Floating drug delivery of nevirapine as a gastroretentive system.
A multiple-unit floating drug delivery system based on gas formation technique was developed, in order to prolong the gastric residence time and to increase the overall bioavailability of the dosage form. The floating bead formulations were prepared by dispersing nevirapine together with calcium carbonate in a mixture of sodium alginate and hydroxypropyl methylcellulose solution and then dripping the dispersion into an acidified solution of calcium chloride. Calcium alginate beads were formed, as the alginate underwent ionotropic gelation by calcium ions, and carbon dioxide developed from the reaction of carbonate salts with acid. The obtained beads were able to float due to CO(2)-gas formation and the gas entrapment by the polymeric membrane. The prepared beads were evaluated for percent drug loading, drug entrapment efficiency, morphology, surface topography, buoyancy, in-vitro release, and release kinetics. The formulations were optimized for different weight ratios of the gas-forming agent and sodium alginate. The beads containing higher amounts of calcium carbonate demonstrated an instantaneous, complete, and excellent floating ability over a period of 24 hours. The increased amount of the gas forming agent did not affect the time to float, but increased the drug release from the floating beads, while increasing the coating level of the gas-entrapped membrane, increased the time to float, and slightly retarded the drug release. Good floating properties and sustained drug release were achieved. Finally, these floating beads seemed to be a promising gastroretentive drug delivery system.
Department of Pharmaceutics, CARISM, SASTRA University, Thirumalaisamudram, Thanjavur - 613 401, Tamil Nadu, India.
Hari Bn
HB
Vedha
Reddy A
RA
Brahma
Rani B
RB
Samyuktha
J Biomater Sci Polym Ed. 2003;14(6):581-8
12901439
J Microencapsul. 2003 May-Jun;20(3):329-47
12881114
Int J Pharm. 2006 Nov 6;324(2):136-43
16828997
Pharm Res. 1997 Jun;14(6):815-9
9210203
Int J Pharm. 2002 Jun 4;239(1-2):81-91
12052693
J Pharm Sci. 1991 Nov;80(11):1062-6
1815057
Chem Pharm Bull (Tokyo). 2009 Oct;57(10):1068-75
19801860
AAPS PharmSciTech. 2000 Jul 02;1(3):E19
14727905
Crit Rev Ther Drug Carrier Syst. 1998;15(3):243-84
9699081
Int J Pharm. 2006 Feb 3;308(1-2):14-24
16343829
Eur J Pharm Biopharm. 2000 Sep;50(2):221-6
10962231
Drug Dev Ind Pharm. 2002 Jul;28(6):621-30
12149954
J Control Release. 1999 Mar 29;58(2):195-205
10053192
J Microencapsul. 2005 Feb;22(1):67-80
16019892
Drug Metab Rev. 2001 May;33(2):149-60
11495501
Biol Pharm Bull. 1993 Nov;16(11):1164-8
8312877
Br J Clin Pharmacol. 1985;19 Suppl 2:77S-83S
3890912
Pharm Res. 1993 Jul;10(7):1087-9
8378252
AAPS PharmSciTech. 2007 Jun 22;8(2):Article 48
17625805
AAPS PharmSciTech. 2005 Oct 19;6(3):E372-90
16353995
Adv Drug Deliv Rev. 1998 Dec 1;34(2-3):191-219
10837678
Pharm Res. 1986 Aug;3(4):208-13
24271583