JP2000273039A - Composition disintegrable in oral cavity - Google Patents
Composition disintegrable in oral cavityInfo
- Publication number
- JP2000273039A JP2000273039A JP2000010452A JP2000010452A JP2000273039A JP 2000273039 A JP2000273039 A JP 2000273039A JP 2000010452 A JP2000010452 A JP 2000010452A JP 2000010452 A JP2000010452 A JP 2000010452A JP 2000273039 A JP2000273039 A JP 2000273039A
- Authority
- JP
- Japan
- Prior art keywords
- ingredient
- composition
- mass
- mannitol
- lactose
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 55
- 210000000214 mouth Anatomy 0.000 title claims abstract description 14
- 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 claims abstract description 21
- 229930195725 Mannitol Natural products 0.000 claims abstract description 21
- 239000000594 mannitol Substances 0.000 claims abstract description 21
- 235000010355 mannitol Nutrition 0.000 claims abstract description 21
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims abstract description 20
- 239000008101 lactose Substances 0.000 claims abstract description 20
- 229920002678 cellulose Polymers 0.000 claims abstract description 19
- 238000000034 method Methods 0.000 claims abstract description 17
- 239000001913 cellulose Substances 0.000 claims abstract description 16
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims abstract description 11
- 229920002472 Starch Polymers 0.000 claims abstract description 11
- 229960000913 crospovidone Drugs 0.000 claims abstract description 11
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims abstract description 11
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims abstract description 11
- 235000019698 starch Nutrition 0.000 claims abstract description 10
- 239000000314 lubricant Substances 0.000 claims abstract description 9
- 238000004519 manufacturing process Methods 0.000 claims abstract description 9
- 239000004480 active ingredient Substances 0.000 claims abstract description 8
- 229920002785 Croscarmellose sodium Polymers 0.000 claims abstract description 7
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229960001681 croscarmellose sodium Drugs 0.000 claims abstract description 7
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims abstract description 7
- 239000008107 starch Substances 0.000 claims description 6
- 239000007884 disintegrant Substances 0.000 claims description 5
- 239000011230 binding agent Substances 0.000 claims description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 abstract description 26
- 235000010980 cellulose Nutrition 0.000 abstract description 18
- 235000019359 magnesium stearate Nutrition 0.000 abstract description 13
- 239000003795 chemical substances by application Substances 0.000 abstract description 10
- 229920002261 Corn starch Polymers 0.000 abstract description 8
- 239000008120 corn starch Substances 0.000 abstract description 8
- 229920000881 Modified starch Polymers 0.000 abstract description 5
- 238000009826 distribution Methods 0.000 abstract description 5
- 235000000346 sugar Nutrition 0.000 abstract description 4
- 150000002148 esters Chemical class 0.000 abstract description 2
- 230000027119 gastric acid secretion Effects 0.000 abstract description 2
- 230000002496 gastric effect Effects 0.000 abstract description 2
- 239000003112 inhibitor Substances 0.000 abstract description 2
- 239000000454 talc Substances 0.000 abstract description 2
- 229910052623 talc Inorganic materials 0.000 abstract description 2
- 239000004615 ingredient Substances 0.000 abstract 6
- 210000004400 mucous membrane Anatomy 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 32
- 238000000748 compression moulding Methods 0.000 description 21
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 14
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 14
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 12
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 12
- 230000000052 comparative effect Effects 0.000 description 8
- 238000001035 drying Methods 0.000 description 7
- 238000002360 preparation method Methods 0.000 description 7
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 5
- 235000013539 calcium stearate Nutrition 0.000 description 5
- 239000008116 calcium stearate Substances 0.000 description 5
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 4
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 4
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 4
- 229950008138 carmellose Drugs 0.000 description 4
- 238000005469 granulation Methods 0.000 description 4
- 230000003179 granulation Effects 0.000 description 4
- 239000002245 particle Substances 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 235000010724 Wisteria floribunda Nutrition 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 239000006191 orally-disintegrating tablet Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- -1 troches Substances 0.000 description 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 2
- 239000011575 calcium Substances 0.000 description 2
- 229910052791 calcium Inorganic materials 0.000 description 2
- 238000013329 compounding Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000004108 freeze drying Methods 0.000 description 2
- 229960001680 ibuprofen Drugs 0.000 description 2
- 230000001771 impaired effect Effects 0.000 description 2
- 229940041616 menthol Drugs 0.000 description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- GFWRVVCDTLRWPK-KPKJPENVSA-N sofalcone Chemical compound C1=CC(OCC=C(C)C)=CC=C1\C=C\C(=O)C1=CC=C(OCC=C(C)C)C=C1OCC(O)=O GFWRVVCDTLRWPK-KPKJPENVSA-N 0.000 description 2
- 229950004782 sofalcone Drugs 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000811 xylitol Substances 0.000 description 2
- 235000010447 xylitol Nutrition 0.000 description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 2
- 229960002675 xylitol Drugs 0.000 description 2
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000004880 Polyuria Diseases 0.000 description 1
- 229920001218 Pullulan Polymers 0.000 description 1
- 239000004373 Pullulan Substances 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 239000002585 base Substances 0.000 description 1
- 238000010009 beating Methods 0.000 description 1
- 230000003115 biocidal effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 239000007910 chewable tablet Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 230000035619 diuresis Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 239000003485 histamine H2 receptor antagonist Substances 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 239000005554 hypnotics and sedatives Substances 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940116317 potato starch Drugs 0.000 description 1
- 229920003124 powdered cellulose Polymers 0.000 description 1
- 235000019814 powdered cellulose Nutrition 0.000 description 1
- 210000002307 prostate Anatomy 0.000 description 1
- 235000019423 pullulan Nutrition 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 1
- 238000005096 rolling process Methods 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 229940075430 wheat dextrin Drugs 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、口腔内で速やかに
崩壊し、かつ、製造工程、流通過程及び保存時に実用上
十分な強度を有する口腔内崩壊性組成物、及びその製造
方法に関する。TECHNICAL FIELD The present invention relates to an orally disintegratable composition which rapidly disintegrates in the oral cavity and has practically sufficient strength during the production process, distribution process and storage, and a method for producing the same.
