JP2001072578A - Tablet quickly disintegrable in oral cavity - Google Patents
Tablet quickly disintegrable in oral cavityInfo
- Publication number
- JP2001072578A JP2001072578A JP2000187822A JP2000187822A JP2001072578A JP 2001072578 A JP2001072578 A JP 2001072578A JP 2000187822 A JP2000187822 A JP 2000187822A JP 2000187822 A JP2000187822 A JP 2000187822A JP 2001072578 A JP2001072578 A JP 2001072578A
- Authority
- JP
- Japan
- Prior art keywords
- bitterness
- rapidly disintegrating
- disintegrating tablet
- essential oil
- lyso
- 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.)
- Granted
Links
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は苦味が低減された口
腔内速崩壊錠に関し、更に詳細には、苦味低減成分を配
合することで、苦味を有する医薬成分を被覆することな
く配合することができる口腔内速崩壊錠に関する。[0001] The present invention relates to a rapidly disintegrating tablet in the oral cavity with reduced bitterness, and more particularly, to blend a bitterness reducing component without coating a pharmaceutical component having bitterness. To a rapidly disintegrating tablet in the mouth.
【０００２】[0002]
【従来の技術】近年、患者のＱＯＬ（Quality of lif
e）向上のため嚥下能力の低い高齢者や小児にとって服
用しやすい剤形として、口腔内速崩壊錠が注目されてい
る。しかし、苦味を有する医薬成分を口腔内速崩壊錠に
配合した場合には、錠剤が口腔内で直ちに崩壊するため
に苦味を有する医薬成分が口腔内に暴露されてしまう。
しかもこの際、水無しで服用されることから一般の内服
錠よりも苦味を長時間に亘って強く感じることになり、
服用し易いことが特徴である口腔内速崩壊錠の大きなデ
メリットとなっている。上記の問題を解決するため、口
腔内速崩壊錠に配合される苦味を有する医薬成分を、エ
チルセルロース、オイドラギット等の高分子で被覆し、
錠剤が口腔内で崩壊しても該医薬成分が直接暴露されな
いようにする方法（特表平６−５０２１９４号公報）が
提案されている。しかし、上記方法において、水系のコ
ーティング剤で苦味を有する医薬成分を被覆しても、そ
の膜の強度が弱いため充分な被覆効果が得られない。こ
れに対して有機溶剤でのコーティングは充分な被覆効果
が得られるが、被覆物の残留溶媒や製造時の作業環境、
例えば作業者の有機溶媒の吸入、作業時の発火及び爆発
の危険性等が問題となる。また、これらの被覆には長時
間の作業と設備を要するというデメリットもある。更
に、苦味を充分に抑制し打錠時の膜の破損を防止するた
めに被覆層を厚くすると医薬成分の溶出が遅延し、例え
ば溶出試験において、６０分後でもわずかに３０％程度
しか医薬成分が溶出しない製剤となってしまう。2. Description of the Related Art In recent years, the quality of life (QOL) of patients has been increasing.
e) Oral quick disintegrating tablets are attracting attention as a dosage form that can be easily taken by elderly people and children with low swallowing ability for improvement. However, when a pharmaceutical ingredient having a bitter taste is incorporated into a rapidly disintegrating tablet in the oral cavity, the tablet immediately disintegrates in the oral cavity, so that the pharmaceutical ingredient having a bitter taste is exposed in the oral cavity.
In addition, at this time, since it is taken without water, the bitter taste will be felt more strongly for a long time than ordinary internal tablets,
This is a major disadvantage of a rapidly disintegrating tablet in the oral cavity, which is characterized by being easy to take. In order to solve the above-mentioned problems, a pharmaceutical ingredient having a bitter taste to be blended into an orally rapidly disintegrating tablet is coated with a polymer such as ethyl cellulose and Eudragit,
A method has been proposed in which the pharmaceutical component is not directly exposed even if the tablet disintegrates in the oral cavity (Japanese Patent Publication No. Hei 6-502194). However, in the above method, even if the pharmaceutical component having a bitter taste is coated with an aqueous coating agent, a sufficient coating effect cannot be obtained because the strength of the film is weak. On the other hand, coating with an organic solvent can provide a sufficient coating effect, but the residual solvent of the coating and the working environment during production,
For example, inhalation of the organic solvent by a worker, danger of ignition and explosion at the time of work, and the like become problems. In addition, these coatings have the disadvantage of requiring a long operation and equipment. Furthermore, when the coating layer is thickened to sufficiently suppress bitterness and prevent breakage of the film at the time of tableting, the dissolution of the pharmaceutical component is delayed. Will not elute.
【０００３】一方、顆粒剤、散剤、液剤等の分野におい
ても、従来から苦味を低減する技術が開発されている。
例えば、苦味を低減するために、いわゆる高甘味度甘味
剤に分類されるステビア（特開平１０−１０１５８２号
公報）或いはアスパルテーム（特開平２−５６４１６号
公報）を配合するもの、香料と甘味剤とを組合せて配合
するもの（例えば、特開平１０−２７３４３５号公
報）、糖アルコールと高甘味度甘味剤の一つであるソー
マチンを配合するもの（例えば、特開平１０−３０６０
３８号公報）、糖アルコールによるもの（例えば、特開
平１０−５３５３８号公報）、精油または精油成分によ
るもの（例えば、特開平５−２５５１２６号公報）、酸
性リン脂質によるもの（例えば、特開昭６２−２６５２
３４号公報、特開平８−９８９７号公報、特開平７−６
７５５２号公報等）など、多数の提案がなされている。
しかし、これらはあくまでも水と共に服用されることを
前提とした一般的な製剤における苦味低減の技術であ
り、水無しで服用されることを予定する口腔内速崩壊錠
にこれらの技術をそのまま適用しても、その苦味の低減
効果が十分ではなく、実用的な口腔内速崩壊錠を得るこ
とができなかった。On the other hand, in the fields of granules, powders, liquids and the like, techniques for reducing bitterness have been developed.
For example, in order to reduce bitterness, those containing stevia (Japanese Patent Application Laid-Open No. 10-101582) or aspartame (Japanese Patent Application Laid-Open No. 2-56416) classified as so-called high-intensity sweeteners, flavors and sweeteners (For example, JP-A-10-273435) and a combination of a sugar alcohol and thaumatin which is one of high-intensity sweeteners (for example, JP-A-10-3060).
No. 38), those based on sugar alcohols (for example, JP-A-10-53538), those based on essential oils or essential oil components (for example, JP-A-5-255126), those based on acidic phospholipids (e.g. 62-2652
No. 34, JP-A-8-9897, JP-A-7-6
Numerous proposals have been made.
However, these are techniques for reducing bitterness in general preparations on the premise that they are taken together with water, and these techniques are directly applied to intraorally rapidly disintegrating tablets that are scheduled to be taken without water. However, the effect of reducing bitterness was not sufficient, and a rapidly disintegrating tablet in the oral cavity could not be obtained.
