Pharmaceutical composition comprising dapagliflozin
Inventors
Shah, Vaibhavi • Redasani, Vijayendrakumar • Ghongade, Anant
Assignees
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Publication Number
US-11020412-B2
Publication Date
2021-06-01
Expiration Date
Abstract
The present invention relates to solid oral pharmaceutical compositions comprising amorphous dapagliflozin. The invention further relates to a process for the preparation of the said pharmaceutical compositions. The said compositions are administered orally for the treatment of diabetes mellitus. The said compositions provide the desired immediate release of dapagliflozin and were found to be stable under accelerated conditions.
Core Innovation
The invention relates to solid oral immediate-release pharmaceutical tablet compositions comprising amorphous dapagliflozin. The amorphous dapagliflozin is characterized by a d(0.5) in the range from 20 m to 75 m, and the tablet includes one or more surfactants.
A key aspect of the compositions is the weight ratio of dapagliflozin to the surfactant being from about 1:0.1 to 1:10. The disclosed formulations include surfactants such as polysorbates, including micro-encapsulated polysorbate 80, and other surfactants and excipients mentioned in the document.
The disclosure further characterizes performance through in-vitro immediate-release dissolution and stability. Immediate-release dissolution is reported under USP II paddle conditions at pH 4.5, and accelerated stability is reported at 40C/75% RH in HDPE containers with silica gel and in Alu-Alu blisters, including retention of dissolution behavior and control of impurities and assay.
Claims Coverage
The partial content includes two independent claims, each defined by amorphous dapagliflozin particle size, an immediate-release tablet format, and a specified dapagliflozin-to-surfactant weight ratio. The second independent claim additionally specifies micro-encapsulated polysorbate 80 and an explicit impurity limit after storage in either HDPE or Alu-Alu blister.
Amorphous dapagliflozin with controlled particle size for immediate release
A pharmaceutical tablet composition comprising amorphous dapagliflozin having a d(0.5) in the range from 20 m to 75 m, wherein the tablet is an immediate release tablet.
Dapagliflozin-to-surfactant weight ratio in an immediate release tablet
The weight ratio of dapagliflozin to the surfactant is from about 1:0.1 to 1:10 in a pharmaceutical tablet composition.
Micro-encapsulated polysorbate 80 with impurity limit after storage
An immediate release tablet comprising amorphous dapagliflozin (d(0.5) 20 m to 75 m) and a surfactant which is micro-encapsulated polysorbate 80, wherein after storage at 40C and 75% relative humidity in a HDPE container or in an Alu-Alu blister for 6 months, the tablet contains no more than 1.0% of total dapagliflozin impurities.
Overall, the claim coverage centers on immediate-release tablets containing amorphous dapagliflozin with a specified d(0.5), combined with surfactants at a defined dapagliflozin-to-surfactant weight ratio, and, for the second independent claim, a specific micro-encapsulated polysorbate 80 selection plus a post-storage total impurity limit.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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