JPH044293B2 - - Google Patents

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Publication number
JPH044293B2
JPH044293B2 JP56061541A JP6154181A JPH044293B2 JP H044293 B2 JPH044293 B2 JP H044293B2 JP 56061541 A JP56061541 A JP 56061541A JP 6154181 A JP6154181 A JP 6154181A JP H044293 B2 JPH044293 B2 JP H044293B2
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JPS56167617A (en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

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  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Feeding, Discharge, Calcimining, Fusing, And Gas-Generation Devices (AREA)
  • Separation Using Semi-Permeable Membranes (AREA)
  • External Artificial Organs (AREA)
  • Control Of Throttle Valves Provided In The Intake System Or In The Exhaust System (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (AREA)

Description

【発明の詳細な説明】 本発明は、医薬を人体のような流体環境に排出
する浸透性医薬製剤に関する。
医薬を胃腸管に排出するための、錠剤の形で製
造される浸透性医薬製剤は、フエリツクステーウ
エス（Felix Theeuwes）とタケルヒグチ
（Takeru Higuchi）の両者に付与されたアメリ
カ国特許第3845770号及び同第3916899号明細書で
公知である。これらの特許明細書に示されている
典型的な医薬製剤は医薬を含有している区画室を
包囲している半透性壁から成つている。この半透
性壁は、外部流体に対しては透過性であるが、医
薬の通過に対しては実質的に不透過性である。こ
の半透性壁には、これを貫通して系から医薬を排
出するための通路がある。系は、流体が半透性壁
を通つて区画室に壁の透過性と壁を横切る浸透圧
の圧力勾配によつて決まる速度で連続浸透して可
溶性の医薬を含有する溶液を形成し、この溶液を
系から時間の経過に沿つて分配することによつて
医薬を放出する。
フエリツクステーウエスに付与されたアメリカ
国特許第4036228号明細書において、特許権者は、
排出困難な医薬、特に水性タイプの流体に実際上
不溶性である医薬を排出する浸透性医薬製剤を開
示している。この製剤は、これに酸性成分と塩基
性成分から成る起泡性カツプルを満たすことによ
つて使用される。作用下においてその製剤が流体
環境中にあると、その起泡性カツプルは、流体を
製剤に浸透させ、それによつてカツプルを湿潤
し、反応させ、そして起泡性溶液を製剤内に生成
させる。起泡性溶液は製剤内に中性状態を作り出
し、そしてその医薬を製剤から分配する。このア
メリカ国特許は、それ自体酸性環境中で限定され
た溶解性を示す医薬の排出、塩基性成分だけの使
用及び使用環境における起泡の生成には指向して
いない。
本発明は、多くの抗炎症剤が浸透性医薬製剤か
ら制御された速度で排出するのは困難であるとい
うことの発見にある。抗炎症剤は、胃液のような
水性の酸性環境において溶解性が乏しく、従つて
これら医薬は、浸透性医薬製剤からの排出時に胃
液と接触して沈殿する。この現象は、医薬製剤の
半透性壁の通路出口においてその外表面に起こ
り、そこに医薬を沈殿、蓄積させる。沈殿した医