【０００４】[0004]
【発明が解決しようとする課題】本発明は、以上のよう
に、苦味を有する医薬成分を被覆することなく、水無し
で服用してもその苦味を殆ど感じずに容易に服用できる
口腔内速崩壊錠を提供することを課題とする。SUMMARY OF THE INVENTION As described above, the present invention relates to an intraoral speed which can be easily taken without coating a pharmaceutical ingredient having a bitter taste and without feeling the bitter taste even when taken without water. It is an object to provide a disintegrating tablet.
【０００５】[0005]
【課題を解決するための手段】上記課題を解決するため
鋭意検討した結果、本発明者らは、従来から苦味を低減
することが知られている精油と、高甘味度甘味剤および
／または酸性リン脂質またはそのリゾ体の組合せが、特
異的に顕著な苦味低減効果を発揮することを見出し、か
かる知見に基づいて本発明を完成するに至った。As a result of diligent studies to solve the above-mentioned problems, the present inventors have found that essential oils which have been known to reduce bitterness, high-potency sweeteners and / or acidic sweeteners The present inventors have found that a combination of a phospholipid or a lyso form thereof specifically exhibits a remarkable bitterness reducing effect, and have completed the present invention based on such findings.
【０００６】即ち、本発明は、（１）苦味を有する医薬
成分と、精油並びに高甘味度甘味剤および／または酸性
リン脂質若しくはそのリゾ体からなる苦味低減成分とを
含有することを特徴とする口腔内速崩壊錠、（２）苦味
低減成分が精油および高甘味度甘味剤からなる上記
（１）に記載の口腔内速崩壊錠、（３）苦味低減成分が
精油および酸性リン脂質若しくはそのリゾ体からなる上
記（１）に記載の口腔内速崩壊錠、（４）苦味低減成分
が精油、高甘味度甘味剤および酸性リン脂質若しくはそ
のリゾ体からなる上記（１）に記載の口腔内速崩壊錠、
（５）苦味を有する医薬成分が被覆されていないことを
特徴とする上記（１）に記載の口腔内速崩壊錠、（６）
苦味を有する医薬成分がアセトアミノフェンである、上
記（１）に記載の口腔内速崩壊錠、（７）精油がハッカ
油である上記（１）に記載の口腔内速崩壊錠、（８）高
甘味度甘味剤がステビア、アスパルテームから選択され
る一又は二である上記（１）に記載の口腔内速崩壊錠、
および（９）酸性リン脂質またはそのリゾ体が大豆レシ
チンである上記（１）に記載の口腔内速崩壊錠を提供す
るものである。That is, the present invention is characterized by comprising (1) a pharmaceutical ingredient having a bitter taste, and an essential oil and a bitterness reducing ingredient comprising a high-intensity sweetener and / or an acidic phospholipid or a lyso-form thereof. An orally rapidly disintegrating tablet, (2) an orally rapidly disintegrating tablet according to the above (1), wherein the bitterness reducing component comprises an essential oil and a high-intensity sweetener, and (3) an essential oil and an acidic phospholipid or a lysozoate thereof. (1) the intraoral rapid disintegrating tablet according to the above (1), (4) the intraoral rapid dissolving tablet according to the above (1), wherein the bitterness-reducing component comprises an essential oil, a high-intensity sweetener and an acidic phospholipid or a lyso-form thereof. Disintegrating tablets,
(5) The orally rapidly disintegrating tablet according to the above (1), wherein the pharmaceutical ingredient having a bitter taste is not coated.
(8) the orally rapidly disintegrating tablet according to (1), wherein the pharmaceutical ingredient having bitterness is acetaminophen, (7) the essential oil is peppermint oil, The orally rapidly disintegrating tablet according to the above (1), wherein the high-sweetness sweetener is one or two selected from stevia and aspartame,
And (9) The intraoral rapidly disintegrating tablet according to the above (1), wherein the acidic phospholipid or its lyso form is soy lecithin.
【０００７】[0007]
【発明の実施の形態】以下に本願発明について詳細に説
明するが、本願明細書において口腔内速崩壊錠とは、口
腔内で唾液の存在下、咀嚼無しに約９０秒、好ましくは
約６０秒より短い時間で崩壊する固形医薬製剤をいう。BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, the present invention will be described in detail. In the specification of the present application, a rapidly disintegrating tablet in the oral cavity means, for about 90 seconds, preferably about 60 seconds without chewing in the presence of saliva in the oral cavity. A solid pharmaceutical formulation that disintegrates in a shorter time.
【０００８】本発明で用いられる苦味を有する医薬成分
としては、一般に経口的に投与される医薬成分の中で苦
味を有するものが挙げられる。とりわけ、水を飲むこと
のできない状況下で服用せざるを得ないことが想定され
る頓用の医薬成分、例えば、解熱鎮痛薬、抗ヒスタミン
剤、抗アレルギー剤、交感神経興奮剤、副交感神経遮断
剤、中枢興奮薬、Ｈ2ブロッカー、制酸剤、消炎酵素
剤、抗炎症剤、気管支拡張剤、抗菌剤、鎮咳剤、去痰
剤、抗コリン剤、止しゃ剤、催眠鎮静薬、利胆薬、血圧
降下剤、骨格筋弛緩薬、乗り物酔い予防・治療薬等、あ
るいは日常的に簡便に服用できることが期待される骨粗
しょう症治療薬、ビタミン類、生薬類などの中で苦味を
有するものが好ましく、例えば、アセトアミノフェン、
イブプロフェン、ケトプロフェン等の解熱鎮痛剤；マレ
イン酸クロルフェニラミン、ｄ-マレイン酸クロルフェ
ニラミン、ジフェンヒドラミンまたはその塩類、塩酸プ
ロメタジン、塩酸イソチペンジル、フマル酸クレマスチ
ン、塩酸イプロヘプチン、塩酸シプロヘプタジン、ジフ
ェニルピラリンまたはその塩類、マレイン酸ジメチンデ
ン、塩酸トリプロリジン、塩酸ホモクロルシクリジン、
塩酸アゼラスチン、イブジラスト、クロモグリク酸ナト
リウムまたはその塩類、オキサトミド、アンレキサノク
ス、マレイン酸カルビノキサミン、メキタジン、トラニ
ラスト、レピリナスト、フマル酸エメダスチン、塩酸オ
ザグレル、タザノラスト、ペミロラストまたはその塩
類、トシル酸スプラタスト等の抗ヒスタミン剤、抗アレ
ルギー剤；塩酸フェニルプロパノールアミン等の交感神
経興奮剤；ベラドンナ（総）アルカロイド、ヨウ化イソ
プロパミド等の副交感神経遮断剤；カフェイン、無水カ
フェイン等の中枢興奮薬；ファモチジン、シメチジン、
塩酸ラニチジン、ニザチジン、塩酸ロキサチジンアセタ
ート等のＨ2ブロッカー；炭酸マグネシウム、軽質無水
ケイ酸、メタケイ酸アルミン酸マグネシウム、合成ヒド
ロタルサイト等の制酸剤；塩化リゾチーム、セラペプタ
ーゼ等の消炎酵素剤；トラネキサム酸等の抗炎症剤；塩
酸メチルエフェドリン(d体,dl体を含む)、塩酸エフェド
リン等の気管支拡張剤；コデイン、リン酸コデイン、リ
ン酸ジヒドロコデイン、臭化水素酸デキストロメトルフ
ァン、ノスカピン、ジメモルファン、グアヤコールスル
ホン酸、グアイフェネシン等の鎮咳剤；グアヤコールス
ルホン酸カリウム、塩酸ブロムヘキシン等の去痰剤；ウ
