JP2008150395A - 医薬組成物 - Google Patents
医薬組成物 Download PDFInfo
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- JP2008150395A JP2008150395A JP2008049742A JP2008049742A JP2008150395A JP 2008150395 A JP2008150395 A JP 2008150395A JP 2008049742 A JP2008049742 A JP 2008049742A JP 2008049742 A JP2008049742 A JP 2008049742A JP 2008150395 A JP2008150395 A JP 2008150395A
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Abstract
【解決手段】アスコマイシンまたはアスコマイシン誘導体、例えばアスコマイシンまたは33−エピ−クロロ−33−デスオキシ−アスコマイシンを、担体媒体とともに固体分散体に製剤化することにより目的の医薬組成物を得た。
【選択図】図1
Description
−ヒドロキシプロピルセルロース(HPC)またはその誘導体(HPC誘導体の例は、水性媒体、例えば水中で、2%水性溶液中で25℃で測定して、例えば、約400cpsより低い、例えば150cpsより低い、低い動的粘度を有するものを含む。好ましいHPC誘導体は、低い置換の程度を有し、平均分子量は200,000ダルトンより低い、例えば、50,000から150,000ダルトンの間である。商品として入手可能なHPCの例は、Aqualon社から入手可能なKlucel LF、Klucel EFおよびKlucel JF;および日本ソーダから入手可能なNisso HPC−Lを含む);
−ポリエチレングリコール(PEG)(例は、1000から9000ダルトンの間、例えば約1800から7000の間の分子量を有するPEG、例えば、PEG2000、PEG4000またはPEG6000(Handbook of Pharmaceutical Excipients)を含む);
−例えば、Gattefosse社から商品名Gelucir、例えば、Gelucir 44/14、53/10、50/13、42/12または35/10で入手可能な飽和ポリグリコシル化グリセリド;または
−シクロデキストリン、例えば、β−シクロデキストリンまたはα−シクロデキストリン(適当なβ−シクロデキストリンの例はメチル−β−シクロデキストリン;ジメチル−β−シクロデキストリン;ヒドロキシプロピル−β−シクロデキストリン;グリコシル−β−シクロデキストリン;マルトシル−β−シクロデキストリン;スルフォ−β−シクロデキストリン;β−シクロデキストリンのスルフォ−アルキルエーテル、例えば、スルフォ−C1−4アルキルエーテルを含む。α−シクロデキストリンの例は、グルコシル−α−シクロデキストリンおよびマルトシル−α−シクロデキストリンを含む。)
を含む。
−例えば、その内容を引用して本明細書に包含させるFiedler, H. P. "Lexikon der Hilfsstoffe fuer Pharmazie, Kosmetik und Angrenzende Gebiete", Editio Cantor, D-7960 Aulendorf, 3rd revised and expanded edition(1989)に記載のような、商品名、PluronicまたはPoloxamerとして既知のような、ポリオキシエチレン−ポリオキシプロピレン−コポリマーおよびブロックコポリマー(好ましいポリオキシエチレン−ポリオキシプロピレンブロックポリマーは、BASF社から入手可能なPoloxamer 188である);
−例えば、Amerchol社から商品として入手可能なSolulan、例えばSolulan C24として既知のエトキシル化コレステリン;
−ビタミン誘導体、例えばEastman社から入手可能なトコフェロールポリエチレングリコールサクシネート(TPGS)のようなビタミンE誘導体;
−ドデシル硫酸ナトリウムまたはラウリル硫酸ナトリウム;
−胆汁酸またはその塩、例えばコール酸、グリコール酸またはその塩、例えば、コール酸ナトリウム;または
−レシチン
を含む。
a)例えば、心臓、肺、複合心肺、肝臓、腎臓、膵臓、皮膚または角膜移植片の受容者の処置のための臓器または組織の同種または異種移植拒絶反応の処置および予防。例えば、骨髄移植の後のような移植片対宿主病の予防もまた適用される。
