JP2016074697A - 過活動膀胱の治療のための医薬製剤 - Google Patents
過活動膀胱の治療のための医薬製剤 Download PDFInfo
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- JP2016074697A JP2016074697A JP2015227923A JP2015227923A JP2016074697A JP 2016074697 A JP2016074697 A JP 2016074697A JP 2015227923 A JP2015227923 A JP 2015227923A JP 2015227923 A JP2015227923 A JP 2015227923A JP 2016074697 A JP2016074697 A JP 2016074697A
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- DHRXPBUFQGUINE-UHFFFAOYSA-N n-(2-hydroxypropyl)benzenesulfonamide Chemical compound CC(O)CNS(=O)(=O)C1=CC=CC=C1 DHRXPBUFQGUINE-UHFFFAOYSA-N 0.000 description 1
- FGTVYMTUTYLLQR-UHFFFAOYSA-N n-ethyl-1-phenylmethanesulfonamide Chemical compound CCNS(=O)(=O)CC1=CC=CC=C1 FGTVYMTUTYLLQR-UHFFFAOYSA-N 0.000 description 1
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- 229960002016 oxybutynin chloride Drugs 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- JQCXWCOOWVGKMT-UHFFFAOYSA-N phthalic acid diheptyl ester Natural products CCCCCCCOC(=O)C1=CC=CC=C1C(=O)OCCCCCCC JQCXWCOOWVGKMT-UHFFFAOYSA-N 0.000 description 1
- 229960001963 pilocarpine nitrate Drugs 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229920002959 polymer blend Polymers 0.000 description 1
- 239000011148 porous material Substances 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- AMMPRZCMKXDUNE-UHFFFAOYSA-N trihexyl 2-hydroxypropane-1,2,3-tricarboxylate Chemical compound CCCCCCOC(=O)CC(O)(C(=O)OCCCCCC)CC(=O)OCCCCCC AMMPRZCMKXDUNE-UHFFFAOYSA-N 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
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Abstract
Description
本出願は、その全体が参照によって本明細書に組み入れられる、「過活動膀胱の治療のための医薬製剤」と題するMehdi Paborjiにより2010年4月1日に出願された米国特許仮出願番号61/320,202に対して優先権を主張する。
ムスカリン作動薬ビーズ
芯部と
ピロカルピン、セビメリン又は薬学上許容可能なその塩を含む第1の層と
第1のポリマーを含む第2の層をそれぞれ含む複数の第1のビーズを含む医薬組成物である。
ムスカリン拮抗剤ビーズ
芯部と
ムスカリン拮抗剤又は薬学上許容可能なその塩を含む第1の層
をそれぞれ含む複数の第2のビーズを含む医薬組成物である。
医薬製剤
の1つを含む医薬製剤である。
実施例
実施例1:ビーズ製造工程で使用される材料
溶出媒体:0.1NのHCl
攪拌速度:50rpm
容器温度:37℃±0.5℃
試料体積:1.0ml
溶出体積:500ml
実施例3:ビーズ製剤
実施例4:ビーズの形成
実施例7:ムスカリン拮抗剤のビーズ製剤
Claims (21)
- 医薬組成物であって、
芯部;
ピロカルピン又は薬学上許容可能なその塩を含む第1の層;および
ヒドロキシプロピルセルロースおよびエチルセルロースを含む第2の層
