Main Article Content
methylcellulose (HPMC K100M) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and Sodium CMC (SCMC) as bioadhesive polymer. A 32 full factorial design and response surface methodology were used for designing of
experiment, mapping change in responses and deriving optimum formulation. Selected independent variables were amounts HPMC K100M and SCMC polymer while floating lag time (FLT), bioadhesive strength, t50 (time taken to release 50% of drug) and t90 (time taken to release 90% of drug) were selected as dependent variables. Investigation of functionality of individual polymer to predict effect on dependent variable were statistically analyzed using the RSM.Tablets were also evaluated for physical properties, swelling and matrix erosion. Increase in concentration of HPMC and decrease in concentration of SCMC resulted in retardation of drug release. Furthermore, combination of HPMC K100M and sodium bicarbonate along with SCMC was found to affect buoyancy, bioadhesion strength and drug release. Optimized formulation showed values of
dependent variables close to predicted values. Optimized formulation follows Higuchi kinetics with short buoyancy lag time, total buoyancy time of more than 24 hours and could maintain drug release for 24 hours. Content uniformity, hardness, friability, weight variation were all lying within limits. Hence, FBDDS was found to be very promising and alternative approach to increase gastric retention of dosage form and may improve bioavailability.
This is an Open Access article distributed under the terms of the Attribution-Noncommercial 4.0 International License [CC BY-NC 4.0], which requires that reusers give credit to the creator. It allows reusers to distribute, remix, adapt, and build upon the material in any medium or format, for noncommercial purposes only.
Mikos AG, Peppas NA. Bioadhesive analysis of controlled-release
systems. IV. An experimental method for testing the adhesion of
microparticles with mucus. J Control Release 1990;12:31-7.
Hong SI, Oh SY. Dissolution kinetics and physical characterization of
three-layered tablet with poly(ethylene oxide) core matrix capped by
Carbopol. Int J Pharm 2008;356:121-9.
McGinity JW, Koleng JJ, Repka MA, Zhang F. Hot melt extrusion
technology. In: Swarbrik J, editor. Encylopedia of Pharmaceutical
Techonology. 3rd ed. New York: Informa Healthcare USA, Inc; 2005. p.
Trotta M, Gasco MR, Morel S. Release of drugs from oil-water
microemulsions. J Control Release 1989;10:237-43.
Chavanpatil MD, Jain P, Chaudhari S, Shear R, Vavia P. Development of
sustained release gastroretentive drug delivery system for ofloxacin:
In vitro and in vivo evaluation. Int J Pharm 2005;304:178-84.
Deshpande AA, Rhodes CT, Shah NH, Malick AW. Controlled-Release
Drug Delivery Systems for Prolonged Gastric Residence: An Overview.
Drug Dev Ind Pharm 1996;22:531-9.
Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit
Rev Ther Drug Carrier Syst 1998;15:243-84.
Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery
systems: A review. AAPS PharmSciTech 2005;6:E372-90.
Rouge N, Buri P, Doelker E. Drug absorption sites in the gastrointestinal
tract and dosage forms for site-specific delivery. Int J Pharm
Bardonnet PL, Faivre V, Pugh WJ, Piffaretti JC, Falson F. Gastroretentive
dosage forms: Overview and special case of Helicobacter pylori. J
Control Release 2006;111:1-18.
Garg S, Sharma S. Gastroretentive drug delivery systems. Business
Briefing, Available on http://www.touchbriefings.com 2003;160-6.
Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastroretentive
dosage forms. J Control Release 2003;90:143-62.
Singh BN, Kim KH. Floating drug delivery systems: An approach to
oral controlled drug delivery via gastric retention. J Control Release
14. Baumgartner S, Kristl J, VreÄer F, Vodopivec P, Zorko B. Optimization
of floating matrix tablets and evaluation of their gastric residence time.
Int J Pharm 2000;195:125-35.
Khosla R, Davis SS. The effect of tablet size on the gastric emptying of
non-disintegrating tablets. Int J Pharm 1990;62:R9-R11.
Mojaverian P, Vlasses PH, Kellner PE, Rocci ML Jr. Effects of gender,
posture, and age on gastric residence time of an indigestible solid:
Pharmaceutical considerations. Pharm Res 1988;5:639-44.
Srivastava AK, Wadhwa S, Ridhurkar D, Mishra B. Oral sustained
delivery of atenolol from floating matrix tablets formulation and in vitro
evaluation. Drug Dev Ind Pharm 2005;31:367-74.
Chueh HR, Zia H, Rhodes CT. Optimization of sotalol floating and
bioadhesive extended release tablet formulations. Drug Dev Ind Pharm
Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a
novel controlled-release system for gastric retention. Pharm Res
Ingani HM, Timmermans J, MoÃ«s AJ. Conception and in vivo investigation
of peroral sustained release floating dosage forms with enhanced
gastrointestinal transit. Int J Pharm 1987;35:157-64.
Dave BS, Amin AF, Patel MM. Gastroretentive drug delivery system of
ranitidine hydrochloride: Formulation and in vitro evaluation. AAPS
Chowdary KP, Suresh B, Sangeeta B, Reddy GK. Design and evaluation
of diltiazem mucoadhesive tablets for oral controlled release. Saudi
Pharm J 2003;11:201-5.
Varshosaz J, Tavakoli N, Roozbahani F. Formulation and in vitro
characterization of ciprofloxacin floating and bioadhesive extended-
release tablets. Drug Deliv 2006;13:277-85.