b)自己免疫疾患および炎症性疾病、特に、関節炎(例えば、関節リウマチ、慢性進行性関節炎および変形関節炎)およびリウマチ疾患のような自己免疫要素を含む病因の炎症性疾病の処置および予防。本発明の化合物を使用し得る具体的自己免疫疾患は、自己免疫血液学的疾患(例えば、溶血性貧血、形成不全貧血、赤芽球癆および特発性血小板減少症を含む)、全身性エリテマトーデス、多軟骨炎、硬皮症、ウェゲナー肉芽腫、皮膚筋炎、慢性活動性肝炎、重症筋無力症、乾癬、スティーブン−ジョンソン症候群、特発性スプルー、自己免疫炎症性大腸炎(例えば、潰瘍性大腸炎およびクーロン病を含む)、内分泌性眼病、グレーブス病、結節炎、多発性硬化症、原発性胆汁性肝炎、若年性糖尿病(I型糖尿病)、ブドウ膜炎(前および後)、乾燥性角結膜炎および春季角結膜炎、間質性肺線維症、乾癬性関節炎、糸球体腎炎(例えば、特発性ネフローゼ症候群または微小変化ネフローゼ症候群を含むネフローゼ症候群有りおよび無し)および若年性皮膚筋炎を含む。
c)喘息の処置および予防。
d)多剤耐性(MDR)の処置。MDRは、医薬がPgpにより細胞からポンプ輸送で出てしまうため、慣用の化学療法に反応しない癌患者およびAIDS患者で特に問題である。この組成物は、従って、多剤耐性癌または多剤耐性AIDSのような多剤耐性疾病の処置および制御における多の化学療法剤の効果を促進するために有用である。
e)増殖性疾患、例えば、癌、過増殖性皮膚疾患等の処置。
f)真菌感染の処置。
g)炎症の処置および予防、特にステロイドの作用の強化。
h)感染、特にMipまたはMip様因子を有する病原体による感染の処置および予防。
i)FK−506および他のマクロフィリン結合性免疫抑制剤の過剰投与の処置。
a)
−例えば、心臓、腎臓、肝臓、骨髄および皮膚の臓器または組織移植の拒絶反応
−骨髄移植の後のような移植片対宿主病、
−関節リウマチ、全身性紅斑性狼瘡、橋本甲状腺炎、多発性硬化症、重症筋無力症、I型糖尿病およびぶどう膜炎のような自己免疫疾患、
−免疫学的媒介病気の皮膚兆候
の予防および処置
b)乾癬、アトピー性皮膚炎、接触性皮膚炎および更なる湿疹性皮膚炎、脂漏性皮膚炎、扁平苔癬、天疱瘡、水疱性類天疱瘡、表皮水疱症、蕁麻疹、血管性水腫、脈管炎、紅斑、皮膚好酸球増加症、紅斑性狼瘡およびアクネのような炎症性および過増殖性皮膚疾患の処置;および
c)円形脱毛症
のような炎症性疾病、および免疫抑制を必要とする疾病の予防および処置に使用するための抗炎症剤および免疫抑制剤および抗増殖剤として有用である。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物X 9.1
HPMC 3cps 81.8
ラクトース200メッシュ 9.1
組成物(製剤A)は、ラパマイシンおよび担体媒体をエタノール/アセトン混合物に溶解して製造する。無水エタノールは、アセトンと共に1:1重量比で使用する。溶媒を次いで蒸発させ、得られる乾燥残渣を、平均粒子サイズ<0.5mmの細粉末に挽く。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物X 16.7
HPMC 3cps 66.7
Poloxamer 188(BASFから) 16.7
組成物(製剤B)は、実施例1と同様の方法で製造する。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物X 16.7
HPMC 3cps 66.7
TPGS* 16.7
組成物(製剤C)は、実施例1と同様の方法で製造する。
*トコフェロールポリエチレングリコールサクシネート
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物X 10
HPMC 3cps 80
Solulan C24(Amercholから) 10
組成物(製剤D)は、実施例1と同様の方法で製造する。
上記製剤AからDは、錠剤に成形し、カプセルへ充填しまたは粉末化しサシェットにパッケージし得る。
a)医薬投与
化合物X組成物の水性分散体0.5ml(4.0mg活性成分/ラットに対応)を、ポリエチレン管に結合した1mlシリンジで、短吸入麻酔間に胃内挿管法で投与した。6匹の動物を、各組成物製剤A、B、CおよびDで使用した。
b)採血