薬は、浸透性製剤の通路を通る溶液の流れを妨害
する。本発明は、医薬を二酸化炭素生成化合物と
混合することによつてその医薬を排出するもので
ある。ここで、前記化合物は、製剤からの放出時
及び胃領域中の酸との接触時に酸と反応し、二酸
化炭素ガスを生成させるものである。この物理作
用とガスは、付随的に医薬製剤の通路を開放に保
ちながら、医薬を細かく分散した形で医薬製剤か
ら分配する。
本発明を図面を参照して説明すると、第１図は
医薬を排出するのに用いられる浸透性医薬製剤１
０を説明するものである。浸透性医薬製剤１０
は、切欠部に見られる通り、区画室１２を包囲、
形成している半透性重合体から形成される壁１１
から成る。壁１１には、それを貫通して通路１３
があり、該通路１３を介して区画室１２を医薬製
剤１０の外面と接続させ、医薬製剤１０から点で
表される医薬１４とダツシユで表され、二酸化炭
素生成基を有する塩基性化合物１５とを排出する
ようになつている。
第２図は医薬を排出するのに用いられる浸透性
医薬製剤１０を説明するものであるる。この浸透
性医薬製剤は、切欠部に見られる通り、区画室１
２の内側に面している微孔質単層１６を積層して
有する半透性重合体から形成される壁１１から成
つている。図示しないが、もう１つの実施態様に
おいて、微孔質単層１６は半透性壁１１の外表面
にあることもできる。第２図において、装置１０
は壁１１と微孔質単層１６によつて形成される半
透性微孔質積層体を貫通して通路１３を有し、該
通路１３を介して区画室１２を製剤１０の表面と
接続させ、医薬１４及び二酸化炭素生成化合物１
５を製剤１０から排出するようになつている。
浸透性医薬製剤１０の半透性壁は、医薬、二酸
化炭素生成化合物又は病人に悪影響を及ぼさない
半透性物質から形成される。この半透性壁は水及
び生物の流体のような外部流体の通過に対しては
透過性であるが、医薬、溶質などの通過に対して
は本質的に不透過性である重合体物質から形成さ
れる。本発明の製剤を製造するのに有用な選択透
過性の重合体として、セルロースアクリレート、
セルロースジアクリレート、セルローストリアク
リレート、セルロースアセテート、セルロースジ
アセテート、セルローストリアセテート、ポリア
ミド、ポリウレタンなどより成る群から選ばれる
重合体が挙げられる。浸透性医薬製剤の製造に適
当な半透性重合体は、アメリカ国特許第3845770
号、同第3916899号、同第4008719号、同第
4036228号及び同第4111210号明細書に開示されて
いる。第２図に示される実施態様において、半透
性壁１１は、微孔質単層１６と層状配置の関係に
ある半透性単層１１から成る積層体であることが
できる。半透性単層１１は上記の重合体から形成
される。微孔質単層１６は、多数の微孔と製剤に
流体を通す連続微孔路を有する。微孔質単層は、
製剤が使用環境中で作用下にあるとき単層から溶
出又は浸出する細孔形成剤が入つている前記重合
体から成つていることができる。細孔形成剤は無
毒性で、且つ壁を形成している物質と反応しない
ものである。これら細孔形成剤がその単層から除
去されると、その中に微孔路ができ、流体を満た
し、従つて、これら微孔路は、流体を医薬製剤に
入れる手段となる。典型的な細孔形成剤として、
塩化ナトリウム、塩化カリウム、ソルビトール、
マンニトール、ポリエチレングリコール、ヒドロ
キシプロピルメチルセルロース、ヒドロキシプロ
ピルブチルセルロースなどの物質が挙げられる。
半透性単層及び微孔質単層から成る積層壁を有す
る浸透性医薬製剤は、アメリカ国特許第4160452
号明細書に開示されている。
本発明において広範に用いられている医薬とい
う表現には、浸透性医薬製剤から排出して有利且
つ有用な結果を生むことができる任意の化合物、
物質の組成物又はそれらの混合物が包含される。
医薬という用語についてさらに明確に述べると、
これには動物、鳥類、魚類及びは虫類に局所的又
は全身的効果を生む任意の物質が包含される。動
物という用語は山羊、牛、馬、犬、ねこなどのよ
うな霊長類、人間、家畜、愛がん動物及び農放牧
動物を包含する。動物という用語はまたマウス、
ラツト及びモルモツトのような実験動物も包含す
る。本発明の方法によつて排出することができる