ルソデオキシコール酸、ケノデオキシコール酸等の利胆
薬；塩酸ロペラミド等の止しゃ剤；ブロムワレリル尿素
等の催眠鎮静剤；ジアゼパム等の抗不安剤；ジメンヒド
リナート等の乗り物酔い予防・治療薬；塩酸チアミン、
硝酸チアミン、硝酸ビスチアミン、チアミンジスルフィ
ド、チアミンジセチル硫酸エステル塩、塩酸ジセチアミ
ン、フルスルチアミン、塩酸フルスルチアミン、オクト
チアミン、シコチアミン、ビスイブチアミン、ビスベン
チアミン、プロスルチアミン、ベンフォチアミン、ジベ
ンゾイルチアミン、チアミンピロリン酸等のビタミンＢ
1類；リン酸リボフラビンナトリウム等のビタミンＢ
2類；塩酸ピリドキシン等のビタミンＢ6類；パントテン
酸カルシウム；フィトナジオン、メナテトレノン等のビ
タミンＫ類；オウゴン、オウバクなどの生薬末及びその
エキスなどが挙げられる。[0008] The bitter medicinal ingredients used in the present invention include those that have a bitter taste among the medicinal ingredients generally administered orally. Above all, as-needed pharmaceutical ingredients that are supposed to be taken under the condition that you cannot drink water, for example, antipyretic analgesics, antihistamines, antiallergic agents, sympathetic stimulants, parasympathetic blockers, central stimulant, H 2 blockers, antacids, anti-inflammatory enzyme agents, anti-inflammatory agents, bronchodilators, anti-microbial agents, antitussives, expectorants, anticholinergic agents, if antidiarrheal agents, hypnotic sedatives, cholagogues, antihypertensive agents , Skeletal muscle relaxants, motion sickness prevention and treatment drugs, or osteoporosis treatment drugs expected to be able to be taken easily and easily on a daily basis, vitamins, those having a bitter taste among crude drugs are preferable, for example, Acetaminophen,
Antipyretic analgesics such as ibuprofen and ketoprofen; chlorpheniramine maleate, d-chlorpheniramine maleate, diphenhydramine or salts thereof, promethazine hydrochloride, isotipendyl hydrochloride, clemastine fumarate, iproheptin hydrochloride, cyproheptadine hydrochloride, diphenylpyraline or salts thereof, Dimethindene maleate, triprolidine hydrochloride, homochlorcyclidine hydrochloride,
Azelastine hydrochloride, ibudilast, sodium cromoglicate or salts thereof, oxatomide, amlexanox, carbinoxamine maleate, mequitazine, tranilast, repirinast, emedastin fumarate, ozagrel hydrochloride, tazanolast, pemirolast or salts thereof, anti-allergic agents such as anti-allergic agents such as suplatast tosilate, etc. Sympathomimetics such as phenylpropanolamine hydrochloride; parasympathomimetics such as belladonna (total) alkaloids and isopropamide iodide; central stimulants such as caffeine and anhydrous caffeine; famotidine, cimetidine;
Ranitidine hydrochloride, nizatidine, H 2 blockers such as hydrochloric acid roxatidine acetate; magnesium carbonate, light anhydrous silicic acid, magnesium aluminometasilicate, antacids such as synthetic hydrotalcite; lysozyme chloride, anti-inflammatory enzyme agents such as serrapeptase Anti-inflammatory agents such as tranexamic acid; bronchodilators such as methylephedrine hydrochloride (including d- and dl-forms) and ephedrine hydrochloride; codeine, codeine phosphate, dihydrocodeine phosphate, dextromethorphan hydrobromide, noscapine, Antitussives such as dimemorphan, guaiacolsulfonic acid and guaifenesin; expectorants such as potassium guaiacolsulfonic acid and bromhexine hydrochloride; bile drugs such as ursodeoxycholic acid and chenodeoxycholic acid; antiseptic agents such as loperamide hydrochloride; hypnotics such as bromvaleryl urea. ; Anti-anxiety agents such as Zepamu; motion sickness prophylactic or therapeutic drug, such as dimenhydrinate; thiamine hydrochloride,
Thiamine nitrate, bisthiamine nitrate, thiamine disulfide, thiamine dicetyl sulfate, dicetiamine hydrochloride, fursultiamine, fursultiamine hydrochloride, octiamine, shicotiamine, bisibutiamine, bisbenthamine, prosultiamine, benfotiamine, diamine Vitamin B such as benzoylthiamine and thiamine pyrophosphate
Class 1 ; Vitamin B such as sodium riboflavin phosphate
Class 2; vitamin B 6 such as pyridoxine hydrochloride; calcium pantothenate; phytonadione, vitamin K, such as menatetrenone; Scutellaria, like crude drugs powder and extract such as Phellodendron bark.
【０００９】本発明の口腔内速崩壊錠で、苦味の低減効
果が特に顕著に現れる医薬成分としてはアセトアミノフ
ェン、トラネキサム酸、ノスカピンおよび塩酸ブロムヘ
キシンを挙げることができる。苦味を有する医薬成分と
してアセトアミノフェンを用いる際は、その結晶粒子径
が約５０〜約８００μｍ、好ましくは約１００〜５００
μｍの範囲にあるものを選択することができる。アセト
アミノフェンの結晶粒子径が上記の範囲にある場合、特
に苦味の低減効果が著しい。これらの苦味を有する医薬
成分の配合量に特に制限はなく、その投与目的に応じて
適宜選択することができるが、一般には製剤１００重量
部に対して約０．０１〜８０重量部、好ましくは約０．
０５〜７０重量部、特に好ましくは約０．１〜６０重量
部の範囲とすることができる。[0009] Pharmaceutical ingredients which show a particularly remarkable effect of reducing bitterness in the orally rapidly disintegrating tablet of the present invention include acetaminophen, tranexamic acid, noscapine and bromhexine hydrochloride. When acetaminophen is used as a pharmaceutical ingredient having a bitter taste, its crystal particle size is about 50 to about 800 μm, preferably about 100 to 500 μm.
