JP6258214B2 - 注射による誤用に対処可能な錠剤 - Google Patents
注射による誤用に対処可能な錠剤 Download PDFInfo
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- JP6258214B2 JP6258214B2 JP2014545260A JP2014545260A JP6258214B2 JP 6258214 B2 JP6258214 B2 JP 6258214B2 JP 2014545260 A JP2014545260 A JP 2014545260A JP 2014545260 A JP2014545260 A JP 2014545260A JP 6258214 B2 JP6258214 B2 JP 6258214B2
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- 229960000805 nalbuphine Drugs 0.000 description 1
- NETZHAKZCGBWSS-CEDHKZHLSA-N nalbuphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]1(O)CC[C@@H]3O)CN2CC1CCC1 NETZHAKZCGBWSS-CEDHKZHLSA-N 0.000 description 1
- OHKCLOQPSLQCQR-MBPVOVBZSA-N nalmexone Chemical compound O([C@H]1C(CC[C@]23O)=O)C4=C5[C@@]12CCN(CC=C(C)C)[C@@H]3CC5=CC=C4O OHKCLOQPSLQCQR-MBPVOVBZSA-N 0.000 description 1
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- 229960004708 noscapine Drugs 0.000 description 1
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- 229960001027 opium Drugs 0.000 description 1
- 235000019629 palatability Nutrition 0.000 description 1
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- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 235000014214 soft drink Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 229960004739 sufentanil Drugs 0.000 description 1
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical compound C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 238000009492 tablet coating Methods 0.000 description 1
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- 229910052623 talc Inorganic materials 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
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Classifications
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2893—Tablet coating processes
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
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Description
- 薬物耽溺目的で誤用されうる少なくとも1種類の有効成分、
- ポリビニルアセテートとポリビニルピロリドンの混合物、
- キサンタンガム、
- カルボマーおよび/またはアラビアガム
を含んでなる徐放性錠剤形態の経口医薬組成物である。
本発明において、「徐放性」とは、2回の一日用量または単回の一日用量のいずれかで有効成分の投与を可能とする、6時間より長い時間、好ましくは8時間より長い時間、さらには24時間より長い時間にわたる身体への1以上の有効成分の放出を意味する。
- (a)鼻腔および/または咽頭経路を刺激する物質;
- (b)薬物耽溺手段に誤用されうる有効成分の拮抗薬;
- (c)催吐薬物質;
- (d)嫌悪剤としての着色剤;および
- (e)苦味物質;
のうち少なくとも1つまたはそれらの混合物をさらに含んでなり得る。
用語「マトリックス」は、内部構造が組成物の中心から周辺まで均質かつ同一である医薬組成物を表して用いる。
- ポリビニルアセテートとポリビニルピロリドンの混合物;
- キサンタンガム;ならびに
- カーボポールおよび/またはアラビアガム
と混合し、次にこの混合物を打錠する。
- 有効成分をマトリックスの賦形剤と混合すること;
- 所望により造粒すること;および
- 前記混合物を、錠剤が少なくとも4MPa、有利には少なくとも6MPaの耐破砕性を有するように選択した条件下で打錠すること;
- 場合により前記錠剤をコーティングすること
を含んでなる。
剤形中に含まれる有効成分と処方物の一部の賦形剤の間、または処方物の2つの有効成分の間の化学的適合性の問題を克服するために、剤形は有利には多層形態とすることができる。よって、化学的に適合しない成分は分離することができ、例えば、キサンタンガムは有効成分を伴う層に含み、カルボマーは別の層に含むことができる。
「マイクロ錠」とは、直径4mm未満の錠剤を意味する。
実施例10では、実施例9の集団1および2と同一組成の2集団を下記のように(集団1のマイクロ錠10と集団2のマイクロ錠1個)関係づけて、下記の単位組成物を得た(カプセル剤1個の含量)。
Claims (24)
- - 薬物耽溺目的で誤用されうる少なくとも1種類の有効成分、
- 組成物の総重量の20〜60重量%の、ポリビニルアセテートとポリビニルピロリドンとの混合物であって、ポリビニルアセテートとポリビニルピロリドンとの比が80:20である混合物、
- 組成物の総重量の5〜30重量%のキサンタンガム、
- 組成物の総重量の5〜40重量%のカルボマー
を含有する、徐放性錠剤の形態の経口医薬組成物。 - 前記有効成分が、向精神薬、抗精神病薬、精神安定薬、催眠薬、鎮痛薬および抗不安薬を含んでなる群から選択されるものである、請求項1に記載の医薬組成物。
- 前記有効成分が、モルヒネ、オキシコドン、ヒドロコドン、ヒドロモルホン、オキシモルフォン、トラマドール、メタドン、コデイン、フェンタニルおよびブプレノルフィン、カンナビノイド、コカイン、アンフェタミン、ならびにそれらの薬学上許容される塩を含んでなる群に属する、請求項1または2に記載の医薬組成物。
- pH安定剤を含んでなる、請求項1〜3のいずれか一項に記載の医薬組成物。
- 組成物の総重量の0.1〜30重量%のpH安定剤を含んでなる、請求項1〜4のいずれか一項に記載の医薬組成物。
- 組成物の総重量の1〜10重量%のpH安定剤を含んでなる、請求項1〜5のいずれか一項に記載の医薬組成物。
- 下記物質(a)〜(e):
a)鼻腔および/または咽頭経路を刺激する物質;
b)催吐薬物質;
c)嫌悪着色剤;