医薬には中枢神経系作用剤、催眠剤、鎮静剤、精
神神経賦活剤、トランキライザー、抗抑制剤、鎮
痙剤、筋弛緩剤、抗パーキンソン剤、麻酔剤、抗
炎症剤、局所麻酔剤、抗マラリア剤、ホルモン
剤、交感神経興奮剤、利尿剤、駆虫剤、ネオプラ
スチツクス、低血糖症剤、興奮剤、栄養剤のよう
な無機及び有機医薬がある。さらに好ましい実施
態様において、医薬という用語は中性及び酸性環
境に実際上不溶である、すなわち限定された溶解
性を持つ医薬を包含する。すなわち、これらの医
薬はこのような環境中で沈殿するのである。中性
という表現は水及び同様の生物環境を含み、また
酸という表現は胃及びその中に生成する塩酸、腟
及びその中に生成する乳酸などを含む。本明細書
において用いられている酸性体液という熟語は胃
液、腟液などの酸環境を指している。
本発明の方法により、上記環境に排出するのに
適当な医薬の１つの特定の群は、酸性抗炎症剤で
ある。抗炎症剤としては、アリールカルボン酸剤
及びエノル酸剤が挙げられる。アリールカルボン
酸剤の例には、アルクロフエナツク、すなわち、
４−アリルオキシ−３−クロロ−フエニル酢酸；
アスピリン、すなわち、アセチルサリチル酸；フ
エノプロフエン、すなわち、dl−２−（３−フエ
ノキシフエニル）プロピオン酸；フルフエナミン
酸、すなわち、２−（３−トリフルオロメチルア
ニリノ）安息香酸；イブプロフエン、すなわち、
２−（４−イソブチルフエニル）プロピオン酸；
インドメタシン、すなわち、５−メトキシ−２−
メチル−１−（4′−クロロベンゾイル）−３−イン
ドール−酢酸；ケトプロフエン、すなわち、２−
（３−ベンゾイルフエニル）プロピオン酸；メチ
アジニン酸、すなわち、10−メチル−２−フエノ
チアジニル酢酸；ナプロキセン、すなわち、ｄ−
２−（6′−メトキシ−2′−ナフチル）プロピオン
酸；ニフルミン酸、すなわち、３−トリフルオロ
メチル−２−フエニル−アミノニコチン酸；トル
メチン、すなわち、１−メチル−５−ｐ−トルオ
イルピロール−２−酢酸；及びサリンダツク、す
なわち、シス−５−フルオロ−２−メチル−１−
〔ｐ−（メチルスルフイニル）−ベンジリデン〕イ
ンデン−３−酢酸がある。エノル酸剤の例には、
アザプロパゾン、即ち、３−ジメチルアミノ−７
−メチル−１，２−（ｎ−プルピルマロニル）−１
−２，ジヒドロ−１，２，４−ベンゾトリアジ
ン；フエニルブタゾン、即ち、３，５−ジオキソ
−４−ｎ−ブチル−１，２−ジフエニルピラゾリ
ジン；プレナゾン、すなわち、４−プレニル−
１，２−ジフエニル−３，５−ピラゾリジンジオ
ン；サドキシカム、すなわち、４−ヒドロキシ−
２−メチル−Ｎ−（２−チアゾリル）−2H−１，
２−ベンゾチアジン−３−カルボキサミド−１，
１−ジオキシドなどの化合物がある。他の抗炎症
剤には、ジクロフエナツク、すなわち、２−〔２，
６−ジクロロフエニル）アミノ〕ベンゼン酢酸；
及びペルオキシカム、すなわち、2H−１，２−
ベンゾチアジン−３−カルボキサミドがある。
本発明の方法によつて排出することができる、
水に実際上不溶の、又は水に極めてわずかしか溶
解しない他の医薬の例には、ジフエニドール、メ
クリジン塩酸塩、プロクロルペルアジンマレエー
ト、アニシンドン、ジフエナジオーン、エリトリ
チルテトラナイトレート、ジゾキシン、レスパー
ピン、アセタゾールアミド、メタゾールアミド、
ベンドロフルメチアジド、クロルプロパミド、ト
ラザミド、アロプリノール、アルミニウムアスピ
リン、サリチル酸、サリチル酸ナトリウム、サリ
チルアミド、アセトアミノフエン、アセトフエネ
チジン、コルヒチン、メフエナミン酸、オクスフ
エンブタゾン、ゾメピラツク、メソトレキセー
ト、アセチルスルフイソキサゾール、ヒドロコー
チゾン、デスオキシコルチコステロンアセテー
ト、コルチソンアセテート、トリアミノロン、17
−エストラジオール、17−ヒドロキシプロゲステ
ロン、19−ノルプロゲステロン、プレドニソロ
ン、プロゲステロン、ノルエチンドロンアセテー
ト、ノルエチノドレルなどの化合物がある。
医薬製剤中に存在する医薬の量は、ホストに投
与すべき医薬の活性と量に応じて変わる。一般
に、この製剤は、0.5mg〜３ｇ、又はそれ以上の
