WO2004082692A1 - Composition acide active - Google Patents

Composition acide active Download PDF

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Publication number
WO2004082692A1
WO2004082692A1 PCT/JP2004/003479 JP2004003479W WO2004082692A1 WO 2004082692 A1 WO2004082692 A1 WO 2004082692A1 JP 2004003479 W JP2004003479 W JP 2004003479W WO 2004082692 A1 WO2004082692 A1 WO 2004082692A1
Authority
WO
WIPO (PCT)
Prior art keywords
antacid
calcium carbonate
magnesium hydroxide
examples
antacid composition
Prior art date
Application number
PCT/JP2004/003479
Other languages
English (en)
Japanese (ja)
Inventor
Hiroaki Kuga
Yuichiro Kano
Akihiro Tamada
Hiroyuki Kawashima
Original Assignee
Kowa Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kowa Co., Ltd. filed Critical Kowa Co., Ltd.
Priority to JP2005503694A priority Critical patent/JP4669391B2/ja
Priority to KR1020057014559A priority patent/KR101173580B1/ko
Publication of WO2004082692A1 publication Critical patent/WO2004082692A1/fr
Priority to HK06107416A priority patent/HK1087034A1/xx

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/06Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/08Oxides; Hydroxides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/06Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • A61K33/10Carbonates; Bicarbonates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • HELECTRICITY
    • H03ELECTRONIC CIRCUITRY
    • H03GCONTROL OF AMPLIFICATION
    • H03G5/00Tone control or bandwidth control in amplifiers
    • H03G5/005Tone control or bandwidth control in amplifiers of digital signals
    • HELECTRICITY
    • H03ELECTRONIC CIRCUITRY
    • H03GCONTROL OF AMPLIFICATION
    • H03G5/00Tone control or bandwidth control in amplifiers
    • H03G5/02Manually-operated control
    • H03G5/025Equalizers; Volume or gain control in limited frequency bands
    • HELECTRICITY
    • H03ELECTRONIC CIRCUITRY
    • H03GCONTROL OF AMPLIFICATION
    • H03G5/00Tone control or bandwidth control in amplifiers
    • H03G5/16Automatic control
    • H03G5/18Automatic control in untuned amplifiers
    • H03G5/22Automatic control in untuned amplifiers having semiconductor devices

