Sitagliptin in diabetes management: a comprehensive review of therapeutic advantages, formulation challenges, and analytical strategies for oral solution development

Gaurav Sharma*, Harshit Gautam

University institute of Pharmaceutical Education & research, University Kota, Kota, Rajasthan, India

Refer this article

Gaurav Sharma, Harshit Gautam, 2026. Sitagliptin in diabetes management: a comprehensive review of therapeutic advantages, formulation challenges, and analytical strategies for oral solution development. Journal of medical pharmaceutical and allied sciences, V 15, I 4, Pages 32 – 38. Doi: https://doi.org/10.55522/jmpas.V15I4.7103.

ABSTRACT

Sitagliptin is a selective dipeptidyl peptidase-4 (DPP-4) inhibitor that has emerged as a mainstay in the treatment of type 2 diabetes mellitus (T2DM) on account of favourable efficacy, safety and tolerability profile. In this comprehensive review, we discuss the therapeutic advantages of sitagliptin, including its glucose-dependent mechanism of action, low risk of hypoglycemia, weight neutrality and proven cardiovascular safety as demonstrated by the landmark TECOS trial. The tablet formulation has been successful in clinical trials but there are large patient populations (paediatric, geriatric, dysphagic and critically ill) that require alternative liquid dosage forms. The formulation challenges of developing a stable sitagliptin oral solution are discussed, in relation to the moisture sensitivity of the drug, pH-dependent stability and the need to optimise palatability. A critical review of recent patent disclosures and formulation studies in the scientific literature shows that judicious selection of buffering agents (pH 4–6), artificial sweeteners (sucralose, acesulfame-K), preservatives (parabens) and thickening agents (hydroxyethylcellulose) are required for the successful development of an oral solution. Moreover, the review summarises the current literature on the development of analytical methods, emphasising the role of reverse-phase high-performance liquid chromatography (RP-HPLC) and the increasing application of Analytical Quality by Design (AQbD) principles for the development of stable and robust assay methods. Formulation science, analytical chemistry and patient-centric design principles can together meet the unmet clinical need for a commercially available, stable and quality-controlled oral solution of sitagliptin.

Keywords:

Sitagliptin, DPP-4 inhibitors, Formulation development, RP-HPLC, Analytical quality by Design.

Full Text Article