JP6271802B1 - 口腔内崩壊錠 - Google Patents
口腔内崩壊錠 Download PDFInfo
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- JP6271802B1 JP6271802B1 JP2017187417A JP2017187417A JP6271802B1 JP 6271802 B1 JP6271802 B1 JP 6271802B1 JP 2017187417 A JP2017187417 A JP 2017187417A JP 2017187417 A JP2017187417 A JP 2017187417A JP 6271802 B1 JP6271802 B1 JP 6271802B1
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- tablet
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- orally disintegrating
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- 239000006191 orally-disintegrating tablet Substances 0.000 title claims abstract description 19
- 239000003826 tablet Substances 0.000 claims abstract description 76
- 239000004480 active ingredient Substances 0.000 claims abstract description 20
- UBQNRHZMVUUOMG-UHFFFAOYSA-N zonisamide Chemical compound C1=CC=C2C(CS(=O)(=O)N)=NOC2=C1 UBQNRHZMVUUOMG-UHFFFAOYSA-N 0.000 claims abstract description 15
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 14
- 229960000913 crospovidone Drugs 0.000 claims abstract description 14
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 14
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 14
- 229960002911 zonisamide Drugs 0.000 claims abstract description 13
- 239000001913 cellulose Substances 0.000 claims abstract description 9
- 229920002678 cellulose Polymers 0.000 claims abstract description 9
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 9
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims abstract description 8
- 229920002261 Corn starch Polymers 0.000 claims abstract description 7
- 239000008120 corn starch Substances 0.000 claims abstract description 7
- 238000004090 dissolution Methods 0.000 abstract description 14
- 238000010521 absorption reaction Methods 0.000 abstract description 6
- 230000006866 deterioration Effects 0.000 abstract description 2
- 238000004519 manufacturing process Methods 0.000 description 16
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- 239000008187 granular material Substances 0.000 description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 8
- 238000000034 method Methods 0.000 description 8
- 238000004806 packaging method and process Methods 0.000 description 8
- 235000010980 cellulose Nutrition 0.000 description 7
- 238000009826 distribution Methods 0.000 description 7
- 235000010355 mannitol Nutrition 0.000 description 7
- 239000000203 mixture Substances 0.000 description 7
- 239000000654 additive Substances 0.000 description 5
- -1 for example Substances 0.000 description 5
- 238000003860 storage Methods 0.000 description 5
- 239000004372 Polyvinyl alcohol Substances 0.000 description 4
- BZHJMEDXRYGGRV-UHFFFAOYSA-N Vinyl chloride Chemical compound ClC=C BZHJMEDXRYGGRV-UHFFFAOYSA-N 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 235000019359 magnesium stearate Nutrition 0.000 description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 108010011485 Aspartame Proteins 0.000 description 3
- 239000001856 Ethyl cellulose Substances 0.000 description 3
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 3
