Controlled Release Dosage Form Of Paliperidone
Abstract:
An oral osmotic dosage form of paliperidone comprising: a)a core comprising:i.a drug layer; ii.optionally a push layer; iii.A seal-coat layer; b)a semi-permeable membrane having an orifice surrounding said core; wherein said dosage form releases paliperidone in a non-ascending rate of release.
Specification
FIELD OF INVENTION
The invention relates to controlled release dosage form comprising an atypical antipsychotic agent.
More particularly, the invention relates to controlled release dosage form comprising paliperidone or its pharmaceutically acceptable salts thereof.
The invention also relates to a process for preparation of controlled release dosage form comprising paliperidone or its pharmaceutically acceptable salts thereof.
BACKGROUND OF THE INVENTION AND RELATED PRIOR ART
Paliperidone is known as a major active metabolite of risperidone. It is chemically known as (±)-3-[2-[4- (6-fluoro-l, 2-benzisoxazol-3-yl)-l-piperidinyl] ethyl] -6, 7, 8, 9 -tetra hydro-9-hydroxy-2- methyl-4Hpyrido [1,2-a] pyrimidin-4-one. It basically comprises a mixture of both (R) and (S) forms of risperidone and is disclosed in US 4,804,663 and 5,158,952.
Paliperidone is marketed under the trade name INVEGA® in the form of extended release tablet in the U.S. and Europe for the treatment of acute (short-term) as well as maintenance (long-term) treatment of schizophrenia.
Paliperidone has a long half-life - about one day, so it is not a suitable drug for extended delivery. However, side effects such as anxiety, somnolence, dizziness, constipation, extra-pyramidal symptoms may be related to high blood plasma concentration levels restricting the ability to administer a single daily immediate release dose. Many efforts have been taken to control the release of the drug to provide extended release profile, while trying to control possible side-effects.
A number of design options are available to control or modulate the drug release from a dosage form, but osmotic system of delivery is found to be most preferred design to control the release of drug from dosage form as it is independent of pH, presence of food and other physiological factors with respect of other conventional controlled release system.
Commercially available INVEGA® is available as capsule shaped tablet which consists of an osmotically active trilayer core surrounded by a sub-coat and a semi-permeable membrane. The trilayer core is composed of two drug layers containing the drug and excipients, and a push layer containing osmotically active components. There are two precision laser-drilled orifices on the drug-layer dome of the tablet.
Patents/ patent applications, which disclose various osmotic controlled release compositions comprising paliperidone, are disclosed below:
U.S.2004/0092534, U.S.2005/0208132, U.S.2005/0232995, U.S. 2006/0189635, U.S.2009/0202631 and U.S.2009/0227605 disclose an oral dosage form wherein said dosage form comprises a dose D of a benzisoxazole and an oral sustained release dosing structure adapted to sustainably release the benzisoxazole derivative at rates that provide (a) a mean, single dose, maximum plasma concentration Cmax of the benzisoxazole derivative and pharmacologically active metabolites thereof taken together and (b) a mean, single dose, area under a plasma concentration-time curve for AUQnf of the benzisoxazole derivative and pharmacologically active metabolites thereof taken together, which satisfy the relationship about 0.5 ng/mL/mg
Documents
Application Documents
| # |
Name |
Date |
| 1 |
293-che-2010 form-2 05-02-2010.pdf |
2010-02-05 |
| 2 |
293-che-2010 form-1 05-02-2010.pdf |
2010-02-05 |
| 3 |
293-che-2010 drawings 05-02-2010.pdf |
2010-02-05 |
| 4 |
293-che-2010 description(provisional) 05-02-2010.pdf |
2010-02-05 |
| 5 |
293-che-2010 correspondence others 05-02-2010.pdf |
2010-02-05 |
| 6 |
293-CHE-2010 FORM-3 23-03-2010.pdf |
2010-03-23 |
| 7 |
293-CHE-2010 FORM-5 07-02-2011.pdf |
2011-02-07 |
| 8 |
293-CHE-2010 FORM-2 07-02-2011.pdf |
2011-02-07 |
| 9 |
293-CHE-2010 FORM-1 07-02-2011.pdf |
2011-02-07 |
| 10 |
293-CHE-2010 DRAWINGS 07-02-2011.pdf |
2011-02-07 |
| 12 |
293-CHE-2010 CORRESPONDENCE 07-02-2011.pdf |
2011-02-07 |
| 13 |
293-CHE-2010 CLAIMS 07-02-2011.pdf |
2011-02-07 |
| 14 |
293-CHE-2010 FORM-13 13-05-2011.pdf |
2011-05-13 |
| 15 |
293-CHE-2010 FORM-18 13-05-2011.pdf |
2011-05-13 |
| 16 |
293-CHE-2010 FORM-13 13-05-2011.pdf |
2011-05-13 |
| 17 |
293-CHE-2010 FORM-13 15-11-2011.pdf |
2011-11-15 |
| 18 |
293-CHE-2010 FORM-13 16-11-2011.pdf |
2011-11-16 |
| 19 |
293-CHE-2010 CORRESPONDENCE OTHERS 26-08-2013.pdf |
2013-08-26 |
| 20 |
293-CHE-2010-FER.pdf |
2017-02-17 |
| 21 |
293-che-2010-FER_SER_REPLY [17-08-2017(online)].pdf |
2017-08-17 |
| 22 |
293-che-2010-COMPLETE SPECIFICATION [17-08-2017(online)].pdf |
2017-08-17 |
| 23 |
293-CHE-2010-HearingNoticeLetter.pdf |
2017-11-03 |
| 24 |
293-CHE-2010-Written submissions and relevant documents (MANDATORY) [24-11-2017(online)].pdf |
2017-11-24 |
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