Browse > Article
http://dx.doi.org/10.5762/KAIS.2015.16.11.7549

Development of Gastric Retentive Bi-layered Tablet using Floating Drug Delivery System  

Park, Jun-Bom (College of Pharmacy, Sahmyook University)
Publication Information
Journal of the Korea Academia-Industrial cooperation Society / v.16, no.11, 2015 , pp. 7549-7554 More about this Journal
Abstract
The aim of this study was to develop gastric retentive bi-layered tablet using floating drug delivery technique. Metformin was selected as a model drug due to its narrow absorption window as well as very highly water solubility. These properties of metformin led to be difficult controlling the drug release. The bi-layered tablet was prepared with bi-layered compression machine to minimize interference between floating part and controlling part. The tablet weight, appearance and hardness were evaluated after compression process. The times of 'time to floating' and 'Floating duration' were tested for floating ability and drug release study was also carried out to understand drug release behavior. Furthermore, the drug release of bi-layered tablet was compared with marketed metformin tablet with sustained release pattern (Glucopharge XR$^{(R)}$).The floating ability and drug release behaviors were well controlled by changing amounts of $NaHCO_3$ (floating substance) and hydroxypropyl methylcellulose (HPMC; release control material). Bi-layered tablet had 13s of time to float, over 10h of floating duration and very similar drug release behavior compared with Glucopharge XR$^{(R)}$($f_2$: 89.6). Consequently, the bi-layered tablet with floating ability was successfully prepared and these properties can maximize the efficacy of metformin.
Keywords
Bi-layer tablet; Floating Delivery; Gastric retentive; HPMC; Metformin;
Citations & Related Records
연도 인용수 순위
  • Reference
1 R. Damodar et al., Preparation and In-vitro Evaluation of Metformin HCl Tablets Containing Sustained Release Beads for Increasing Therapeutic Window. J Bioequivalence & Bioavailability, Vol. 6, pp. 91-95, 2014.
2 R. Chandrasekaran et al., The influence of calcium ions, acetate and L-glycerate group on the gellan double helix. Carbohydrate Polymer, Vol. 12, pp. 431-442, 1990. DOI: http://dx.doi.org/10.1016/0144-8617(90)90092-7   DOI
3 L. Rojas et al., Metformin: an old but still the best treatment for type 2 diabetes. Diabetology & Metabolic Syndrome, Vol. 5, pp. 1-15, 2013. DOI: http://dx.doi.org/10.1186/1758-5996-5-6   DOI
4 H. Balpande et al., Compatibility study of metformin with pharmaceutical excipients. International Journal of ChemTech Research, Vol. 5, pp. 1684-1693, 2013.
5 G. Namdeo et al., Advances in Gastroretentive Drug Delivery System: An Review, International Journal of Pharmacy and Pharmaceutical Science Research, Vol. 4, pp. 37-48, 2014.
6 J. Patel et al., Formulation and Optimization of Floating Effervescent Tablet of Roxitidine Acetate, International Journal of Pharmaceutical Archives, Vol. 3, pp. 447-452, 2014.
7 B. Singh et al., Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention, Journal of Controlled Release, Vol. 63, pp. 235-259, 2000. DOI: http://dx.doi.org/10.1016/S0168-3659(99)00204-7   DOI
8 P. Jha et al., Pharmaceutical Aspects of Various Floating Drug Delivery System, World Journal of Pharmacy and Pharmaceutical Sciences, Vol. 4, pp. 569-589, 2015.
9 A. Chandel et al., Floating Drug Delivery Systems: A Better Approach, International Current Pharmaceutical Journal, Vol. 1, pp. 110-118, 2012.
10 Hiten Panchal et al., Novel Approach of Bilayer tablet Technology: An Review. Journal of Pharmaceutical Science and Technology, Vol. 4 (4), pp. 892-904, 2012
11 Karel Six et al., Clinical study of solid dispersions of itraconazole prepared by hot-stage extrusion, European Journal of Pharmaceutical Sciences, Vol. 24 (2-3), pp. 179-186, 2005. DOI: http://dx.doi.org/10.1016/j.ejps.2004.10.005   DOI
12 Lara Tutunji et al., Simultaneous determination of irbesartan and hydrochlorothiazide in human plasma using HPLC coupled with tandem mass spectrometry: Application to bioequivalence studies, Journal of Pharmaceutical and Biomedical Analysis, Vol. 51 (4), pp. 985-990, 2010. DOI: http://dx.doi.org/10.1016/j.jpba.2009.10.023   DOI
13 S. El-Zahabya et al., Design and evaluation of gastroretentive levofloxacin floating mini-tablets-incapsule system for eradication of Helicobacter pylori, Saudi Pharmaceutical Journal, Vol. 22, pp. 570-579, 2014. DOI: http://dx.doi.org/10.1016/j.jsps.2014.02.009   DOI
14 S. Jagdale et al., Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride, AAPS PharmSciTech, Vol. 10, pp. 1071-1079, 2009. DOI: http://dx.doi.org/10.1208/s12249-009-9300-8   DOI
15 S. Alshahrani et al., Stability-enhanced Hot-melt Extruded Amorphous Solid Dispersions via Combinations of $Soluplus^{(R)}$ and HPMCAS-HF, AAPS PharmSciTech, Vol. 16, pp. 824-834, 2015. DOI: http://dx.doi.org/10.1208/s12249-014-0269-6   DOI
16 S. Alshehri et al., Mefenamic acid taste-masked oral disintegrating tablets with enhanced solubility via molecular interaction produced by hot melt extrusion technology, Journal of Drug Delivery Science and Technology, Vol. 27, pp. 18-27, 2015. DOI: http://dx.doi.org/10.1016/j.jddst.2015.03.003   DOI
17 P. Sharma et al., Co-processing of hydroxypropyl methylcellulose (HPMC) for improved aqueous dispersibility. International Journal of Pharmaceutics, Vol. 485 (1-2), pp. 348-356, 2015. DOI: http://dx.doi.org/10.1016/j.ijpharm.2015.03.036   DOI
18 G. Rombopoulos et al., Treatment Compliance with Fixed-Dose Combination of Vildagliptin / Metformin in Patients with Type 2 Diabetes Mellitus Inadequately Controlled with Metformin Monotherapy: A 24-Week Observational Study. International Journal of Endocrinology, Vol. 2015, pp. 1-5, 2015. DOI: http://dx.doi.org/10.1155/2015/251485
19 T. Yoshida et al., Salting-out taste-masking system generates lag time with subsequent immediate release, International Journal of Pharmaceutics, Vol. 365 (1-2), pp. 81-88, 2009. DOI: http://dx.doi.org/10.1016/j.ijpharm.2008.08.026   DOI
20 S. Banks et al., The influence of substituted phenols on the sol : gel transition of hydroxypropyl methylcellulose (HPMC) aqueous solutions. Carbohydrate Polymers, Vol. 101 (30), pp. 1198-1204, 2014. DOI: http://dx.doi.org/10.1016/j.carbpol.2013.10.061   DOI
21 M. Rendell, Diabetes "New drug options and old choices", Consultant, Vol. 53, pp. 217-227, 2013.