Design and characterization of hollow/porous floating beads of captopril for pulsatile drug delivery

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Anand Panchakshari Gadad
Annapureddy Dasaratharami Reddy
Panchaxari Mallappa Dandagi
Vinayak S Masthiholimath


The present study was aimed to design and characterize hallow/ porous floating beads of captopril for pulsatile drug delivery for the treatment of hypertension. Captopril, an antihypertensive agent, is one of the most commonly prescribed
drugs for the treatment of patients with hypertension and congestive heart failure.The floating pulsatile concept was applied to increase the gastric residence of the dosage form, having lag phase followed by a burst release.To overcome the limitations of the various approaches for imparting buoyancy, hollow/porous beads were prepared. A preliminary study was done for selection of the polymer (low methoxy pectin and gellan gum) combination. Based on the preliminary studies, an optimized concentration of polymers was selected for formulation design with varying the concentration of sodium bicarbonate. The obtained floating beads were studied for physical characterization, in vitro release, in vivo gamma-scintigraphy study and stability study. Formulation F1E floating beads had a porosity of 38.41% and hollow with bulk density <1. The entrapment
efficiency for formulation F1E was 83.10%, and the particle size of the beads was 1.124 mm. The floating beads showed a two-phase release pattern, with initial lag time in acidic medium followed by rapid pulse release in the phosphate buffer
medium with in vitro release of 96.77% for almost 8 h. The in vivo gastric residence of batch F1E was subjected to gamma-scintigraphy imaging on rabbits to determine the retention of drug (beads) for up to 6 h. This approach suggested use of hollow sodium bicarbonate microparticles as promising floating-pulsatile drug delivery systems for site- and time-specific release of antihypertensive drugs.


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Gadad, A. P., Reddy, A. D., Dandagi, P. M., & Masthiholimath, V. S. (2014). Design and characterization of hollow/porous floating beads of captopril for pulsatile drug delivery. Asian Journal of Pharmaceutics (AJP), 6(2).


Mastiholimath VS, Dandagi PM, Jain SS, Gadad AP, Kulkarni AR. Time

and pH dependent colon specific, pulsatile delivery of theophylline for

nocturnal asthma. Int J Pharm. 2007;328:49-56.

Whitehead L, Collett JH, Fell JT. Amoxycillin release from a floating

dosage form based on alginates. Int J Pharm 2000;210:45-9.

Iannuccelli V, Coppi G, Bernabei MT, Cameroni R. Air compartment

multiple-unit system for prolonged gastric residence. Int J Pharm


Sriamornsak P, Nunthanid J. Calcium Pectinate gel beads for controlled

release drug delivery: Effect of formulation and processing variables

on drug release. J Microencapsul 1999;16:303-13.

Bussmer T, Dashevsky A, Bodmeier R. A pulsatile drug delivery system

based on rupturable-coated hard gelatin capsule. J Control Release


Rajnikanth PS, Balasubramanium J, Mishra B. Preparation and in vitro

characterization of Gellan based floating beads of acetohydroxamic

acid for eradication of H. pylori. Acta Pharm 2007;57:413-27.

Dollery C. Therapeutics Drugs. Churchill Livingstone: 1999. p. 38-43.

Dupuis G, Chambin O, Genelot C, Champion D, Pourcelot Y. Colonic

drug delivery influence of cross-linking agent on pectin beads

properties and role of the shell capsule type. Drug Dev Ind Pharm


Pornsak S, Nartaya T, Satit P. Emulsion gel beads of calcium pectinate

capable of floating on the gastric fluid: Effect of some additives,hardening agent or coating on release behavior of metronidazole. Eur

J Pharm Sci 2005;24:363-73.

Gadad AP, Patil MB, Naduvinamani SN, Mastiholimath VS, Dandagi PM,

Kulkarni AR. Sodium alginate polymeric floating beads for the delivery

of cefpodoxime proxetil. J Appl Polym Sci 2009;114:1921-6.

Claire D, Ali A, Brice M, Yann P, Philippe C, Alf L, et al. Zinc-pectinate

beads as an in vivo self-assembling system for pulsatile drug delivery.

Int J Pharm 2011;414:28-34.

Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for

floating drug delivery system: Effects of CO2 gas-forming agents. Int J

Pharm 2002;239:81-91.

Huimin Y, Huijuan Y, Junyi Z, Junlin Y, Lifan Z. Preparation and evaluation of a novel gastric floating alginate/poloxamer inner-porous beads using foam solution. Int J Pharm 2012;4:211-9.

Mastiholimath VS, Dandagi PM, Gadad AP, Mathews R, Kulkarni AR. In vitro and in vivo evaluation of ranitidine hydrochloride ethyl cellulose floating microparticles. J Microencapsul 2008;25:307-14.

Indian Pharmacopoeia. Ghaziabad (India): Indian pharmacopoeia

commission 1996;1:242-3.

Amrutkar PP, Chaudhari PD, Patil SB. Design and in vitro evaluation of multiparticulate floating drug delivery system of zolpidem tartarate.

Colloids Surf B Biointerfaces 2012;89:182-7.