Those in the range of μm can be selected. When the crystal particle diameter of acetaminophen is in the above range, the effect of reducing bitterness is particularly remarkable. There is no particular limitation on the amount of the pharmaceutical ingredient having such a bitter taste, which can be appropriately selected depending on the purpose of administration. Generally, about 0.01 to 80 parts by weight, preferably about 100 parts by weight of the preparation, preferably About 0.
It can range from 0.5 to 70 parts by weight, particularly preferably from about 0.1 to 60 parts by weight.
【００１０】本発明の口腔内速崩壊錠には、苦味低減成
分として精油並びに高甘味度甘味剤および／または酸性
リン脂質若しくはそのリゾ体が配合される。本発明で使
用することのできる精油としては、ハッカ油、ユーカリ
油、ケイヒ油、ウイキョウ油、チョウジ油、オレンジ
油、レモン油、ローズ油が挙げられ、好ましくはハッカ
油、ケイヒ油、ウイキョウ油、チョウジ油であり、特に
好ましくはハッカ油である。これら精油の配合量は、苦
味を有する医薬成分の配合量やその苦味の強さの程度、
併せて配合される高甘味度甘味剤や酸性リン脂質若しく
はそのリゾ体の配合量によって適宜選択することができ
るが、一般には、製剤１００重量部に対して約０．０１
〜１０重量部、好ましくは約０．０２〜８重量部、特に
好ましくは約０．０５〜５重量部の範囲とすることがで
きる。The orally rapidly disintegrating tablet of the present invention contains an essential oil and a high-intensity sweetener and / or an acidic phospholipid or a lyso-form thereof as a bitterness reducing component. The essential oils that can be used in the present invention include mint oil, eucalyptus oil, cinnamon oil, fennel oil, clove oil, orange oil, lemon oil, rose oil, preferably mint oil, cinnamon oil, fennel oil, Clove oil, particularly preferably mint oil. The amount of these essential oils depends on the amount of the pharmaceutical ingredient having bitterness and the degree of the bitterness,
It can be appropriately selected depending on the amount of the high-intensity sweetener and the acidic phospholipid or the lyso form thereof to be added together, but generally about 0.01 part by weight per 100 parts by weight of the preparation.
It can range from 10 to 10 parts by weight, preferably from about 0.02 to 8 parts by weight, particularly preferably from about 0.05 to 5 parts by weight.
【００１１】本発明で用いられるいわゆる高甘味度甘味
剤は、人工的に合成された甘味剤のうち、その甘味度が
砂糖の数倍以上のもの、好ましくは約１００倍以上のも
のをいい、具体的にはアスパルテーム、ステビア、サッ
カリン、グリチルリチン二カリウム、ソーマチン、スク
ラロース、アセスルファームＫ等が挙げられるが、アス
パルテーム、ステビア等が特に好ましい。これらの高甘
味度甘味剤の配合量は、苦味を有する医薬成分の配合量
やその苦味の強さの程度、併せて配合される精油や酸性
リン脂質若しくはそのリゾ体の配合量によって適宜選択
することができるが、一般には、製剤１００重量部に対
して約０．０１〜２０重量部、好ましくは約０．０５〜
１５重量部、特に好ましくは約０．１〜１０重量部の範
囲とすることができる。The so-called high-intensity sweetener used in the present invention refers to an artificially synthesized sweetener whose sweetness is several times or more, preferably about 100 times or more that of sugar. Specific examples include aspartame, stevia, saccharin, dipotassium glycyrrhizin, thaumatin, sucralose, acesulfame K, and the like, with aspartame and stevia being particularly preferred. The compounding amount of these high-sweetness sweeteners is appropriately selected depending on the compounding amount of the pharmaceutical ingredient having a bitter taste, the degree of the bitterness thereof, and the compounding amount of the essential oil, the acidic phospholipid, or the lyso-form thereof in combination. In general, about 0.01 to 20 parts by weight, and preferably about 0.05 to
It can range from 15 parts by weight, particularly preferably from about 0.1 to 10 parts by weight.
【００１２】本発明で用いられる酸性リン脂質またはそ
のリゾ体は、それ自体苦味低減化作用を有することが知
られており（特開平７-６７５５２号公報）、ホスファ
チジルセリン、ホスファチジン酸、ホスファチジルイノ
シトール、ホスファチジルグリセロール、カルジオリピ
ン等の酸性リン脂質並びにリゾホスファチジルセリン、
リゾホスファチジン酸、リゾホスファチジルイノシトー
ル、リゾホスファチジルグリセロール等のリゾ体であ
る。これらの酸性リン脂質またはそのリゾ体は、大豆レ
シチン、卵黄レシチン等として、各種の動植物から、特
開平８-９８９６号公報に記載の方法に準じて抽出、分
離することにより得ることができる。また、本発明で用
いられる酸性リン脂質またはそのリゾ体としては、例え
ばベネコ−トBMI-60（商品名、花王）として市販されて
いるものを用いることもできる。この酸性リン脂質また
はそのリゾ体の配合量は、苦味を有する医薬成分の配合
量やその苦味の程度、併せて配合される精油や高甘味度
甘味剤の配合量によって適宜選択することができるが、
一般には、製剤１００重量部に対して約０．０１〜２０
重量部、好ましくは約０．０５〜１５重量部、特に好ま
しくは約０．１〜１０重量部の範囲とすることができ
る。It is known that the acidic phospholipid or lyso form thereof used in the present invention has a bitterness reducing action by itself (JP-A-7-67552), and phosphatidylserine, phosphatidic acid, phosphatidylinositol, Phosphatidylglycerol, acid phospholipids such as cardiolipin and lysophosphatidylserine,
It is a lyso-form such as lysophosphatidic acid, lysophosphatidylinositol and lysophosphatidylglycerol. These acidic phospholipids or lyso forms thereof can be obtained by extracting and separating soybean lecithin, egg yolk lecithin and the like from various animals and plants according to the method described in JP-A-8-9896. Further, as the acidic phospholipid or lyso form thereof used in the present invention, for example, those commercially available as VENCOOTE BMI-60 (trade name, Kao) can also be used. The amount of the acidic phospholipid or its lyso form can be appropriately selected depending on the amount of the pharmaceutical ingredient having bitterness, the degree of the bitterness, and the amount of the essential oil or high-intensity sweetener to be added together. ,
Generally, about 0.01 to 20 parts by weight per 100 parts by weight of the preparation.
It can range from about 0.05 to 15 parts by weight, particularly preferably from about 0.1 to 10 parts by weight.