をそれぞれ含む複数の第1のビーズを含み、
前記第2の層の重量は、前記第2の層を塗布する前の前記第1のビーズの重量の約75%〜約250%の間である、
医薬組成物。 - 前記ヒドロキシプロピルセルロースとエチルセルロースの比が、重量で約1:1である、請求項1に記載の医薬品組成物。
- 前記複数の第1のビーズが、0.1NのHCl中に20分間浸漬させたとき、前記組成物中の当初の量のピロカルピンまたは薬学上許容可能なその塩の20%未満を放出し、前記複数の第1のビーズが、前記0.1NのNCl中に浸漬して前記20%未満の量のピロカルピンまたは薬学上許容可能なその塩を放出した後30分の時点で、前記組成物中の当初の量の90%より多くのピロカルピンまたは薬学上許容可能なその塩を放出する、請求項1に記載の医薬品組成物。
- さらにオキシブチニンまたは薬学上許容可能なその塩を含む、請求項1に記載の医薬品組成物。
- 芯部が、セルロースポリマー又は二酸化珪素、又はグルコース、スクロース、ラクトース、マンニトール、キシリトール及びソルビトールから成る群から選択される糖を含む請求項1の医薬組成物。
- 芯部が、最終的に製剤化されるビーズの総重量の約10%〜約50%の間を構成する求項1の医薬組成物。
- 第1の層が、ビーズの総重量の約1%〜約50%の間を構成する請求項1の医薬組成物。
- ビーズが、タルク、モノステアリン酸グリセリル、ステアリン酸カルシウム及びステアリン酸マグネシウムから成る群から選択される粘着性消失剤又は滑剤をさらに含む請求項1の医薬組成物。
- ビーズが、フタル酸系可塑剤、トリメリテート、アジピン酸系可塑剤、セバシン酸系可塑剤、オルガノホスフェート、マレエート、スルホンアミド、グリコール又はポリエーテル、アセチル化モノグリセリド、及びクエン酸アルキルから成る群から選択される可塑剤をさらに含む請求項1の医薬組成物。
- 第1の層が、ベヘン酸グリセリル、脂肪酸のグリセリルエステル、ジベヘン酸グリセリル、ベヘノイルマクロゴグリセリド、ジステアリン酸グリセリル、ジステアリン酸グリセロール、パルミトステアリン酸グリセリル、ラウロイルマクロゴグリセリド、ステアロイルマクロゴグリセリド、Abeitec製品、モノオレイン酸グリセリル、中鎖モノ−及びジ−グリセリド、モノカプリル酸グリセリル、トリカプリル酸/カプリン酸/ステアリン酸グリセリル、水素化植物油、水素化綿実油、水素化大豆油、水素化大豆油とヒマシ油ワックス、ポリオキシエチレン8カプリル酸/カプリン酸グリセリド、ポリオキシエチレン6カプリル酸/カプリン酸グリセリド、ポリオキシエチレン32ラウリン酸グリセリド、ポリオキシエチレン6プロップグリコールエステル、ポリオキシエチレン7ココナッツグリセリド、ポリオキシエチレン30ココナッツグリセリド、ポリオキシエチレン80ココナッツグリセリド、ポリオキシプロピレン15ステアリルエーテル、ポリオキシエチレン26グリセリルエーテル、ポリオキシエチレン35大豆グリセリド、ポリオキシエチレン20ソルビトール、ポリオキシプロピレン3ミリスチルエーテル、ポリオキシプロピレン10セトステアリルエーテル、パーム核油アミドジエタノールアミド、モノオレイン酸トリグリセロール、Sasol製品、水素化ココグリセリド、パルミチン酸セチル、トリミリスチン、トリパルミチン、トリステアリン、水素化パーム油、モノステアリン酸グリセリル、ステアリン酸グリセリル、セテアリールアルコール、セチルアルコール、カプリン酸トリグリセリド、アセチル化グリセリド、グリセリルココエート、及びポリエチレングリコールから成る群から選択される脂質賦形剤をさらに含む請求項1の医薬組成物。
- 医薬製剤であって、
複数の第1のビーズおよび複数の第2のビーズを含み、
前記第1のビーズは、それぞれ、
芯部;
ピロカルピンまたは薬学上許容可能なその塩を含む第1の層;および
ヒドロキシプロピルセルロースおよびエチルセルロースを含む第2の層
を含み、
前記第2の層の重量は、前記第2の層を塗布する前の前記第1のビーズの重量の約75%〜約250%の間であり、
前記第2のビーズは、それぞれ、
芯部;および
ムスカリン拮抗剤または薬学上許容可能なその塩を含む第1の層
を含む、
前記医薬製剤。 - 前記芯部のそれぞれが、セルロースポリマー;二酸化珪素;又は、グルコース、スクロース、ラクトース、マンニトール、キシリトール及びソルビトールから成る群から選択される糖を含む、請求項11の医薬組成物。
- 前記芯部のそれぞれが、最終的に製剤化されるビーズの総重量の約10%〜約90%の間を構成する求項11の医薬組成物。
- 前記第2のビーズのそれぞれの前記第1の層が、ビーズの総重量の約1%〜約50%を構成する請求項11の医薬組成物。
- 前記第1のビーズのそれぞれがさらに、
タルク、モノステアリン酸グリセリル、ステアリン酸カルシウム及びステアリン酸マグネシウムから成る群から選択される粘着性消失剤又は滑剤と
