JP6626492B2 - コハク酸メトプロロールのカプセル剤形 - Google Patents
コハク酸メトプロロールのカプセル剤形 Download PDFInfo
- Publication number
- JP6626492B2 JP6626492B2 JP2017501201A JP2017501201A JP6626492B2 JP 6626492 B2 JP6626492 B2 JP 6626492B2 JP 2017501201 A JP2017501201 A JP 2017501201A JP 2017501201 A JP2017501201 A JP 2017501201A JP 6626492 B2 JP6626492 B2 JP 6626492B2
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- Prior art keywords
- sustained release
- cellulose
- water
- capsule
- core
- Prior art date
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- 239000002775 capsule Substances 0.000 title claims description 35
- RGHAZVBIOOEVQX-UHFFFAOYSA-N Metoprolol succinate Chemical compound OC(=O)CCC(O)=O.COCCC1=CC=C(OCC(O)CNC(C)C)C=C1.COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 RGHAZVBIOOEVQX-UHFFFAOYSA-N 0.000 title claims description 31
- 229960000939 metoprolol succinate Drugs 0.000 title claims description 21
- 239000002552 dosage form Substances 0.000 title description 31
- 238000013268 sustained release Methods 0.000 claims description 43
- 239000012730 sustained-release form Substances 0.000 claims description 43
- 239000000203 mixture Substances 0.000 claims description 24
- 239000006185 dispersion Substances 0.000 claims description 15
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- 229920003176 water-insoluble polymer Polymers 0.000 claims description 9
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group 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 claims description 7
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- 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 claims description 4
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- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 4
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- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 claims description 2
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- 229920000881 Modified starch Polymers 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 229920003144 amino alkyl methacrylate copolymer Polymers 0.000 claims description 2
- 239000008103 glucose Substances 0.000 claims description 2
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 4
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- 229960002237 metoprolol Drugs 0.000 description 4
- IUBSYMUCCVWXPE-UHFFFAOYSA-N metoprolol Chemical compound COCCC1=CC=C(OCC(O)CNC(C)C)C=C1 IUBSYMUCCVWXPE-UHFFFAOYSA-N 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
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- 235000019814 powdered cellulose Nutrition 0.000 description 1
- 235000011962 puddings Nutrition 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 235000015067 sauces Nutrition 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 229940083037 simethicone Drugs 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 229940083575 sodium dodecyl sulfate Drugs 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 239000001959 sucrose esters of fatty acids Substances 0.000 description 1
- 235000010965 sucrose esters of fatty acids Nutrition 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000019270 symptomatic heart failure Diseases 0.000 description 1
- 239000004149 tartrazine Substances 0.000 description 1
- UJMBCXLDXJUMFB-GLCFPVLVSA-K tartrazine Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1\N=N\C1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-GLCFPVLVSA-K 0.000 description 1
- 229960000943 tartrazine Drugs 0.000 description 1
- 235000012756 tartrazine Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 235000010215 titanium dioxide Nutrition 0.000 description 1
- 229960002622 triacetin Drugs 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 235000013618 yogurt Nutrition 0.000 description 1
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
- A61J3/00—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
- A61J3/07—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of capsules or similar small containers for oral use
- A61J3/071—Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of capsules or similar small containers for oral use into the form of telescopically engaged two-piece capsules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
