Author(s):
Umesh Kumar Atneriya, Navin Sainy, Aman Kansare, Deepak Rayakwar, Aamir Sheikh
Email(s):
atneriya@gmail.com , nsainy23@gmail.com , aman.kansare@yahoo.co.in , deepakrayakwar94@gmail.com , emirsheikh97@gmail.com
DOI:
10.52711/0974-360X.2026.00442 
Address:
Umesh Kumar Atneriya1*, Navin Sainy2, Aman Kansare3, Deepak Rayakwar4, Aamir Sheikh5
1School of Pharmacy, Devi Ahilya Vishwavidyalaya, Takshila Campus, Indore, (M.P.), 452020 India.
2,3,4,5Oriental College of Pharmacy and Research, Oriental University, Indore, Madhya Pradesh 452020 India.
*Corresponding Author
Published In:
Volume - 19,
Issue - 7,
Year - 2026
ABSTRACT:
Objective: D-a-Tocopheryl polyethylene glycol 1000 succinate (Vitamin E TPGS) has emerged as a compound of growing interest in recent years like a versatile excipient capable of improving the dissolution properties of poorly soluble drugs. Ezetimibe (EZB), used for lowering cholesterol levels, demonstrates extremely limited water solubility (approximately 0.000602mg/ml) and belongs to BCS Class II, characterized by slow dissolution despite good permeability. Material and Methods: This study focused on formulating a immediate dissolved tablet of EZB utilizing the vitamin E TPGS used as a carrier to increase EZB release rate with expedite its entry into systemic circulation. Initially, various carriers were evaluated based on dissolution studies conducted with solid dispersions (SD). Fast-dissolving tablets were later formulated using direct compression, followed by characterization through X-ray diffraction (XRD) and assessment of their dissolution behavior under in vitro conditions. Results: The successful development of SD incorporating Vitamin E TPGS was verified through X-ray diffraction analysis, which revealed alterations in the physical state of EZB. The dissolution profile studies demonstrated that EZB tablets provided a significantly enhanced release of EZB (93% within 30 min.) approximately ten times greater compared to tablets containing pure EZB alone. Conclusion: Results obtained in this work highlight the potential carrier (vitamin E TPGS) as an innovative carrier, improve the Kinetics of solute release of EZB through this approach, aiming to enhance the therapeutic efficacy in managing elevated cholesterol levels in blood.
Cite this article:
Umesh Kumar Atneriya, Navin Sainy, Aman Kansare, Deepak Rayakwar, Aamir Sheikh. Development of Fast Release Tablet of Ezetimibe by Solid Dispersion Techniques Using Vitamin E-D-α-Tocopheryl polyethylene glycol 1000 succinate as Molecular Biomaterial. Research Journal of Pharmacy and Technology. 2026;19(7):3113-0. doi: 10.52711/0974-360X.2026.00442
Cite(Electronic):
Umesh Kumar Atneriya, Navin Sainy, Aman Kansare, Deepak Rayakwar, Aamir Sheikh. Development of Fast Release Tablet of Ezetimibe by Solid Dispersion Techniques Using Vitamin E-D-α-Tocopheryl polyethylene glycol 1000 succinate as Molecular Biomaterial. Research Journal of Pharmacy and Technology. 2026;19(7):3113-0. doi: 10.52711/0974-360X.2026.00442 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2026-19-7-29
5.0 REFERENCE:
1. Atneriya, U.; Sainy, J.; Chidrawar, V. R.; Sharma, M.; Maheshwari, R. In D-optimal mixture design inspired modified release tablet formulation of lamotrigine for the treatment of seizures: An in-depth characterization, Annales Pharmaceutiques Françaises, Elsevier: 2024; 446-463.
2. Fernandes, G. J.; Kumar, L.; Sharma, K.; Tunge, R.; Rathnanand, M., A review on solubility enhancement of carvedilol—a BCS class II drug. Journal of Pharmaceutical Innovation. 2018; 13: 197-212.
3. Homayun, B.; Lin, X.; Choi, H.-J., Challenges and recent progress in oral drug delivery systems for biopharmaceuticals. Pharmaceutics. 2019; 11 (3): 129.
4. Singh, D.; Bedi, N.; Tiwary, A. K., Enhancing solubility of poorly aqueous soluble drugs: Critical appraisal of techniques. Journal of Pharmaceutical Investigation 2018; 48: 509-526.
5. Zhan, S.; Tang, M.; Liu, F.; Xia, P.; Shu, M.; Wu, X., Ezetimibe for the prevention of cardiovascular disease and all‐cause mortality events. Cochrane Database of Systematic Reviews. 2018; 11.
6. Atneriya, U.; Kapoor, D.; Sainy, J.; Maheshwari, R. In In vitro profiling of fenofibrate solid dispersion mediated tablet formulation to treat high blood cholesterol, Annales Pharmaceutiques Françaises, Elsevier: 2023; pp 284-299.
7. Tian, Y.; Jacobs, E.; Jones, D. S.; McCoy, C. P.; Wu, H.; Andrews, G. P., The design and development of high drug loading amorphous solid dispersion for hot-melt extrusion platform. International Journal of Pharmaceutics 2020; 586: 119545.
8. Pandi, P.; Bulusu, R.; Kommineni, N.; Khan, W.; Singh, M., Amorphous solid dispersions: An update for preparation, characterization, mechanism on bioavailability, stability, regulatory considerations and marketed products. International Journal of Pharmaceutics. 2020; 586: 119560.