フタル酸系可塑剤、トリメリテート、アジピン酸系可塑剤、セバシン酸系可塑剤、オルガノホスフェート、マレエート、スルホンアミド、グリコール又はポリエーテル、アセチル化モノグリセリド、及びクエン酸アルキルから成る群から選択される可塑剤を
含む請求項11の医薬組成物。 - 前記第2のビーズのそれぞれが、可溶性の成膜性ポリマーを含む第2の層をさらに含む、請求項11の医薬組成物。
- 前記第2のビーズのそれぞれの前記第1の層が、ベヘン酸グリセリル、脂肪酸のグリセリルエステル、ジベヘン酸グリセリル、ベヘノイルマクロゴグリセリド、ジステアリン酸グリセリル、ジステアリン酸グリセロール、パルミトステアリン酸グリセリル、ラウロイルマクロゴグリセリド、ステアロイルマクロゴグリセリド、Abeitec製品、モノオレイン酸グリセリル、中鎖モノ−及びジ−グリセリド、モノカプリル酸グリセリル、トリカプリル酸/カプリン酸/ステアリン酸グリセリル、水素化植物油、水素化綿実油、水素化大豆油、水素化大豆油とヒマシ油ワックス、ポリオキシエチレン8カプリル酸/カプリン酸グリセリド、ポリオキシエチレン6カプリル酸/カプリン酸グリセリド、ポリオキシエチレン32ラウリン酸グリセリド、ポリオキシエチレン6プロップグリコールエステル、ポリオキシエチレン7ココナッツグリセリド、ポリオキシエチレン30ココナッツグリセリド、ポリオキシエチレン80ココナッツグリセリド、ポリオキシプロピレン15ステアリルエーテル、ポリオキシエチレン26グリセリルエーテル、ポリオキシエチレン35大豆グリセリド、ポリオキシエチレン20ソルビトール、ポリオキシプロピレン3ミリスチルエーテル、ポリオキシプロピレン10セトステアリルエーテル、パーム核油アミドジエタノールアミド、モノオレイン酸トリグリセロール、Sasol製品、水素化ココグリセリド、パルミチン酸セチル、トリミリスチン、トリパルミチン、トリステアリン、水素化パーム油、モノステアリン酸グリセリル、ステアリン酸グリセリル、セテアリールアルコール、セチルアルコール、カプリン酸トリグリセリド、アセチル化グリセリド、グリセリルココエート、及びポリエチレングリコールから成る群から選択される脂質賦形剤をさらに含む請求項11の医薬組成物。
- (a)0.5〜50mgの間の用量でのピロカルピン又は薬学上許容可能なその塩と
(b)0.1〜100mgの間の用量でのムスカリン拮抗剤又は薬学上許容可能なその塩を含む請求項11の医薬製剤。 - 前記ムスカリン拮抗剤が、オキシブチニンである、請求項18に記載の医薬製剤。
- 複数の第1のビーズおよび複数の第2のビーズを含有する医薬組成物であって、
前記第1のビーズのそれぞれが、
(i)セルロースポリマー;二酸化珪素;又は、グルコース、スクロース、ラクトース、マンニトール、キシリトール及びソルビトールからなる群から選択される糖を含む、芯部;
(ii)ピロカルピンまたは薬学上許容可能なその塩を含む第1の層;
(iii)ヒドロキシエチルセルロース、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、カルボキシメチルセルロース、マルトデキストリン、スクロース、修飾デンプン、アルギン酸の塩、カラギーナン、ポリビニルピロリドン(PVP)およびポリビニルポリピロリドン(PVPP)からなる群から選択される可溶性の成膜性ポリマー;および、エチルセルロース、セルロースアセテートフタレート、ヒドロキシプロピルメチルセルロースフタレート、不溶性のゴム、ポリメタクリレート、ポリビニルアルコール、セラック及びポリ酢酸フタル酸ビニルから成る群から選択される不溶性の成膜性ポリマー;および
(iv)タルク、モノステアリン酸グリセリル、ステアリン酸カルシウム及びステアリン酸マグネシウムから成る群から選択される粘着性消失剤又は滑剤
を含み、
前記芯部は、最終的に製剤化されたビーズの総重量の10%〜50%の間を構成し、
前記第1の層は、最終的に製剤化されたビーズの総重量の1%〜50%の間を構成し、
前記医薬品組成物は、前記ピロカルピンまたは薬学上許容可能なその塩を0.5〜50mgの間の用量で含み、および前記ムスカリン拮抗剤または薬学上許容可能なその塩を0.1〜100mgの間の用量で含む、
前記医薬品組成物。 - 前記第2のビーズがそれぞれ、
セルロースポリマー;二酸化珪素;又は、グルコース、スクロース、ラクトース、マンニトール、キシリトール及びソルビトールからなる群から選択される糖を含む芯部;および
ムスカリン拮抗剤または薬学上許容可能なその塩を含む第1の層
を含み、
前記芯部は、最終的に製剤化されたビーズの総重量の10%〜90%の間を構成し、および
前記第1の層は、最終的に製剤化されたビーズの総重量の1%〜50%の間を構成する、
請求項19に記載の医薬品組成物。
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