Eudragit L/HPMCAS Blend Enteric-Coated Lansoprazole Pellets: Enhanced Drug Stability and Oral Bioavailability

Abstract

Abstract. The objectives of the present work were to use blends of Eudragit L and hydroxypropyl methylcellulose acetate succinate (HPMCAS) as enteric film coatings for lansoprazole (LSP) pellets. The entericcoated pellets were prepared with a fluid-bed coater. The influence of the blend ratio, type of plasticizer, plasticizer level, coating level, and curing conditions on gastric stability in vitro drug release and drug stability was evaluated. Furthermore, the bioavailability of the blend-coated pellets in beagle dogs was also performed. The blend-coated pellets exhibited significant improvement of gastric stability and drug stability compared to the pure polymer-coated pellets. Moreover, the AUC values of blend-coated pellets were greater than that of the pure polymer-coated pellets. It was concluded that the using blends of Eudragit L and HPMCAS as enteric film coatings for LSP pellets improved the drug stability and oral bioavailability.

The Influence of HPC-L and Eudragit L30 D-55 on Delayed Release Omeprazole Magnesium Multiple-Unit Pellet System

“…The gastric stability and drug release of uncoated pellets were very poor, demonstrating that all of the drugs were degraded when pellets were immersed in acid medium for 10 min. Fang et al are observed that the pellets were coated with film-forming agents, and the films of coated pellets were excellent without damage in acidic medium and had better stability in neutral/alkaline medium and improved oral bioavailability of the drug [3,32,33]. The drug-loaded pellets were coated with hypromellose as a filmforming agent [20] and HPC-L as a binder or disintegrant in the powder layering process on spherical cores to fabricate round spheres and rapid dissolution [6,19].…”

“…Whereas, the formulations F5, F6, and F7 contain super disintegrant HPC-L which has fasten the release of drug from the formulations. An increased coating level led to an amplified extent of diffusion pathways and increasing duration of the drug to diffuse through the coating membrane [3].…”

“…The polymer at lower pH and the carboxyl groups are not ionized and render them insoluble ` [21,22]. At higher pH (≥5), the carboxylic groups became ionized, causing polymer to dissolve and specifically drug delivered in intestinal site [3][4][5]. Hence, formulation F8 shows 100% drug release in 30 min due to efficient amount of Eudragit and disintegrant.…”

“…Among the polymers, Eudragit L 30D was the most widely used anionic copolymer in pharma industry. It is easily redispersed into water with the assistance of small amounts of organic base, resulting in redispersed latex at pH 2-3, and ionized at pH ≥5 [3][4][5]. Low-substituted hydroxypropyl cellulose (L-HPC) was used as a binder and disintegrant in the powder layering process on spherical cores and to prepare pellets.…”

“…It belongs to BCS class II drugs, which has poor solubility and high permeability. The dissolution problems of poorly water-soluble drugs have been largely solved to improve drug absorption and bioavailability using pelletization technique [3]. Pelletization technique is a unique and economical approach to overcome drug problems such as poor bioavailability that is related with the delivery of hydrophobic drugs, including those that are poorly soluble in aqueous as well as organic media [7].…”