医薬を含み、例えば、個々の製剤は25mg、50mg、
125mg、250mg、1.5ｇなどの量で医薬を含有して
いる。医薬は、分散体、顆粒、粉末、圧縮塊、フ
イルムなどの形態のような各種形態で製剤中に存
在することができる。また、医薬は結合剤、希釈
剤、分散剤、安定剤、染料などの添加剤と混合す
ることができる。有利な医薬、それらの溶解性、
それらの投与量は、マツクパブリツシング社
（Mack Publishing Co.）（イーストン
〔Easton〕、ペンシルバニア〔Penna〕）刊行のレ
ミングトン（Remington）著「フアーマシユー
テイカル サイエンセス（Pharmaceutical
Sciences）」第15版 （1975年）；サウンダー社（Saunder Company） （フイラデルフイア〔Philadelphia〕、ペンシル
バニア）刊行のフアルコナー（Falconer）他著
「ザ ドラツグ、ザ ナース、ザ ペーシヤント、
インクルーデイング カレント ドラツグ ハン
ドブツク（The Drug，the Nurse，the
Patient，Including Current Drug Handbook）」
（1974〜1976年）；メデイカル エコノミツクス社
（Medical Economics Co.）（オラデル
〔Oradell〕、ニユージヤージー〔N.J.〕）刊行の
「フイジシアン デスク レフアレンス
（Physician Desk Reference）」第33版（1979
年）、「アン オブ アラージー（Ann.of
Allergy）」第41巻、第75〜77ページ（1979年）；
「アルゼニム フオルシユ（Arzenim.Forsch.）」
第25巻、第1629〜1635ページ（1975年）；及びJ.
Inter.Med.Res.第７巻、第335〜338ページ（1979
年）においてこの技術分野に知られている。
本発明の目的に適当なガス生成化合物は、製薬
上許容でき、そしてａ）半透性壁を横切つて濃度
勾配を示し、且つ医薬製剤中に流体を浸透させ、
ｂ）緩衝剤として作用し、且つ医薬製剤に入つて
くる流体に溶解して医薬を含有する溶液を形成
し、ｃ）医薬製剤の外側において通路を囲む隣接
区域のPHを医薬の沈殿速度を下げるのに十分高い
値まで上昇させ、そしてｄ）医薬製剤の外側で、
通路の環境界面においてその環境の酸と反応し
て、医薬を細かく分散した形で医薬製剤から放出
させる二酸化炭素の起泡を生成させる固体の塩基
性化合物が好ましい。この塩基性化合物には、ア
ルカリ金属炭酸塩及び重炭酸塩、アルカリ土類金
属炭酸塩及び重炭酸塩、並びにそれらの混合物の
ような無毒性の金属炭酸塩及び重炭酸塩がある。
好ましい化合物は、水に可溶で、且つ環境の酸と
接触して速やかに起泡を生成するものである。水
中での溶解度が異なる化合物の混合物を水に非常
によく溶解しうる少なくとも１種の化合物ととも
に使用することもできる。典型的化合物として炭
酸リチウム、炭酸ナトリウム、炭酸カリウム、重
炭酸リチウム、重炭酸ナトリウム、重炭酸カリウ
ム、炭酸マグネシウム、炭酸カルシウム、重炭酸
マグネシウムなどの塩がある。炭酸アンモニウ
ム、重炭酸アンモニウム、セスキ炭酸アンモニウ
ム、セスキ炭酸ナトリウムなどの塩も有用なガス
生成化合物である。これらの化合物は、水に溶解
するとき７より大きいPH、通常８と12の間のPHを
示す。任意であるが、共通イオン効果のない医薬
とガス生成化合物を選ぶのがしばしば望ましく、
かくして医薬製剤に入つてくる流体中のそれらそ
れぞれの溶解度は最大になる。区画室に収容され
る塩基性化合物又はその混合物の量は一般に約
0.5mg〜３ｇ、又はそれ以上、好ましくは25〜750
mgである。塩基性化合物及びそれらの水中におけ
る溶解度についてはケミカル ラバー社
（Chemical Rubber Co.）（クリーブランド
〔Cleveland〕、オハイオ〔Ohio〕）刊行の「ザ
ハンドブツク オブ ケミストリー アンド フ
イジツクス（The Handbook of Chemistry
and Physics）」第48版（1968年）に開示されて
いる。
医薬及び塩基性化合物は、また、結合剤及び潤
滑剤として用いることができる。医薬及び塩基性