d)苦味物質;
e)薬物耽溺目的で誤用されうる有効成分の拮抗薬
のうち少なくとも1以上またはそれらの混合物をさらに含んでなる、請求項1〜6のいずれか一項に記載の医薬組成物。 - 薬物耽溺目的で誤用されうる前記有効成分の拮抗薬が、ナロキソンもしくはナルトレキソンまたはそれらの薬学上許容される塩の1つである、請求項7に記載の医薬組成物。
- 外被を有する、請求項1〜8のいずれか一項に記載の医薬組成物。
- 前記外被が、エチルセルロース誘導体およびメタクリルポリマーの群から選択される少なくとも1種類の徐放性ポリマーから形成される、請求項9に記載の医薬組成物。
- エチルセルロースの外被を含んでなる、請求項9または10に記載の医薬組成物。
- マトリックス錠、多層錠またはマイクロ錠の形態である、請求項1〜11のいずれか一項に記載の医薬組成物。
- 付着防止剤、打錠時に錠剤の凝集性を改善しうる薬剤、増量剤、滑沢剤、可塑剤、充填剤、甘味剤および着色剤を含んでなる群から選択される少なくとも1種類の薬学上許容される賦形剤を含んでなる、請求項12に記載のマトリックス錠。
- 薬物耽溺目的の注射による誤用に対処するために使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 薬物耽溺目的の鼻腔経路を介した誤用に対処するための医薬として使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 薬物耽溺目的の経口経路を介した誤用に対処するための医薬として使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 不慮の誤用に対処するための医薬として使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 1日1回投与しうる医薬として使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 1日2回投与しる医薬として使用するための、請求項1〜13のいずれか一項に記載の医薬組成物。
- 下記の工程:
- 有効成分をマトリックスの賦形剤と混合すること;
- 所望により造粒すること;および
- 前記混合物を、錠剤が少なくとも4MPaの耐破砕性を有するように選択した条件下で打錠すること
を含んでなる、請求項12または13に記載のマトリックス錠を製造する方法。 - 前記錠剤が少なくとも6MPaの耐破砕性を有する、請求項20に記載の方法。
- 打錠工程が、実際の打錠工程の前または打錠工程中に、打錠する混合物または打錠工具を加熱工程に曝さずに行われる、請求項20または21に記載の方法。
- 前記マトリックス錠をコーティングする工程をさらに含んでなる、請求項20および22のいずれか一項に記載の方法。
- 前記外被の硬化工程をさらに含んでなる、請求項23に記載の方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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FR1161249A FR2983409B1 (fr) | 2011-12-06 | 2011-12-06 | Comprime susceptible de lutter contre le detournement par voie injectable |
FR1161249 | 2011-12-06 | ||
PCT/EP2012/074671 WO2013083710A1 (fr) | 2011-12-06 | 2012-12-06 | Comprime susceptible de lutter contre le detournement par voie injectable |
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EP (1) | EP2787980B1 (ja) |
JP (1) | JP6258214B2 (ja) |
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ES (1) | ES2702328T3 (ja) |
FR (1) | FR2983409B1 (ja) |
HK (1) | HK1202797A1 (ja) |
IL (1) | IL232966B (ja) |
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CA2919892C (en) | 2013-08-12 | 2019-06-18 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
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EP3210630A1 (en) * | 2016-02-29 | 2017-08-30 | G.L. Pharma GmbH | Abuse-deterrent pharmaceutical compositions |
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ES2292775T3 (es) * | 2001-07-06 | 2008-03-16 | Penwest Pharmaceuticals Co. | Formulaciones de liberacion prolongada de oximorfona. |
DE20220917U1 (de) * | 2001-08-06 | 2004-08-19 | Euro-Celtique S.A. | Zusammensetzungen zur Verhinderung des Missbrauchs von Opioiden |
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Also Published As
Publication number | Publication date |
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EP2787980B1 (fr) | 2018-10-24 |
US20140322321A1 (en) | 2014-10-30 |
FR2983409A1 (fr) | 2013-06-07 |
CN104080445A (zh) | 2014-10-01 |
IL232966B (en) | 2020-04-30 |
US10987309B2 (en) | 2021-04-27 |
ES2702328T3 (es) | 2019-02-28 |
JP2015500264A (ja) | 2015-01-05 |
HK1202797A1 (en) | 2015-10-09 |
FR2983409B1 (fr) | 2013-12-27 |
CA2858331C (fr) | 2020-06-16 |
AU2012347200A8 (en) | 2014-08-07 |
IL232966A0 (en) | 2014-07-31 |
WO2013083710A1 (fr) | 2013-06-13 |
CN104080445B (zh) | 2018-01-02 |
ZA201404108B (en) | 2015-11-25 |
AU2012347200A1 (en) | 2014-07-17 |
CA2858331A1 (fr) | 2013-06-13 |
EP2787980A1 (fr) | 2014-10-15 |
AU2012347200B2 (en) | 2017-11-09 |
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