Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2484888 | Journal of Pharmaceutical Sciences | 2012 | 12 Pages |
Abstract
Among various strategies of gastroretentive drug delivery systems (DDSs) developed to prolong the gastric residence time and to increase the overall bioavailability, effervescent multipleâunit floating DDSs (muFDDSs) were studied here. These systems consist of drug (losartan)â and effervescent (sodium bicarbonate)âcontaining pellets coated with a blended polymeric membrane, which was a mixture of gastrointestinal tract (GIT)âsoluble and GITâinsoluble polymers. The addition of GITâsoluble polymers, such as hydroxypropyl methylcellulose, polyethylene glycol (PEG) 6000, PEG 600, and Kollicoat® IR, greatly increased the water uptake ability of the GITâinsoluble polymers (Eudragit® NE, RS, and RL; Surelease®; and Kollicoat® SR) and caused them to immediately initiate the effervescent reaction and float, but the hydrated films should also be impermeable to the generated CO2 to maintain floatation and sufficiently flexible to withstand the pressure of carbon dioxide to avoid rupturing. The study demonstrated that the water uptake ability and mechanical properties could be applied as screening tools during the development of effervescent muFDDSs. The optimized system of SRT(5)P600(5) (i.e., a mixture of 5% Kollicoat® SR and 5% PEG 600) with a 20% coating level began to completely float within 15 min and maintained its buoyancy over a period of 12 h with a sustainedârelease effect.
Keywords
Related Topics
Health Sciences
Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
YingâChen Chen, LinâWen Lee, HsiuâO Ho, Chen Sha, MingâThau Sheu,