Abstract
Blends of aqueous dispersion of a hydrophobic and hydrophilic polymer, namely Surelease®: hydroxypropyl methylcellulose (Surelease®: HPMC E15) were used as coating materials to control the drug release from coated pellets of the highly water soluble drug metoprolol succinate. Varying the polymer blends, ranges of drug release patterns were obtained at pH 6.8. The present study dealt with diffusion of drug through plasticized Surelease®/ hydroxypropyl methylcellulose (HPMC E15) films prepared by coating of drug and polymers onto non-pareil seeds using the solution layering technique. The release of metoprolol succinate from coated pellets was decreased with increased coating load of polymer. The optimized formulation was obtained by 3² full factorial design. The release profile revealed that the optimized formulation follows zero order release kinetics. The stability data showed no interaction for storage at 25ºC and 60% relative humidity.
Highlights
Developing oral sustained release systems for freely water soluble drugs having strong first pass metabolism has always posed a challenge to the pharmaceutical technologist
The polymer is usually used in combination with a secondary polymer such as hydroxypropyl methylcellulose (HPMC E15) which confers the film a more hydrophilic nature and alters its structure by virtue of pores and channels through which the drug substance can diffuse more to control the release properties of a drug formulation (Aulton, Bdul-Razzak, Hogan, 1981)
The present study investigated the coating effect of a combination of Surelease® and HPMC E15 on drug release of highly water soluble metoprolol succinate in a coating pan
Summary
Developing oral sustained release systems for freely water soluble drugs having strong first pass metabolism has always posed a challenge to the pharmaceutical technologist Most of these highly water soluble drugs, if not formulated properly, are released at a high rate and are. Pellets as a drug delivery system offer technological advantages and better flow properties, less friable dosage form, narrow particle size distribution, ease of coating, and uniform packing (Siepmann, Siepmann, Walther, Macrae, Bodmeier, 2005) It has therapeutic advantages such as less irritation of the gastrointestinal tract, a low risk of side effects associated with dose dumping and reduction of the variation in gastric emptying rates (Evdokia, 2000). Sustained release multiparticulate tablets of metoprolol succinate were prepared by the compression technique in which sustained release pellets were mixed with the cushning agent micro-crystalline cellulose (Avicel® PH 102), superdisintegrant Indion 414 and lubricant magnesium stearate
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