Formulation Development and Invitro Evaluation of Gliclazide Pellets using Superdisintegrants by Extrusion Spheronization Technique
DOI:
https://doi.org/10.37285/ijpsn.2023.16.1.2Abstract
Introduction: Gliclazide is a sulfonylurea derivative used for the treatment of type 2 Diabetes, it is an anti-diabetic drug it is marketed under the brand name Diamicron. It is taken orally and used when dietary changes, lack of exercise, and weight loss are not sufficient.
Aim: The principal objective of this work was to develop, formulate and evaluate the pellet formulations prepared with the incorporation of different super disintegrants in different ratios and in different combinations. In this research work, the drug gliclazide was chosen as a model drug and it was formulated into fast-dissolving pellets, which can be compressed into pelltabs and can also be filled into capsules.
Methods: Pellets were prepared by extrusion and Spheronization containing microcrystalline cellulose (MCC) and using gliclazide as a model drug with different super disintegrants namely croscarmellose sodium, crospovidone and sodium starch glycolate in different ratios, and in different combinations. Thus, in the present study, gliclazide pellets were developed using Extrusion-Spheronization for immediate drug delivery. The pellets were evaluated for percentage drug content, flow properties, friability, size analysis, shape analysis, disintegration test, and dissolution studies. Preformulation studies were then performed using solubility studies, partition co-efficient studies, infrared spectroscopy, and drug-excipients compatibility studies between the drug and selected excipients (croscarmellose sodium, crospovidone, and sodium starch glycolate) investigated.
Results: Formulations containing MCC, super disintegrants, and drugs in different ratios of 60/0/40, 55/5/40, and 50/10/40 w/w of croscarmellose sodium, crospovidone, and sodium starch glycolate were found to show faster release of the drug for 9 hours. Croscarmellose sodium releases the drug as it disintegrates the pellets. Sodium starch glycolate releases the drug by inducing swelling in the pellet matrix. Unlike the other two super disintegrants, there was no apparent change in the swelling capability of the pellets of polymer crospovidone (Polyplasdone XL10) in water. The percentage increase in diameter for Ac-Di-Sol (croscarmellose sodium), Primojel (sodium starch glycolate), and Polyplasdone XL10 were 104%, 251%, and 29% in water.
Conclusions: Various types of super disintegrants can be investigated for their suitability in formulating pellets. In vivo drug release rate, and bioavailability studies on animals and humans may be carried out to assess the superiority of the pellets over the tablet dosage form.
Downloads
Metrics
Keywords:
In Vitro Evaluation, Gliclazide, Pellets, Superdisintegrants, Extrusion Spheronization Technique
Downloads
Published
How to Cite
Issue
Section
References
Zhao N, Augsburger LL. The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets. AAPS PharmSciTech. 2005;6(1):E120-6.
Wang L, Wang J, Lin X, Tang X. Preparation and in vitro evaluation of gliclazide sustained-release matrix pellets: formulation and storage stability. Drug Dev Ind Pharm. 2010;36(7):814-822.
Tank D, Karan K, Gajera BY, Dave RH. Investigate the effect of solvents on wet granulation of microcrystalline cellulose using hydroxypropyl methylcellulose as a binder and evaluation of rheological and thermal characteristics of granules. Saudi Pharm J SPJ Off Publ Saudi Pharm Soc. 2018;26(4):593-602.
Taj Y, Pai RS, Kusum Devi V, Singh G. Taste Masked Orally Disintegrating Pellets of Antihistaminic and Mucolytic Drug: Formulation, Characterization, and In Vivo Studies in Human. Dutta S, ed. Int Sch Res Not. 2014;2014:504536.
Singh G, Pai RS, Devi VK. Optimization of pellets containing solid dispersion prepared by extrusion/spheronization using central composite design and desirability function. J Young Pharm. 2012;4(3):146-156.
Rahman MA, Ali J. Development and in vitro Evaluation of Enteric Coated Multiparticulate System for Resistant Tuberculosis. Indian J Pharm Sci. 2008;70(4):477-481.
Patel H, Pandey N, Patel B, Ranch K, Bodiwala K, Vyas B. Enhancement of in vivo hypoglycemic effect of gliclazide by developing self-microemulsifying pellet dosage form. Futur J Pharm Sci. 2020;6(1):17. doi:10.1186/s43094-020-00034-0
Fielden KE, Newton JM, O’Brien P, Rowe RC. Thermal Studies on the Interaction of Water and Microcrystalline Cellulose. J Pharm Pharmacol. 2011;40(10):674-678.
