JP2020532517A - 高濃度プリドピジン製剤 - Google Patents
高濃度プリドピジン製剤 Download PDFInfo
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- JP2020532517A JP2020532517A JP2020511937A JP2020511937A JP2020532517A JP 2020532517 A JP2020532517 A JP 2020532517A JP 2020511937 A JP2020511937 A JP 2020511937A JP 2020511937 A JP2020511937 A JP 2020511937A JP 2020532517 A JP2020532517 A JP 2020532517A
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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Abstract
Description
本出願は、2017年8月30日出願の米国特許仮出願第62/552、071号に基づく優先権を主張するものである。上記出願の開示内容は、参照により本明細書中に援用される。
本明細書に記載の固形単位用量製剤と、
ハンチントン病、パーキンソン病、医原性または非医原性のパーキンソン症候群、LID誘発ジスキネジアを含む薬物誘発性ジスキネジアなどのジスキネジア、ジストニア、トゥレット病、医原性または非医原性の精神病及び幻覚症、統合失調症または統合失調症様障害、気分または不安障害、躁うつ病、うつ病、強迫性疾患、睡眠障害、自閉スペクトラム症、ADHD、加齢性認知障害、アルコールまたは麻薬物質の乱用に関連する障害、アルツハイマー病、及びレッツ症候群からなる群より選択される疾患に罹患した対象においてその疾患を治療するかまたはその疾患の進行を遅延させるための固形単位製剤の使用説明書と、を備えた、パッケージを提供する。
(b)固形単位用量の容量が0.30mlであり、固形単位用量製剤が67.5〜180mgのプリドピジンを含有するか、
(c)固形単位用量の容量が0.21mlであり、固形単位用量製剤が67.5〜135mgのプリドピジンを含有するか、または、
(d)固形単位用量の容量が0.13mlであり、固形単位用量製剤が67.5mgのプリドピジンを含有する、条項1に記載の固形単位用量製剤。
(a)条項1〜41のいずれかに記載の固形単位用量製剤と、
(b)ハンチントン病、パーキンソン病、医原性または非医原性のパーキンソン症候群、ジスキネジア、ジストニア、トゥレット病、医原性または非医原性の精神病及び幻覚症、統合失調症または統合失調症様障害、気分または不安障害、躁うつ病、うつ病、強迫性疾患、睡眠障害、自閉スペクトラム症、ADHD、加齢性認知障害、アルコールまたは麻薬物質の乱用に関連する障害、アルツハイマー病、及びレッツ症候群からなる群より選択される疾患に罹患した対象においてその疾患を治療するかまたはその疾患の進行を遅延させるための固形単位製剤の使用説明書と、を備えた、パッケージ。
Clinicaltrials.gov Clinical Trial Identifier NCT02006472, "A Phase 2, to Evaluating the Safety and Efficacy of Pridopidine Versus Placebo for Symptomatic Treatment in Patients With Huntington's Disease."
de Yebenes JG, Landwehrmeyer B, Squitieri F, Reilmann R, Rosser A, Barker RA, Saft C, Magnet MK, Sword A, Rembratt A, Tedroff J; MermaiHD study investigators, "Pridopidine for the treatment of motor function in patients with Huntington's disease (MermaiHD): a phase 3, randomised, double-blind, placebo-controlled trial," Lancet Neurol. 2011 Dec;10(12):1049-57. doi: 10.1016/S1474-4422(11)70233-2. Epub 2011 Nov 7.
Geva et al. (2016). Pridopidine activates neuroprotective pathways impaired in Huntington Disease . HMG 25(18): 3975-87.
Huntington Study Group HART Investigators, "A randomized, double-blind, placebo-controlled trial of pridopidine in Huntington's disease," Mov Disord. 2013 Sep;28(10):1407-15. doi: 10.1002/mds.25362. Epub 2013 Feb 28.
Lindskov Krog P, Osterberg O, Gundorf Drewes P, Rembratt A, Schultz A, Timmer W. "Pharmacokinetic and tolerability profile of pridopidine in healthy-volunteer poor and extensive CYP2D6 metabolizers, following single and multiple dosing" Eur J Drug Metab Pharmacokinet. 2013 Mar;38(1):43-51. Epub 2012 Sep 5.
Mangal et al. "Superdisintegrants: An Updated Review" International Journal of Pharmacy and Pharmaceutical Science Research 2012; 2(2) 26-35.
Mohanachandran et al., "Superdisintegrants: An Overview" International Journal of Pharmaceutical Sciences Review and Research Volume 6, Issue 1, January - February 2011; Article-022.
Osterberg, et al. "A single center, randomized, placebo-controlled, double-blind study to evaluate the safety, tolerability, and pharmacokinetics of multiple-ascending doses of pridopidine in healthy volunteers" Poster presented at Sixth Annual Huntington Disease Clinical Research Symposium, Nov 2012, Seattle, Washington, USA. Neurotherapeutics.
2005年6月7日に発行された米国特許第6、903、120号(Sonesso, et al.)
