Abstract
The purpose of writing this review on floating drug delivery systems (FDDS) was to compile the recent literature with special focus on the principal mechanism of floatation to achieve gastric retention. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. This review also summarizes the in vitro techniques, in vivo studies to evaluate the performance and application of floating systems, and applications of these systems. These systems are useful to several problems encountered during the development of a pharmaceutical dosage form.
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References
Hirtz J. The git absorption of drugs in man: a review of current concepts and methods of investigation.Br J Clin Pharmacol. 1985;19:77S-83S.
Ponchel G, Irache JM. Specific and non-specific bioadhesive particulate system for oral delivery to the gastrointestinal tract.Adv Drug Del Rev. 1998;34:191–219.
Lenaerts VM, Gurny R. Gastrointestinal Tract-Physiological variables affecting the performance of oral sustained release dosage forms. In: Lenaerts V, Gurny R, eds.Bioadhesive Drug Delivery System. Boca Raton, FL: CRC Press; 1990.
Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled-release system for gastric retention.Pharm Res. 1997;14:815–819.
Rednick AB, Tucker SJ. Sustained release bolus for animal husbandry. US patent 3 507 952. April 22, 1970.
Davis SS, Stockwell AF, Taylor MJ, et al. The effect of density on the gastric emptying of single and multiple unit dosage forms.Pharm Res. 1986;3:208–213.
Urguhart J, Theeuwes F. Drug delivery system comprising a reservoir containing a plurality of tiny pills. US patent 4 434 153. February 28, 1994.
Mamajek RC, Moyer ES. Drug dispensing device and method. US Patent 4 207 890. June 17, 1980.
Fix JA, Cargill R, Engle K. Controlled gastric emptying. III. Gastric residence time of a non-disintegrating geometric shape in human volunteers.Pharm Res. 1993;10:1087–1089.
Kedzierewicz F, Thouvenot P, Lemut J, Etienne A, Hoffman M, Maincent P. Evaluation of peroral silicone dosage forms in humans by gamma-scintigraphy.J Control Release. 1999;58:195–205.
Groning R, Heun G. Oral dosage forms with controlled gastrointestinal transit.Drug Dev Ind Pharm. 1984;10:527–539.
Groning R, Heun G. Dosage forms with controlled gastrointestinal passage—studies on the absorption of nitrofurantion.Int J Pharm. 1989;56:111–116.
Desai S. A Novel Floating Controlled Release Drug Delivery System Based on a Dried Gel Matrix Network [master's thesis]. 1984 Jamaica, NY, St John's University.
Vantrappen GR, Peeters TL, Janssens J. The secretory component of interdigestive migratory motor complex in man.Scand J Gastroenterol. 1979;14:663–667.
Wilson CG, Washington N. The stomach: its role in oral drug delivery. In: Rubinstein MH, ed.Physiological Pharmacetical: Biological Barriers to Drug Absorption. Chichester, UK: Ellis Horwood; 1989:47–70.
Desai S, Bolton S. A floating controlled release drug delivery system: in vitro- in vivo evaluation.Pharm Res. 1993;10:1321–1325.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention.J Control Release. 2000;63:235–259.
Timmermans J, Andre JM. Factors controlling the buoyancy and gastric retention capabilities of floating matrix capsules: new data for reconsidering the controversy.J Pharm Sci. 1994;83:18–24.
Mojaverian P, Ferguson RK, Vlasses PH, et al. Estimation of gastric residence time of the Heidelberg capsules in humans: effect of varying food composition.Gastroenterology. 1985;89:392–397.
Bechgaard H, Ladefoged K. Distribution of pellets in gastrointestinal tract. The influence on transit time exerted by the density or diameter of pellets.J Pharm Pharmacol. 1978;30:690–692.
Garg S, Sharma S.Gastroretentive drug delivery systems. Business Briefing: Pharmatech 2003 Web Site. 5 th edition. May 2003. Available at: http://www.touchbriefings.com/cdps/cditem.cfm?NID=17&CID=5. Accessed: October 6, 2005.
Timmermans J, Gansbeke VB, Moes AJ. Assessing by gamma scintigraphy the in vivo buoyancy of dosage forms having known size and floating force profiles as a function of time. Vol I.Proceedings of the 5th International Conference on Pharmacy Technology. Paris, France APGI. 1989, 42–51.
