US 2021/0267957 A1 · METHYLPHENIDATE COMPOSITIONS FOR TREATMENT OF ATTENTION DEFICIT HYPERACTIVITY DISORDER

Abstract

A solid, oral pharmaceutical composition is described. The solid, oral pharmaceutical composition includes methylphenidate or a pharmaceutical salt thereof, wherein an in vivo absorption model of the solid, oral pharmaceutical composition has a function selected from the group consisting of: a single Weibull function, a double Weibull function, and a sigmoid eMax function. A correlation of a plurality of fractions of an in vitro dissolution of the solid, oral pharmaceutical composition with a same plurality of fractions of an in vivo absorption of the solid, oral pharmaceutical composition is non-linear. A method of treating a condition in a subject having a disorder or condition responsive to the administration of methylphenidate is also described. The method includes orally administering to the subject an effective amount of the solid, oral pharmaceutical composition.

Claims32

Dependent claims

1-18. (canceled)

A method of treating a condition in a subject having a disorder or condition responsive to the administration of methylphenidate, comprising:

orally administering to the subject an effective amount of a solid, oral pharmaceutical composition comprising:
methylphenidate or a pharmaceutical salt thereof,
wherein an in vivo absorption model of the solid, oral pharmaceutical composition has a function selected from the group consisting of:
(i) a single Weibull function:
r
⁢
⁢
1
⁢
(
t
)
=
e
-
(
(
time
td
)
SS
)
wherein td is a time necessary to absorb 63.2% of the methylphenidate or a pharmaceutical salt thereof released, and ss is a sigmoidicy factor;
(ii) a double Weibull function:
r
⁢
⁢
2
⁢
(
t
)
=
ff
·
e
-
(
(
time
td
)
SS
)
+
(
1
-
ff
)
·
e
-
(
(
time
td
1
)
SS
⁢
⁢
2
)
wherein ff is a fraction of a dose released in a 1st process, td is a time necessary to absorb 63.2% of the dose released in the 1st process, td1 is a time necessary to absorb 63.2% of a dose released in the 2nd process, ss is a sigmoidicy factor for the 1st process, and ss1 is a sigmoidicity factor for the 2nd process;
and
(iii) a sigmoid eMax function:
r
v
⁢
i
⁢
t
⁢
r
⁢
o
⁡
(
t
)
=
t
⁢
i
⁢
m
⁢
e
g
⁢
a
EC
ga
+
tim
⁢
e
g
⁢
a
wherein EC is a time to release 50% of the methylphenidate or a pharmaceutical salt thereof, and ga is a parameter characterizing the shape of an absorption curve of the methylphenidate or a pharmaceutical salt thereof;
and
a correlation of a plurality of fractions of an in vitro dissolution of the solid, oral pharmaceutical composition with a same plurality of fractions of an in vivo absorption of the solid, oral pharmaceutical composition is non-linear;
thereby producing an improvement in a behavior or an ability related to the disorder or condition over a period of time,
wherein the administering reduces the variation in efficacy, or likelihood or severity of rebound, or both, of over the period of time.

103 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/316,252Filed 10 May 2021

Priority

25 Jan 2019

Published

2 Sep 2021

Term ends

Not estimatedThe source records don’t support an estimate.

Classification14 codes

A61K 31/4458
Non condensed piperidines, e.g. piperocaine: only substituted in position 2, e.g. methylphenidate
A61P 25/00
Drugs for disorders of the nervous system
A61K 9/0053
Galenical forms characterised by the site of application: mouth and digestive tract, i.e. intraoral and peroral administration
A61K 9/2009
Excipients; Inactive ingredients: inorganic compounds

Family

Application62/796,918Us provisional application · filed 25 Jan 2019

Application62/962,355Us provisional application · filed 17 Jan 2020

Application17/315,133Continuation · filed 7 May 2021

Application17/316,252Continuation

US 2021/0275511 A1Published application

US 2021/0267957 A1This patent

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

Methylphenidate compositions for treatment of attention deficit hyperactivity disorder

Life of this patent

Methylphenidate compositions for treatment of attention deficit hyperactivity disorder

Life of this patent

Abstract

Claims32