Determination of the release mechanism of Theophylline from pellets coated with Surelease (R)-A water dispersion of ethyl cellulose
Artikel i vetenskaplig tidskrift, 2017

The aim of this study was to investigate the water transport over free standing films based on the aqueous ethyl cellulose (EC) coating Surelease (R) and the drug (Theophylline) release mechanism from coated pellets. It was found that the main drug release rate from pellets was controlled by a diffusion mechanism. However, the drug release rate was altered by addition of sodium chloride to the external release medium. A decrease in the drug release rate when sodium chloride is added to the release medium has traditionally been used to indicate an osmotic drug release mechanism. However, our findings that the release rate decreased by sodium chloride addition could be explained by sodium chloride diffusing through the coating layer into the inner parts of the pellets, decreasing the solubility of Theophylline. This gave a reduced drug concentration gradient over the coating layer and thus a slower release rate. Furthermore, this study shows, as expected, that the transport of water through Surelease (R) films into the pellets was faster than the transport out of Theophylline (approx. seven times), which was the reason why the pellets were swelling during the release. It was also shown that the drug release rate, determined for both whole dose release and for single pellets, decreased with increasing thickness (from 16 to 51 mm) of the coating layer controlling the drug release rate.

Polymer-Films

Plasticizers

Molecular-Weight

Coated pellets

Controlled drug release

Aqueous based coating

Permeability

Surelease (R)

Delivery

Ethylcellulose

Ethyl cellulose

Colon

Film Coatings

Stability

Författare

Jurgita Kazlauske

SuMo Biomaterials

Chalmers, Kemi och kemiteknik, Tillämpad kemi, Farmaceutisk teknologi

M. M. Cafaro

Universita degli Studi di Salerno

D. Caccavo

Universita degli Studi di Salerno

M. Marucci

AstraZeneca AB

G. Lamberti

Universita degli Studi di Salerno

A. A. Barba

Universita degli Studi di Salerno

Anette Larsson

Chalmers, Kemi och kemiteknik, Tillämpad kemi, Farmaceutisk teknologi

SuMo Biomaterials

International Journal of Pharmaceutics

0378-5173 (ISSN)

Vol. 528 1-2 345-353

Ämneskategorier

Läkemedelskemi

DOI

10.1016/j.ijpharm.2017.05.073