Definitions

  • the present invention combines the fast-acting and long-lasting action of acid neutralization, and causes a reactive acid secretion.
  • the present invention relates to an antacid composition containing no aluminum.
  • Gastrointestinal medications generally relieve symptoms such as excessive gastric acidity, heartburn, discomfort in the stomach, stomach bloating, leaning, heavy stomach, chest stomach, belching, brushing, vomiting, excessive drinking, and stomach pain. Therefore, most commercially available gastrointestinal drugs contain antacids that neutralize hydrochloric acid secreted into the stomach and inactivate pepsin.
  • Gastrointestinal drugs containing antacids are required to neutralize stomach acid immediately after taking the drug, and to quickly relieve symptoms, to neutralize secreted hydrochloric acid, and to maintain its effect. . It is also an important factor that the pH in the stomach does not cause the repulsive acid secretion caused by tilting to the alkaline side.
  • an antacid formulation containing no aluminum for example, an antacid composition comprising calcium hydrogen phosphate or the like and an antacid containing no aluminum has been reported, and the pH in the stomach can be increased by the composition. It is moderately controlled, and the duration of action can be maintained (Japanese Patent Application Laid-Open No. 11-124,334). However, it is necessary to increase the dose to obtain a sufficient antacid effect. As a result, problems such as reduced compliance and restrictions on the combination of other medicinal ingredients have arisen, and are not always satisfactory. Disclosure of the invention
  • an object of the present invention is to provide an antacid composition which has both quick action and long-lasting acid neutralizing action, does not cause reactive acid secretion, and further does not contain aluminum.
  • the present inventors have conducted intensive studies on the antacid composition.As a result, if the three components of magnesium hydroxide, sodium hydrogen carbonate and calcium carbonate are blended so as to exhibit a constant pH, aluminum is contained. Instead, the present inventors have found that an antacid composition having rapid and sustained action of acid neutralization and no reactive acid secretion can be obtained, and thus completed the present invention.
  • the present invention relates to an antacid composition containing no aluminum, which contains magnesium hydroxide, sodium hydrogen carbonate and calcium carbonate, has a maximum pH of 5 to 7 in a modified Fox test, and does not contain aluminum. It offers things.
  • the antacid composition of the present invention is useful as an antacid compounded in gastrointestinal drugs.
  • FIG. 1 is a diagram showing a change in pH determined by a modified Fuchs test. BEST MODE FOR CARRYING OUT THE INVENTION
  • magnesium hydroxide used in the present invention examples include commercially available products such as Kyo-Sui Mag (manufactured by Kyowa Chemical) and magnesium hydroxide (manufactured by Tomita Pharmaceutical).
  • the mixing amount of magnesium hydroxide is preferably from 0.01 to 20% by weight, more preferably from 0.1 to 10% by weight, and particularly preferably from 1 to 7% by weight, based on the total amount of the preparation.
  • Examples of the sodium hydrogen carbonate used in the present invention include commercially available products such as sodium bicarbonate (made by Asahi Glass) and sodium hydrogen carbonate (made by Oriental Pharmaceutical Industries).
  • the compounding amount of sodium hydrogencarbonate is preferably 1 to 50% by weight, more preferably 5 to 40% by weight, and particularly preferably 10 to 30% by weight based on the total amount of the preparation.
  • Examples of the calcium carbonate used in the present invention include calcium carbonate, precipitated calcium carbonate, porei containing calcium carbonate as a main component, Borei Sekiishi or squid bone.
  • Commercially available products include precipitated calcium carbonate (manufactured by Bihoku Powder Chemical Industry), precipitated calcium carbonate (manufactured by Oriental Yakuhin Kogyo) and the like.
  • the amount of the carbonated calcium is preferably from 10 to 80% by weight, more preferably from 15 to 70% by weight, and particularly preferably from 20 to 60% by weight, based on the total amount of the preparation.
  • the antacid composition of the present invention contains the above three components, and has a maximum reached PH of 5 to 7 in a modified Fuchs test. Is necessary to prevent That is, if the maximum reached PH is less than 5, sufficient immediate action and sustainability cannot be obtained, and if it exceeds 7, reactive acid secretion occurs.
  • the modified Fox method test is a test method performed under the following conditions. That is, in 50 mL of 0.1 N hydrochloric acid kept at 37 ° C. and 2 ° C., the antacid composition corresponding to one dose was added. In addition, the test is started, and the pH is measured every 2 minutes up to 10 minutes after the start to evaluate the rapid effect of the antacid effect.
  • 0.1 N hydrochloric acid is added dropwise at a rate of 2 mL / min, and the pH is measured every 2 minutes to evaluate the sustainability of the antacid effect.
  • the test keep stirring the test solution with a stirrer.
  • the mass ratio of magnesium hydroxide to sodium hydrogen carbonate is preferably 1: 0.1 to 15, more preferably 1: 1 to 12, 1: 3 to 9 are particularly preferred.
  • the mass ratio between 7K magnesium oxide and calcium carbonate is preferably 1: 1 to 40, more preferably 1: 3 to 30, and particularly preferably 1: 5 to 20.
  • the mass ratio of sodium hydrogencarbonate to calcium carbonate is preferably from 0.1 to 15: 1 to 40, more preferably from 1 to 12: 3 to 30, and particularly preferably from 3 to 9: 5 to 20.