【００１３】本発明の口腔内速崩壊錠は、上記した本発
明の必須構成成分である苦味を有する医薬成分、精油並
びに高甘味度甘味剤および／または酸性リン脂質若しく
はそのリゾ体を配合する点を除き、一般に口腔内速崩壊
錠を製造する方法で製造することができ、具体的には例
えば特開平１０−１８２４３６号公報に記載される方
法、即ち上記本発明の必須構成成分に加えてエリスリト
ール、結晶セルロースおよび崩壊剤を配合する方法に従
って製造することができる（以下の実施例１〜５を参
照）。また、本発明の口腔内速崩壊錠には、その発明の
効果に支障のない限り、一般の固形製剤の製造に用いら
れる種々の添加剤を配合することもできる。The orally rapidly disintegrating tablet of the present invention comprises the above-mentioned essential components of the present invention, a pharmaceutical ingredient having a bitter taste, an essential oil, a high-intensity sweetener and / or an acidic phospholipid or a lyso-form thereof. Can be produced by a method for producing a rapidly disintegrating tablet in the mouth, specifically, for example, a method described in JP-A-10-182436, that is, erythritol in addition to the above essential components of the present invention. , Microcrystalline cellulose and a disintegrant (see Examples 1 to 5 below). Further, the rapidly disintegrating buccal tablet of the present invention can also contain various additives used in the production of general solid preparations, as long as the effects of the present invention are not hindered.
【００１４】本発明の口腔内速崩壊錠に精油、高甘味度
甘味剤および／または酸性リン脂質若しくはそのリゾ体
を同時に配合する場合には、その錠剤の硬度低下を防ぐ
ために多孔性ケイ酸カルシウムを配合することもでき
る。この場合の多孔性ケイ酸カルシウムの配合量は、本
発明の口腔内速崩壊錠１００重量部に対して約０．５〜
３０重量部の範囲で配合することが好ましい。ここで用
いられる多孔性ケイ酸カルシウムは、フローライトＲＥ
（商品名、徳山曹達）として市販のものを容易に入手す
ることができる。When essential oil, a high-intensity sweetener and / or an acidic phospholipid or its lyso-form is simultaneously added to the orally rapidly disintegrating tablet of the present invention, porous calcium silicate is used to prevent the tablet from decreasing in hardness. Can also be blended. The amount of the porous calcium silicate in this case is about 0.5 to about 100 parts by weight of the orally rapidly disintegrating tablet of the present invention.
It is preferable to mix in a range of 30 parts by weight. The porous calcium silicate used here is FLORITE RE
(Commercial name, Soda Tokuyama) can be easily obtained from the market.
【００１５】本発明で配合される精油（例えば、ハッカ
油）は、未包装形態で放置すると、保存期間中に揮発し
ていまう。精油（例えば、ハッカ油）の量が少なくなる
と、本発明の苦味マスキング効果は減少し、苦味を感じ
るようになる。また、本発明の錠剤は、高湿度下にさら
されて保存されると、吸湿硬度低下を起こす。そこで、
本発明の口腔内速崩壊錠の包装形態は、ストリップ包
装、ブリスター包装、瓶包装などの気密容器が好まし
く、とりわけ気密性の高いアルミストリップ包装やブリ
スター包装を内袋（例えば、アルミニウム箔、ポリエチ
レンフィルム）に入れた包装が特に好ましい。The essential oil (eg, peppermint oil) formulated in the present invention volatilizes during the storage period when left unpackaged. As the amount of essential oil (eg, peppermint oil) is reduced, the bitter masking effect of the present invention is reduced and the bitter taste is felt. Moreover, the tablet of the present invention causes a decrease in moisture absorption hardness when stored under high humidity. Therefore,
The packaging form of the orally rapidly disintegrating tablet of the present invention is preferably an airtight container such as a strip package, a blister package, and a bottle package. Particularly, a highly airtight aluminum strip package or a blister package is preferably used in an inner bag (for example, aluminum foil, polyethylene film). )) Are especially preferred.
【００１６】[0016]
【実施例】以下に、本発明の実施例、比較例および比較
試験を挙げて、更に具体的に本発明を説明する。 実施例１：精油＋高甘味度甘味剤＋大豆レシチン＋多孔
性ケイ酸カルシウム エリスリトール３０ｇ、結晶セルロース（セオラスＫＧ
８０１）８．４１ｇ、クロスポビドン２．４５ｇ、大豆
レシチン（ベネコ−トＢＭＩ−６０）１．０ｇ、多孔性
ケイ酸カルシウム（フローライトＲＥ）２ｇ、ステビア
０．２５ｇ、アスパルテーム０．５ｇを乳鉢にとり、薄
荷油１００μｌを添加して、乳棒で展延させる。得られ
た粉末にアセトアミノフェン１５ｇとステアリン酸マグ
ネシウム０．３ｇを混合し、１３ｍｍの臼と平面の杵を
用い、打錠圧１４００ｋｇ／杵でオートグラフ（ＡＧ−
５０００Ｂ、島津製作所）にて、錠剤重量６００ｍｇで
製錠した。EXAMPLES The present invention will be described more specifically with reference to examples, comparative examples and comparative tests of the present invention. Example 1: Essential oil + high-intensity sweetener + soy lecithin + porous calcium silicate 30 g erythritol, crystalline cellulose (Seolas KG
801) 8.41 g, crospovidone 2.45 g, soy lecithin (Benecote BMI-60) 1.0 g, porous calcium silicate (Fluorite RE) 2 g, stevia 0.25 g, and aspartame 0.5 g in a mortar. Add 100 μl of light oil and spread with pestle. 15 g of acetaminophen and 0.3 g of magnesium stearate were mixed with the obtained powder, and an autograph (AG-
5000B, Shimadzu Corporation) at a tablet weight of 600 mg.
【００１７】実施例２：精油＋高甘味度甘味剤＋大豆レ
シチン エリスリトール３０ｇ、結晶セルロース（セオラスＫＧ
８０１）９．９１ｇ、クロスポビドン２．４５ｇ、大豆
レシチン（ベネコ−トＢＭＩ−６０）１．５ｇ、ステビ
ア０．２５ｇ、アスパルテーム０．５ｇを乳鉢にとり、
薄荷油１００μｌを添加し、乳棒で展延させる。得られ
た粉末にアセトアミノフェン１５ｇとステアリン酸マグ
ネシウム０．３ｇを混合し、１３ｍｍの臼と平面の杵を
用い、打錠圧１４００ｋｇ／杵でオートグラフ（ＡＧ−
５０００Ｂ、島津製作所）にて、錠剤重量６００ｍｇで
製錠した。Example 2: Essential oil + high-intensity sweetener + soybean lecithin erythritol 30 g, crystalline cellulose (Ceolas KG)
801) 9.91 g, crospovidone 2.45 g, soy lecithin (Benecote BMI-60) 1.5 g, stevia 0.25 g, aspartame 0.5 g are placed in a mortar,
Add 100 μl of light oil and spread with a pestle. 15 g of acetaminophen and 0.3 g of magnesium stearate were mixed with the obtained powder, and an autograph (AG-
5000B, Shimadzu Corporation) at a tablet weight of 600 mg.