Yang L, Fassihi R. Zero order release kinetics from self correcting floatable configuration drug delivery system.J Pharm Sci. 1996;85:170–173.
Burns SJ, Attwood D, Barnwell SG. Assessment of a dissolution vessel designed for use with floating and erodible dosage forms.Int J Pharm. 1998;160:213–218.
Joseph NJ, Laxmi S, Jayakrishnan A. A floating type oral dosage from for piroxicam based on hollow microspheres: in vitro and in vivo evaluation in rabbits.J Control Release. 2002;79:71–79.
Sheth PR, Tossounian JL. Sustained release pharmaceutical capsules. US patent 4,126,672. November 21, 1978.
Soppimath KS, Kulkarni AR, Rudzinski WE, Aminabhavi TM. Microspheres as floating drug delivery system to increase the gastric residence of drugs.Drug Metab Rev. 2001;33:149–160.
Ichikawa M, Watanabe S, Miyake Y. A new multiple unit oral floating dosage system. I: Preparation and in vitro evaluation of floating and sustained-release kinetics.J Pharm Sci. 1991;80:1062–1066.
Ichikawa M, Watanabe S, Miyake Y. Granule remaining in stomach. US patent 4 844 905. July 4, 1989.
Yang L, Esharghi J, Fassihi R. A new intra gastric delivery system for the treatment of helicobacter pylori associated gastric ulcers: in vitro evaluation.J Control Release. 1999;57:215–222.
Ozdemir N, Ordu S, Ozkan Y. Studies of floating dosage forms of furosemide: in vitro and in vivo evaluation of bilayer tablet formulation.Drug Dev Ind Pharm. 2000;26:857–866.
Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery: effects of CO2 gas forming agents.Int J Pharm. 2002;239:81–91.
Li S, Lin S, Daggy BP, Mirchandani HL, Chien TW. Effect of formulation variables on the floating properties of gastric floating drug delivery system.Drug Dev Ind Pharm. 2002;28:783–793.
Li S, Lim S, Chien TW, Daggy BP, Mirchandani HL. Statistical optimization of gastric floating system for oral controlled delivery of calcium.AAPS PharmSciTech. 2001;2:E1.
Penners G, Lustig K, Jorg PVG. Expandable pharmaceutical forms. US patent 5 651 985. July 29, 1997.
Fassihi R, Yang L. Controlled release drug delivery systems. US patent 5 783 212. July 21, 1998.
Talwar N, Sen H, Staniforth JN. Orally administered controlled drug delivery system providing temporal and spatial control. US patent 6 261 601. July 17, 2001.
Michaels AS, Bashwa JD, Zaffaroni A. Integrated device for administering beneficial drug at programmed rate. US patent 3 901 232. August 26, 1975.
Michaels AS. Drug delivery device with self actuated mechanism for retaining device in selected area. US patent 3 786 813. January 22, 1974.
Baumgartner S, Kristel J, Vreer F, Vodopivec P, Zorko B. Optimisation of floating matrix tablets and evaluation of their gastric residence time.Int J Pharm. 2000;195:125–135.
Moursy NM, Afifi NN, Ghorab DM, El-Saharty Y. Formulation and evaluation of sustained release floating capsules of Nicardipine hydrochloride.Pharmazie. 2003;58:38–43.
Atyabi F, Sharma HL, Mohammed HAH, Fell JT. In vivo evaluation of a novel gastro retentive formulation based on ion exchange resins.J Control Release. 1996;42:105–113.
Thanoo BC, Sunny MC, Jayakrishnan A. Oral sustained release drug delivery systems using polycarbonate microspheres capable of floating on the gastric fluids.J Pharm Pharmacol. 1993;45:21–24.
Nur AO, Zhang JS. Captopril floating and/or bioadhesive tablets: design and release kinetics.Drug Dev Ind Pharm. 2000;26:965–969.
Bulgarelli E, Forni F, Bernabei MT. Effect of matrix composition and process conditions on casein gelatin beads floating properties.Int J Pharm. 2000;198:157–165.
Whitehead L, Collett JH, Fell JT. Amoxycillin release from a floating dosage form based on alginates.Int J Pharm. 2000;210:45–49.
Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: effect of formulation and processing parameters on drug release.Eur J Pharm Sci. 2003;18:37–45.