動物は、この実験の一日前に、頸静脈に永久カニューレを装着された。0.5ml静脈血(頸静脈)を各ラットから回収し、2.5ml EDTA管に貯蔵した。2匹の動物(1と2、3と4、5と6)の血液サンプルを貯蔵し、分析まで−80℃で貯蔵した。サンプルを投与前、投与後10分、30分、60分、120分、300分、480分および1440分に取った。
c)生物分析
血液サンプルを逆相HPLCを使用して分析した。
表1は、ラットに化合物Xを投与した後に回収した薬物動態データを示す。
上記の見込みのある結果に続いて、相対的生物学的利用能の検討を、絶食ビーグル犬で、1mg/kg体重の投与量を使用して行った。それぞれ化合物X 10mg含有する硬ゼラチンカプセルを、8匹のイヌに、4方向ラテンスフェアデザインで投与した;イヌにカプセル投与6時間後に食事を与え、化合物Xの濃度を48時間にわたり測定した。化合物Xの同様の血中濃度プロフィールが全てのイヌで見られ、血中の化合物Xの最終半減期は10から40時間の間であった。平均ピークレベル140ng/mlおよび約1600ng.時間/mlの0−48時間の平均AUCレベルが観察された。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物Y 20
HPMC 3cps 80
組成物(製剤E)は、化合物Yおよび担体媒体をエタノール/アセトン混合物に溶解して製造する。溶媒を次いで蒸発させ、得られる乾燥残渣を挽く。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物Y 20
HPMC 3cps 70
Poloxamer 188 10
組成物(製剤F)は、実施例5と同様の方法で製造する。
以下の成分を含む固体分散体組成物を製造する(重量部):
化合物Y 20
HPMC 3cps 75
ラウリルスルホン酸ナトリウム 5
組成物(製剤G)は、実施例5と同様の方法で製造する。
上記製剤EからGは、錠剤に成形し、カプセルへ充填しまたは粉末化しサシェットにパッケージし得る。
a)医薬投与
医薬組成物の水性分散体0.5ml(4.0mg活性成分/ラットに対応)を、ポリエチレン管に結合した1mlシリンジで、短吸入麻酔間に胃内挿管法で投与した。6匹の動物を、各組成物製剤E、FおよびGで使用した。
b)採血
動物は、この実験の一日前に、頸静脈に永久カニューレを装着された。0.5ml静脈血(頸静脈)を各ラットから回収し、2.5ml EDTA管に貯蔵した。2匹の動物(1と2、3と4、5と6)の血液サンプルを貯蔵し、分析まで−80℃で貯蔵した。サンプルを投与前、投与後10分、30分、60分、120分、300分、480分および1440分に取った。
c)生物分析
血液サンプルを逆相HPLCを使用して分析した。
結果を図1および2にプロットし、その中でng/ml(垂直軸)が時間(水平軸)に対してプロットされている。
図1は、製剤Fが、製剤Eまたは製剤Gの投与後に観察される血中レベルよりも実質的に高い血中レベルをもたらすことを示す。
図2は、製剤Fが、餌と共に投与した時、高い血中レベルをもたらすことを示す。
化合物Yは、X線解析で測定して、組成物E、FおよびG中で、製剤中および6カ月貯蔵後に無定形の形である。
製剤E、FおよびGの、相対的溶解速度を試験する。37℃での撹拌したドデシル硫酸ナトリウムの0.2重量%水溶液において、30分後に、10mg化合物Yを含むそれぞれの挽いた組成物から、80%を越える利用可能な化合物Yが放出され、溶解することが判明する。92%の利用可能な組成物Yが製剤Eから放出される。これは、当量の結晶性化合物Yからの30分後の約5%放出に匹敵する。
Claims (34)
- 33−エピ−クロロ−33−デスオキシ−アスコマイシンおよび担体媒体を含む固体分散体の形態の経口投与用医薬組成物。
- 担体媒体が水溶性ポリマーまたはシクロデキストリンを含む、請求項1に記載の組成物。
- 水溶性ポリマーがヒドロキシプロピルメチルセルロースである、請求項2に記載の組成物。
- 水溶性ポリマーがポリビニルピロリドンである、請求項2に記載の組成物。
- 組成物の全重量に対して30重量%以下の33−エピ−クロロ−33−デスオキシ−アスコマイシンを含む、請求項1〜4のいずれかに記載の組成物。
- 組成物がさらに界面活性剤を含む、請求項1〜5のいずれかに記載の組成物。
- 界面活性剤がポリオキシエチレン−ポリオキシプロピレンコポリマーまたはブロックコポリマーである、請求項6に記載の組成物。
- 組成物の全重量に対して20重量%以下の界面活性剤を含む、請求項6または7に記載の組成物。
- 組成物が界面活性剤を含まない、請求項1〜5のいずれかに記載の組成物。
