Orally disintegrating tablet containing asenapine
Inventors
GUJJAR, Chaitanya Yogananda • RALLABANDI, Bala Ramesha Chary • PATWARI, Pradip Shivraj • Fitzner, Ansgar
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-10307400-B2
Publication Date
2019-06-04
Expiration Date
Abstract
The present invention relates to an orally disintegrating tablet (ODT) containing asenapine maleate and to a process for preparing the ODT. In a first aspect, the present invention relates to an ODT containing asenapine maleate and low substituted hydroxypropylcellulose. In a second aspect, the present invention relates to an ODT containing crystalline asenapine maleate and the ODT is prepared using conventional tabletting techniques as direct compression and granulation. In a third aspect, the present invention relates to an ODT containing asenapine maleate and a carboxylic acid, and to the use of a carboxylic acid for enhancing storage stability of an asenapine maleate containing ODT.
Core Innovation
The described invention relates to orally disintegrating tablets containing asenapine maleate. The problem addressed is providing an asenapine maleate orally disintegrating tablet that dissolves rapidly and disintegrates adequately while also maintaining stability under storage conditions.
The invention achieves high dissolution by using a low substituted hydroxypropylcellulose solid matrix. It further achieves adequate disintegration in compressed tablets even with crystalline asenapine maleate, including crystalline monoclinic form H, using conventional tabletting approaches rather than lyophilization or blister-based Zydis® processing.
To enhance storage stability of asenapine maleate orally disintegrating tablets, the invention includes a carboxylic acid excipient. The carboxylic acid is described as being present at about 0.2 to 2.0% w/w, with examples including tartaric, succinic, fumaric, maleic, and other carboxylic acids, and storage performance is characterized by stability testing at 40°C/75% RH.
Claims Coverage
The document includes two independent claims. Both independent claims center on an orally disintegrating tablet comprising asenapine maleate, a specified carboxylic acid loading, and pharmaceutical excipients, together with defined stability performance at 40°C and 75% rH for at least 3 months relative to a tablet without carboxylic acid.
Orally disintegrating tablet with asenapine maleate, carboxylic acid, and stability at 40°C/75% rH
An orally disintegrating tablet comprising asenapine maleate, a carboxylic acid in an amount of 0.2 to 2.0% by weight based on total weight of the tablet, and one or more pharmaceutical excipients, wherein the tablet is stable at 40°C and 75% rH for at least 3 months compared to a tablet having no carboxylic acid.
Orally disintegrating tablet with asenapine maleate, carboxylic acid, and stability at 40°C/75% rH
An orally disintegrating tablet comprising asenapine maleate, a carboxylic acid in an amount of 0.75 to 2.5% by weight based on total weight of the tablet, and one or more pharmaceutical excipients, wherein the tablet is stable at 40°C and 75% rH for at least 3 months compared to a tablet having no carboxylic acid.
Across the independent claims, the core inventive coverage is the combination of asenapine maleate in an orally disintegrating tablet with a carboxylic acid at a specified weight range and one or more pharmaceutical excipients, requiring stability at 40°C/75% rH for at least 3 months compared to a tablet without carboxylic acid.
Stated Advantages
Stability at 40°C and 75% rH for at least 3 months compared to a tablet having no carboxylic acid.
Documented Applications
No documented applications found
Interested in licensing this patent?