Asmussen B, Cremer K, Hoffmann HR, Ludwig K, Roreger M. Expandable gastroretentive therapeutic system with controlled active substance release in gastrointestinal tract. US patent 6 290 989. September 18, 2001.
El-Kamel AH, Sokar MS, Al Gamal SS, Naggar VF. Preparation and evaluation of ketoprofen floating oral drug delivery system.Int J Pharm. 2001;220:13–21.
Illum L; Ping H. Gastroretentive controlled release microspheres for improved drug delivery. US patent 6 207 197. March 27, 2001.
Streubel A, Siepmann J, Bodmeier R. Floating microparticles based on low density foam powder.Int J Pharm. 2002;241:279–292.
Sheth PR, Tossounian JL. Novel sustained release tablet formulations. 4 167 558. September 11, 1979.
Ushomaru K, Nakachimi K, Saito H. Pharmaceutical preparations and a method of manufacturing them. US patent 4 702 918. October 27, 1987.
Bolton S, Desai S. Floating sustained release therapeutic compositions. US patent 4 814 179. March 21, 1989.
Kawashima Y, Niwa T, Takeuchi H, Hino T, Ito Y. Preparation of multiple unit hollow microspheres (microballoons) with acrylic resins containing tranilast and their drug release characteristics (in vivo).J Control Release. 1991;16:279–290.
Dennis A, Timminis P, Lel K. Buoyant controlled release powder formulation. US patent 5 169 638. December 8, 1992.
Spickett RGW, Vidal JLF, Escoi JC. Antacid preparation having prolonged gastric residence. US patent 5,288,506. February 22, 1993.
Franz MR, Oth MP. Sustained release, bilayer buoyant dosage form. US patent 5 232 704. August 3, 1993.
Wu W, Zhou Q, Zhang HB, Ma GD, Fu CD. Studies on nimodipine sustained release tablet capable of floating on gastric fluids with prolonged gastric resident time.Yao Xue Xue Bao. 1997;32:786–790.
Wong PSL, Dong LC, Edgren DE, Theeuwes F. Prolonged release active agent dosage form adapted for gastric retention. US patent 6 120 803. September 19, 2000.
Mitra SB. Sustained release oral medicinal delivery device. US patent 4 451 260. May 29, 1984.
Harrigan BM. Drug delivery device for preventing contact of undissolved drug with the stomach lining. US patent 4 055 178. October 25, 1977.
Erni W, Held K. The hydrodynamically balanced system: a novel principle of controlled drug release.Eur Neurol. 1987;27:215–275.
Sheth PR, Tossounian J. The hydrodynamically balanced systems (HBS): a novel drug delivery system for oral use.Drug Dev Ind Pharm. 1984;10:313–339.
Degtiareva H, Bogdanov A, Kahtib Z, etal.. The use of third generation antacid preparations for the treatment of patients with nonulcerous dyspeosia and peptic ulcer complicated by reflux esophagus [in Chinese].Liakrs' ka sprava. 1994;5–6:119–122.
Fabregas JL, Claramunt J, Cucala J, Pous R, Siles A. In vitro testing of an antacid formulation with prolonged gastric residence time (Almagate flot coat).Drug Dev Ind Pharm. 1994;20:1199–1212.
Washington N, Washington C, Wilson CG, Davis SS. What is liquid Graviscon? A comparison of four international formulations.Int J Pharm. 1986;34:105–109.
Katayama H, Nishimura T, Ochi S, Tsuruta Y, Yamazaki Y. Sustained release liquid preparation using sodium alginate for eradication ofHelicobacter pylori.Biol Pharm Bull. 1999;22:55–60.
Yuasa H, Takashima Y, Kanaya Y. Studies on the development of intragastric floating and sustained release preparation. 1. Application of calcium silicate as floating carrier.Chem Pharm Bull (Tokyo). 1996;44:1361–1366.
Kohri N, Naasani I, Iseki K. Improving the oral bioavailability of sulphiride by a gastric retained form in rabbits.J Pharm Pharmacol. 1995;48:371–374.
Hilton AK, Deasy PB. In vitro and in vivo evaluation of an oral sustained release floating dosage form of amoxycillin trihydrate.Int J Pharm. 1992;86:79–88.
Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y. Hollow micropheres for use as a floating controlled drug delivery system in stomach.J Pharm Sci. 1992;81:135–140.