2011年4月12日に発行された米国特許第7、923、459号(Gauthier,et al.)
2013年10月10日に公開された米国特許出願公開第2013/0267552−A1号(Waters et al.)
2014年12月25日に公開された米国特許出願公開第2014/0378508−A1号(Bassan et al.)
2015年7月23日に公開された米国特許出願公開第2015/0202302A1号(Licht et al.)
USP 711 DISSOLUTION. 2016. 33(4) Fourth Interim Revision Announcement. Nov 21, 2016.
CSID:25948790, http://www.chemspider.com/Chemical-Structure.25948790.html (accessed 23:27, Jul 15, 2016).
CSID:7971505, http://www.chemspider.com/Chemical-Structure.7971505.html (accessed 23:33, Jul 15, 2016).
Claims (34)
- 固形単位用量製剤であって、
治療有効量のプリドピジンと、
少なくとも1つの薬学的に許容される賦形剤と、を含有し、
前記固形単位用量製剤が所定の容積を有し、
前記固形単位用量製剤の前記容積に対する前記プリドピジンの量が135〜600mg/ml、135〜400mg/ml、または175〜370mg/mlである、固形単位用量製剤。 - 前記固形単位用量製剤が、約67.5mg、約75mg、約90mg、約100mg、約112.5mg、約125mg、約135mg、約150mg、約175mg、約180mg、または約200mgの前記プリドピジンを含有する、請求項1に記載の固形単位用量製剤。
- (a)前記固形単位用量の前記容量が0.5mlであり、前記固形単位用量製剤が90〜200mgの前記プリドピジンを含有するか、
(b)前記固形単位用量の前記容量が0.37mlであり、前記固形単位用量製剤が67.5〜200mgの前記プリドピジンを含有するか、
(c)前記固形単位用量の前記容量が0.30mlであり、前記固形単位用量製剤が67.5〜180mgの前記プリドピジンを含有するか、
(d)前記固形単位用量の前記容量が0.21mlであり、前記固形単位用量製剤が67.5〜135mgの前記プリドピジンを含有するか、または、
(e)前記固形単位用量の前記容量が0.13mlであり、前記固形単位用量製剤が67.5mgの前記プリドピジンを含有する、請求項1または2に記載の固形単位用量製剤。 - 前記固形単位用量製剤が、67.5mgの前記プリドピジン、75mgの前記プリドピジン、90mgの前記プリドピジン、100mgの前記プリドピジン、112.5mgの前記プリドピジン、125mgの前記プリドピジン、135mgの前記プリドピジン、150mgの前記プリドピジン、175mgの前記プリドピジン、180mgの前記プリドピジン、または200mgの前記プリドピジンを含有する、請求項1〜3のいずれかに記載の固形単位用量製剤。
- 固形単位用量製剤が、錠剤またはゼラチンカプセルの形態である、請求項1〜4のいずれかに記載の固形単位用量製剤。
- 前記固形単位用量製剤が、錠剤の形態であり、任意選択でオーバーコート層によってコーティングされている、請求項5に記載の固形単位用量製剤。
- 前記固形単位用量製剤が、カプセルの形態である、請求項5に記載の固形単位用量製剤。
- 前記固形単位用量製剤は、37°C±0.5°CのpH6.8のリン酸塩緩衝液を収容したUSP#2溶解装置内で50回転毎分の回転速度で試験した場合には、30分以内に前記プリドピジンの80%を放出する、請求項1〜7のいずれかに記載の固形単位用量製剤。
- 前記薬学的に許容される賦形剤が、充填剤、流動化剤、滑沢剤、崩壊剤、及びそれらの任意の組み合わせからなる群より選択される、請求項1〜8のいずれかに記載の固形単位用量製剤。
- 前記充填剤が、微結晶セルロース、糖球、ラクトース、ソルビトール、デキストロース、スクロース、マンニトール、二塩基性または三塩基性リン酸カルシウム、硫酸カルシウム、デンプン、リタラック(retalac)、及びそれらの任意の組み合わせからなる群より選択される、請求項9に記載の固形単位用量製剤。
- 前記充填剤が、ケイ化微結晶セルロースである、請求項10に記載の固形単位用量製剤。
- 前記充填剤の含有量が、
前記固形単位用量製剤の約26〜80重量%、
前記固形単位用量製剤の約15〜80重量%、
前記固形単位用量製剤の26〜46重量%、
前記固形単位用量製剤の約36重量%、
前記固形単位用量製剤の50〜70重量%、または、
前記固形単位用量製剤の約60重量%である、請求項9〜11のいずれかに記載の固形単位用量製剤。 - 前記滑沢剤が、フマル酸ステアリルナトリウム、ステアリン酸、ステアリン酸マグネシウム、ステアリン酸カルシウム、ステアリン酸亜鉛、タルク、ベヘン酸グリセリル、モノステアリン酸グリセリル、及びそれらの任意の組み合わせからなる群より選択される、請求項9に記載の固形単位用量製剤。