- 208000018737 Parkinson disease Diseases 0.000 description 3
- 239000000605 aspartame Substances 0.000 description 3
- 235000010357 aspartame Nutrition 0.000 description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 3
- 229960003438 aspartame Drugs 0.000 description 3
- 239000011230 binding agent Substances 0.000 description 3
- 238000010828 elution Methods 0.000 description 3
- 229920001249 ethyl cellulose Polymers 0.000 description 3
- 235000019325 ethyl cellulose Nutrition 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 238000009516 primary packaging Methods 0.000 description 3
- 238000009517 secondary packaging Methods 0.000 description 3
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 3
- 235000012239 silicon dioxide Nutrition 0.000 description 3
- 239000000454 talc Substances 0.000 description 3
- 229910052623 talc Inorganic materials 0.000 description 3
- 229940126585 therapeutic drug Drugs 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000004743 Polypropylene Substances 0.000 description 2
- 229920001328 Polyvinylidene chloride Polymers 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 239000002274 desiccant Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 239000005033 polyvinylidene chloride Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 1
- OEPOKWHJYJXUGD-UHFFFAOYSA-N 2-(3-phenylmethoxyphenyl)-1,3-thiazole-4-carbaldehyde Chemical compound O=CC1=CSC(C=2C=C(OCC=3C=CC=CC=3)C=CC=2)=N1 OEPOKWHJYJXUGD-UHFFFAOYSA-N 0.000 description 1
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 1
- DCXXMTOCNZCJGO-UHFFFAOYSA-N Glycerol trioctadecanoate Natural products CCCCCCCCCCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC DCXXMTOCNZCJGO-UHFFFAOYSA-N 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 239000001110 calcium chloride Substances 0.000 description 1
- 229910001628 calcium chloride Inorganic materials 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000000748 compression moulding Methods 0.000 description 1
- 230000002542 deteriorative effect Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000007922 dissolution test Methods 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
Images
Classifications
-
- 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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
Abstract
Description
また、具体的な水分値を測定する錠剤は、例えば製造から3か月以内の錠剤である。
エチルセルロース(6質量部)をエタノールに溶解させた溶液とタルク(1.5質量部)を水に懸濁させた懸濁液を混合してコーティング液を調製した。ゾニサミド(25質量部)、D-マンニトール(1.5質量部)、軽質無水ケイ酸(0.5質量部)、及びアスパルテーム(0.5質量部)を流動層造粒機に投入して、先に調製したコーティング液を用いて流動層造粒し、得られた造粒物を乾燥した。この造粒物にSmart EX(登録商標) 0D50(155.4質量部、フロイント産業株式会社:D-マンニトール、ポリビニルアルコール(完全けん化物)、及び低置換度ヒドロキシプロピルセルロースを含む)、クロスポビドン(6質量部)、及びアスパルテーム(2質量部)を加えて混合した。さらに、この混合物にステアリン酸マグネシウム(1.6質量部)を加えて混合して打錠用の顆粒とし、ロータリー打錠機を用いて圧縮成型して口腔内崩壊錠(有効成分25 mg、直径8 mm及び厚み3.85 mmの碁石状、質量200 mg/錠、硬度約10 kgf)を調製した。この錠剤にPVC/PVDC/PVCの一次包装及びアルミピローの二次包装を施した。
製造直後の本発明の錠剤(包装前)に含まれる水分量を赤外線水分法により測定したところ0.8%であった。また、本発明の錠剤を25℃65%RH(開放)及び25℃75%RH(開放)の条件下で3日間放置したところ、錠剤中の平衡水分量はそれぞれ1.5%及び1.8%であった。一方、トレリーフOD錠25 mg(大日本住友製薬株式会社)を包装から取り出し、放置することなく直ちに水分量を赤外線水分法により測定したところ1.9%であった。また、トレリーフOD錠25 mgを包装から取り出した後に25℃65%RH(開放)及び25℃75%RH(開放)の条件下で3日間放置したところ、錠剤中の平衡水分量はそれぞれ3.0%及び3.8%であった。
