Methods and dosage forms for controlled delivery of paliperidone and risperidone

Inactive Publication Date: 2005-10-20
ALZA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0032] The present invention is designed for once-a-day administration of an oral dosage form to deliver paliperidone or risperidone for more than about 22 hours utilizing a capsule-shaped tablet. This approximately 22 hours of release is at a substantially ascending rate of release from the core with 90% delivery occurring at about 20 hours. This novel profile p

Problems solved by technology

Additionally, since paliperidone has a long half-life of about one day, it is not a typical candidate for extended delivery.
However, side effects such as anxiety, somnolence, dizziness, constipation, extrapyramidal symptoms, and orthostatic hypotension may be related to high blood plasma concentration levels restricting the ability to administer a single daily immediate release dose.
The low drug loading requirement presents problems in formulating compositions and fabricating dosage forms that are suitable for oral administration that deliver at the desired rate of release for an extended period of time.
Furthermore, this art does not identify delivery of paliperidone much less delivery of paliperidone through oral controlled release delivery.
This art does not disclose preferred release rates and does not teach or motivate toward an ascending rate of release, much less such releas

Method used

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  • Methods and dosage forms for controlled delivery of paliperidone and risperidone
  • Methods and dosage forms for controlled delivery of paliperidone and risperidone
  • Methods and dosage forms for controlled delivery of paliperidone and risperidone

Examples

Experimental program
Comparison scheme
Effect test

example 1

Paliperidone Capsule Shaped Tablet, Trilayer 1.9 mg System

[0155] A dosage form adapted, designed and shaped as an osmotic drug delivery device is manufactured as follows: 100 g of paliperidone, 7345 g of polyethylene oxide with average molecular weight of 200,000, and 2000 g of sodium chloride, USP are added to a fluid bed granulator bowl. Next a binder solution is prepared by dissolving 800 g of hydroxypropylmethyl cellulose identified as 2910 having an average viscosity of 5 cps in 9,200 g of water. The dry materials are fluid bed granulated by spraying with 6750 g of binder solution. Next, the wet granulation is dried in the granulator to an acceptable moisture content, and sized using by passing through a 7-mesh screen. Next, the granulation is transferred to a blender and mixed with 5 g of butylated hydroxytoluene as an antioxidant and lubricated with 50 g of stearic acid.

[0156] Next, a second drug compartment composition is prepared as follows: 280 g of paliperidone and 9165...

example 2

Paliperidone Capsule Shaped Tablet, Trilayer 0.5 mg System

[0163] A dosage form adapted, designed and shaped as an osmotic drug delivery device is manufactured as follows: 25 g of paliperidone, 7420 g of polyethylene oxide with average molecular weight of 200,000, and 2000 g of sodium chloride, USP are added to a fluid bed granulator bowl. Next a binder solution is prepared by dissolving 800 g of hydroxypropylmethyl cellulose identified as 2910 having an average viscosity of 5 cps in 9,200 g of water. The dry materials are fluid bed granulated by spraying with 6750 g of binder solution. Next, the wet granulation is dried in the granulator to an acceptable moisture content, and sized using by passing through a 7-mesh screen. Next, the granulation is transferred to a blender and mixed with 5 g of butylated hydroxytoluene as an antioxidant and lubricated with 50 g of stearic acid.

[0164] Next, a second drug compartment composition is prepared as follows: 70 g of paliperidone and 9375 g...

example 3

Paliperidone Capsule Shaped Tablet, Trilayer 15 mg System

[0171] A dosage form adapted, designed and shaped as an osmotic drug delivery device was manufactured as follows: 900 g of paliperidone, 6544 g of polyethylene oxide with average molecular weight of 200,000, and 2000 g of sodium chloride, USP were added to a fluid bed granulator bowl. Next a binder solution was prepared by dissolving 800 g of polyvinylpyrrolidone identified as K29-32 having an average molecular weight of 40,000 in 9,200 g of water. The dry materials were fluid bed granulated by spraying with 6750 g of binder solution. Next, the wet granulation was dried in the granulator to an acceptable moisture content, and sized using by passing through a 7-mesh screen. Next, the granulation was transferred to a blender and mixed with 5 g of butylated hydroxytoluene as an antioxidant and lubricated with 50 g of stearic acid.

[0172] Next, a second drug compartment composition was prepared as follows: 2100 g of paliperidone ...

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Abstract

Dosage forms and methods for providing a substantially ascending rate of release of paliperidone or risperidone are provided. The sustained release dosage forms provide therapeutically effective average steady-state plasma paliperidone or risperidone concentrations when administered once per day. This once-a-day dosing regimen results in only one peak plasma paliperidone or risperidone concentration occurrence in each 24 hour period. In addition, the peak plasma paliperidone or risperidone concentration occurs at a later time following dose administration and exhibits a lesser magnitude than the peak plasma paliperidone or risperidone concentration that occurs following administration of paliperidone or risperidone in an immediate-release dosage form.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a continuation-in-part or application Serial No. 10 / 629,211 and claims benefit, under 35 USC 119(e), to U.S. provisional patent application No. 60 / 399,590, filed Jul. 29, 2002, and 60 / 406,005 filed Aug. 26, 2002, all of which are incorporated herein by reference.FIELD OF THE INVENTION [0002] This invention pertains to the controlled delivery of pharmaceutical agents and methods, dosage forms and devices. In particular, the invention is directed to methods, dosage forms and devices for the controlled delivery of paliperidone or risperidone, with reduced degradation of the active agent. BACKGROUND OF THE INVENTION [0003] The art is replete with descriptions of oral dosage forms for the controlled release of pharmaceutical agents. While a variety of sustained release dosage forms for delivering certain drugs exhibiting short half-life may be known, not every drug may be suitably delivered from those dosage forms because...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K31/519
CPCA61K9/0004A61K31/519A61K31/506A61K9/0053A61K9/2086A61K9/209
Inventor YAM, NYOMI V.REYES, IRANDAVAR, NIPUNAYER, ATUL D.LEE, JULIESEROFF, SONYAGUPTA, SUNEEL K.SATHYAN, GAYATRI
Owner ALZA CORP
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