  • the method for producing the antacid composition of the present invention is not particularly limited, and can be produced by, for example, uniformly mixing magnesium hydroxide, sodium hydrogen carbonate and calcium carbonate with a commonly used machine.
  • the following drugs and additives can be used in the antacid composition of the present invention as needed.
  • the drug include antacids, stomachic, digestive medicine, intestinal medicine, antidiarrheal, analgesic / spasmodic, gastric mucosa repair agent, vitamins, antifoaming agents, etc.
  • Examples of the antacid other than the above include, for example, magnesium carbonate, aminoaminoacetic acid, mouth extract, magnesium silicate and the like.
  • stomachic examples include, but are not limited to, anis seed, aloe, fennel, konkon, zaku, prolonged life grass, oegon, oakbak, oren, processed garlic, gaju, katsuko, calamus root, dried ginger, citrus, kid, keich, gentian, gentian Kopoku, Goshu, Pepper, Colombo, Consulango, Sansho, Yamana, Shisoshi, Shukusha, Shokyouyo, Shoshuku, Blue Peel, Ishimine, Centaurium Grass, Sempuri, Soju, Soyou, Great Fragrance, Daiyo, Chikusenjin , Cock, capsicum, spruce, animal gall (including urethane), oyster, nutmeg, nin Gin, heart strength (including syrup strength), repellency (hihatsu), biyakuju, hop, homica extract, rape leaf (silica), mockup, jakchi, ryutan, ryou
  • Digestive agents include, for example, starch digestive enzymes, protein digestive enzymes, fat digestive enzymes, fibrin digestive enzymes, ursodesoxycholate, oxycholanates, colic acid, bile powder, bile extract (end) , Dehydrocholic acid, animal bile (including urethane) and the like.
  • intestinal medicine examples include live intestinal bacteria components, red buds, red buds, asenyaku, bamboo shoots, sweet potatoes, gennoshoko and the like.
  • antidiarrheals examples include acrylonitrile, berberine chloride, guaiacol, creosote, phenyl salicylate, guaiacol carbonate, berberine tannate, bismuth subsalicylate, bismuth subnitrate, bismuth subcarbonate, bismuth subgallate
  • examples include tannic acid, albumin tannate, methylene thymol tannin, thiol orcin, pectin, medicinal charcoal, calcium lactate, aceniak, squid, opaque, oren, kujin, gennoshoko, quintuplets, hawthorn, sempuri, and squid.
  • analgesic and antispasmodic agents include oxyphencycline hydrochloride, dicycline hydrochloride, methixene hydrochloride, scopolamine hydrobromide, methyl atatopine bromide, methyl anisotropine bromide, methyl scopolamine bromide, methyl bromide- 1-hyoscyamine, methylpenactidium bromide, belladonna extract, isopropamide iodide, diphenylpiperidinomethyldioxolan iodide, oral extract, oral root total alkaloid citrate, Examples include papaverine hydrochloride, ethyl aminobenzoate, engosaku, kanzo, kopoku, and peony.
  • gastric viscosity repair agent examples include sodium azulene sulfonate, aldioxa, glycyrrhizic acid and salts thereof and licorice extract, L-glutamine, copper copper chlorophyllin potassium, copper copper chlorophyllin sodium, histidine hydrochloride, pig gastric wall pepsin degradation product, Porcine gastric wall acid hydrolyzate, methylmethionine sulfonium chloride, Akebashi Kashiwa, Engosaku, Kanzo, and the like.
  • vitamins examples include nicotinic acid amide, calcium pantothenate, Piochin, vitamins or their derivatives or salts thereof, vitamin B 2 or its derivatives or salts thereof, vitamin B 6 or a derivative or a salt thereof, bi evening Min C Or a derivative thereof or a salt thereof.
  • antifoaming agent examples include dimethylpolysiloxane.
  • additives include excipients, binders, disintegrants, lubricants, coloring agents, flavoring agents, and the like.
  • excipient examples include lactose, starches, crystalline cellulose, sucrose, mannitol, light caffeic anhydride and the like.
  • binder examples include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, alpha-monostarch, bolivier pyrrolidone, polyvinyl alcohol, and pullulan.
  • disintegrant examples include carmellose, carmellose calcium, croscarmellose sodium, crosbopidone, corn starch, low-substituted hydroxypropyl cellulose and the like.
  • Lubricants include magnesium stearate, talc and the like.
  • coloring agent examples include tar dyes and iron sesquioxide.
  • Flavoring agents include stevia, aspartame, flavors and the like.
  • the antacid composition of the present invention is manufactured into powders, granules, tablets, chewable tablets, film-coated tablets, dragees, drinks, soft capsules, hard capsules, gels, etc. according to the purpose. it can.
  • magnesium hydroxide magnesium hydroxide: manufactured by Tomita Pharmaceutical Co., Ltd.
  • sodium hydrogen carbonate sodium bicarbonate: manufactured by Asahi Glass
  • 40Omg of precipitated calcium carbonate precipitated calcium carbonate: manufactured by Bihoku Powder Chemical Industry Co., Ltd.
  • Comparative Example 2 30 Omg of sodium bicarbonate and 40 Omg of precipitated calcium carbonate were taken and uniformly mixed in a mortar to obtain an antacid composition.
  • the immediate effect and persistence of antacid activity were examined in a modified Fuchs test.
  • the index of the immediate effect of the antacid effect was the pH 10 minutes after the start of the test at which the pH reached the maximum, and the index of the sustained antacid effect was the time until the pH became 3.5 or less.
  • the modified Fuchs test if the pH after 10 minutes is 6 or more, it is regarded as fast-acting, and if the time until the pH becomes 3.5 or less is 40 minutes or more, it is persistent Was considered.
  • the index of rebound acid secretion was evaluated at the highest pH reached. The results are shown in Table 1, Table 2 and Figure 1.

