Enhancement of Drugs Bioavailability by Floating Drug Delivery System – A Review

Vairappan Kamalakkannan, Ayarivan Puratchikody, Viswanadhan Vasantha Prasanth, Krishnamoorthi Masilamani

Abstract


Gastric emptying is a complex process and one of the most important obstacles in the better absorption and enhances bioavailability of oral drug delivery system. In recent years various scientific and technological advancements have been made in the research and development of oral drug delivery systems to overcoming physiological adversities, such as short gastric residence times (GRT) and unpredictable gastric emptying time (GET). In order to avoid such adversities, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hour via floating drug delivery system. Floating delivery systems or hydro dynamically controlled systems are low density systems that have sufficient buoyancy to float over the gastric content and remain buoyant in the stomach. The recent development of these systems includes their physiological and formulation variables affecting the gastric retention and to design the single and multiple-unit floating systems and their formulation, evaluation aspects are covered in detail. This article aims at reviewing the numerous techniques that has been designed till date for optimizing floating drug delivery system (FDDS), and also summarize the evaluation of FDDS of tablet dosage forms.


Keywords


Gastro retentive systems, effervescent systems, non effervescent systems, gastric residence time, floating drug delivery systems, buoyancy.

Full Text:

PDF

References


Arora S, Ahuja A. Floating drug delivery system: A Review. J. AAPS Pharm Sci Tech 2005; Vol.6 (03): 372-390.

Babu VBM, Khar RK. In vitro and In vivo studies of sustained release floating dosage forms containing salbutamol sulphate. Pharmazie 1990; 45: 268-270.

Baumgartner S, Kristl J, Vrecer F. Optimization of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000; 195: 125-135.

Bolton S, Desai S. US Patent, 4 814, 179, March 21, 1989.

Bolton S, Izevbehai PH, Desai S. Floating sustained release therapeutic compositions, US Patent 4 814, 178. March 21, 1989.

Cargill R, Cadwell LJ, Engle K, Fix JA, Porter PA, Gardner CR. Controlled gastric emptying: I. Effects of physical properties on gastric residence times of non disintegrating geometric shapes in beagle dogs. Pharm Res 1988; 5: 533-536.

Chawla G, Gupta P, Koradia V, Bansal AK. Gastroretention: A Means to address regional variability in intestinal drug absorption. Pharm Tech 2003; 27: 250-268.

Cheuh HR, Zia H, Rhodes CT. Optimization of sotalol floating and bioadhesive

extended release tablet formulations. Drug Dev and Ind Pharm 1995; 21: 1725-1747.

Chien YM. Novel drug delivery system, 3rd Ed. Vol. 1. New York: Marcel Dekker 1992; 139-196.

C.K. Kokate, A.P. Purohit & S.B. Gokhale. Pharmacognosy. Nirali Prakashan, 27th Edition 2004; 190.

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.

Degen LP, Peng F, Collet A, Rossi L, Ketterer S, Serrano Y, et al. Blockade of GRP receptors inhibits gastric emptying and gallbladder contraction but accelerates small intestinal transit. Gastroenterology 2001; 120:361-8.

Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled-release system for gastric retention. Pharm Res 1997; 14:815-819.

Deshpande AA, Rhodes CT, Shah NH, Malick AW. Controlled-release drug delivery systems for prolonged gastric residence: An overview. Drug Dev and Ind Pharm 1996; 22:631-9.

El-Kamel AH, Sokar MS, Algamal SS, Naggar VF. Preparation and evaluation of ketoprofen floating oral delivery system. Int J Pharm 2001; 220: 13-21.

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.

Gaba Punam, Gaba Monica, Garg Rajeev, Gupta GD. Available at http://www.pharmainfo.net/reviews/floating-microspheres review, 2008.

Garg Sanjay, Sharma Shringi. Business Briefing. Pharmtech 2003; 160-166.

Garima C, Piyush G, Vishal K and Arvind KB. Gastroretention: A Means to Address Regional Variability in intestinal drug Absorption. Pharma Tech 2003; 27: 50-68.

Gergogiannis YS, Rekkas DM, Dallos PP, Chailis NH. Floating and swelling characteristics of various excipients used in controlled release technology. Drug Dev and Ind Pharm 1993; 19: 1061-1081.

