, 히드록시 에틸셀룰로오스, 폴록사머, 카르복시비닐폴리머에서 선택한 1종 이상의 수용성 고분자 물질의 용액에 흡착한 후에 아르기닌, 리신, 히스티딘, 메글루민, 에글루민에서 선택된 1종 이상의 수용성 염기성 유기화합물을 혼합하여 타정한 이부프로펜 정제 조성물.Ibuprofen is water-soluble at least one selected from polyvinylpyrrolidone (povidone), polyethylene glycols, hydroxypropyl cellulose, hydroxypropylmethylcellulose, gum arabic, gelatin, hydroxyethyl cellulose, poloxamer, and carboxyvinyl polymer An ibuprofen tablet composition obtained by adsorbing at least one water-soluble basic organic compound selected from arginine, lysine, histidine, meglumine, and eglumine after adsorbing to a solution of a high molecular material. 제 1항에 있어서, 수용성 염기성 유기화합물이 이부프로펜 1에 대해 중량비로 0.1 내지 1.5의 비로 함유함을 특징으로 하는 이부프로펜 정제 조성물.The ibuprofen tablet composition according to claim 1, wherein the water-soluble basic organic compound is contained in a ratio of 0.1 to 1.5 by weight relative to ibuprofen 1. 제 2항에 있어서, 수용성 고분자 물질이 이부프로펜 1에 대해 중량비로 0.001 내지 0.5의 비로 함유함을 특징으로 하는 이부프로펜 정제 조성물.The ibuprofen tablet composition according to claim 2, wherein the water-soluble polymer material is contained in a ratio of 0.001 to 0.5 by weight relative to ibuprofen 1. 제 1항에 있어서, 수용성 염기성 유기화합물을 혼합한 후 붕해제 및 기타 약제학적 첨가제를 섞어 직타하여 제조하는 것을 특징으로 하는 이부프로펜 정제 조성물.The ibuprofen tablet composition according to claim 1, wherein the ibuprofen tablet composition is prepared by mixing a water-soluble basic organic compound, followed by mixing a disintegrant and other pharmaceutical additives. 제 2항에 있어서, 수용성 고분자 물질을 물 또는 에탄올, 이소프로필알콜등 유기용매에 녹여 고분자 물질의 용액을 만든후 이부프로펜과 연합, 건조한 후 여기에 수용성 염기성 유기화합물과 붕해제 및 기타 약제학적 첨가제를 혼합하여 습식공정을 거친후 타정하여 제조하는 것을 특징으로 하는 이부프로펜 정제 조성물.The method of claim 2, wherein the water-soluble polymer material is dissolved in water or an organic solvent such as ethanol or isopropyl alcohol to form a solution of the polymer material, and then combined with ibuprofen and dried, whereby a water-soluble basic organic compound, a disintegrant and other pharmaceutical additives Ibuprofen tablet composition, characterized in that the manufacturing by mixing and then going through a wet process.
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040106915A (en) * 2003-06-05 2004-12-20 한국유나이티드제약 주식회사 Formulation and manufacturing process solubilized ibuprofen soft capsules
CN107198676A (en) * 2017-06-23 2017-09-26 江苏神龙药业股份有限公司 A kind of ibuprofen injection for intravenously administrable

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US5028625A (en) * 1989-06-20 1991-07-02 American Home Products Corporation Acid addition salt of ibuprofen and meglumine
DK0424028T3 (en) * 1989-10-17 1996-01-29 Merck & Co Inc S (+) - ibuprofen-L-amino acid and S (+) - ibuprofen-D-amino acid as an improved analgesic with accelerated onset
IT1264856B1 (en) * 1993-06-21 1996-10-17 Zambon Spa PHARMACEUTICAL COMPOSITION WITH ANALGESIC ACTIVITY
DE4444051A1 (en) * 1994-12-10 1996-06-13 Rhone Poulenc Rorer Gmbh Pharmaceutical, oral preparation
GB9603699D0 (en) * 1996-02-21 1996-04-17 Boots Co Plc Therapeutic composition
IT1301966B1 (en) * 1998-07-30 2000-07-20 Zambon Spa PHARMACEUTICAL COMPOSITIONS WITH ANALGESIC ACTIVITY
US6551617B1 (en) * 2000-04-20 2003-04-22 Bristol-Myers Squibb Company Taste masking coating composition

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040106915A (en) * 2003-06-05 2004-12-20 한국유나이티드제약 주식회사 Formulation and manufacturing process solubilized ibuprofen soft capsules
CN107198676A (en) * 2017-06-23 2017-09-26 江苏神龙药业股份有限公司 A kind of ibuprofen injection for intravenously administrable

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