【００１８】実施例３：精油＋高甘味度甘味剤 アセトアミノフェン１５ｇ、エリスリトール３９．７
ｇ、結晶セルロース（セオラスＫＧ８０１）７．１６
ｇ、クロスポビドン２ｇ、ステビア０．２５ｇ、アスパ
ルテーム０．５ｇを乳鉢にとり、薄荷油１００μｌを添
加し、乳棒で展延させる。その後、精製水を適量加え、
練合後、４０℃で１６時間真空乾燥した。得られた造粒
末を１６メッシュにて整粒後、その整粒末６．４７ｇに
対して、ステアリン酸マグネシウムを０．０３ｇ混合
し、１３ｍｍの臼と平面の杵を用い、打錠圧１４００ｋ
ｇ／杵でオートグラフ（ＡＧ−５０００Ｂ、島津製作
所）にて、錠剤重量６５０ｍｇで製錠した。Example 3: Essential oil + high sweetness sweetener 15 g of acetaminophen, 39.7 erythritol
g, crystalline cellulose (CEOLUS KG801) 7.16
g, crospovidone 2 g, stevia 0.25 g, and aspartame 0.5 g are placed in a mortar, 100 μl of thin oil is added, and spread with a pestle. Then, add an appropriate amount of purified water,
After kneading, it was vacuum dried at 40 ° C. for 16 hours. The obtained granulated powder was sized with 16 mesh, and 0.03 g of magnesium stearate was mixed with 6.47 g of the sized powder, and a tableting pressure of 1400 k was applied using a 13 mm die and a flat punch.
The tablet weight was 650 mg with an autograph (AG-5000B, Shimadzu Corporation) using a g / punch.
【００１９】実施例４：精油＋高甘味度甘味剤＋大豆レ
シチン＋多孔性ケイ酸カルシウム エリスリトール３０ｇ、結晶セルロース（セオラスＫＧ
８０１）８．４１ｇ、クロスポビドン２．４５ｇ、大豆
レシチン（ベネコ−トＢＭＩ−６０）１．０ｇ、特殊ケ
イ酸カルシウム（フローライトＲＥ）２ｇ、ステビア
０．２５ｇ、アスパルテーム０．５ｇを乳鉢にとり、薄
荷油１００μｌを添加し、乳棒で展延させる。得られた
粉末にトラネキサム酸１２．５ｇとステアリン酸マグネ
シウム ０．３ｇを混合し、１３ｍｍの臼と平面の杵を
用い、打錠圧１４００ｋｇ／杵でオートグラフ（ＡＧ−
５０００Ｂ、島津製作所）にて、錠剤重量５７５ｍｇで
製錠した。Example 4: Essential oil + high-intensity sweetener + soy lecithin + porous calcium silicate 30 g of erythritol, crystalline cellulose (Ceolas KG)
801) 8.41 g, crospovidone 2.45 g, soy lecithin (Benecote BMI-60) 1.0 g, special calcium silicate (Fluorite RE) 2 g, stevia 0.25 g, aspartame 0.5 g are placed in a mortar, Add 100 μl of light oil and spread with a pestle. To the obtained powder, 12.5 g of tranexamic acid and 0.3 g of magnesium stearate were mixed, and using a 13 mm die and a flat punch, an autograph (AG-
5000B, Shimadzu Corporation) at a tablet weight of 575 mg.
【００２０】実施例５：精油＋高甘味度甘味剤＋多孔性
ケイ酸カルシウム エリスリトール９００ｇ、結晶セルロース（セオラスＫ
Ｇ８０１）１６０．５ｇ、クロスポビドン７２ｇ、多孔
性ケイ酸カルシウム（フローライトＲＥ）１８ｇ、黄色
５号アルミニウムレーキ０．３６ｇを流動層造粒機（Ｆ
Ｄ−３ＳＮ、パウレック）にて、精製水を噴霧すること
により造粒し、その後、流動層乾燥し、造粒末を得る。
パワーミル（昭和機械工作所）にて整粒後、整粒末を得
る。別に結晶セルロース（セオラスＫＧ８０１）５４．
９８ｇ、ステビア２．５ｇ、アスパルテーム５ｇを乳鉢
にとり、薄荷油１ｍｌを添加して乳棒で展延させて薄荷
油倍散末を得る。この薄荷油倍散末に、整粒末３８３．
６２ｇ、アセトアミノフェン１５０ｇとステアリン酸マ
グネシウム３ｇを混合し、混合末を得る。この混合末
を、ロータリー式打錠機にて、１３ｍｍの臼と平面の杵
を用い、打錠圧１４００ｋｇ／杵で、錠剤重量６００ｍ
ｇで製錠した。Example 5: Essential oil + high-intensity sweetener + porous calcium silicate 900 g of erythritol, crystalline cellulose (Seolas K)
G801) 160.5 g, crospovidone 72 g, porous calcium silicate (Fluorite RE) 18 g, yellow No. 5 aluminum lake 0.36 g were charged with a fluid bed granulator (F).
D-3SN, Powrex) to granulate by spraying purified water, followed by drying in a fluidized bed to obtain a granulated powder.
After sizing with a power mill (Showa Machine Works), sieved powder is obtained. Separately, crystalline cellulose (Ceolas KG801)
98 g, stevia 2.5 g, and aspartame 5 g are placed in a mortar, 1 ml of thin oil is added, and spread with a pestle to obtain a thin oil double powder. The sized powder 383.
62 g, 150 g of acetaminophen and 3 g of magnesium stearate are mixed to obtain a mixed powder. This mixed powder was tableted with a rotary tableting machine using a 13 mm die and a flat punch at a tableting pressure of 1400 kg / punch and a tablet weight of 600 m.
g.
【００２１】比較例１：高甘味度甘味剤 アセトアミノフェン１５ｇ、エリスリトール３０ｇ、結
晶セルロース（セオラスＫＧ８０１）１．１５ｇ、クロ
スポビドン２．５ｇ、ステビア０．２５ｇ、アスパルテ
ーム０．５ｇ、ステアリン酸マグネシウムを０．３ｇを
混合し、１３ｍｍの臼と平面の杵を用い、打錠圧１４０
０ｋｇ／杵でオートグラフ（ＡＧ−５０００Ｂ、島津製
作所）にて、錠剤重量６００ｍｇで製錠した。Comparative Example 1: 15 g of a high-potency sweetener, acetaminophen, 30 g of erythritol, 1.15 g of crystalline cellulose (Ceolas KG801), 2.5 g of crospovidone, 0.25 g of stevia, 0.5 g of aspartame, and 0.5 g of magnesium stearate 0.3 g and mixed with a 13 mm die and a flat punch.
Tablets were produced at a tablet weight of 600 mg with an autograph (AG-5000B, Shimadzu Corporation) using 0 kg / punch.