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Otolaryngology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Cette invention concerne une composition acide active sans aluminium, comprenant un hydroxyde de magnésium, un hydrogènecarbonate de sodium et un carbonate de calcium, dont le pH maximum selon le procédé Fuchs modifié se situe entre 5 et 7. La composition de l'invention, qui combine rapidité d'action et persistance de son action de déacidification, ne provoque pas de sécrétion par ricochet et ne contient pas d'aluminium
PCT/JP2004/003479 2003-03-18 2004-03-16 Composition acide active WO2004082692A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2005503694A JP4669391B2 (ja) 2003-03-18 2004-03-16 制酸剤組成物
KR1020057014559A KR101173580B1 (ko) 2003-03-18 2004-03-16 제산제 조성물
HK06107416A HK1087034A1 (en) 2003-03-18 2006-06-30 Actacid composition

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2003072997 2003-03-18
JP2003-072997 2003-03-18

Publications (1)

Publication Number Publication Date
WO2004082692A1 true WO2004082692A1 (fr) 2004-09-30

Family

ID=33027784

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2004/003479 WO2004082692A1 (fr) 2003-03-18 2004-03-16 Composition acide active

Country Status (6)

Country Link
JP (1) JP4669391B2 (fr)
KR (1) KR101173580B1 (fr)
CN (1) CN100342860C (fr)
HK (1) HK1087034A1 (fr)
TW (1) TWI344844B (fr)
WO (1) WO2004082692A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006131555A (ja) * 2004-11-05 2006-05-25 Dai Ichi Seiyaku Co Ltd 制酸剤組成物
KR101047042B1 (ko) * 2004-11-23 2011-07-06 동화약품주식회사 생체이용율을 향상시킨 경구용 제제
JP2011148831A (ja) * 2011-04-28 2011-08-04 Daiichi Sankyo Healthcare Co Ltd 制酸剤組成物

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103961368B (zh) * 2013-12-05 2017-01-04 广西大学 蒙脱石负载的氢氧化钙抗酸剂
CN104478268A (zh) * 2014-12-12 2015-04-01 宜兴天力化工纳米科技有限公司 一种碳酸钙碳酸氢钠复合剂及其制备方法

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS584725A (ja) * 1981-04-01 1983-01-11 ラボラトア・ユマン−フアルム・エス・ア 消化剤として有用な治療用組成物
JPH06239756A (ja) * 1993-02-15 1994-08-30 Ss Pharmaceut Co Ltd 制酸剤組成物
JPH08259445A (ja) * 1995-01-27 1996-10-08 Takeda Chem Ind Ltd 胃排出能改善性医薬組成物
JPH11501950A (ja) * 1996-01-08 1999-02-16 アストラ・アクチエボラーグ プロトンポンプ抑制剤および制酸剤またはアルギネートを含有する経口用医薬剤形
JPH11124334A (ja) * 1997-08-19 1999-05-11 Eisai Co Ltd 制酸剤組成物
JP2000219625A (ja) * 1999-01-29 2000-08-08 Dai Ichi Seiyaku Co Ltd 医薬組成物
WO2003024449A1 (fr) * 2001-09-19 2003-03-27 Abbott Laboratories Formulations pharmaceutiques pour la protection de composes pharmaceutiques contre des milieux acides

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0656677A (ja) * 1992-08-03 1994-03-01 Lion Corp 制酸剤組成物

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS584725A (ja) * 1981-04-01 1983-01-11 ラボラトア・ユマン−フアルム・エス・ア 消化剤として有用な治療用組成物
JPH06239756A (ja) * 1993-02-15 1994-08-30 Ss Pharmaceut Co Ltd 制酸剤組成物
JPH08259445A (ja) * 1995-01-27 1996-10-08 Takeda Chem Ind Ltd 胃排出能改善性医薬組成物
JPH11501950A (ja) * 1996-01-08 1999-02-16 アストラ・アクチエボラーグ プロトンポンプ抑制剤および制酸剤またはアルギネートを含有する経口用医薬剤形
JPH11124334A (ja) * 1997-08-19 1999-05-11 Eisai Co Ltd 制酸剤組成物
JP2000219625A (ja) * 1999-01-29 2000-08-08 Dai Ichi Seiyaku Co Ltd 医薬組成物
WO2003024449A1 (fr) * 2001-09-19 2003-03-27 Abbott Laboratories Formulations pharmaceutiques pour la protection de composes pharmaceutiques contre des milieux acides

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006131555A (ja) * 2004-11-05 2006-05-25 Dai Ichi Seiyaku Co Ltd 制酸剤組成物
KR101047042B1 (ko) * 2004-11-23 2011-07-06 동화약품주식회사 생체이용율을 향상시킨 경구용 제제
JP2011148831A (ja) * 2011-04-28 2011-08-04 Daiichi Sankyo Healthcare Co Ltd 制酸剤組成物

Also Published As

Publication number Publication date
TW200509950A (en) 2005-03-16
KR101173580B1 (ko) 2012-08-13
JPWO2004082692A1 (ja) 2006-06-22
KR20050107577A (ko) 2005-11-14
CN100342860C (zh) 2007-10-17
TWI344844B (en) 2011-07-11
JP4669391B2 (ja) 2011-04-13
CN1761474A (zh) 2006-04-19
HK1087034A1 (en) 2006-10-06

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