US 8,802,143 B2Granted

Method for treating neurodegenerative disorders with oral dosage formulation containing both immediate-release and sustained-release drugs

AssigneeCenter Laboratories, Inc.

InventorsGuang-Tzuu Shane, Chien-Fen Chen, Chuen-Lin Din, Hui-Ling Tsai, Pei-Chen Tsai

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Abstract

Disclosed herein is a method for treating patient suffering from a disorder related to central nervous system with an oral dosage formulation that contains both sustained-release and immediate-release drugs. The sustained-release drug in the oral dosage formulation is memantine, and the formulation provides an average blood level Cmax of the memantine in a range of about 10-24 ng/mL during an average Tmax of about 10-45 hours. The immediate-release drug in the oral dosage formulation is an acetylcholinesterase inhibitor (AChEI), and the formulation provides an average blood level Cmax of the AChEI in a range of about 12-38 ng/mL during an average Tmax of less than about 4 hours.

Claims8

Dependent claims

A method for treating a patient suffering from dementia or Alzheimer's disease comprising:

administering to the patient an oral dosage formulation as defined in Table 1 or 2, wherein the formulation provides an average blood level Cmax of memantine in a range of about 10-24 ng/mL during an average Tmax of about 10-45 hours, and an average blood level Cmax of donepezil in a range of about 12-38 ng/mL during an average Tmax of less than about 4 hours;
TABLE 1
Ingredients
Weight, mg
Sustained Release (SR) Pellet-1 Formulation
microcrystalline cellulose
100
Memantine HCl
20
hydroxypropyl methyl cellulose
6.0
Polyethylene glycol
0.6
Subtotal
126.6
SR-Coating-1 Formulation
microcrystalline cellulose
31.7
Talc
31.7
hydroxypropyl methyl cellulose
0.8
Total
190.7
Immediate Release (IR) Granule-1 Formulation
Donepezil HCl
10
microcrystalline cellulose
115
Pre-gelatinized starch
15
Total
140
IR/SR Tablet-1 Formulation
SR Pellet-1/SR-Coating-1
190
IR Granule-1
140
polyvinyl polypyrrolidone
10
Magnesium Stearate
2
Total
342
TABLE 2
Ingredients
Weight, mg
SR Pellet-2 Formulation
Polymethyl methacrylate
100
Memantine HCl
20
hydroxypropyl methyl cellulose
6.0
Polyethylene glycol
0.6
Subtotal
126.6
SR-Coating-2 Formulation
microcrystalline cellulose
22.3
Ethyl cellulose
3.0
TiO2
5.6
hydroxypropyl methyl cellulose
0.6
Total
158.1
IR Granule-2 Formulation
Donepezil HCl
10
microcrystalline cellulose
115
Pre-gelatinized starch
15
Total
140
IR/SR Tablet-2 Formulation
SR Pellet-2/SR-Coating-2
158
IR Granule-2
140
polyvinyl polypyrrolidone
10
Magnesium Stearate
2
Total
310.

86 more elements

Dependencies are inferred from the claim text.

Facts

Application: 13/071,520Filed 25 Mar 2011 · continuation in part
Priority: 30 Sep 2009
Published: US 2011/0171302 A114 Jul 2011
Granted: 12 Aug 2014
Term ends: Not estimatedThe source records don’t support an estimate.

Classification11 codes

A61K 45/06
Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00: mixtures of active ingredients without…
A61K 9/1635
Organic macromolecular compounds: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, polyacrylates
A61K 9/2077
Characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets;…: tablets…
A61K 9/2081
Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets: with microcapsules or…

Family

Application61/247,057Us provisional application · filed 30 Sep 2009
PCT/CN2010/001519Parent of this continuation-in-part · filed 29 Sep 2010
US 2011/0171302 A1Pre-grant publication · published 14 Jul 2011
Application13/063,462Parent of this continuation-in-part
US 2012/0177735 A1Published application
US 8,815,288 B2Related patent
US 8,802,143 B2This patent

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