【０００２】[0002]
【従来の技術】医薬品分野等における経口用固形製剤の
従来の剤形としては、錠剤、カプセル剤、トローチ剤、
チュアブル錠、顆粒剤、散剤などが知られているが、高
齢者、小児や嚥下困難な患者に対しては、必ずしも服用
のし易い剤形とは言えず、改善の検討が進められてい
る。2. Description of the Related Art Conventional dosage forms of solid oral preparations in the pharmaceutical field and the like include tablets, capsules, troches,
Chewable tablets, granules, powders, and the like are known, but for elderly people, children, and patients who have difficulty swallowing, it is not necessarily a dosage form that is easy to take, and improvements are being studied.
【０００３】例えば、凍結乾燥法を利用した口腔内溶解
型製剤の他に、特開平５−２７１０５４号公報、ＷＯ９
３／１５７２４号公報、特開平６−２１８０２８号公
報、特開平８−１９５８９号公報等に記載の口腔内崩壊
性錠が知られている。しかしながら、凍結乾燥法を利用
した口腔内溶解型製剤は急速な崩壊性を有するが、錠剤
硬度の測定が不可能なほど脆いといった欠点がある。ま
た、各公報に記載の口腔内崩壊性錠は、一種の湿製錠剤
を製造しその後乾燥する方法であり、得られた製剤は適
度の空隙率を有する多孔性の錠剤となり、軟らかくて崩
壊性に優れているものの、湿潤粉体は流動性が悪く、充
填、圧縮すると充填ばらつきが大きく、打錠機と粉体と
の付着を生じやすい。この問題を解決するための方法と
しては特殊な充填・成型機が必要となる。また、特表平
６−５０２１９４号公報には、被覆及び／または非被
覆された薬物、崩壊剤、水と接触して高粘度を生じ
ない膨張剤または可溶剤を圧縮成型した口腔内崩壊錠が
記載されている。しかし本公報記載の方法では、味の良
い可溶剤としてのマンニトールやキシリトールのような
糖類を用いると圧縮成型時に打錠障害があり作業適性が
悪いものや口腔内で崩壊するのに時間がかかるものがあ
る。[0003] For example, in addition to an oral dissolution-type preparation utilizing a freeze-drying method, Japanese Patent Application Laid-Open No. 5-27054, WO9
Orally disintegrating tablets described in 3/15724, JP-A-6-218028, JP-A-8-19589 and the like are known. However, the oral dissolution-type preparation utilizing the freeze-drying method has a rapid disintegration property, but has a drawback that the tablet hardness is too brittle to measure. In addition, the orally disintegrating tablets described in each gazette are a method of producing a kind of wet tablet and then drying, and the obtained preparation becomes a porous tablet having an appropriate porosity, and is soft and disintegrable. However, the wet powder has poor fluidity, and when filled and compressed, the dispersion of filling is large, and the powder tends to adhere to the tableting machine. As a method for solving this problem, a special filling and molding machine is required. JP-A-6-502194 discloses an orally disintegrating tablet obtained by compression-molding a coated and / or uncoated drug, a disintegrant, a swelling agent or a solvent which does not generate a high viscosity upon contact with water. Has been described. However, in the method described in this publication, when a saccharide such as mannitol or xylitol as a good-tasting solvent is used, there is a tableting obstacle at the time of compression molding, which causes poor workability or a time-consuming disintegration in the oral cavity. There is.
【０００４】[0004]
【発明が解決しようとする課題】本発明の目的は、口腔
内で速やかに崩壊し、かつ製造工程及び流通過程におい
て実用上十分な強度を有する口腔内崩壊性組成物を提供
することにある。SUMMARY OF THE INVENTION An object of the present invention is to provide an orally disintegrating composition which rapidly disintegrates in the oral cavity and has practically sufficient strength in the production and distribution processes.