Greminger JK, Krumer K. Alkyl and Hydroxyalkyl cellulose. In Davidson, RL, editor. Handbook of Water Soluble Gums and Resins, New York: McGraw Hill Book Co 1980; 3-25.

Groning R, Heun G. Dosage forms with controlled gastrointestinal passage-studies on the absorption of nitrofurantion. Int J Pharm 1989; 56:111-116.

Groning R, Heun G. Oral dosage forms with controlled gastrointestinal transit. Drug Dev and Ind Pharm 1984; 10:527-539.

Gu TH, Chen SX, Zhu JB, Song DJ, Guo JZ, Hou JM. Pharmacokinetics and pharmacodynamics of diltiazem floating tablets. Chung Kao Yao Li Hsuesh Pao 1992; 13: 527-531.

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.

Hetal N Kikani. A Thesis on Floating Drug Delivery System. The North Gujarat University, Patan 2000-2001; 11-12.

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.

Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carrier Syst 1998;15:243-83.

Iannucelli V, Coppi G, Bernabei MT, Camerorni R. Air compertment multiple-unit system for prolonged gastric residence. Part-I. Formulation study. Int J Pharm 1998; 174:4754.

Ichikawa M, Kato T, Kawahara M, Watanabe S, Kayano M. A new multiple-unit oral floating dosage system. II: in vivo evaluation of floating and sustained-release characteristics with p-aminobenzoic acid and isosorbide dinitrate as model drugs. J Pharm Sci 1991; 80:1153-1156.

Jain NK. Progress in Controlled and Novel Drug Delivery Systems, 1st Ed. CBS Publishers and Distributors, New Delhi 2004; 84-85.

Jayanthi G, Jayaswal SB, Srivastava AK. Formulation and evaluation of terfenadine micro balloons for oral controlled release Pharmazie 1995; 50: 769-770.

Kawashima Y, Nima T, Takeuchi H, Hino T, Itoh Y. Hollow microspheres for use as a floating controlled drug delivery system in the stomach. J Pharm Sci (USA) 1998; 81: 135-140.

Kawashima Y, Niwa T, Takeuchi H, Hino, Ito Y. Preparation of multiple unit hollow microspheres (microballoons) with acrylic resin containing tranilast and their drug release characteristics (in vitro) and floating behavior (in vivo) . J Cont Rel 1991; 16: 279-290.

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 Rel 1999; 58: 195-205.

Kydoneius A. Controlled Release Technologies. 2nd Ed. New York: Marcel Dekker; 1991; 24-109.

Lenaerts VM, Gurny R. Gastrointestinal Tract- Physiological variables affecting the performance of oral sustained release dosage forms. Bioadhesive Drug Delivery System. Boca Raton, FL: CRC Press; 1990.

Li VHK, Robinson JR, Lee VHL. Influence of drug properties and routes of administration on the design of sustained and controlled release systems. In Robinson JR, Lee BV, editors Controlled Drug Delivery: Fundamentals and Applications. New York: Marcel Dekker 1987; 3-21.

Libermann, Lachman, Schwartz. Pharmaceutical dosage forms-Tablets volume1, volume 2, volume 3: 131-158.

Mamajek RC, Moyer ES, inventors. Drug dispensing device and method. US Patent 4 207 890. June 17, 1980.

Mathur P, Saroha Kamal. Floating drug delivery system: An Innovative acceptable approach in gastroretentive drug delivery. Scholar Research Library 2010; 2: 257-270.

Mayavanshi AV and Gajjar SS. Floating drug delivery systems to increase gastric retention of drugs: A Review. Research Journal of Pharmacy and Technology 2008; 4: 345-348.

Mojaverian P, Vlasses PH, Kellner PE, Rocci ML. Effects of gender, posture, and age on gastric residence time of indigestible solid: pharmaceutical considerations. Pharm Res 1988; 10: 639-664.

Muller-Lissner SA, Blum AL. The effect of specific gravity and eating on gastric emptying of slow-release capsules. New Engl J Med 1981; 304: 1365-1366.

N R Jimenez-Castellanos, H Zia and C T Rhodes. Mucoadhesive Drug Delivery Systems. Drug Dev and Ind Pharmacy 1993; 19: 143.

