Sitagliptin and its formulations: a comprehensive review

Mohamed, Asmaa Abdelaziz Abdelaziz; Rahi, Firas A

	Sitagliptin and its formulations: a comprehensive review
Al-Zahraa Journal for Health and Medical Sciences
Volume 3, Issue 4, December 2025, Pages 72-84 PDF (586.33 K)
Document Type: Review Article
Authors
asmaa abdelaziz Abdelaziz Mohamed^* ¹; Firas A Rahi²
¹pharmaceutics department, College of Pharmacy, Al-Zahraa University for women, Karbala, Iraq
²al-nisour college university
Abstract
Sitagliptin (SIT), an oral dipeptidyl peptidase-4 (DPP-4) inhibitor used in the management of type 2 diabetes, has been formulated in various ways to optimize its delivery and improve patient outcomes. The conventional dosage form is immediate-release tablets, which allow for quick absorption. However, researchers have explored advanced formulations, including extended-release matrix tablets, such as those created with xanthan gum matrices, which can yield approximately 99.6% drug release over a period of 10 hours. Additionally, polymeric micro/nanoparticles have been developed, offering sustained release profiles ranging from 12 to 24 hours. These innovative approaches aim to enhance the therapeutic efficacy of Sitagliptin while minimizing peaks and troughs in drug levels, ultimately leading to better glycemic control and improved patient adherence to treatment regimens. Fixed‐dose combination tablets (notably SIT+metformin) such as Janumet (immediate-release) and Janumet XR (extended-release) have been introduced to simplify therapy. Emerging carriers – including SIT-loaded nanoparticles, transdermal patches, and mucoadhesive buccal films – have shown promise in bypassing first‐pass metabolism and sustaining drug release. These formulation innovations aim to enhance SIT’s bioavailability, extend its action, and improve patient adherence.
Keywords
sitagliptin; polymers. Excipients; solubility

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