【０００５】[0005]
【課題を解決するための手段】上記の問題点を解決すべ
く鋭意検討した結果、マンニトールをベースとし、崩壊
剤、セルロース類、滑沢剤、並びにデンプン類及び乳糖
の少なくとも一種を含有したものを圧縮成型することに
より、口腔内で速やかに崩壊し、かつ、製造工程及び流
通過程において実用上十分な強度を有する口腔内崩壊性
組成物が得られることを見いだし、本発明を完成させ
た。As a result of intensive studies to solve the above-mentioned problems, a mannitol-based product containing a disintegrating agent, a cellulose, a lubricant, and at least one of starch and lactose has been proposed. It has been found that an orally disintegrating composition which rapidly disintegrates in the oral cavity and has practically sufficient strength in the production process and the distribution process can be obtained by compression molding, thereby completing the present invention.
【０００６】即ち、本発明は、マンニトール、崩壊剤、
セルロース類、滑沢剤、並びにデンプン類及び乳糖の少
なくとも１種を含有する口腔内で速やかに崩壊し、実用
上十分な強度を有する口腔内崩壊性組成物である。That is, the present invention relates to mannitol, a disintegrant,
It is an orally disintegratable composition containing celluloses, a lubricant, and at least one of starches and lactose, which rapidly disintegrates in the oral cavity and has practically sufficient strength.
【０００７】[0007]
【発明の実施の形態】本発明において、口腔内で速やか
に崩壊するとは、水を用いないで服用した際に口腔内に
おいて６０秒以内に組成物全量が細かく崩壊・分散する
ことをいう。BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, rapid disintegration in the oral cavity means that the whole composition is finely disintegrated and dispersed in the oral cavity within 60 seconds when taken without using water.
【０００８】本発明に用いられる崩壊剤としては、カル
メロース、クロスポビドン、クロスカルメロースナトリ
ウム、カルメロースカルシウム、低置換度ヒドロキシプ
ロピルセルロースを挙げることができ、好ましくはクロ
スポビドン、クロスカルメロースナトリウムである。こ
れらの成分は１種又は２種以上を用いることができる。
セルロース類としては、粉末セルロース、結晶セルロー
ス等を挙げることができ、少なくとも１種を用いること
ができる。結合剤としては、ヒドロキシプロピルセルロ
ース、ヒドロキシプロピルメチルセルロース、ポリビニ
ルピロリドン、プルラン等が挙げられ、１種又は２種以
上を用いることができる。滑沢剤としては、ステアリン
酸マグネシウム、ステアリン酸カルシウム、シュガーエ
ステル、タルク、硬化油、ポリエチレングリコール等を
挙げることができ１種又は２種以上用いることができ
る。デンプン類としては、部分α化デンプン、トウモロ
コシデンプン、馬鈴薯デンプン、コメデンプン、コムギ
デンプン、デキストリンなどを挙げることができ１種又
は２種以上用いることができる。Examples of the disintegrant used in the present invention include carmellose, crospovidone, croscarmellose sodium, carmellose calcium, and low-substituted hydroxypropylcellulose, preferably crospovidone and croscarmellose sodium. . One or more of these components can be used.
Examples of the celluloses include powdered cellulose and crystalline cellulose, and at least one of them can be used. Examples of the binder include hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, pullulan and the like, and one or more kinds can be used. Examples of the lubricant include magnesium stearate, calcium stearate, sugar ester, talc, hydrogenated oil, polyethylene glycol, and the like, and one or more kinds can be used. Examples of the starches include partially pregelatinized starch, corn starch, potato starch, rice starch, wheat starch, dextrin and the like, and one or more kinds can be used.
【０００９】本発明においては、デンプン類、乳糖は圧
縮成型時における障害を低減する効果があることからこ
れらの成分とマンニトールとの配合比は重要である。デ
ンプン類を用いる場合には、マンニトールとデンプン類
の質量比は１０：１〜１：１の範囲が適当であるが、好
ましくは４：１〜７：５である。乳糖を用いる場合に
は、マンニトールと乳糖の質量比は１０：１〜１：１０
の範囲が適当であるが、好ましくは４：１〜１：１であ
る。また、組成物全量に対する各成分の配合比に関して
は、結合剤では組成物全量に対し０〜１０質量％の範囲
で用いることができる。滑沢剤では、通常、組成物全量
に対して、微量〜２質量％の範囲が用いられるが、本発
明においては、効果を損なわない範囲で圧縮成型障害を
緩和するために、２質量％を越えて添加することも可能
である。In the present invention, the ratio of starch and lactose to mannitol is important, since starch and lactose have the effect of reducing the obstacles during compression molding. When starches are used, the weight ratio of mannitol to starch is suitably in the range of 10: 1 to 1: 1 but preferably in the range of 4: 1 to 7: 5. When lactose is used, the mass ratio between mannitol and lactose is 10: 1 to 1:10.
Is appropriate, but preferably from 4: 1 to 1: 1. As for the mixing ratio of each component to the total amount of the composition, the binder can be used in the range of 0 to 10% by mass based on the total amount of the composition. In the lubricant, a range of a trace amount to 2% by mass is usually used based on the total amount of the composition. In the present invention, 2% by mass is used in order to alleviate the compression molding failure as long as the effect is not impaired. It is also possible to add more.
