Abstract
Effervescent multiple-unit floating drug delivery systems (muFDDSs) consisting of drug (lorsartan)- and effervescent (sodium bicarbonate)-containing pellets were characterized in this study. The mechanical properties (stress and strain at rupture, Young’s modulus, and toughness) of these plasticized polymeric films of acrylic (Eudragit RS, RL, and NE) and cellulosic materials (ethyl cellulose (EC), and Surelease) were examined by a dynamic mechanical analyzer. Results demonstrated that polymeric films prepared from Surelease and EC were brittle with less elongation compared to acrylic films. Eudragit NE films were very flexible in both the dry and wet states. Because plasticizer leached from polymeric films during exposure to the aqueous medium, plasticization of wet Eudragit RS and RL films with 15% triethyl citrate (TEC) or diethyl phthalate (DEP) resulted in less elongation. DEP might be the plasticizer of choice among the plasticizers examined in this study for Eudragit RL to provide muFDDSs with a short time for all pellets to float (TPF) and a longer period of floating. Eudragit RL and RS at a 1∶1 ratio plasticized with 15% DEP were optimally selected as the coating membrane for the floating system. Although the release of losartan from the pellets was still too fast as a result of losartan being freely soluble in water, muFDDSs coated with Eudragit RL and RS at a 1∶1 ratio might have potential use for the sustained release of water-insoluble or the un-ionized form of drugs from gastroretentive drug delivery systems.
Highlights
Based on recently published literature and patents applied for, gastroretentive drug delivery systems (DDSs, GRDDSs) that are retained in the stomach for a prolonged and predictable period of time are one of the advanced approaches for novel drug-delivery systems [1,2]
GRDDSs are appropriate for drugs with a narrow absorption window [3,4,5], drugs that act locally in a part of the gastrointestinal (GI) tract (GIT) such as antibiotic administration for Helicobacter pylori eradication to treat peptic ulcers [6,7,8], drugs which are unstable in intestinal fluids [3,9,10], and drugs that exhibit poor solubility in the intestinal tract [11,12]
Plasticized polymeric coating films for achieving rapid floating and a longer period of floating in a sustained-release manner were characterized for the effervescent multiple-unit floating drug delivery systems (muFDDSs) developed in the present study
Summary
Based on recently published literature and patents applied for, gastroretentive drug delivery systems (DDSs, GRDDSs) that are retained in the stomach for a prolonged and predictable period of time are one of the advanced approaches for novel drug-delivery systems [1,2]. The development of various approaches for GRDDSs, including low-density systems/floating systems, high-density systems/nonfloating systems, mucoadhesive or bioadhesive systems, expansion systems, magnetic systems, supraporous hydrogels, and raftforming systems, was reviewed [13,14]. Low-density systems or floating DDSs (FDDSs) are further divided into non-effervescent and effervescent systems based on the mechanism of buoyancy. If their bulk density is lower than that of gastric fluid, and they remain buoyant in the stomach for a prolonged period. From formulation and technological points of view, FDDSs are considerably easy and a logical approach for developing GRDDSs
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