化合物は、水溶性結合剤に混合されるか、又は水
と接触すると医薬及び塩基性化合物を放出する水
不溶性結合剤に混合される。典型的な水溶性結合
剤には、ポリ（エチレングリコール）、ゼラチン、
寒天、カルボキシセルロース、エチルメチル−セ
ルロース、ポリ（ビニルアルコール）、ポリ（ビ
ニルピロリドン）、水溶性殿粉誘導体などがある。
典型的な潤滑剤には、ステアリン酸、ステアリン
酸マグネシウム、ステアリン酸亜鉛などがある。
使用される結合剤及び潤滑剤の量は一般に約0.1
〜150mg、又はそれ以上である。
本発明の浸透性医薬製剤は、標準的な方法で製
造される。例えば、１つの実施態様において、医
薬を塩基性化合物及び他の成分と、ボールミルで
粉砕し、カレンダリングし、撹拌し、そして所定
の形状にプレス成形することによつて混合する。
医薬製剤の壁を形成する物質は、浸漬、モールデ
イング又は噴霧によつて、プレス成形された混合
物に適用することができる。壁を適用する１つの
方法は空気懸濁法である。空気懸濁法は、単層か
ら、又は複雑層から形成される壁を作るのに用い
ることができる。空気懸濁法は、アメリカ国特許
第2799241号；J.Am.Pharm.Assoc.第48巻、第
451〜459ページ（1959年）；及び同第49巻、第82
〜84ページ（1960年）に記載されている。壁を貫
通する浸透通路又は孔は機械的にドリリングする
か、レーザーでドリリングするか、パンチングす
るか、又はダイで切ることによつて作られる。レ
ーザーを用いて通路を形成する方法はアメリカ国
特許第3916899号及び同第4088864号明細書に記載
されている。他の標準的な製造方法は「モダーン
プラスチツク エンサイクロペデイア
（Modern Plastic Encyclopedia）」第46巻、第62
〜70ページ（1969年）；マツク パブリツシング
社（イーストン、ペンシルバニア）刊行の、「レ
ミングトンズ フアーマシユーテイカル サイエ
ンセス」第14版、第1649〜1698ページ（1970
年）；及びリー アンド フエビガー社（Lea
＆ Febiger Co.）（フイラデルフイア
〔Philadelphia〕、ペンシルバニア〔Penn.〕）刊行
のラチマン（Lachman）他著「ザ セラピー
アンド プラクテイス オブ インダストリアル
フアーマシー（The Therapy and Practice
of Industrial Pharmacy）第197〜225ページ
（1970年）に記載されている。
次の実施例は本発明を単に説明するだけのもの
であり、いずれの点でも本発明の範囲を限定する
ものと考えるべきでない。
実施例 １ 非ステロイド系抗炎症剤のインドメタシンナト
リウムの排出のための経口浸透性医薬製剤を次の
ようにして製造した。医薬製剤の区画室にいれる
ための医薬組成物を、105.2mgのインドメタシン
ナトリウム三水和物、142mgの重炭酸カリウム、
5.0mgのポリビニルピロリドン及び7.1mgのステア
リン酸を完全に配合し、次いでその均質な配合物
を予備区画室形成用医薬調合物に圧縮成形するこ
とによつて調製した。次に、圧縮成形した医薬調
合物を空気懸濁機に入れ、微孔質単層形成組成物
を被覆した。微孔質単層組成物は、45重量％の、
アセチル含量が39.8％のセルロースアセテート、
27.5重量％のヒドロキシプロピルメチルセルロー
ス及び27.5重量％のポリエチレングリコール4000
から成つていた。微孔質単層は、塩化メチレン−
95％エタノール溶剤（80：20、重量：重量）から
形成した。微孔質単層は厚さ５ミルであつた。
次に、半透性外層を空気懸濁機中で微孔質単層
の上に積層した。半透性層形成組成物は50重量％
の、アセチル含量が39.8％のセルロースアセテー
ト及び50重量％の、アセチル含量が32％のセルロ
ースアセテートから成つていた。半透性単層は塩
化メチレンと95％エタノールから成る混合溶剤
（80：20、重量：重量）から適用した。この系を
乾燥し、そして10ミルの通路を積層壁を貫通して
レーザーでドリリングした。この系は、インドメ
タシンを８mg／時間の速度で放出する。この医薬
製剤は作用下において通路出口端で酸性胃液と接
触すると、医薬をケバ状態で分散させる二酸化炭