Hoffman BB. Therapy of Hypertension. In: Brunton LL, Lazo JS,
Parker KL, editors. Goodman and Gilmanâ€™s the pharmacological basis
of therapeutics. 11th ed. New York: McGraw-Hill; 2006. p. 845-68.
Kendall MJ, Maxwell SR, Sandberg A, Westergren G. Controlled release
metoprolol. Clinical pharmacokinetic and therapeutic implications. Clin
Feliciano NR, Bouvet AA, Redalieu E, Castellana J, Luders RC,
Schwartz DJ, et al. Pharmacokinetic and pharmacodynamic comparison
of an osmotic release oral metoprolol tablet and the metoprolol
conventional tablet. Am Heart J 1990;120:483-9.
Good W, Leeson LJ, Zak SL, Wagner WE, Meeker JB, Arnold JD. Oros
controlled-release formulations of metoprolol: An approach to the
development of a system for once daily administration. Br J Clin
Pharmacol 1985;19 Suppl 2:231S-8S.
Lucker P, Moore G, Wieselgren I, Olofsson B, Bergstrand R.
Pharmacokinetic and pharmacodynamic comparison of metoprolol
CR/ZOK once daily with conventional tablets once daily and in divided
doses. J Clin Pharmacol 1990;30(2 Suppl):S17-27.
Sandberg A, Abrahamsson B, Svenheden A, Olofsson B, Bergstrand R.
Steady-state bioavailability and day-to-day variability of a multiple-unit
(CR/ZOK) and a single-unit (OROS) delivery system of metoprolol after
once-daily dosing. Pharm Res 1993;10:28-34.
Kendall M, Akhlaghi S, Hughes B, Lewis H. Is metoprolol CR/ZOK more
selective than conventional metoprolol and atenolol? J Clin Pharmacol
Cochran WG, Cox GM. Experimental designs. 2nd ed. New York: John
Wiley and Sons, Inc; 1957.
Bhavsar MD, Tiwari SB, Amiji MM. Formulation optimization for the
nanoparticles-in-microsphere hybrid oral delivery system using factorial
design. J Control Release 2006;110:422-30.
Singh B, Ahuja N. Response surface optimization of drug delivery
system. In: Jain NK, editor. Progress in controlled and novel drug
delivery systems. 1 st ed. New Delhi, India: CBS Publishers and
Distributors; 2004. p. 470-9.
Singh B, Ahuja N. Pharmaceutical experimental design (Drugs and the
Pharmaceutical Sciences, Vol. 92). In: Lewis GA, Mathieu D, Phan-Tan-
Luu R, editors. 1st ed. New York: Marcel Dekker; 1999. p. 498. Int J
Singh B, Dahiya M, Saharan V, Abuja N. Optimizing drug delivery
systems using systematic design of experiments. Part II: Retrospect
and prospects. Crit Rev Ther Drug Carrier Syst 2005;22:215-93.
Singh B, Kumar R, Abuja N. Optimizing drug delivery systems using
systematic design of experiments. Part I: Fundamental aspects. Crit
Rev Ther Drug Carrier Syst 2005;22:27-105.
USP: United States Pharmacopoeia. 23rd ed. United States of America:
Twin Brook Park Wag; 2006.
Chavanpatil MD, Jain P, Chaudhari S, Shear R, Vavia PR. Novel sustained
release, swellable and bioadhesive gastroretentive drug delivery system
for ofloxacin. Int J Pharm 2006;316:86-92.
Lalla JK, Gurnancy RA. Polymers for mucosal delivery-swelling and
mucoadhesive delivery. Indian Drugs 2002;39:270-6.
Grabovac V, Guggi D, Bernkop-Schnurch A. Comparison of the
mucoadhesive properties of various polymers. Adv Drug Deliv Rev
Tamburic S, Craig DQ. A comparison of different in vitro methods
for measuring mucoadhesive performance. Eur J Pharm Biopharm
Peppas NA, Huang Y. Nanoscale technology of mucoadhesive
interactions. Adv Drug Deliv Rev 2004;56:1675-87.
Dorozynski P, Jachowicz R, Kulinowski P, Kwiecinski S, Szybinski K,
Skorka T, et al. The macromolecular polymers for the preparation of
hydrodynamically balanced systems--methods of evaluation. Drug Dev
Ind Pharm 2004;30:947-57.
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution
profiles. Eur J Pharm Sci 2001;13:123-33.
Shah VP, Tsong Y, Sathe P, Liu JP. In vitro dissolution profile comparison--
statistics and analysis of the similarity factor, f2. Pharm Res 1998;15:889-96.
Mazzo DJ. International stability testing. USA: Interpharm press, Inc;
Whitehead L, Fell JT, Collett JH, Sharma HL, Smith A. Floating
dosage forms: An in vivo study demonstrating prolonged gastric
retention. J Control Release 1998;55:3-12.
Bolton S, Bon C. Pharmaceutical statistics: Practical and clinical
applications. 5th ed. New York: Marcel Dekker, Inc; 2010.
Schwartz JB, Oâ€™Connor RE, Schnaare RL. Optimization techniques in
pharmaceutical formulation and processing. In: Banker GS, Rhodes CT,
editors. Modern pharmaceutics. 4 th Revised and Expanded ed.
New York: Marcell Dekker, Inc; 2002. p. 607-26.