A gastro retentive floating drug delivery system with multiple-unit minitab's based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system floated completely within 3 min and maintained the buoyancy over a period of 12 h. The drug release was controlled and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the controlled release properties were achieved in the multiple-unit floating drug delivery system developed in this present study. The analysis of the parameter dissolution data after storage at 40 degrees C and 75% RH for 3 months showed, no significant change indicating the two dissolution profiles were considered to be similar (f2 value is more than 50).
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http://dx.doi.org/10.1208/s12249-008-9090-4 | DOI Listing |
AAPS PharmSciTech
December 2014
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok-Nakhonsawan Road, Phitsanulok, 65000, Thailand.
Tackiness caused by the gas-entrapped membrane (Eudragit(®)RL 30D) was usually observed during storage of the effervescent floating tablets, leading to failure in floatation and sustained release. In this work, common anti-tacking agents (glyceryl monostearate (GMS) and talc) were used to solve this tackiness problem. The impact of anti-tacking agent on the properties of free films and corresponding floating tablets was investigated.
View Article and Find Full Text PDFColloids Surf B Biointerfaces
February 2013
Shri Neminath Jain Brahmacharyashram's, Shriman Sureshdada Jain College of Pharmacy (PG Course), Neminagar, Chandwad, Dist. Nashik 423 101, Maharashtra, India.
The purpose of present research was to develop and optimize sustained release floating pellets of alfuzosin hydrochloride which has narrow absorption window in proximal intestine to improve patient compliance and therapeutic efficacy in the treatment of benign prostatic hyperplasia. The system was designed to provide drug loaded pellets coated with three successive coatings over Celphere(®) (microcrystalline cellulose pellets) - drug layer, effervescent layer (HPMC and sodium bicarbonate) and gas entrapped polymeric membrane (Kollicoat(®) SR 30D). A 3(2) factorial design was employed with HPMC:sodium bicarbonate and Kollicoat(®) SR 30D concentration as independent variables while drug release and floating lag time were the dependent variables.
View Article and Find Full Text PDFInt J Pharm
July 2012
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, China.
The purpose of this research was to develop a novel gastroretentive multiparticulate system with floating ability. This system was designed to provide drug-loaded pellets coated with three successive coatings-the retarding film (ethyl cellulose), the effervescent layer (sodium bicarbonate) and the gas-entrapped polymeric membrane (Eudragit RL 30D). The floating pellets were evaluated for SEM, floating characteristic parameters, in vitro release and bioavailability in New Zealand rabbits.
View Article and Find Full Text PDFJ Young Pharm
October 2010
Department of Pharmaceutics, CARISM, SASTRA University, Thirumalaisamudram, Thanjavur - 613 401, Tamil Nadu, India.
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.
View Article and Find Full Text PDFAAPS PharmSciTech
September 2008
Novel Drug Delivery Systems Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506009, Andhra Pradesh, India.
A gastro retentive floating drug delivery system with multiple-unit minitab's based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the drug. The system consists of the drug-containing core units prepared by direct compression process, which are coated with three successive layers of an inner seal coat, effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an polymethacrylates (Eudragit RL30D, RS30D, and combinations of them). Only the system using Eudragit RL30D and combination of them as a gas-entrapped polymeric membrane could float.
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