素の気泡を生成させて起泡する溶液を放出する。
実施例 ２ インドメタシンを制御して連続排出する経口浸
透性医薬製剤を前記の一般的操作を行うことによ
つて作つた。本製剤において、区画室は56.4％の
炭酸カリウム、37.6％のインドメタシンナトリウ
ム三水和物、３％のプロビドン （Providone
）及び３％のステアリン酸から成る医薬調合物
を収容していた。圧縮成形後の調合物は、直径
7.93mm、面積1.6cm2及び密度1.65ｇ／mlを有してい
た。製剤は45重量％の、アセチル含量が39.8％の
セルロースアセテート、45重量％のソルビトール
及び10重量％のポリエチレングリコール400から
本質的に成る微孔質内層を含む積層された壁を有
していた。内層は塩化メチレン−メタノール−水
（62：35：３重量比）から成る溶剤から適用した。
この微孔質単層の上に半透性層を積層した。半透
性層は50重量％の、アセチル含量が39.8％のセル
ロースアセテート及び50重量％の、アセチル含量
が32％のセルロースアセテートから成つている。
半透性層は塩化メチレンとメタノール（80：20重
量比）から成る溶剤から適用した。微孔質形成層
は、厚さ５ミルで、半透性層は厚さ2.4ミルであ
つた。この製剤は、９ミルの通路を有し、インド
メタシンを８mg／時間の速度で排出した。この製
剤は、通路の環境界面において、及び通路付近の
製剤の壁の上において急速な沈殿を実質的に起こ
さずに医薬を排出する。
実施例 ３ 微孔質形成単層が厚さ１ミル、半透性単層が厚
さ2.7ミルで、医薬の放出速度が８mg／時間であ
る点を除いて実施例２に記載の条件を用いて実施
例２の操作を繰り返した。
実施例 ４ (a)微孔質単層が厚さ５ミル、半透性単層が厚さ
3.4ミル及び医薬製剤の医薬放出速度が６mg／時
間である、及び(b)微孔質単層が厚さ５ミル、半透
性単層が厚さ1.7ミル及び系の医薬放出速度が12
mg／時間である実施例１及び２の浸透性医薬製剤
を本実施例で製造した。
実施例 ５ 胃腸管中でアリールカルボン酸系抗炎症剤を放
出する一連の経口浸透性医薬製剤を本発明に従つ
て調製する。この製剤は、40〜250mgのインドメ
タシンナトリウム、好ましくは85〜125mgのイン
ドメタシンナトリウム三水和物（これは70〜100
mgのインドメタシンに相当する）、50〜300mg、好
ましくは130〜190mgの重炭酸カリウム、２〜20
mg、好ましくは５〜10mgの結合剤及び２〜20mg、
好ましくは５〜10mgの潤滑剤を収容する。この製
剤は、0.10〜0.16mmの厚さを持つ18〜25mgの重さ
の内側微孔質形成単層と0.035〜0.100mmの厚さを
持つ６〜20mgの重さの外側半透性単層を有する。
この製剤は0.18〜0.38mmの通路を有し、医薬を５
〜15mg／時間の速度で放出する。
本発明により生まれる予期されない利点は第３
図及び第４図に認められる。第３図はガス生成塩
基性化合物なしで製造した浸透性医薬製剤からの
インドメタシンの放出を示している。この製剤
は、塩酸を含有する人工胃液の存在下で医薬を放
出するが、しかしながら医薬は製剤の壁及び通路
の出口部に沈殿し、従つて医薬は環境の流体中に
は認められない。医薬は第３図に示されるように
時間基準で分析されている。第４図は、塩基性の
ガス生成化合物により製造した浸透性医薬製剤か
らのインドメタシンの放出を示している。この製
剤は作用下において本発明による両人工胃腸管液
に医薬を放出する。
【図面の簡単な説明】
第１図は、縮尺して製図したものでないが、医
薬を排出するのに用いられ、半透性壁によりつく
られた浸透性医薬製剤の切欠図であり、第２図
は、縮尺して製図したものでないが、医薬を排出
するのに用いられる、微孔質半透性壁により作ら
れた浸透性医薬製剤の切欠図であり、第３図は、
浸透性医薬製剤からガス生成化合物なしで放出さ
れる貧溶解性医薬の放出パターンを示すグラフで
あり、そして第４図は、浸透性医薬製剤からガス
生成化合物とともに放出される貧溶解性医薬の放
出パターンを示すグラフである。 １０…浸透性医薬製剤、１１…半透性壁、１２
…区画室、１３…通路、１４…医薬、１５…塩基
性化合物、１６…微孔質単層。

