Pharmaceutical composition comprising dapagliflozin
Inventors
Shah, Vaibhavi • Redasani, Vijayendrakumar • Ghongade, Anant
Assignees
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Publication Number
US-11660308-B2
Publication Date
2023-05-30
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 compositions comprising amorphous dapagliflozin as a first active ingredient. The amorphous dapagliflozin is characterized by a particle size distribution having a d(0.5) in the range from 20 μm to 75 μm, and the composition further includes one or more surfactants to form the solid oral dosage.
A second active ingredient is also included, selected from biguanides, sulfonylureas, thiazolidinediones, alpha-glucosidase inhibitors, DPP4 inhibitors, PPAR agonists, meglitinides, and SGLT2 inhibitors, or from a defined list of specific antidiabetic agents that includes metformin, phenformin, glyburide, glimepiride, glipizide, gliclazide, chlorpropamide, pioglitazone, rosiglitazone, troglitazone, acarabose, voglibose, miglitol, sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin, saraglitazar, muraglitazar, peliglitazar, tesaglitazar, repaglinide, nateglinide, canagliflozin and ertugliflozin.
The key formulation relationship is that the weight ratio of dapagliflozin to the surfactant is from about 1:0.1 to 1:10. The disclosed compositions also include specific surfactant classes and excipient classes within the solid oral immediate-release dosage forms, together with dissolution and stability observations and reported bioequivalence to FARXIGA®.
Claims Coverage
Two independent claims are identified. Both claims share the same core formulation constraints: amorphous dapagliflozin with a defined d(0.5) range and a specified dapagliflozin:surfactant weight ratio, together with a second selected active ingredient and one or more surfactants.
Solid oral composition with amorphous dapagliflozin particle size and surfactant ratio
A solid oral composition comprising amorphous dapagliflozin having a d(0.5) in the range from 20 μm to 75 μm, and one or more surfactants, wherein the weight ratio of dapagliflozin to the surfactant is from about 1:0.1 to 1:10.
Solid oral combination with a second active ingredient from a defined group
The solid oral composition further comprising a second active ingredient selected from the group consisting of biguanides, sulfonylureas, thiazolidinediones, alpha-glucosidase inhibitors, DPP4 inhibitors, PPAR agonists, meglitinides, and SGLT2 inhibitors, together with amorphous dapagliflozin and one or more surfactants under the stated weight ratio.
Solid oral composition with a second active ingredient selected from a specified antidiabetic list
A solid oral composition comprising amorphous dapagliflozin having a d(0.5) in the range from 20 μm to 75 μm, a second active ingredient selected from the group consisting of metformin, phenformin, glyburide, glimepiride, glipizide, gliclazide, chlorpropamide, pioglitazone, rosiglitazone, troglitazone, acarabose, voglibose, miglitol, sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin, saraglitazar, muraglitazar, peliglitazar, tesaglitazar, repaglinide, nateglinide, canagliflozin and ertugliflozin, and one or more surfactants, wherein the weight ratio of dapagliflozin to the surfactant is from about 1:0.1 to 1:10.
Across both independent claims, the claim coverage is directed to solid oral compositions containing amorphous dapagliflozin with a specified d(0.5) range and a specified dapagliflozin-to-surfactant weight ratio, combined with a second active ingredient selected from defined antidiabetic drug groupings and one or more surfactants.
Stated Advantages
Improved solid oral formulation performance, as supported by dissolution/release constraints stated in dependent claims.
Stability performance under accelerated stability conditions is reported.
Bioequivalence to FARXIGA® is reported.
Documented Applications
Solid oral immediate-release pharmaceutical compositions containing amorphous dapagliflozin and one or more surfactants, including tablet formulations.
Use of the compositions with a second active ingredient selected from defined antidiabetic drug classes, including combinations such as metformin in the specified list for the second independent claim.
Bioequivalence testing of an example formulation versus FARXIGA® in a human crossover study.
Accelerated stability evaluation under the reported accelerated stability condition.
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