8 Al-Shammary, A. A. G.; Kouzani, A. Z.; Kaynak, A.; Khoo, S. Y.; Norton, M.; Gates, W., Soil bulk density estimation methods: A review. Pedosphere. 2018; 28(4): 581-596.
9 Jasim, A. M.; Hasan, H. F.; Awady, M. J., Preparation of Vorapaxar loaded with Vitamin E TPGS and PVA emulsified PLGA nanoparticles In vitro studies. Research Journal of Pharmacy and Technology. 2019; 12 (9): 4503-4510.
10 Papas, A. M., Vitamin E TPGS and its applications in nutraceuticals. In Nutraceuticals, Elsevier: 2021; pp 991-1010.
11 Molavi, F.; Hamishehkar, H.; Nokhodchi, A., Impact of tablet shape on drug dissolution rate through immediate released tablets. Advanced Pharmaceutical Bulletin. 2020; 10 (4): 656.
12 Esha, P.; Dedania, Z.; Dedania, R.; Jain, V., UV Spectroscopic Method Development and Validation for the Simultaneous Estimation of Pitavastatin Calcium and Ezetimibe in Combined Pharmaceutical Formulation. 2021.
13 Huang, S.; Williams, R. O., Effects of the preparation process on the properties of amorphous solid dispersions. AAPS PharmSciTech. 2018; 19: 1971-1984.
14 Nickerson, B.; Kong, A.; Gerst, P.; Kao, S., Correlation of dissolution and disintegration results for an immediate-release tablet. Journal of Pharmaceutical and Biomedical Analysis. 2018; 150: 333-340.
15 Conceição, J.; Adeoye, O.; Cabral-Marques, H. M.; Lobo, J. M. S., Cyclodextrins as excipients in tablet formulations. Drug Discovery Today. 2018; 23 (6): 1274-1284.
16 Dhahir, R. K.; Al-Kotaji, M., Formulation of orally disintegrating tablets of cinnarizine by using direct compression method. Int J Appl Pharm. 2019; 11 (1): 117-123.
17 Al-Hashemi, H. M. B.; Al-Amoudi, O. S. B., A review on the angle of repose of granular materials. Powder Technology. 2018; 330: 397-417.
18 Kaleem, M. A.; Alam, M. Z.; Khan, M.; Jaffery, S. H. I.; Rashid, B., An experimental investigation on accuracy of Hausner Ratio and Carr Index of powders in additive manufacturing processes. Metal Powder Report. 2021; 76: S50-S54.
19 Saker, A.; Cares-Pacheco, M.-G.; Marchal, P.; Falk, V., Powders flowability assessment in granular compaction: What about the consistency of Hausner ratio? Powder Technology. 2019; 354: 52-63.
20 Wünsch, I.; Finke, J. H.; John, E.; Juhnke, M.; Kwade, A., A mathematical approach to consider solid compressibility in the compression of pharmaceutical powders. Pharmaceutics. 2019; 11(3): 121.
21 Khaled, S. A.; Alexander, M. R.; Irvine, D. J.; Wildman, R. D.; Wallace, M. J.; Sharpe, S.; Yoo, J.; Roberts, C. J., Extrusion 3D printing of paracetamol tablets from a single formulation with tunable release profiles through control of tablet geometry. AAPS Pharmscitech. 2018; 19: 3403-3413.
22 Hasan, A.; Abd Elghany, M.; Sabry, S., Design and characterization of intra-oral fast dissolving tablets containing diacerein-solid dispersion. Journal of Applied Pharmaceutical Science. 2020; 10 (6): 044-053.
23 Akhtar, M. S., Formulation and evaluation of fast dissolving tablets of antiepileptic drug. Universal Journal of Pharmaceutical Research. 2019; 4 (6): 20-24.
24 Nayak, S.; Rakshita, A.; Kamath, S., Study of post compression parameters of various marketed paracetamol tablets in India. PharmaTutor. 2019; 7 (2): 35-42.
25 Soni, H.; Ghulaxe, C.; Upadhyay, S.; Pillai, S., Development and in vitro evaluation of an oral floating tablet of metronidazole. Journal of Drug Delivery and Therapeutics. 2018; 8(2): 83-86.
26 Berardi, A.; Bisharat, L.; Quodbach, J.; Rahim, S. A.; Perinelli, D. R.; Cespi, M., Advancing the understanding of the tablet disintegration phenomenon–an update on recent studies. International Journal of Pharmaceutics. 2021; 598: 120390.
27 Zhao, Y.; Li, W.; Shi, Z.; Drennen III, J. K.; Anderson, C. A., Prediction of dissolution profiles from process parameters, formulation, and spectroscopic measurements. Journal of Pharmaceutical Sciences. 2019; 108(6): 2119-2127.
28 Paarakh, M. P.; Jose, P. A.; Setty, C.; Peterchristoper, G., Release kinetics–concepts and applications. International Journal of Pharmacy Research & Technology (IJPRT). 2018; 8(1): 12-20.
29 Mircioiu, C.; Voicu, V.; Anuta, V.; Tudose, A.; Celia, C.; Paolino, D.; Fresta, M.; Sandulovici, R.; Mircioiu, I., Mathematical modeling of release kinetics from supramolecular drug delivery systems. Pharmaceutics. 2019; 11(3): 140.