【００２２】比較例２：精油 エリスリトール３０ｇ、結晶セルロース（セオラスＫＧ
８０１）１２．１６ｇ、クロスポビドン２．４５ｇを乳
鉢にとり、薄荷油１００μｌを添加し、乳棒に展延させ
る。得られた粉末にアセトアミノフェン１５ｇとスアリ
テン酸マグネシウムを０．３ｇ混合し、１３ｍｍの臼と
平面の杵を用い、打錠圧１４００ｋｇ／杵でオートグラ
フ（ＡＧ−５０００Ｂ、島津製作所）にて、錠剤重量６
００ｍｇで製錠した。Comparative Example 2: 30 g of erythritol essential oil, crystalline cellulose (Seolas KG)
801) 12.16 g of crospovidone and 2.45 g of crospovidone are placed in a mortar, 100 μl of light oil is added, and spread on a pestle. 15 g of acetaminophen and 0.3 g of magnesium salitenate were mixed with the obtained powder, and using a 13 mm die and a flat punch, an autograph (AG-5000B, Shimadzu Corporation) was used at a tableting pressure of 1400 kg / punch. Tablet weight 6
Tablets were made at 00 mg.
【００２３】比較試験 上記実施例１〜４で得られた本発明の口腔内速崩壊錠、
並びに比較製剤１および２の口腔内速崩壊錠のそれぞれ
の硬度、口溶け時間を調べ、苦味を評価した。苦味の評
価には下記スコアを用い、服用後１０秒後の苦味と服用
後６０秒後の苦味とに分けて評価した。 苦味の評価スコア 苦味をほとんど感じない：０ 苦味をわずかに感じる：１ 苦味を感じる：２ 苦味を強く感じる：３ スコアが０〜１である場合は、苦味について服用に問題
ない程度であり、２〜３である場合は、苦味のため服用
しずらい程度である。結果を、下記表１に示す。Comparative Test The orally rapidly disintegrating tablet of the present invention obtained in Examples 1 to 4 above,
The hardness and dissolution time in the mouth of each of the oral preparations of Comparative Formulations 1 and 2 were examined, and the bitterness was evaluated. The following score was used for the evaluation of bitterness, and the evaluation was made separately for the bitterness 10 seconds after ingestion and the bitterness 60 seconds after ingestion. Bitter taste evaluation score Bitter taste is hardly felt: 0 Bitterness is slightly felt: 1 Bitterness is felt: 2 Bitterness is strongly felt: 3 When the score is 0 to 1, there is no problem in taking the bitterness. When it is ３3, it is difficult to take it due to bitterness. The results are shown in Table 1 below.
【００２４】[0024]
【表１】 [Table 1]
【００２５】上記表１によれば、精油または高甘味度甘
味剤のいずれか一方のみを配合した口腔内速崩壊錠（比
較例１および２）における苦味低減効果は十分ではない
のに対して、本発明の口腔内速崩壊（実施例１〜５）に
おいてはその苦味が現実の服用に全く問題のない程度ま
で低減された。特に、服用の６０秒後における苦味を低
減している点で、本発明の口腔内速崩壊錠の優れた効果
が明らかである。According to Table 1 above, the bitterness reducing effect of the orally rapidly disintegrating tablet containing only one of the essential oil and the high-sweetness sweetener (Comparative Examples 1 and 2) is not sufficient. In the rapid disintegration in the oral cavity of the present invention (Examples 1 to 5), the bitterness was reduced to such an extent that there was no problem at all in taking it. In particular, the excellent effect of the orally rapidly disintegrating tablet of the present invention is apparent in that bitterness is reduced 60 seconds after ingestion.
【００２６】実施例６ 実施例５で得た錠剤をアルミストリップ包装し、４０
℃、相対湿度７５％で６ヶ月保存した錠剤の硬度、口溶
け時間、苦味を評価した。苦味の評価は表１におけると
同様である。Example 6 The tablets obtained in Example 5 were packaged in aluminum strips,
The hardness, dissolution time in mouth, and bitterness of the tablets stored at 6 ° C. and 75% relative humidity for 6 months were evaluated. The evaluation of bitterness is the same as in Table 1.
【００２７】比較例３ 実施例５で得た錠剤をガラス瓶に入れ、開栓状態で４０
℃、相対湿度７５％で６ヶ月保存した錠剤の硬度、口溶
け時間、苦味を評価した。苦味の評価は表１におけると
同様である。実施例６および比較例３の評価結果を表２
に示す。Comparative Example 3 The tablets obtained in Example 5 were placed in a glass bottle,
The hardness, dissolution time in mouth, and bitterness of the tablets stored at 6 ° C. and 75% relative humidity for 6 months were evaluated. The evaluation of bitterness is the same as in Table 1. Table 2 shows the evaluation results of Example 6 and Comparative Example 3.
Shown in
【００２８】[0028]
【表２】 [Table 2]
【００２９】表２から明らかなごとく、本発明の口腔内
速崩壊錠はアルミストリップ包装のような気密性の高い
包装形態とすることが好ましい。As is clear from Table 2, the rapidly disintegrating tablet in the oral cavity of the present invention is preferably in a highly airtight package such as an aluminum strip package.
【００３０】[0030]
【発明の効果】本願発明の口腔内速崩壊錠は、苦味を有
する医薬成分を被覆していないにも関わらず、水無しで
服用してもその苦味を殆ど感じずに服用することができ
る。そのため、医薬成分を被覆する場合に比べて低コス
トで製造できるばかりでなく、時と場所を選ばないで必
要な医薬成分を服用できるという点で、医療分野におい
て極めて有用な製剤となるものである。The orally rapidly disintegrating tablet of the present invention can be taken with almost no bitterness even when taken without water, even though it is not coated with a bitter pharmaceutical ingredient. Therefore, in addition to being able to be manufactured at a lower cost than in the case of coating with a pharmaceutical component, it is a very useful formulation in the medical field in that the required pharmaceutical component can be taken at any time and place. .
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 ＦＩ テーマコート゛(参考） Ａ６１Ｋ 47/44 Ａ６１Ｋ 47/44 47/46 47/46 Ａ６１Ｐ 25/04 Ａ６１Ｐ 25/04 ──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. 7 Identification symbol FI theme coat ゛ (Reference) A61K 47/44 A61K 47/44 47/46 47/46 A61P 25/04 A61P 25/04
Claims (9)
甘味度甘味剤および／または酸性リン脂質若しくはその
リゾ体からなる苦味低減成分とを含有することを特徴と
する口腔内速崩壊錠。An orally rapidly disintegrating tablet comprising a pharmaceutical ingredient having a bitter taste and an essential oil and a bitterness-reducing component comprising a high-intensity sweetener and / or an acidic phospholipid or a lyso-form thereof.
剤からなる請求項１に記載の口腔内速崩壊錠。2. The orally rapidly disintegrating tablet according to claim 1, wherein the bitterness reducing component comprises an essential oil and a high-sweetness sweetener.
若しくはそのリゾ体からなる請求項１に記載の口腔内速
崩壊錠。3. The orally rapidly disintegrating tablet according to claim 1, wherein the bitterness reducing component comprises an essential oil and an acidic phospholipid or a lyso form thereof.
よび酸性リン脂質若しくはそのリゾ体からなる請求項１
に記載の口腔内速崩壊錠。4. The bitterness-reducing component comprises an essential oil, a high-intensity sweetener, and an acidic phospholipid or a lyso-form thereof.
