US 10,500,162 B2Granted

Methods and compositions particularly for treatment of attention deficit disorder

AssigneePurdue Pharma L.P.

InventorsRicardo Alberto Vargas Rincon, Joseph Reiz

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Abstract

There is described, inter alia, a coated bead comprising: (a) a granule; (b) a first layer coated over the granule, the first layer comprising a first amount of an active pharmaceutical ingredient comprising a central nervous system stimulant; and (c) a second layer coated over the first layer, the second layer being present in an amount sufficient to substantially delay release of the active pharmaceutical ingredient in the first layer until after the coated bead reaches a distal intestine portion of a subject to whom the coated bead is administered; and (d) the third layer coated over the second layer, the third layer comprising a second amount of the active pharmaceutical ingredient, the third layer being configured to permit substantially immediate release of the active pharmaceutical ingredient comprised therein. Embodiments related to a solid oral pharmaceutical composition are also described.

Claims28

Dependent claims

A method of treating Attention Deficit Hyperactivity Disorder (ADHD) in a subject in need thereof, the method comprising administering to the subject an oral solid pharmaceutical composition comprising an immediate release methylphenidate hydrochloride component and a controlled/delayed release methylphenidate hydrochloride component, wherein the immediate release methylphenidate component and the controlled/delayed release methylphenidate component, together, provide 25, 35, 45, 55, 70, 85, or 100 mg of methylphenidate hydrochloride;

and wherein
the oral solid pharmaceutical composition, when administered to the subject in a fed state, provides a pharmacokinetic profile comprising:
an average ±standard deviation methylphenidate AUC0-4 of 21160.21±6420.56 pg·hr/mL;
an average ±standard deviation methylphenidate AUC8-12 of 29392.15±8453.72 pg·hr/mL;
and
an average ±standard deviation methylphenidate AUC12-16 of 36653.88±11521.14 pg·hr/mL
when the oral solid pharmaceutical composition provides 100 mg of methylphenidate hydrochloride, or dose proportional AUC values thereof, when the oral solid pharmaceutical composition provides 25, 35, 45, 55, 70, or 85 mg methylphenidate hydrochloride;
and further wherein the oral solid pharmaceutical composition provides efficacious treatment of ADHD for 16 hours after a single oral administration;
and further wherein the oral solid pharmaceutical composition has the following in vitro methylphenidate dissolution profile:
Time
Methylphenidate
(hours)
(% dissolved)
1
NLT 15%
4
18-38%
8
35-55%
12
68-98
16
NLT 68
when tested according to the USP paddle method, 100 rpm, at 37° C.;
(i) starting with 900 ml simulated gastric fluid for 2 hours, (ii) followed by 900 ml phosphate buffer pH 6.0 for 4 hours, and (iii) for the 7th hour onwards, 900 mL of phosphate buffer pH 7.4;
USP <711> Acceptance Table 2.

23 more elements

and wherein
the oral solid pharmaceutical composition, when administered to the subject in a fed state, provides a pharmacokinetic profile comprising:
an average ±standard deviation methylphenidate Cmax0-4 of 9248.95±1886.65 pg/mL;
and
an average ±standard deviation methylphenidate Cmax8-16 of 10667.64±3017.29 pg/mL;
when the oral solid pharmaceutical composition comprises 100 mg of methylphenidate hydrochloride, or dose proportional Cmax values thereof, when the oral solid pharmaceutical composition comprises 25, 35, 45, 55, 70, or 85 mg methylphenidate hydrochloride;
wherein the oral solid pharmaceutical composition provides efficacious treatment of ADHD for 16 hours after a single oral administration;
and further wherein the oral solid pharmaceutical composition has the following in vitro methylphenidate dissolution profile:
Time
Methylphenidate
(hours)
(% dissolved)
1
NLT 15%
4
18-38%
8
35-55%
12
68-98
16
NLT 68
when tested according to the USP paddle method, 100 rpm, at 37° C.;
(i) starting with 900 ml simulated gastric fluid for 2 hours, (ii) followed by 900 ml phosphate buffer pH 6.0 for 4 hours, and (iii) for the 7th hour onwards, 900 mL of phosphate buffer pH 7.4;
USP <711> Acceptance Table 2.

22 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/185,730Filed 9 Nov 2018 · continuation
Priority: CA 290291127 Aug 2015
Published: US 2019/0000769 A114 Mar 2019
Granted: 10 Dec 2019
Term ends: Not estimatedThe source records don’t support an estimate.

Classification13 codes

A61K 9/5078
Having two or more different coatings optionally including drug-containing subcoatings: with drug-free core
A61K 9/14
Medicinal preparations characterised by special physical form: particulate form, e.g. powders, Processes for size reducing of pure drugs or the…
A61K 9/1676
With an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface: having a drug-free core…
A61K 9/48
Medicinal preparations characterised by special physical form: preparations in capsules, e.g. of gelatin, of chocolate

Family

Application62/122,847Us provisional application · filed 31 Oct 2014
Application14/928,276Parent of this continuation · filed 30 Oct 2015
Application15/958,413Parent of this continuation · filed 20 Apr 2018
US 9,974,752 B2Parent of this continuation · filed 22 May 2018
Application16/120,999Parent of this continuation · filed 4 Sep 2018
US 10,111,839 B2Parent of this continuation · filed 30 Oct 2018
US 2019/0076370 A1Pre-grant publication · published 14 Mar 2019
US 10,292,939 B2Parent of this continuation
US 2016/0120819 A1Published application
US 2018/0235895 A1Published application
US 2019/0000769 A1Published application
US 10,500,162 B2This patent

From the US filing history. Foreign family members aren’t listed.

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