【００１０】本発明に適用される有効成分は、医薬品又
は食品分野で用いられるものであればいずれであっても
よい。例えば、胃粘膜修復剤、Ｈ2受容体拮抗薬、胃酸
分泌抑制薬、解熱鎮痛剤、抗生剤、ビタミン剤、抗ヒス
タミン剤、催眠鎮静剤・抗不安剤、高脂血症用剤、糖尿
病用剤、利尿剤、不整脈用剤、アレルギー用剤、前立腺
用剤等を挙げることができ、１種又は２種以上を組み合
わせて用いることができる。[0010] The active ingredient applicable to the present invention may be any active ingredient used in the pharmaceutical or food fields. For example, gastric mucosal repair agent, H2 receptor antagonist, gastric acid secretion inhibitor, antipyretic analgesic, antibiotic, vitamin, antihistamine, hypnotic sedative / anxiolytic, hyperlipidemia, diabetes, diuresis Agents, agents for arrhythmia, agents for allergy, agents for prostate, and the like, and one or a combination of two or more thereof can be used.
【００１１】また、有効成分の性状は、粉末状、結晶
状、油状、溶液状などいずれでもよく、また水溶性はも
ちろんのこと、難水溶性の有効成分（水に対する溶解度
０.１ｍｇ／ｍｌ未満）にも適用できる。更に、微粉化
した有効成分（平均粒子径２０μｍ未満）への適用も可
能である。The active ingredient may be in the form of powder, crystal, oil, solution or the like. The active ingredient is not only water-soluble but also poorly water-soluble (solubility in water of less than 0.1 mg / ml). ) Is also applicable. Further, application to a finely divided active ingredient (average particle diameter of less than 20 μm) is also possible.
【００１２】有効成分の配合量は、配合目的及びその物
理化学的性質によるが組成物全量に対して、通常０.０
０１〜７０質量％、好ましくは０.１〜５０質量％、更
に好ましくは０.１〜２０質量％程度である。The compounding amount of the active ingredient depends on the purpose of the compounding and its physicochemical properties, but is usually 0.0 based on the total amount of the composition.
It is about 0.01 to 70% by mass, preferably about 0.1 to 50% by mass, and more preferably about 0.1 to 20% by mass.
【００１３】また、本発明の効果を損なわない範囲で、
徐放性基剤、香料、甘味料、着色剤等を添加することが
できる。[0013] In addition, as long as the effects of the present invention are not impaired,
Sustained-release bases, flavors, sweeteners, coloring agents and the like can be added.
【００１４】本発明の口腔内崩壊性組成物は、錠剤剤等
の固形剤を製造する通常の製造設備が使用可能で、乾燥
状態で圧縮成型して製造する。例えば全ての配合成分
を混合し、圧縮成型する直打法、全て若しくは一部の
配合成分を乾式造粒して得た造粒物に、残りの成分を加
えて混合後、圧縮成型する方法、配合成分の一部を湿
式造粒し乾燥して得た造粒物に、残りの成分を加えて混
合後、圧縮成型する方法、滑沢剤を除く配合成分を湿
式造粒し乾燥して得た造粒物に、滑沢剤を加えて混合
後、圧縮成型する方法等を挙げることができる。造粒法
は、湿式造粒法が好ましく、具体的には流動層造粒機、
転動攪拌造粒機等を用いることができる。また、造粒時
に使用できる溶媒としては、水、アルコール、含水アル
コール等を挙げることができ、そのまま、あるいはこれ
らに結合剤を含有させて用いることができる。The orally disintegrating composition of the present invention can be produced by compression-molding in a dry state, using a usual production facility for producing a solid preparation such as a tablet. For example, a direct beating method in which all the components are mixed and compression-molded, a method in which all or some of the components are dry-granulated, and the remaining components are added and mixed, followed by compression molding, A method of wet-granulating a part of the blended components, adding the remaining components to the granulated product obtained by drying and mixing, compression molding, and wet-granulating the blended components excluding the lubricant and drying. A method may be used in which a lubricant is added to the granulated product, mixed, and then compression molded. The granulation method is preferably a wet granulation method, specifically, a fluidized bed granulator,
A rolling agitating granulator or the like can be used. Examples of the solvent that can be used at the time of granulation include water, alcohol, and hydrated alcohol, and these can be used as they are or with a binder added thereto.
【００１５】本発明で得られる口腔内崩壊性組成物の形
状は、通常円形であるが、三角形等の異形でもよく、表
面にフィルムコーティングや糖衣を施すこともできる。The shape of the orally disintegrating composition obtained in the present invention is usually circular, but may be irregular such as triangular, and the surface may be coated with a film or sugar-coated.
【００１６】また、本発明は、実用上十分な強度を有す
ることを特徴としている。ここで云う実用上十分な強度
とは、ＰＴＰ包装に適用可能な強度であり、配送や携帯
にも充分耐えうるものをいい、強度の目安としては、例
えば錠剤の場合には硬度を指標として用いることができ
る。その硬度は、錠剤の大きさ、形状により異なるが、
例えば直径約８．０ｍｍ以下の場合には、１０Ｎ以上、
直径１２.０ｍｍを越える場合は２０Ｎ以上が好まし
い。Further, the present invention is characterized in that it has sufficient strength for practical use. The practically sufficient strength referred to herein is a strength applicable to PTP packaging, which means that it can sufficiently withstand delivery and carrying. For example, in the case of tablets, hardness is used as an index. be able to. Its hardness depends on the size and shape of the tablet,
For example, when the diameter is about 8.0 mm or less, 10 N or more,
When the diameter exceeds 12.0 mm, 20N or more is preferable.