Alves-Silva I, Marreto RN, Gelfuso GM, Sá-Barreto LCL, Lima EM, Cunha-Filho MSS. Preparation of benznidazole pellets for immediate drug delivery using the extrusion spheronization technique. Drug Dev Ind Pharm. 2017;43(5):762-769.
Kumar A, Saharan VA. A Comparative Study of Different Proportions of Superdisintegrants: Formulation and Evaluation of Orally Disintegrating Tablets of Salbutamol Sulphate. Turkish J Pharm Sci. 2017;14(1):40-48.
Lam M, Asare-Addo K, Nokhodchi A. Rapid releasing naproxen Liqui-Pellet using effervescent agent and neusilin US2. Iran J Basic Med Sci. 2021;24(1):108-115.
Otsuka M, Gao J, Matsuda Y. Effect of Amount of Added Water During Extrusion- Spheronization Process on Pharmaceutical Properties of Granules. Drug Dev Ind Pharm. 1994;20(19):2977-2992.
Garekani HA, Aftabi SF, Nia FF, Javidi M, Nokhodchi A, Sadeghi F. Synergistic effect of polyethylene glycol and superdisintegrant on dissolution rate enhancement of simvastatin in pellet formulation. Pharm Dev Technol. 2019;24(6):720-728.
Rojas J, Guisao S, Ruge V. Functional assessment of four types of disintegrants and their effect on the spironolactone release properties. AAPS PharmSciTech. 2012;13(4):1054-1062.
Lam M, Ghafourian T, Nokhodchi A. Optimising the release rate of naproxen liqui-pellet: a new technology for emerging novel oral dosage form. Drug Deliv Transl Res. 2020;10(1):43-58.
Issa MG, Pessole L, Takahashi AI, Andréo Filho N, Ferraz HG. Physicochemical and dissolution profile characterization of pellets containing different binders obtained by the extrusion-spheronization process. Brazilian J Pharm Sci. 2012;48(3 SE-):379-388.
Broesder A, Bircan SY, de Waard AB, Eissens AC, Frijlink HW, Hinrichs WLJ. Formulation and In Vitro Evaluation of Pellets Containing Sulfasalazine and Caffeine to Verify Ileo-Colonic Drug Delivery. Pharmaceutics. 2021;13(12).
El-Mahdi IM, El-Shhibia SA. Effect of spheronizer plate design on the spheronization of ketoprofen. Futur J Pharm Sci. 2017;3(2):153-157.
Rezaei H, Lim CJ, Lau A, Sokhansanj S. Size, shape and flow characterization of ground wood chip and ground wood pellet particles. Powder Technol. 2016;301:737-746.
Couper JR, Penney WR, Fair JR, Walas SM, eds. Chapter 12 - Disintegration, Agglomeration, and Size Separation of Particulate Solids. In: Chemical Process Equipment (Second Edition). Second Edi. Gulf Professional Publishing; 2005:359-395.
Podczeck F, Knight P. The Evaluation of Formulations for the Preparation of Pellets with High Drug Loading by Extrusion/Spheronization. Pharm Dev Technol. 2006;11(3):263-
Umprayn K, Chitropas P, Amarekajorn S. Influence of Process Variables on Physical Properties of the Pellets Using Extruder and Spheronizer. Drug Dev Ind Pharm. 1999;25(1):46-61.
Shah RB, Tawakkul MA, Khan MA. Comparative evaluation of flow for pharmaceutical powders and granules. AAPS PharmSciTech. 2008;9(1):250-258.
Zakowiecki D, Szczepanska M, Hess T, et al. Preparation of delayed-release multiparticulate formulations of diclofenac sodium and evaluation of their dissolution characteristics using biorelevant dissolution methods. J Drug Deliv Sci Technol. 2020;60:101986.
Markl D, Zeitler JA. A Review of Disintegration Mechanisms and Measurement Techniques. Pharm Res. 2017;34(5):890-917.
Berardi A, Janssen PHM, Dickhoff BHJ. Technical insight into potential functional- related characteristics (FRCs) of sodium starch glycolate, croscarmellose sodium and crospovidone. J Drug Deliv Sci Technol. 2022;70:103261.
Saharan VA, Choudhury PK. Dissolution rate enhancement of gliclazide by ordered mixing. Acta Pharm. 2011;61(3):323—334.