- A61K9/5078—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Public Health (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Inorganic Chemistry (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
a)不活性コア、
b)コハク酸メトプロロールを含み、不活性コアを覆う薬剤層、及び
c)薬剤層を覆う徐放性層
を含む。
a)コハク酸メトプロロールの溶液又は分散体を用いて不活性コアを被覆して、薬剤層被覆コアを得る工程、
b)徐放性ポリマーの溶液又は分散体を用いて、工程a)の薬剤層被覆コアを被覆する工程、及び
c)工程b)の徐放性コアを、適切なサイズのカプセル内に充填する工程、
を含む。
1)コハク酸メトプロロール及びオパドライ(登録商標)クリアを精製水に添加して、分散体を形成させた。
2)工程1)の分散体を糖球の上に噴霧して、薬剤被覆コアを形成した。
3)エチルセルロースをイソプロピルアルコール及び精製水中に分散させた。
4)ヒドロキシプロピルメチルセルロース、タルク、及びクエン酸トリエチルを、工程3)の分散体中へ添加した。
5)工程4)の分散体を工程2)の薬剤被覆コアの上に噴霧して、徐放性の分散単位を形成した。
6)工程5)の単位を、タルクで潤滑した。
7)工程6)の潤滑した徐放性の分散単位を、サイズ4のカプセル殻内に充填した。
実施例1で調製したカプセル及びToprol−XL(登録商標)錠剤を使用して、溶解試験を実施した。
ソフトウェアPhoenix WinNonlin(登録商標)6.4及びPhoenix IVIVC Toolkit2.2を使用して、実施例1の薬物動態プロファイル(Cmax及びAUC)を予測した。予測された実施例1の薬物動態値を、摂食条件下及び絶食条件下で、Toprol−XL(登録商標)錠剤の薬物動態値と比較した。表2は、シミュレーションによる実施例1の生物学的同等性のデータを示す。
Claims (8)
- 被覆された分散単位の形態である、コハク酸メトプロロールの徐放性カプセル剤であって、前記被覆された分散単位が、
a)不活性コア、
b)コハク酸メトプロロールを含み、不活性コアを覆う薬剤層、及び
c)前記薬剤層被覆コアを覆う徐放性層
を含み、
前記徐放性層が、水溶性又は水不溶性ポリマーを含み、且つ、薬剤層被覆コアの重量に基づき、5%から20%の量で存在し、
前記不活性コアが水溶性コアを含み、
前記コハク酸メトプロロールは、前記カプセル剤の総重量の約30%から約70%の量で存在し、
前記カプセルがスプリンクルカプセルの形態である、徐放性カプセル剤。 - 前記水溶性コアが、糖、微結晶セルロース、セルロース、デンプン、加工デンプン、又はそれらの混合物で構成される、請求項1記載の徐放性カプセル剤。
- 前記糖が、グルコース、マンニトール、ラクトース、キシリトール、デキストロ―ス、及びスクロースからなる群から選択される、請求項2記載の徐放性カプセル剤。
- 前記水溶性のポリマーが、ヒドロキシプロピルメチルセルロース、ヒドロキシエチルセルロース、ポリエチレングリコール、ポリ(エチレンオキシド)、ヒドロキシプロピルセルロース、カルボキシメチルセルロース、キサンタンガム、デンプン、及びそれらの混合物からなる群から選択される、請求項1記載の徐放性カプセル剤。
- 前記水不溶性ポリマーが、セルロースエーテル、セルロースエステル、ポリメタクリル酸エステル共重合体、アミノアルキルメタクリレート共重合体、ポリ酢酸ビニルとポリビニルピロリドンとの共重合体、及びそれらの混合物からなる群から選択される、請求項1記載の徐放性カプセル剤。
- 前記セルロースエーテルがエチルセルロースである、請求項5記載の徐放性カプセル剤。
- 前記水不溶性のポリマーが細孔形成剤を更に含む、請求項5記載の徐放性カプセル剤。
- 前記細孔形成剤が、低粘度等級のヒドロキシプロピルメチルセルロース、アルギン酸ナトリウム、糖及び糖アルコール、低分子量ポリエチレングリコール、ポリビニルアルコール、並びにそれらの混合物からなる群から選択される、請求項7記載の徐放性カプセル剤。
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US201462022316P | 2014-07-09 | 2014-07-09 | |
US62/022,316 | 2014-07-09 | ||
PCT/IB2015/055195 WO2016005934A1 (en) | 2014-07-09 | 2015-07-09 | Capsule dosage form of metoprolol succinate |
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JP2017523164A JP2017523164A (ja) | 2017-08-17 |
JP6626492B2 true JP6626492B2 (ja) | 2019-12-25 |
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US (1) | US9504655B2 (ja) |
EP (1) | EP3166599A4 (ja) |
JP (1) | JP6626492B2 (ja) |
AU (1) | AU2015287299A1 (ja) |
BR (1) | BR112017000468A2 (ja) |
CA (1) | CA2954474C (ja) |
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EP3768378A4 (en) | 2018-03-22 | 2021-11-17 | InCarda Therapeutics, Inc. | INNOVATIVE METHOD OF SLOWING THE VENTRICULAR RATE |
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US5246714A (en) | 1985-10-11 | 1993-09-21 | Aktiebolaget Hassle | Drug preparation |
US6156342A (en) * | 1998-05-26 | 2000-12-05 | Andex Pharmaceuticals, Inc. | Controlled release oral dosage form |
HUP0303886A3 (en) * | 2001-12-19 | 2005-05-30 | Astrazeneca Ab | New film coating composition for coating of pharmaceutical compositions |
SE0201110D0 (sv) * | 2002-04-12 | 2002-04-12 | Astrazeneca Ab | New film coating |
US7314640B2 (en) * | 2003-07-11 | 2008-01-01 | Mongkol Sriwongjanya | Formulation and process for drug loaded cores |
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US20070009589A1 (en) * | 2005-07-07 | 2007-01-11 | Kandarapu Raghupathi | Extended release compositions |
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WO2009087663A2 (en) * | 2007-11-30 | 2009-07-16 | Sun Pharmaceutical Industries Ltd. | Oral controlled release coated tablet |
CA2775111C (en) * | 2009-09-25 | 2019-12-31 | Opko Curna, Llc | Treatment of filaggrin (flg) related diseases by modulation of flg expression and activity |
AR091857A1 (es) * | 2012-07-25 | 2015-03-04 | Sova Pharmaceuticals Inc | INHIBIDORES DE CISTATIONIN-g-LIASA (CSE) |
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EP3166599A4 (en) | 2017-12-20 |
US9504655B2 (en) | 2016-11-29 |
WO2016005934A1 (en) | 2016-01-14 |
US20160143856A1 (en) | 2016-05-26 |
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