- 前記滑沢剤が、ステアリン酸マグネシウムである、請求項13に記載の固形単位用量製剤。
- 前記滑沢剤の含有量が、
前記固形単位用量製剤の約0.5〜2.0重量%、
前記固形単位用量製剤の約0.5〜1.5重量%、または、
前記固形単位用量製剤の約1.0重量%である、請求項13または14に記載の固形単位用量製剤。 - 前記崩壊剤が、超崩壊剤である、請求項9に記載の固形単位用量製剤。
- 前記崩壊剤が、クロスカルメロースナトリウム、クロスポビドン、デンプングリコール酸ナトリウム、及びポラクリリンカリウムからなる群より選択される、請求項16に記載の固形単位用量製剤。
- 前記崩壊剤の含有量が、
前記固形単位用量製剤の約1.9〜3.6重量%であるか、または、
前記固形単位用量製剤の約2.9重量%である、請求項16または17に記載の固形単位用量製剤。 - 前記プリドピジンが、プリドピジン塩基またはプリドピジン塩として提供される、請求項1〜18のいずれかに記載の固形単位用量製剤。
- 前記プリドピジンが、プリドピジン塩酸塩である、請求項1〜19のいずれかに記載の固形単位用量製剤。
- 前記容積が0.37mlであり、
76.2mg〜127mgの前記プリドピジン塩酸塩を含有する、請求項20に記載の固形単位用量製剤。 - 前記容積が0.37mlであり、
84.7mgの前記プリドピジン塩酸塩を含有する、請求項21に記載の固形単位用量製剤。 - 前記容積が0.37mlであり、
112.9mgの前記プリドピジン塩酸塩を含有する、請求項21に記載の固形単位用量製剤。 - 超崩壊剤をさらに含有する、請求項21に記載の固形単位用量製剤。
- ウェット顆粒を含む、請求項1〜24のいずれかに記載の固形単位用量製剤。
- 前記固形単位用量製剤が、毎日2回または3回の投与に適合する、請求項1〜25のいずれかに記載の固形単位用量製剤。
- ハンチントン病、パーキンソン病、医原性または非医原性のパーキンソン症候群、ジスキネジア、LID誘発性ジスキネジアを含む薬物誘発性ジスキネジア、ジストニア、トゥレット病、医原性または非医原性の精神病及び幻覚症、統合失調症または統合失調症様障害、気分または不安障害、躁うつ病、うつ病、強迫性疾患、睡眠障害、自閉スペクトラム症、ADHD、加齢性認知障害、アルコールまたは麻薬物質の乱用に関連する障害、アルツハイマー病、及びレッツ症候群からなる群より選択される疾患に罹患した対象を治療する方法であって、
治療を必要とする対象に対して、請求項1〜26のいずれかに記載の固形単位用量製剤を投与するステップを含む、方法。 - 神経変性疾患またはドーパミン関連疾患に罹患した対象を治療する方法であって、
治療を必要とする対象に対して、請求項1〜26のいずれかに記載の固形単位用量製剤を毎日1回投与するステップを含む、方法。 - パッケージであって、
(a)請求項1〜26のいずれかに記載の固形単位用量製剤と、
(b)ハンチントン病、パーキンソン病、医原性または非医原性のパーキンソン症候群、ジスキネジア、LID誘発性ジスキネジアを含む薬物誘発性ジスキネジア、ジストニア、トゥレット病、医原性または非医原性の精神病及び幻覚症、統合失調症または統合失調症様障害、気分または不安障害、躁うつ病、うつ病、強迫性疾患、睡眠障害、自閉スペクトラム症、ADHD、加齢性認知障害、アルコールまたは麻薬物質の乱用に関連する障害、アルツハイマー病、及びレッツ症候群からなる群より選択される疾患に罹患した対象においてその疾患を治療するかまたはその疾患の進行を遅延させるための前記固形単位用量製剤の使用説明書と、を備えた、パッケージ。 - 請求項25に記載の固形単位用量製剤を製造する方法であって、
ウェット顆粒を作製するステップを含む、方法。 - プリドピジンと、水及び/または有機の溶液とを、結合剤を含めてまたは含めずに、互いに混合させて、ウェット顆粒を作製するステップをさらに含む、請求項30に記載の方法。
- プリドピジンと、1以上の顆粒内賦形剤と、水及び/または有機溶液の溶液とを、結合剤を含めてまたは含めずに、ウェット顆粒を調製するステップをさらに含み、
前記顆粒内賦形剤が、充填剤、崩壊剤、またはそれらの組み合わせである、請求項30に記載の方法。 - 固形単位用量製剤であって、
所定量のプリドピジンと、
少なくとも1つの薬学的に許容される賦形剤と、
請求項30〜32のいずれかに記載の方法により製造されたウェット顆粒と、を含有し、
前記固形単位用量製剤が所定の容積を有し、
前記固形単位用量製剤の前記容積に対する前記プリドピジンの量が135〜600mg/mlである、固形単位用量製剤。 - 前記プリドピジンが、ミニ錠剤の形態で提供される、請求項5、6及び33のいずれかに記載の固形単位用量製剤。
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