Mazer N, Abhisch E, Gfeller JC, etal.. Intragastric behaviour and absorption kinetics of a normal and floating modified release capsules of isardipine under fasted and fed conditions.J Pharm Sci. 1988; 77:647–657.
Hashim H, Li WPA. Improving the release characteristics of water soluble drugs from hydrophilic sustained release matrices b in situ gas generation.Int J Pharm. 1987;35:201–209.
Chen GL, Hao WH. In vitro performance of floating sustained release capsules of verapamil.Drug Dev Ind Pharm. 1998;24:1067–1072.
Ichikawa M, Watanabe S, Miyake Y. A new multiple-unit oral floating dosage system. II: In vivo evaluation of floating and sustained-release characteristics with para amino benzoic acid and iso sorbide di nitrate as model drugs.J Pharm Sci. 1991;80:1153–1156.
Cheuh HR, Zia H, Rhodes CT. Optimization of Sotalol floating and bioadhesive extended release tablet formulation.Drug Dev Ind Pharm. 1995;21:1725–1747.
USP 28 NF 23. Rockville, MD: US Pharmacopeia; 2005:2413.
Pillay V, Fassihi R. Evaluation and comparision of dissolution data derived from different modified release dosage forms: an alternative method.J Control Release. 1998;55:45–55.
Kawashima Y, Niwa T, Takeuchi H, Hino T, Ito Y. Hollow microspheres for use as floating controlled drug delivery system in stomach.J Pharm Sci. 1992;81:135–140.
Sakuma S, Sudo R, Suzuki N, Kikuchi H, Akashi M, Hayashi M. Mucoadhesion of polystyrene nanoparticles having surface hydrophilic polymeric chains in gastrointestinal tract.Int J Pharm. 1999;177:161–172.
Babu VBM, Khar RK. In vitro and In vivo studies of sustained release floating dosage forms containing salbutamol sulphate.Pharmazie. 1990;45:268–270.
Chen J, Blevins WE, Park H, Park K. Gastric retention properties of superporous hydrogel composites.J Control Release. 2000;64:39–51.
Menon A, Ritschel WA, Sakr A. Development and evaluation of a monolithic floating dosage form for furosemide.J Pharm Sci. 1994; 83:239–245.
Whitehead L, Fell JT, Collett JH, Sharma HL, Smith A. In vivo study demonstrating prolonged gastric retention.J Control Release. 1998;55:3–12.
Oth M, Franz M, Timmermans J, Moes A. The bilayer floating capsule: a stomach directed drug delivery system for misoprostal.Pharm Res. 1992;9:298–302.
Miyazaki S, Yamaguchi H, Yokouchi C, Takada M, Huo WM. Sustained release and intra gastric floating granules of indomethacin using chitosan in rabbits.Chem Pharm Bull (Tokyo). 1988;36: 4033–4038.
Malcolm SL, Allen JG, Bird H, etal.. Single dose pharmacokinetics of Madopar HBS in volunteers.Eur Neurol. 1987;27:28S-35S.
Rouge N, Allémann E, Gex-Fabry M, et al. Comparative pharmacokinetic study of a floating multiple unit capsule, a high density multiple unit capsule and an immediate release tablet containing 25 mg atenolol.Pharm Acta Helv. 1998;73:81–87.
Crevoisier C, Hoevels B, Zurcher G, Da Prada M. Bioavailability of L-dopa after Madopar HBS administration in healthy volunteers.Eur Neurol. 1987;27:36S-46S.
Marion MH, Stochi F, Malcolm SL, Quinn NP, Jenner P, Marsden CD. Single dose studies of a slow release preparation of Levodopa and benserazide (Madopar HBS) in Parkinson's disease.Eur Neurol. 1987;27:54S-58S.
Cook JD, Carriaga M, Kahn SG, Schalch W, Skikne BS. Gastric delivery system for ion supplementation.Lancet. 1990;335:1136–1139.
Blaser MJ. Hypothesis on the pathogenesis and natural history ofHelicobacter pylori induced inflammation.Gastroenterology. 1992; 102:720–727.
Gibaly EI. Development and evaluation of novel floating chitosan microcapsules: comparision with non floating chitosan microspheres.Int J Pharm. 2002;249:39–47.
Sato Y, Kawashima Y. In vitro and in vivo evaluation of riboflavin containing microballoons for a floating controlled drug delivery system in healthy human volunteers.J Control Release. 2003;93: 39–47.
