Optimized Formulation of Sitagliptin Fast Dissolving Tablets Using Statistical Design Techniques
Abstract
The study focused on developing and statistically optimizing sitagliptin-loaded fast-dissolving tablets (FDTs) utilizing a systematic DoE-based approach to enhance oral drug delivery and patient compliance in type 2-diabetes management. FDTs were prepared via direct compression with varying concentrations of variable excipients, Crospovidone (superdisintegrant) and Avicel 102 (binder) as part of a 3² full factorial design. The study assessed their impact on formulation attributes specifically hardness and disintegration time, alongside pre- and post-compression characteristics, dissolution performance, and stability over time. All developed formulations met pharmacopoeial standards. The optimized batch (B7) disintegrated in 34±3 seconds with adequate hardness of 4.5±0.09 kg/cm² and achieved 99.11% drug release within 30 minutes. Statistical analysis confirmed significant effects of both excipients, with crospovidone having a greater influence on disintegration. Stability studies over three months indicated no significant changes in key parameters. The results demonstrated a robust, cost-effective sitagliptin FDTs with improved dissolution properties, particularly beneficial for those with dysphagia or requiring immediate pharmacological response.
Keywords:
Sitagliptin, fast dissolving tablet, factorial design, Crospovidone, Avicel 102, disintegration timeDOI
https://doi.org/10.25004/IJPSDR.2025.170404References
Masih A, Kumar A, singh S, Tiwari AK. Fast dissolving tablets: A Review. International Journal of Current Pharmaceutical Research. 2017;9(2):8-18. Available from: doi.org/10.22159/ijcpr.2017v9i2.17382
Okuda Y, Irisawa Y, Okimoto K, Osawa T, Yamashita S. Further improvement of orally disintegrating tablets using micronized ethyl cellulose. International Journal of Pharmaceutics. 2012;423(2):351–9. Available from: doi.org/10.1016/j.ijpharm.2011.10.050
Patel D, Patel D J, Shah S, Shah A. Formulation and evaluation of fast dissolving tablet of nebivolol and valsartan. International Journal of Pharmaceutical Sciences and Research. 2020;11(11):5530-5539. Available from: doi.org/10.13040/IJPSR.0975-8232.11(11).5530-39
Basu B, Bagadiya A, Makwana S, Vipul V, Batt D, Dharamsi A. Formulation and evaluation of fast dissolving tablets of cinnarizine using superdisintegrant blends and subliming material. Journal of Advanced Pharmaceutical Technology & Research. 2011;2(4):266. Available from: doi.org/10.4103/2231-4040.90885
Sharma D. Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate for Respiratory Disorders. ISRN Pharmaceutics. 2013;2013:1–8. Available from: doi.org/10.1155/2013/674507
Satpute MM, Tour NS. Formulation and in vitro evaluation of fast dissolving tablets of metoprolol tartrate. Brazilian Journal of Pharmaceutical Sciences. 2013;49(4):783–92. Available from: doi.org/10.1590/s1984-82502013000400018
Plosker GL. Sitagliptin: A review of its use in patients with type 2 Diabetes Mellitus. Drugs. 2014;74(2):223–42. Available from: doi.org/10.1007/s40265-013-0169-1
Scott LJ. Sitagliptin: A Review in Type 2 Diabetes. Drugs. 2017;77(2):209-224. Available from: doi.org/10.1007/s40265-016-0686-9
Sharma D, Singh G, Kumar D, Singh M. Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate, Cetirizine Hydrochloride in Combined Pharmaceutical Dosage Form: A New Era in Novel Drug Delivery for Pediatrics and Geriatrics. Journal of Drug Delivery. 2015;2015:1–10. Available from: doi.org/10.1155/2015/640529
Yamuna B, Reshma T, Mahammed N. Quality by design (QbD) based approach for development of fast dissolving tablets. International Journal of Pharmaceutical Sciences and Research. 2023;14(4):1642-48. Available from: doi.org/10.13040/IJPSR.0975-8232.14(4).1642-48