- 水溶性ポリマーが組成物の全重量に対して95重量%以下のヒドロキシプロピルメチルセルロースである、請求項2〜9のいずれかに記載の組成物。
- 33−エピ−クロロ−33−デスオキシ−アスコマイシン対担体の重量比が1:4より小さい、請求項2〜9のいずれかに記載の組成物。
- ポリマーがポリビニルピロリドンを含む、請求項2〜7のいずれかに記載の組成物。
- 33−エピ−クロロ−33−デスオキシ−アスコマイシンが無定形または実質的に無定形である、請求項1〜12のいずれかに記載の組成物。
- 組成物がさらにラクトースを含む、請求項1〜13のいずれかに記載の組成物。
- 単位投与形の請求項1〜14のいずれかに記載の組成物。
- カプセルまたは錠剤の請求項1〜15のいずれかに記載の組成物。
- さらに腸溶性コーティングを含む、請求項15または16に記載の組成物。
- さらに抗酸化剤を含む、請求項1〜17のいずれかに記載の組成物。
- 抗酸化剤がブチル化ヒドロキシトルエン、DL−α−トコフェロール、プロピルガレート、アスコルビルパルミテートおよびギ酸からなる群から選択される、請求項18に記載の組成物。
- 組成物がさらに分解剤を含む、請求項1〜19のいずれかに記載の組成物。
- 組成物がさらに滑沢剤を含む、請求項1〜20のいずれかに記載の組成物。
- さらに水溶性サッカロースを含む、請求項1〜21のいずれかに記載の組成物。
- さらに微結晶性セルロースを含む、請求項1〜22のいずれかに記載の組成物。
- 炎症性もしくは過増殖性皮膚疾患の処置または予防用薬剤の製造のための、請求項1〜23のいずれかに記載の組成物の使用。
- 33−エピ−クロロ−33−デスオキシ−アスコマイシンおよび担体媒体を含む医薬組成物の製造方法であって、
(a)溶媒中に33−エピ−クロロ−33−デスオキシ−アスコマイシンを懸濁させて懸濁液を製造すること、
(b)1またはそれ以上の担体成分を該溶媒と組み合せること、および
(c)該懸濁液をスプレー乾燥し、医薬組成物を製造すること、
を含む方法。 - 続いて医薬組成物を単位投与形に成形する請求項25に記載の方法。
- 続いて医薬組成物を錠剤に成形するか、またはカプセルに充填する、請求項25または26に記載の方法。
- 33−エピ−クロロ−33−デスオキシ−アスコマイシンをスプレー乾燥によって固体分散体に成形する、請求項25に記載の方法。
- 溶媒が有機溶媒または有機溶媒の混合物である、請求項25に記載の方法。
- 担体成分がポリオキシエチレン−ポリオキシプロピレンコポリマーまたはブロックコポリマーを含む、請求項25〜29のいずれかに記載の方法。
- 担体成分がポリビニルピロリドンを含む、請求項25〜30のいずれかに記載の方法。
- 担体成分が微結晶性セルロースを含む、請求項25〜31のいずれかに記載の方法。
- 担体成分が水溶性サッカロースを含む、請求項25〜32のいずれかに記載の方法。
- 担体成分がラクトースを含む、請求項25〜32のいずれかに記載の方法。
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GBGB9514397.0A GB9514397D0 (en) | 1995-07-14 | 1995-07-14 | Organic compounds |
GB9514397.0 | 1995-07-14 | ||
GBGB9515025.6A GB9515025D0 (en) | 1995-07-21 | 1995-07-21 | Organic compounds |
GB9515025.6 | 1995-07-21 |
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JP2003273402A Withdrawn JP2004002457A (ja) | 1995-07-14 | 2003-07-11 | 医薬組成物 |
JP2008049742A Expired - Lifetime JP5522901B2 (ja) | 1995-07-14 | 2008-02-29 | 医薬組成物 |
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JP2003273402A Withdrawn JP2004002457A (ja) | 1995-07-14 | 2003-07-11 | 医薬組成物 |
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