【００１７】[0017]
【発明の効果】口腔内において速やかに崩壊し、かつ製
造工程及び流通過程において実用上十分な強度を有する
口腔内崩壊性組成物、及びその製造方法を提供すること
が可能となった。According to the present invention, it is possible to provide an orally disintegrating composition which rapidly disintegrates in the oral cavity and has practically sufficient strength in the production and distribution processes, and a method for producing the same.
【００１８】[0018]
【実施例】以下に実施例及び試験例を挙げて本発明を更
に詳しく説明する。The present invention will be described in more detail with reference to the following examples and test examples.
【００１９】実施例１ マンニトール２７７ｇ、乳糖８１ｇ、結晶セルロース２
００ｇ、クロスポビドン５０ｇを秤り、これにステアリ
ン酸マグネシウムを組成物全量に対して１質量％になる
ように加え、ロータリー式打錠機（菊水製作所製）を用
い、圧縮成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠
剤を得た。Example 1 277 g of mannitol, 81 g of lactose, crystalline cellulose 2
00 g and crospovidone 50 g were weighed, and magnesium stearate was added to the composition in an amount of 1% by mass with respect to the total amount of the composition, and the mixture was compression-molded using a rotary tableting machine (manufactured by Kikusui Seisakusho) to obtain 1 tablet mass. 280 mg, 9 mm diameter tablets were obtained.
【００２０】実施例２ マンニトール２７７ｇ、乳糖８１ｇ、トウモロコシデン
プン５９ｇ、部分α化デンプン５９ｇ、結晶セルロース
９０ｇ、クロスカルメロースナトリウム３０ｇを混合し
て、バーチカルグラニュレーター（パウレック社製）で
水を用いて造粒した後、流動層造粒機（大川原社製）で
乾燥し、ステアリン酸マグネシウムを組成物全量に対し
て１質量％になるように加え、ロータリー式打錠機（菊
水製作所製）を用い圧縮成型し、１錠質量２８０ｍｇ、
直径９ｍｍの錠剤を得た。Example 2 277 g of mannitol, 81 g of lactose, 59 g of corn starch, 59 g of partially pregelatinized starch, 90 g of crystalline cellulose, and 30 g of croscarmellose sodium were mixed and produced using a vertical granulator (manufactured by Powrex) using water. After granulation, the mixture is dried with a fluidized bed granulator (manufactured by Okawara Co., Ltd.), magnesium stearate is added in an amount of 1% by mass based on the total amount of the composition, and the mixture is compressed using a rotary tableting machine (manufactured by Kikusui Seisakusho). Molded, 280 mg per tablet,
A tablet having a diameter of 9 mm was obtained.
【００２１】実施例３ マンニトール３８５ｇ、乳糖１７０ｇ、結晶セルロース
１０８ｇ、クロスポビドン３６ｇを混合して、流動層造
粒機（大川原社製）で７％ヒドロキシプロピルセルロー
ス（ＨＰＣ−Ｌ）アルコール溶液を用いてＨＰＣ−Ｌ
が、仕込み全量に対して１質量％になるまで造粒した後
乾燥し、ステアリン酸マグネシウムと硬化油の混合物
（質量比１：２）を組成物全量に対して２質量％になる
ように加え、ロータリー式打錠機（菊水製作所製）を用
い、圧縮成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠
剤を得た。Example 3 385 g of mannitol, 170 g of lactose, 108 g of crystalline cellulose and 36 g of crospovidone were mixed, and the mixture was mixed with a 7% hydroxypropylcellulose (HPC-L) alcohol solution using a fluid bed granulator (Okawara). HPC-L
Was granulated to 1% by mass based on the total amount of the preparation, dried, and a mixture of magnesium stearate and hydrogenated oil (mass ratio 1: 2) was added so as to be 2% by mass based on the total amount of the composition. Using a rotary tableting machine (manufactured by Kikusui Seisakusho), compression molding was performed to obtain a tablet having a mass of 280 mg per tablet and a diameter of 9 mm.
【００２２】実施例４ マンニトール３８５ｇ、乳糖１７０ｇ、結晶セルロース
１０８ｇ、クロスポビドン３６ｇを混合して、流動層造
粒機（大川原社製）で７％ＨＰＣ−Ｌの水／アルコール
（質量比１：１）溶液を用いてＨＰＣ−Ｌが仕込み全量
に対して３質量％になるまで造粒した後乾燥し、ステア
リン酸マグネシウムを組成物全量に対して０.５質量％
になるように加え、ロータリー式打錠機（菊水製作所
製）を用い、圧縮成型し、１錠質量２８０ｍｇ、直径９
ｍｍの錠剤を得た。Example 4 385 g of mannitol, 170 g of lactose, 108 g of crystalline cellulose and 36 g of crospovidone were mixed, and the mixture was mixed with a 7% HPC-L water / alcohol (mass ratio 1: 1) in a fluidized bed granulator (manufactured by Okawara Co., Ltd.). ) Using the solution, HPC-L was granulated until it became 3% by mass based on the total amount, and dried, and magnesium stearate was added to 0.5% by mass based on the total amount of the composition.