2. The rapidly disintegrating tablet in the oral cavity according to item 1.
いことを特徴とする請求項１に記載の口腔内速崩壊錠。5. The orally rapidly disintegrating tablet according to claim 1, wherein the pharmaceutical ingredient having a bitter taste is not coated.
ェンである、請求項１に記載の口腔内速崩壊錠。6. The orally rapidly disintegrating tablet according to claim 1, wherein the pharmaceutical ingredient having a bitter taste is acetaminophen.
口腔内速崩壊錠。7. The orally rapidly disintegrating tablet according to claim 1, wherein the essential oil is peppermint oil.
ームから選択される一又は二である請求項１に記載の口
腔内速崩壊錠。8. The orally rapidly disintegrating tablet according to claim 1, wherein the high-intensity sweetener is one or two selected from stevia and aspartame.
シチンである請求項１に記載の口腔内速崩壊錠。9. The orally rapidly disintegrating tablet according to claim 1, wherein the acidic phospholipid or its lyso form is soy lecithin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2000187822A JP3389205B2 (en) | 1999-06-29 | 2000-06-22 | Oral quick disintegrating tablets |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP11-183624 | 1999-06-29 | ||
| JP18362499 | 1999-06-29 | ||
| JP2000187822A JP3389205B2 (en) | 1999-06-29 | 2000-06-22 | Oral quick disintegrating tablets |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2001072578A true JP2001072578A (en) | 2001-03-21 |
| JP3389205B2 JP3389205B2 (en) | 2003-03-24 |
Family
ID=26501982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000187822A Expired - Lifetime JP3389205B2 (en) | 1999-06-29 | 2000-06-22 | Oral quick disintegrating tablets |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3389205B2 (en) |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004099510A (en) * | 2002-09-09 | 2004-04-02 | Ss Pharmaceut Co Ltd | Hypnogenic solid preparation |
| JP2005272401A (en) * | 2004-03-25 | 2005-10-06 | Tendou Seiyaku Kk | Chewable tablet |
| JP2008099682A (en) * | 2006-09-22 | 2008-05-01 | Sanei Gen Ffi Inc | Composition containing functional raw material and/or extract |
| WO2012005365A1 (en) | 2010-07-09 | 2012-01-12 | 帝人ファーマ株式会社 | Particle coating preparation |
| WO2012029655A1 (en) * | 2010-08-30 | 2012-03-08 | 国立大学法人東北大学 | Agent for controlling hemodialysis-induced cramps |
| JP2017521368A (en) * | 2014-06-11 | 2017-08-03 | マリンクロッド エルエルシー | Spray-dried compositions having different dissolution profiles and methods for their preparation |
| JP2021004217A (en) * | 2019-06-27 | 2021-01-14 | 小林製薬株式会社 | Oral composition |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7360460B2 (en) * | 2019-06-07 | 2023-10-12 | あゆみ製薬株式会社 | Orally disintegrating tablet and its manufacturing method |
-
2000
- 2000-06-22 JP JP2000187822A patent/JP3389205B2/en not_active Expired - Lifetime
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004099510A (en) * | 2002-09-09 | 2004-04-02 | Ss Pharmaceut Co Ltd | Hypnogenic solid preparation |
| JP2005272401A (en) * | 2004-03-25 | 2005-10-06 | Tendou Seiyaku Kk | Chewable tablet |
| JP2008099682A (en) * | 2006-09-22 | 2008-05-01 | Sanei Gen Ffi Inc | Composition containing functional raw material and/or extract |
| WO2012005365A1 (en) | 2010-07-09 | 2012-01-12 | 帝人ファーマ株式会社 | Particle coating preparation |
| WO2012029655A1 (en) * | 2010-08-30 | 2012-03-08 | 国立大学法人東北大学 | Agent for controlling hemodialysis-induced cramps |
| JP2017521368A (en) * | 2014-06-11 | 2017-08-03 | マリンクロッド エルエルシー | Spray-dried compositions having different dissolution profiles and methods for their preparation |
| US11464741B2 (en) | 2014-06-11 | 2022-10-11 | SpecGx LLC | Spray dried compositions having different dissolution profiles and processes for their preparation |
| JP2021004217A (en) * | 2019-06-27 | 2021-01-14 | 小林製薬株式会社 | Oral composition |
Also Published As
| Publication number | Publication date |
|---|---|
| JP3389205B2 (en) | 2003-03-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US20030161879A1 (en) | Tablets quickly disintegrating in mouth | |
| JP4551092B2 (en) | Orally rapidly disintegrating tablets | |
| TW586941B (en) | Quickly disintegratable pharmaceutical composition | |
| JP4435424B2 (en) | Tablets that disintegrate quickly in the oral cavity | |
| JP5177447B2 (en) | Film preparation having fast solubility and flexibility | |
| KR101465803B1 (en) | Orally disintegratable tablet | |
| KR20030094272A (en) | Tablets quickly disintegrating in oral cavity | |
| JP2009263298A (en) | Oral composition having masked disagreeable taste | |
| EP2397161B1 (en) | Disintegrating particle composition and rapidly disintegrating compression-molded material comprising same | |
| EP1047407A1 (en) | Process for manufacturing bite-dispersion tablets | |
| PT1145711E (en) | Flash-melt oral dosage formulation | |
| US20090136569A1 (en) | Rapidly disintergrating tablet in oral cavity | |
| JP5158318B2 (en) | Orally disintegrating tablets | |
| JP2007269716A (en) | Cetirizine hydrochloride-containing particle | |
| JP2006070046A (en) | Quick disintegrable solid preparation | |
| WO2007119792A1 (en) | Dry direct compression fast disintegrating tablet | |
| JP5054940B2 (en) | Tablet composition | |
| JP2003034655A (en) | Fast degradable solid tablet | |
| JP2001072578A (en) | Tablet quickly disintegrable in oral cavity | |
| JP4358117B2 (en) | Orally disintegrating tablets | |
| JP5204976B2 (en) | Fast disintegrating tablets containing iguratimod | |
| JP2002087965A (en) | In-mouth disintegrable aspirin-containing tablet | |
| JP5062872B2 (en) | Orally disintegrating tablets with reduced unpleasant taste | |
| WO2001000178A1 (en) | Tablets quickly disintegrating in mouth | |
| JP2005306770A (en) | Intraoral quick collapse type preparation and method for producing the same |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20011204 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 3389205 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20090117 Year of fee payment: 6 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100117 Year of fee payment: 7 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100117 Year of fee payment: 7 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100117 Year of fee payment: 7 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20100117 Year of fee payment: 7 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20110117 Year of fee payment: 8 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20110117 Year of fee payment: 8 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120117 Year of fee payment: 9 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20120117 Year of fee payment: 9 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20130117 Year of fee payment: 10 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20130117 Year of fee payment: 10 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20140117 Year of fee payment: 11 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| EXPY | Cancellation because of completion of term |