JP6479658B2 - 超速崩壊錠剤及びその製造方法 - Google Patents
超速崩壊錠剤及びその製造方法 Download PDFInfo
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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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
- A61K9/14—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
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Description
[態様1]
水中崩壊時間が15秒未満で、錠剤硬度が10N以上である崩壊性錠剤であって、酸型カルボキシメチルセルロースからなる第1の崩壊剤成分を含む口腔内崩壊錠剤。
[態様2]
さらに結晶セルロースを含む態様1記載の口腔内崩壊錠剤。
[態様3]
さらに炭酸水素塩を含む態様1又は2記載の口腔内崩壊錠剤。
[態様4]
錠剤の比表面積が0.75乃至1.50mm2/mgである、態様1乃至3のいずれか一項に記載の口腔内崩壊錠剤。
[態様5]
崩壊性粒子組成物を薬効成分と混合し、得られた混合物を打錠することを含む、態様1乃至4のいずれか一項に記載の口腔内崩壊錠剤の製造方法。
[態様6]
崩壊性粒子組成物を製造するときに湿式造粒工程を含む態様5記載の口腔内崩壊錠剤の製造方法。
[態様7]
崩壊性粒子組成物を製造するときに二段造粒工程を含む、態様5又は6記載の口腔内崩壊錠剤の製造方法。
[態様8]
打錠圧縮力1乃至30kNを加えて打錠する、態様5乃至7のいずれか一項に記載の口腔内崩壊錠剤の製造方法。
[態様9]
打錠圧縮力2乃至30kNを加えて打錠する、態様8記載の口腔内崩壊錠剤の製造方法。
[態様10]
態様5乃至9のいずれか一項に記載の口腔内崩壊錠剤の製造方法に用いる、酸型カルボキシメチルセルロースからなる第1の崩壊剤成分を含む崩壊性粒子組成物。
硬度:デジタル木屋式硬度計(KHT-40N、株式会社藤原製作所)を用いて、硬度(N)を測定した。
水中崩壊時間:日本薬局方記載の方法(ただし、補助盤なし)に従い、崩壊試験器(NT−400、富山産業株式会社)を用いて、水中崩壊時間を測定した。ただし、炭酸水素塩含有錠剤については、補助筒を用いた方法で測定した。硬度および崩壊時間はそれぞれ4〜6回の測定を行い、それらの平均値を測定結果とした。
(1)平均粒子径:50〜200ミクロン、(2)水分:0.5〜6重量%。
平均粒子径:崩壊性粒子組成物2gを、φ75mm自動振とう篩器(M−2型、筒井理化学器械株式会社)を用いて測定する。
水分:崩壊性粒子組成物5gをハロゲン水分測定器(HB43型、メトラートレド株式会社)を用いて測定する。
第一湿式造粒工程として、マンニトール(D−マンニトール、メルク株式会社)280g、カルメロース(NS−300、五徳薬品株式会社)75g、結晶セルロース(セオラスPH−101、旭化成ケミカルズ株式会社)100gを流動層造粒機(LAB−1、株式会社パウレック)に投入し、精製水240gを24g/minの速度で噴霧することによって造粒し、さらに、第二湿式造粒工程として、クロスポビドン(ポリプラスドンINF−10、アイエスピー・ジャパン株式会社)40gを添加し、精製水300gを10g/minにて噴霧することによって、造粒物(本発明の崩壊性粒子組成物)を得た。尚、造粒物は以下の物性値を有していた。(1)平均粒子径:93ミクロン、(2)水分:2.3重量%。
得られた造粒物を簡易錠剤成形機(HANDTAB−100、市橋精機株式会社)を用い、打錠圧縮力3乃至6kNにおいて打錠し、直径8.0mm、隅角平錠、重量100乃至200mgの本発明の実施例1〜6の錠剤を得た。
得られた造粒物99.5重量部に、ステアリン酸マグネシウム(太平化学産業株式会社)0.5重量部を加え混合し、簡易錠剤成形機(HANDTAB−100、市橋精機株式会社)を用い、打錠圧縮力6kN及び8kNにおいて打錠し、直径8.0mm、R6.5、重量250mgの比較例1〜2の錠剤を得た。
こうして製造された本発明の錠剤、及び、比較例で得られた錠剤の各種物性値を以下の表に示す。表1のデータから、本発明の口腔内崩壊錠剤は水中崩壊時間が15秒未満の高い崩壊性、及び、10N以上である高い錠剤硬度を有する超速崩壊錠剤であることが示されている。
Claims (7)
- 水中崩壊時間が15秒未満で、錠剤硬度が10N以上である崩壊性錠剤であって、酸型カルボキシメチルセルロース及びクロスポビドンを含む崩壊剤成分、並びに、糖又は糖アルコールから成る賦形剤を含み、比表面積が0.90乃至1.50mm2/mgである口腔内崩壊錠剤。
- さらに結晶セルロースを含む請求項1記載の口腔内崩壊錠剤。
- 酸型カルボキシメチルセルロース及びクロスポビドンを含む崩壊剤成分、並びに、糖又は糖アルコールから成る賦形剤を含む崩壊性粒子組成物を薬効成分と混合し、得られた混合物を打錠することを含む、請求項1又は2に記載の口腔内崩壊錠剤の製造方法。
- 崩壊性粒子組成物を製造するときに湿式造粒工程を含む請求項3記載の口腔内崩壊錠剤の製造方法。
- 崩壊性粒子組成物を製造するときに二段造粒工程を含む、請求項3又は4記載の口腔内崩壊錠剤の製造方法。
- 打錠圧縮力1乃至30kNを加えて打錠する、請求項3乃至5のいずれか一項に記載の口腔内崩壊錠剤の製造方法。
- 打錠圧縮力2乃至30kNを加えて打錠する、請求項6記載の口腔内崩壊錠剤の製造方法。
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