In addition, using a rotary tableting machine (manufactured by Kikusui Seisakusho), compression molding was performed, and the weight of one tablet was 280 mg and the diameter was 9
mm tablets were obtained.
【００２３】実施例５ 微粉化したソファルコン（平均粒子径１０μｍ）６０
ｇ、マンニトール３２５ｇ、乳糖１７０ｇ、結晶セルロ
ース１０８ｇ、クロスポビドン３６ｇを混合して、流動
層造粒機（大川原社製）で７％ＨＰＣ−Ｌのアルコール
溶液を用いてＨＰＣ−Ｌが仕込み全量に対して、２質量
％になるまで造粒した後乾燥し、ステアリン酸マグネシ
ウムを組成物全量に対して２質量％になるように加え、
ロータリー式打錠機（菊水製作所製）を用い、圧縮成型
し、１錠質量２８０ｍｇ、直径９ｍｍの錠剤を得た。Example 5 Finely powdered sofalcone (average particle diameter 10 μm) 60
g, 325 g of mannitol, 170 g of lactose, 108 g of crystalline cellulose, and 36 g of crospovidone, and HPC-L was charged with a 7% HPC-L alcohol solution using a fluidized bed granulator (manufactured by Okawara Co.) to the total amount. After granulating to 2% by mass and drying, magnesium stearate is added to 2% by mass based on the total amount of the composition,
Using a rotary tableting machine (manufactured by Kikusui Seisakusho), compression molding was performed to obtain a tablet having a mass of 280 mg per tablet and a diameter of 9 mm.
【００２４】実施例６ マンニトール２７７ｇ、乳糖８１ｇ、トウモロコシデン
プン５９ｇ、部分α化デンプン５９ｇ、結晶セルロース
７２ｇ、クロスカルメロースナトリウム３０ｇを混合し
て、転動流動造粒機（不二パウダル社製）で７％ＨＰＣ
−Ｌの水／アルコール（質量比１：１）溶液を用いてＨ
ＰＣ−Ｌが仕込み全量に対して３質量％になるまで造粒
した後乾燥し、ステアリン酸マグネシウムとステアリン
酸カルシウムの混合物（質量比１：１）を組成物全量に
対して１質量％になるように加え、ロータリー式打錠機
（菊水製作所製）を用い、圧縮成型し、１錠質量２８０
ｍｇ、直径９ｍｍの錠剤を得た。Example 6 277 g of mannitol, 81 g of lactose, 59 g of corn starch, 59 g of partially pregelatinized starch, 72 g of crystalline cellulose, and 30 g of croscarmellose sodium were mixed, and the mixture was mixed with a tumbling fluidized granulator (manufactured by Fuji Paudal). 7% HPC
-H in water / alcohol (1: 1 by weight) solution
After granulating until the PC-L becomes 3% by mass with respect to the total amount of the preparation, drying is performed, and the mixture of magnesium stearate and calcium stearate (mass ratio 1: 1) is adjusted to 1% by mass with respect to the total amount of the composition. In addition, using a rotary tableting machine (manufactured by Kikusui Seisakusho), compression molding was performed, and one tablet weighed 280.
mg and a tablet having a diameter of 9 mm were obtained.
【００２５】実施例７ イブプロフェン４０ｇ、マンニトール２４７ｇ、乳糖７
１ｇ、トウモロコシデンプン５９ｇ、部分α化デンプン
５９ｇ、結晶セルロース７２ｇ、クロスカルメロースナ
トリウム３０ｇを混合して、転動流動造粒機（不二パウ
ダル社製）で７％ＨＰＣ−Ｌの水／アルコール（質量比
１：１）溶液を用いてＨＰＣ−Ｌが仕込み全量に対して
３質量％になるまで造粒した後乾燥し、ステアリン酸マ
グネシウムとステアリン酸カルシウムの混合物（質量比
１：１）を組成物全量に対して０.７５質量％、メント
ールを０.１質量％になるように加え、ロータリー式打
錠機（菊水製作所製）を用い、圧縮成型し、１錠質量２
８０ｍｇ、直径９ｍｍの錠剤を得た。Example 7 40 g of ibuprofen, 247 g of mannitol, lactose 7
1 g, corn starch 59 g, partially pregelatinized starch 59 g, microcrystalline cellulose 72 g, and croscarmellose sodium 30 g were mixed, and the mixture was subjected to a 7% HPC-L water / alcohol (trade name) using a tumbling fluidized granulator (manufactured by Fuji Paudal). Using a solution, HPC-L was granulated using a solution until the amount became 3% by mass with respect to the total amount, and then dried. A mixture of magnesium stearate and calcium stearate (mass ratio 1: 1) was used as a composition. 0.75% by mass and menthol to 0.1% by mass are added to the total amount, and compression molding is performed using a rotary tableting machine (manufactured by Kikusui Seisakusho), and one tablet is weighed 2%.
