Gastric floating matrix tablets: Design and optimization using combination of polymers

Prajapati, Shailesh; Patel, Laxmanbhai; Patel, Dasharath

doi:10.2478/v10007-008-0006-3

Abstract

The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X₁), Carbopol 934P (X₂) and sodium alginate (X₃), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t₅₀) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties.

References

A. A. Deshpande, C. T. Rhodes, N. H. Shah, A. W. Malick, Controlled-release drug delivery systems for prolonged gastric residence: an overview, Drug. Dev. Ind. Pharm. 22 (1996) 631-539; DOI: 10.3109/03639049609063217.10.3109/03639049609063217
Search in Google Scholar
S. J. Hwang, H. Park and K. Park, Gastric retentive drug-delivery systems, Crit. Rev. Ther. Drug. Carrier. Syst. 15 (1998) 243-283.
Search in Google Scholar
A. A. Deshpande, N. H. Shah, C. T. Rhodes and A. W. Malick. Development of a novel controlled-release system for gastric retention, Pharm. Res. 14 (1997) 815-819; DOI: 10.1023/A:101217-1010492.
Search in Google Scholar
S. S. Davis, A. F. Stockwell, M. J. Taylor, J. G. Hardy, D. R. Whalley, C. G. Wilson, H. Bechgaard and F. N. Christensen, The effect of density on the gastric emptying of single and multiple-unit dosage forms, Pharm. Res. 3 (1986) 208-213; DOI: 10.1023/A: 1016334629169.
Search in Google Scholar
R. Groning and G. Heun, Dosage forms with controlled gastrointestinal passage-studies on the absorption of nitrofurantoin, Int. J. Pharm. 56 (1989) 111-116; DOI: 10.1016/0378-5173(89)90003-3.10.1016/0378-5173(89)90003-3
Search in Google Scholar
A. Streubel, J. Siepmann and R. Bodmeier, Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release, Eur. J. Pharm. Sci. 18 (2003) 37-45; DOI: 10.1016/S0928-0987(02)00223-3.10.1016/S0928-0987(02)00223-3
Search in Google Scholar
Martindale - The Extra Pharmacopoeia, 31^st ed., Pharmaceutical Press, London 1996, pp. 1217-1218.
Search in Google Scholar
M. Albright Lisa, Use of domperidone as a prokinetic and antiemetic, health and wellness, Int. J. Pharm. Comp. 9 (2005) 120-125.
Search in Google Scholar
B. Mehta, P. Doshi, M. Joshi and M. Dattat, Floating Osmotic Device for Controlled Release Drug Delivery, U.S. Pat. 9,92,897 3 March 2003.
Search in Google Scholar
K. Naonori, H. Yatabe, K. Iseki and M. Katsumi, A new type of pH independent controlled release tablet, Int. J. Pharm. 68 (1991) 255-264; DOI: 10.1016/0378-5173(91)90147-G.10.1016/0378-5173(91)90147-G
Search in Google Scholar
K. Thomma and T. Zimmer, Retardation of weakly basic drug with diffusion tablet, Int. J. Pharm. 58 (1990) 197-202; DOI: 10.1016/0378-5173(90)90195-A.10.1016/0378-5173(90)90195-A
Search in Google Scholar
P. R. Sheth and J. L. Tossounian, Sustained Release Tablet Formulations, U.S. Pat. 4,140,755 2 Feb 1979.
Search in Google Scholar
M. Rosa, H. Zia and T. Rhodes, Dosing and testing in-vitro of a bioadhesive and floating drug delivery system for oral application. Int. J. Pharm. 105 (1994) 65-70; DOI: 10.1016/0378-5173(94)90236-4.10.1016/0378-5173(94)90236-4
Search in Google Scholar
British Pharmacopoeia, HMSO, London 2000, pp. 732.
Search in Google Scholar
N. A. Peppas, Analysis of Fickian and non-Fickian drug release from polymers, Pharm. Acta Helv. 60 (1985) 110-111.
Search in Google Scholar
S. Li, S. Lin, Y. W. Chein, B. P. Daggy and H. L. Mirchandani, Statistical optimisation of gastric floating system for oral controlled delivery of calcium, AAPS Pharm. Sci. Tech. 2 (2001) article 1; http://www.pharmscitech.com. http://www.pharmscitech.com10.1208/pt020101
Search in Google Scholar
S. Li, S. Lin, B. P. Daggy, H. L. Mirchandani and Y. W. Chein, Effect of HPMC and carbopol on the release and the floating properties of gastric floating drug delivery system using factorial design, Int. J. Pharm. 253 (2003) 13-22; DOI: 10.1016/S0378-5173(02)00642-7.10.1016/S0378-5173(02)00642-7
Search in Google Scholar
F. Kedzierewicz, P. Thouvenot, J. Lemut, A. Etienne, M. Hoffman and P. Maincent, Evaluation of peroral silicone dosage forms in humans by gamma-scintigraphy, J. Control. Rel. 58 (1999) 195-205; DOI: 10.1016/S0168-3659(98)00154-0.10.1016/S0168-3659(98)00154-0
Search in Google Scholar

Gastric floating matrix tablets: Design and optimization using combination of polymers

Abstract

Paradigm

My account