Development of a sustained-release microcapsule for delivery of metoprolol succinate.

Abstract:

:Sustained-release (SR) formulations of metoprolol succinate (MS) may minimize fluctuations in plasma concentration and decrease the resulting adverse events. The aim of the present study was to optimize the loading capacity of microcapsules and the SR of MS. A uniform design method was applied to optimize the formulation of SR microcapsules, composed of ethyl cellulose and polyethylene glycol 6,000, in one step via emulsion-solvent diffusion. In vitro release was studied, and the in vivo bioavailability of MS following dosing with novel microcapsules was compared with a commercially available MS formulation in beagle dogs. The present methodology achieved an entrapment efficiency of 83.2%, with 96.1% of drug released in vitro in 18 h, and the release was close to linear over a 12-h period. Pharmacokinetic studies of MS microcapsules in beagle dogs demonstrated a superior SR profile compared with conventional SR tablets. MS microcapsules were developed with high encapsulation efficiency, which had desirable SR properties in vitro and in vivo.

journal_name

Exp Ther Med

authors

Song L,He S,Ping Q

doi

10.3892/etm.2017.4247

subject

Has Abstract

pub_date

2017-05-01 00:00:00

pages

2435-2441

issue

5

eissn

1792-0981

issn

1792-1015

pii

ETM-0-0-4247

journal_volume

13

pub_type

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