80 mg tablets having a diameter of 9 mm were obtained.
【００２６】実施例８ 微粉化したソファルコン（平均粒子径１０μｍ）６０
ｇ、マンニトール３２５ｇを混合して、流動層造粒機
（大川原社製）で７％ＨＰＣ−Ｌのアルコール溶液を用
いてＨＰＣ−Ｌが仕込み全量に対して２質量％になるま
で造粒したのち乾燥し、直打用乳糖１７０ｇ、結晶セル
ロース１０８ｇ、クロスポビドン３６ｇを混合し、ステ
アリン酸マグネシウムを組成物全量に対して２質量％を
加え、ロータリー式打錠機（菊水製作所）を用い、圧縮
成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠剤を得
た。Example 8 Finely powdered sofalcone (average particle size 10 μm) 60
g and 325 g of mannitol, and granulated in a fluidized-bed granulator (manufactured by Okawara Co., Ltd.) using an alcohol solution of 7% HPC-L until the amount of HPC-L becomes 2% by mass with respect to the total amount. After drying, 170 g of lactose for direct compression, 108 g of crystalline cellulose and 36 g of crospovidone were mixed, and 2% by mass of magnesium stearate was added to the total amount of the composition, and compression molding was performed using a rotary tableting machine (Kikusui Seisakusho). Then, a tablet having a mass of 280 mg per tablet and a diameter of 9 mm was obtained.
【００２７】実施例９ イブプロフェン４０ｇ、結晶セルロース７２ｇを混合し
て、転動造粒機（不二パルダル社製）で７％７％ＨＰＣ
−Ｌの水／アルコール（質量比１：１）溶液を用いてＨ
ＰＣ−Ｌが仕込み全量の３質量％になるまで造粒したの
ち乾燥し、直打用乳糖７１ｇ、トウモロコシデンプン５
９ｇ、クロスポビドン５９ｇ、マンニトール２７０ｇを
加え、ステアリン酸マグネシウムとステアリン酸カルシ
ウムの混合物（質量比１：１）を組成物全量に対して
０．７５質量％、メントールを０．１質量％になるよう
に加え、ロータリー式打錠機（菊水製作所製）を用い、
圧縮成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠剤を
得た。Example 9 40 g of ibuprofen and 72 g of crystalline cellulose were mixed, and the mixture was subjected to 7% 7% HPC using a tumbling granulator (manufactured by Fuji Pardal).
-H in water / alcohol (1: 1 by weight) solution
PC-L was granulated until it reached 3% by mass of the whole amount, dried, then lactose for direct hitting 71 g, corn starch 5
9 g, crospovidone 59 g and mannitol 270 g were added, and a mixture of magnesium stearate and calcium stearate (mass ratio 1: 1) was adjusted to 0.75 mass% and menthol to 0.1 mass% with respect to the total amount of the composition. In addition, using a rotary tableting machine (manufactured by Kikusui Seisakusho),
By compression molding, a tablet having a mass of 280 mg per tablet and a diameter of 9 mm was obtained.
【００２８】比較例１ 微粉化したソファルコン（平均粒子径１０μｍ）３０
ｇ、マンニトール３３７ｇ、乳糖８１ｇ、トウモロコシ
デンプン１１８ｇ、カルメロース３０ｇを混合して、流
動層造粒機（大川原社製）で水／アルコール（質量比
１：１）溶液を用いて造粒した後乾燥し、ステアリン酸
マグネシウムを組成物全量に対して２質量％になるよう
に加え、ロータリー式打錠機（菊水製作所製）を用い、
圧縮成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠剤を
得た。COMPARATIVE EXAMPLE 1 Pulverized Sofalcon (average particle diameter 10 μm) 30
g, 337 g of mannitol, 81 g of lactose, 118 g of corn starch and 30 g of carmellose, granulated with a fluidized bed granulator (manufactured by Okawara Co.) using a water / alcohol (mass ratio 1: 1) solution, and dried. , Magnesium stearate was added so as to be 2% by mass based on the total amount of the composition, and a rotary tableting machine (manufactured by Kikusui Seisakusho) was used.
By compression molding, a tablet having a mass of 280 mg per tablet and a diameter of 9 mm was obtained.
【００２９】比較例２ 砂糖２７７ｇ、乳糖８１ｇ、結晶セルロース７０ｇ、カ
ルメロースカルシウム３０ｇを混合して、転動流動造粒
機（不二パウダル社製）で水／アルコール（質量比１：
１）溶液を用いて造粒した後乾燥し、ステアリン酸マグ
ネシウムを組成物全量に対して１質量％になるように加
え、ロータリー式打錠機（菊水製作所製）を用い、圧縮
成型し、１錠質量２８０ｍｇ、直径９ｍｍの錠剤を得
た。Comparative Example 2 277 g of sugar, 81 g of lactose, 70 g of crystalline cellulose, and 30 g of carmellose calcium were mixed, and the mixture was mixed with water / alcohol (mass ratio 1: 1) using a tumbling fluidized granulator (manufactured by Fuji Paudal).