Parshuramkar P, Khobragade D, Kashyap P. Comprehension of Quality by Design in the Development of Oral Solid Dosage Forms. Journal of Young Pharmacists, 2023; 15(3):406-418. Available from: doi.org/10.5530/jyp.2023.15.56
Zhu Y, Yu J, Zhou G, Gu Z, Adu-Frimpong M, Deng W, et al. Piperine fast disintegrating tablets comprising sustained-release matrix pellets with enhanced bioavailability: formulation, in vitro and in vivo evaluation. Pharmaceutical Development and Technology. 2020;25(5):617–24. Available from: doi.org/10.1080/10837450.2020.1725892
Kathpalia H, Venkatesh A, Sathe N. Topical Film Forming Clotrimazole Emulgel, Indian Journal of Pharmaceutical Education and Research. 2023;57(2s):s250-s261. Available from: doi.org/IndJPhaEdRes-57-2s-29
Chauhan A, Rohilla S, Jain S, Direct compression method. World Journal of Pharmacy and Pharmaceutical Sciences. 2019;8(9):692-701. Available from: doi.org/ 10.20959/wjpps20199-14588
Maheshwari S, Singh A, Varshney AP, Sharma A. Advancing oral drug delivery: The science of fast dissolving tablets. Intelligent Pharmacy. 2024;2(4):580–7. Available from: doi.org/10.1016/j.ipha.2024.01.011
Fahmy R, Kassem M. Enhancement of famotidine dissolution rate through liquisolid tablets formulation: In vitro and in vivo evaluation. European Journal of Pharmaceutics and Biopharmaceutics. 2008;69(3):993–1003. Available from: doi.org/10.1016/j.ejpb.2008.02.017
Rada SK, Kumari A. Fast dissolving tablets: waterless patient compliance dosage forms. Journal of Drug Delivery and Therapeutics. 2019;9(1):303–17. Available from: doi.org/10.22270/jddt.v9i1.2292
Rane DR, Gulve HN, Patil VV, Thakare VM, Patil VR. Formulation and evaluation of fast dissolving tablet of albendazole. International Current Pharmaceutical Journal. 2012;1(10):311–6. Available from: doi.org/10.3329/icpj.v1i10.11848
Tiwari R, Siddiqui MohdH, Mahmood T, Farooqui A, Tiwari M, Ahsan F. Formulation and Optimization of Polyherbal Fast Dissolving Tablet of Curcumin, Quercetin and Rutin. International Journal of Pharmaceutical Science and Drug Research. 2021;661–70. Available from: doi.org/10.25004/ijpsdr.2021.130609
Kotagale N, Maniyar M, Somvanshi S, Umekar M, Patel CJ.. Eudragit-S, Eudragit-L and cellulose acetate phthalate coated polysaccharide tablets for colonic targeted delivery of azathioprine. Pharmaceutical Development and Technology. 2010;15(4):431–437. Available from: doi.org/10.3109/10837450903264401
Saif A, M. Alburyhi M, Alwan Noman M. Formulation and Evaluation of Ketoprofen Fast Dissolving Tablets. International Journal of Sciences. 2018;4(09):27–39. Available from: doi.org/10.18483/ijSci.1789
Gunda R, Suresh Kumar J, Babu CA, Anjaneyulu M. Formulation development and evaluation of lamotrigine sustained release tablet using 32 factorial designs. International Journal of Pharma Sciences and Research. 2015;6(4): 1746-1752. Available from: doi.org/10.13040/IJPSR.0975-8232.6(4).1746-52
The Guideline, I.H. Stability Testing: Requirements for New Dosage Forms Q1C. 1996. Available from: database.ich.org/sites/default/files/Q1C Guideline.pdf
Eisa AM, El-Megrab NA, El-Nahas HM. Formulation and evaluation of fast dissolving tablets of haloperidol solid dispersion. Saudi Pharmaceutical Journal. 2022;30(11):1589–602. Available from: doi.org/10.1016/j.jsps.2022.09.002
Babu A, Akhtar MdS. Overview of formulation and evaluation of fast dissolving tablet: A promising tablet dosage form. Journal of Applied Pharmaceutical Science. 2020;8(3):1–9. Available from: doi.org/10.18231/j.joapr.2020.v.8.i.3.1.9
Borse BL, Bendale AR, Borse SL Naphade VD, Jadhav AG. Formulation and Evaluation of Mouth Dissolving Tablet Rivaroxaban and its Validation. Biosciences Biotechnology Research Asia. 2022;19(4):943–54. Available from: doi.org/10.13005/bbra/3043
Published
Abstract Display: 257 
PDF Downloads: 227 How to Cite
Issue
Section
Copyright (c) 2025 Devyani G. Bhadane, Sachin B. Somwanshi
This work is licensed under a Creative Commons Attribution 4.0 International License.