Claims (1)

    【特許請求の範囲】
  1. １ 流体の通過に対しては透過性であるが、医薬
    の通過に対しては実質的に不透過性である半透性
    の重合体壁、この壁によつて包囲、形成された区
    画室および前記壁中に形成された前記医薬を排出
    するための通路から成り、前記区画室は、酸流体
    環境で沈殿する医薬と、二酸化炭素生成基を有す
    る非毒性塩基性化合物を含み、該塩基性化合物は
    区画室中に吸収される流体に可溶性であり、か
    つ、この流体に対して前記の壁を横切つて浸透圧
    の圧力勾配を示す、医薬を酸流体環境に排出する
    ための浸透性医薬製剤において、該医薬製剤の外
    側で該塩基性化合物を該酸流体環境と反応させる
    ことにより、通路の出口でガスを発生させ、泡立
    ちを生じさせ該通路の出口で医薬の沈殿を少なく
    することを特徴とする、通路の出口と酸流体環境
    の界面における医薬の沈殿を少なくするように改
    良された浸透性医薬製剤。
JP6154181A 1980-04-25 1981-04-24 Permeation device Granted JPS56167617A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US06/143,644 US4265874A (en) 1980-04-25 1980-04-25 Method of delivering drug with aid of effervescent activity generated in environment of use

Publications (2)

Publication Number Publication Date
JPS56167617A JPS56167617A (en) 1981-12-23
JPH044293B2 true JPH044293B2 (ja) 1992-01-27

Family

ID=22504961

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Application Number Title Priority Date Filing Date
JP6154181A Granted JPS56167617A (en) 1980-04-25 1981-04-24 Permeation device

Country Status (11)

Country Link
US (1) US4265874A (ja)
EP (1) EP0040899B1 (ja)
JP (1) JPS56167617A (ja)
AT (1) ATE9267T1 (ja)
DE (1) DE3165901D1 (ja)
DK (1) DK152482C (ja)
ES (2) ES267593Y (ja)
GR (1) GR73519B (ja)
IE (1) IE51216B1 (ja)
NZ (1) NZ196561A (ja)
PT (1) PT72796B (ja)

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