例2に従って、加湿により水分を吸収した本発明の錠剤(25℃75%RHの開放条件下で3日間放置したもの、水分1.8%)をさらに70℃で8日間保存し、溶出特性を日本薬局方の溶出試験法に従って測定し、製造直後の錠剤の溶出特性と比較した。結果を図1に示す。製造直後の錠剤(水分0.8%)の30、45、及び60分後の有効成分の溶出率はそれぞれ91.2%、97.9%、及び99.7%であるのに対して、加湿後、更に70℃の恒温恒湿器で保管した本発明の錠剤ではそれぞれ77.4%、90.1%、及び95.4%であった。一方、加湿後、更に70℃の恒温恒湿器で保管したトレリーフOD錠25mg(水分3.8%)について同様に溶出特性を測定したところ、包装から取り出した直後の錠剤(水分1.9%)の30、45、及び60分後の有効成分の溶出率がそれぞれ91.2%、95.3%、及び96.5%であるのに対して、加湿後、更に70℃の恒温恒湿器で保管したでは溶出率がそれぞれ21.5%、31.8%、及び41.3%に低下していた(図2)。
Claims (1)
- ゾニサミドを有効成分として含む口腔内崩壊錠であって、製剤用添加物として結晶セルロース及びトウモロコシデンプンを含有せず、クロスポビドン及び低置換度ヒドロキシプロピルセルロースを含み、錠剤の全質量に対してクロスポビドンの量が1質量%以上、10質量%以下である口腔内崩壊錠。
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JP2017187417A JP6271802B1 (ja) | 2017-09-28 | 2017-09-28 | 口腔内崩壊錠 |
PCT/JP2017/035381 WO2019064468A1 (ja) | 2017-09-28 | 2017-09-29 | 口腔内崩壊錠 |
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JP2017187417A JP6271802B1 (ja) | 2017-09-28 | 2017-09-28 | 口腔内崩壊錠 |
Publications (2)
Publication Number | Publication Date |
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JP6271802B1 true JP6271802B1 (ja) | 2018-01-31 |
JP2019059702A JP2019059702A (ja) | 2019-04-18 |
Family
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JP2017187417A Active JP6271802B1 (ja) | 2017-09-28 | 2017-09-28 | 口腔内崩壊錠 |
Country Status (2)
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JP (1) | JP6271802B1 (ja) |
WO (1) | WO2019064468A1 (ja) |
Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH03130214A (ja) * | 1989-07-20 | 1991-06-04 | Dainippon Pharmaceut Co Ltd | 不快な味が遮蔽された速放性製剤 |
WO2009102038A1 (ja) * | 2008-02-13 | 2009-08-20 | Dainippon Sumitomo Pharma Co., Ltd. | 口腔内崩壊錠 |
JP2012036140A (ja) * | 2010-08-10 | 2012-02-23 | Kyoto Pharmaceutical Industries Ltd | 苦味を抑制した速崩壊錠 |
CN107095853A (zh) * | 2017-04-01 | 2017-08-29 | 重庆康刻尔制药有限公司 | 一种口腔崩解片崩解剂组合及其使用方法 |
JP2017165768A (ja) * | 2015-03-13 | 2017-09-21 | 大原薬品工業株式会社 | ロスバスタチンカルシウムを含有する錠剤 |
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2017
- 2017-09-28 JP JP2017187417A patent/JP6271802B1/ja active Active
- 2017-09-29 WO PCT/JP2017/035381 patent/WO2019064468A1/ja active Application Filing
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH03130214A (ja) * | 1989-07-20 | 1991-06-04 | Dainippon Pharmaceut Co Ltd | 不快な味が遮蔽された速放性製剤 |
WO2009102038A1 (ja) * | 2008-02-13 | 2009-08-20 | Dainippon Sumitomo Pharma Co., Ltd. | 口腔内崩壊錠 |
JP2012036140A (ja) * | 2010-08-10 | 2012-02-23 | Kyoto Pharmaceutical Industries Ltd | 苦味を抑制した速崩壊錠 |
JP2017165768A (ja) * | 2015-03-13 | 2017-09-21 | 大原薬品工業株式会社 | ロスバスタチンカルシウムを含有する錠剤 |
CN107095853A (zh) * | 2017-04-01 | 2017-08-29 | 重庆康刻尔制药有限公司 | 一种口腔崩解片崩解剂组合及其使用方法 |
Non-Patent Citations (1)
Title |
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鷹取敏仁: "製剤化のサイエンス 臨床で使いやすい薬をめざして 第52回 トレリーフOD錠25mg", ファルマシア, vol. Vol. 53, No.2, JPN6017044698, 1 February 2017 (2017-02-01), pages pp. 167-169 * |
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Publication number | Publication date |
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WO2019064468A1 (ja) | 2019-04-04 |
JP2019059702A (ja) | 2019-04-18 |
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