1) Granulation using a solution, followed by drying. Magnesium stearate was added in an amount of 1% by mass based on the total amount of the composition, and compression molding was performed using a rotary tableting machine (manufactured by Kikusui Seisakusho). A tablet having a tablet mass of 280 mg and a diameter of 9 mm was obtained.
【００３０】比較例３ キシリトール３５５ｇ、トウモロコシデンプン８１ｇ、
結晶セルロース７０ｇ、クロスポビドン２６ｇ、軽質無
水ケイ酸２４ｇを混合して、流動層造粒機（大川原社
製）で水／アルコール（質量比１：１）溶液を用いて造
粒した後乾燥し、ステアリン酸カルシウムを組成物全量
に対して１質量％になるように加え、ロータリー式打錠
機（菊水製作所製）を用い、圧縮成型し、１錠質量２８
０ｍｇ、直径９ｍｍの錠剤を得た。Comparative Example 3 355 g of xylitol, 81 g of corn starch,
70 g of crystalline cellulose, 26 g of crospovidone, and 24 g of light anhydrous silicic acid were mixed, granulated with a fluidized bed granulator (manufactured by Okawara Co., Ltd.) using a water / alcohol (mass ratio 1: 1) solution, and dried. Calcium stearate was added in an amount of 1% by mass based on the total amount of the composition, and the mixture was compression-molded using a rotary tableting machine (manufactured by Kikusui Seisakusho), and the mass of one tablet was 28%.
0 mg tablets having a diameter of 9 mm were obtained.
【００３１】試験例 実施例及び比較例で得られた口腔内崩壊性組成物につい
て下記の試験を行った。 １.硬度試験 錠剤硬度計（シュロイニゲル社製）を用いて測定した。
測定は３〜５回行い、その平均値を算出した。 ２.口腔内崩壊試験 健康な成人男子の口腔内に組成物を水なし（水分を口に
含まず）で含ませ、組成物が口腔内の唾液のみで完全に
崩壊、分散するまでの時間を測定した。Test Examples The following tests were carried out on the orally disintegrating compositions obtained in Examples and Comparative Examples. 1. Hardness test The hardness was measured using a tablet hardness tester (Schleunigel).
The measurement was performed three to five times, and the average value was calculated. 2. Oral disintegration test The composition of a healthy adult male is contained in the oral cavity without water (water is not contained in the mouth), and the time required for the composition to completely disintegrate and disperse with only saliva in the oral cavity is measured. It was measured.
【００３２】試験結果 結果を表１に示した。表１から実施例１〜９の組成物
は、いずれも圧縮成型時の障害（杵、臼への付着や、き
しみ）がなく良好に圧縮成型できた。また、口腔内崩壊
試験での崩壊時間はいずれも、６０秒以内であった。ま
た、硬度は３０Ｎ以上であった。一方、比較例において
は、比較例１は、圧縮成型時に充分な機械的な強度が得
られなかった。比較例２は、圧縮成型時の障害は認めら
れなかったが、口腔内崩壊試験において６０秒を越えて
も崩壊しなかった。比較例３は、圧縮成型できなかっ
た。Test Results The results are shown in Table 1. From Table 1, all of the compositions of Examples 1 to 9 were able to be favorably compression-molded without any obstacles (attachment to punches and dies, creaking) during compression molding. The disintegration time in the oral disintegration test was all within 60 seconds. The hardness was 30 N or more. On the other hand, in Comparative Example 1, Comparative Example 1 did not have sufficient mechanical strength during compression molding. In Comparative Example 2, no failure was observed at the time of compression molding, but in the oral disintegration test, it did not disintegrate even after more than 60 seconds. In Comparative Example 3, compression molding could not be performed.
【００３３】[0033]
【表１】試験結果 [Table 1] Test results
Claims (7)
沢剤、並びにデンプン類及び乳糖の少なくとも１種を含
有する口腔内で速やかに崩壊し、実用上十分な強度を有
する口腔内崩壊性組成物。An orally disintegrating composition containing mannitol, a disintegrant, a cellulose, a lubricant, and at least one of starch and lactose, which disintegrates rapidly in the oral cavity and has practically sufficient strength. .
腔内崩壊性組成物。2. The orally disintegrating composition according to claim 1, further comprising a binder.
ロースナトリウムである請求項１又は２記載の口腔内崩
壊性組成物。3. The orally disintegrating composition according to claim 1, wherein the disintegrant is crospovidone or croscarmellose sodium.
０：１〜１：１である請求項１〜３のいずれか記載の口
腔内崩壊性組成物。4. The method of claim 1, wherein the weight ratio of mannitol to starch is 1
The orally disintegrating composition according to any one of claims 1 to 3, which is 0: 1 to 1: 1.
１：１０である請求項１〜３のいずれか記載の口腔内崩
壊性組成物。5. The mass ratio of mannitol to lactose is 10: 1 to 1.
The orally disintegrating composition according to any one of claims 1 to 3, wherein the composition is 1:10.
か記載の口腔内崩壊性組成物。6. The orally disintegrating composition according to claim 1, which comprises an active ingredient.
記載の口腔内崩壊性組成物の製造方法。7. The method for producing an orally disintegratable composition according to claim 1, which is compression-molded.
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| JP11-12081 | 1999-01-20 | ||
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