Nayak AK, Maji R and Das B. Gastroretentive drug delivery systems: a review. Asian Journal of Pharmaceutical and Clinical Research 2001; 31: 9.

Palin KJ. Lipids and oral drug delivery. Pharm Int 1985: 11: 272-279.

Patel GM, Floating drug delivery system: An innovative approach to prolong gastric retention. www.pharmainfo.net, 2007.

Petrakis IE, Kogerakis N, Vrachassotakis N, Stiakakis I, Zacharioudakis G, Chalkiadakis G. Hyperglycemia attenuate erythromycin-induced acceleration of solid-phase gastric emptying in healthy subjects. Abdom Imaging 2002; 27:309-14.

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.

Prabahakara Prabhu et.al. Indian journal of pharmaceutical education and research 2008; 193.

Rajendra Jangde et.al. The Pharmaceutical Magazine. March, 2008: 1-3.

Rednick AB, Tucker SJ, inventors. Sustained release bolus for animal husbandry. US patent 3 507 952. April 22, 1970.

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.

Rubinstein A, Friend DR. Specific delivery to the gastrointestinal tract, in: A.J. Domb (Ed.), Polymeric Site-Specific Pharmacotherapy, Wiley, Chichester 1994; 282–283.

Sangekar S. Evaluation of effect of food and specific gravity of the tablets on gastric retention time. International Journal of Pharmaceutics 1987; 35(3): 34-53.

Shah SH, Patel JK, Patel NV. Stomach specific floating drug delivery system: A review. Int J Pharm Res 2009; 1(3): 623-633.

Sheth PR and Tossounian JL. The Hydrodynamically Balanced System: A Novel Drug Delivery System for Oral Use. Drug Dev and Ind Pharm 1984; 10 (2): 313-339.

Sheth PR, Tossounian JL, Sustained release tablet formulations. US Patent 4 140, 755. February 20, 1979.

Silang R, Regalado M, Cheng TH, Wesson DE. Prokinetic agents increase plasma albumin in hypoalbuminemic chronic dialysis patients with delayed gastric emptying. Am J Kidney Dis 2001; 37:287-93.

Simoni P, Cerre C, Cipolla A, et al. Bioavailability study of a new sinking, enteric coated ursodeoxycholic acid formulation. Pharmacol Res 1995; 31:115–119.

Singh BN and Kim KH. Floating Drug Delivery Systems: An Approach to Oral Controlled Drug Delivery via Gastric Retention. J. Controlled Release 2000; 63 (1-2): 235-259.

Streubel A, Siepmann J, Bodmeier R. Multiple-unit Gastroretentive drug delivery: a new preparation method for low density microparticles. J Microencapsul 2003; 20: 329 – 47.

Talukder R and Fissihi R. Gastroretentive Delivery Systems: A Mini review. Drug Dev and Ind Pharm 2004; 30: 1019-1028.

Timmermans J and Moes A J. Measuring the resulting weight of an immersed tests material II: Examples of kinetic determination applied for monolithic dosage forms Acta Pharma Tech 1990; 36: 176-180.

Urguhart J, Theeuwes F, inventors. Drug delivery system comprising a reservoir containing a plurality of tiny pills. US patent 4 434 153. February 28, 1994.

Whitehead L, Fell JT, Collett JH. Development of a gastroretentive dosage form. Eur J Pharm Sci 1996; 4: S182.

Xu W L, Tu X D and Lu Z D. Development of Gentamycin sulfate sustained-release tablets remaining-floating in stomach. Yao Hsueh Pao 1991; 26: 541-545.

Yang L, Eshraghi J, Fassihi R. A new intragastric delivery system for the treatment of Helicobacter pyloriassociated gastric ulcer: in vitro evaluation. J. Control. Release 1999; 57: 215–222.

Yyas SP and Roop KK. Controlled Drug Delivery Concepts and Advances. 1st Ed. New Delhi 2002; 196-217.


Refbacks

  • There are currently no refbacks.




Copyright (c)

               AR Journals

18K, Street 1st, Gaytri Vihar, Pinto Park, Gwalior, M.P. India

Copyright@arjournals.org (Design) 2009-2021

 

Follow @arjournals on Twitter