Shimpi S, Chauhan B, Mahadik KR, Paradkar A. Preparation and evaluation of diltiazem hydrochloride-Gelucire 43/01 floating granules prepared by melt granulation.AAPS PharmSciTech. 2004;5: E43.
Dave BS, Amin AF, Patel MM. Gastroretentive drug delivery system of ranitidine hydrochloride: formulation and in vitro evaluation.AAPS PharmSciTech. 2004;5:E34.
Sriamornsak P, Thirawong N, Puttipipatkhachorn S. Morphology and buoyancy of oil-entrapped calcium pectinate gel beads.The AAPS Journal. 2004;6:E24.
Reddy L, Murthy R. Floating dosage systems in drug delivery.Crit Rev Ther Drug Carrier Syst. 2002;19:553–585.
Chitnis V, Malshe VS, Lalla JK. Bioadhesive polymers synthesis, evaluation and application in controlled release tablets.Drug Dev Ind Pharm. 1991;17:879–892.
Rouge N, Leroux JC, Cole ET, Doelker E, Buri P. Prevention of sticking tendency of floating mini tablets filled into hard gelatin capsules.Eur J Pharm Biopharm. 1997;43:165–171.
Phuapradit W. Influence of Tablet Buoyancy on Oral Absorption of Sustained Release Acetaminophen Matrix Tablets [dissertation]. 1989, Jamaica, NY, St John's University.
Phuapradit W, Bolton S. Influence of tablet density on oral absorption of sustained release acetaminophen matrix tablets.Drug Dev Ind Pharm. 1991;17:1097–1107.
Gupta SK. Stability studies of ampicillin floating tablets (Ampiflot) and buffered Ampiflot [master's thesis]. 1987, Jamaica, NY, St John's University.
Machida Y, Inouye K, Tokumura T, Iwata M, Nagai T. Preparation and evaluation of intragastric buoyant preparations.Drug Des Deliv. 1989;4:155–161.
Gu TH, Chen SX, Zhu JB, Song DJ, Guo JZ, Hou JM. Pharmacokinetics and pharmacodynamics of diltiazem floating tablets [in Chinese]Chung Kao Yao Li Hsuesh Pao. 1992;13:527–531.
Watanbe K, Machida Y, Takayama M, Iwta M, Nagai T. Preparation and evaluation of intragastric floating tablets having pH independent buoyancy and sustained release property.Arch Pract Pharm Yakuzaigaku. 1993;53:1–7.
Rouge N, Cole ET, Doelker E, Buri P. Buoyancy and drug release patterns of floating minutesitablets containing piretanide and atenolol as model drugs.Pharm Dev Technol. 1998;3:73–84.
Inouye K, Machida Y, Sannan T, Nagai T. Buoyant sustained release tablets based on chitosan.Drug Des Deliv. 1988;2: 165–175.
Inagni HM, Timmermans J, Moes AJ. Conception and in vivo investigation of peroral sustained release floating dosage forms with enhanced gastrointestinal transit.Int J Pharm. 1987;35:157–164.
Gustafson JH, Weissman L, Weinfeld RE, Holazo AA, Khoo KC, Kalpan SA. Clinical bioavailability evaluation of a controlled release formulation of diazepam.J Pharmacokinet Biopharm. 1981;9:679–691.
Khattar D, Ahuja A, Khar RK. Hydrodynamically balanced systems as sustained release dosage form for Propranalol hydrochloride.Pharmazie. 1990;45:356–358.
Simoni P, Cerre C, Cipolla A, etal.. Bioavailability study of a new sinking, enteric coated ursodeoxycholic acid formulation.Pharmacol Res. 1995;31:115–119.
Jayanthi G, Jayaswal SB, Srivastava AK. Formulation and evaluation of terfenadine microballoons for oral controlled release.Pharmazie. 1995;50:769–770.
Inouye K, Machida Y, Sannan T, Nagai T. Buoyant sustained release tablets based on chitosan.Drug Des Deliv. 1989;4: 55–67.
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Published: October 19, 2005
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Arora, S., Ali, J., Ahuja, A. et al. Floating drug delivery systems: A review. AAPS PharmSciTech 6, 47 (2005). https://doi.org/10.1208/pt060347
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DOI: https://doi.org/10.1208/pt060347