Formulation and evaluation of controlled release ethylcellulose and polyethylene glycol microspheres containing metoprolol tartrate.

Autor: Malipeddi VR; Amity Institute of Pharmacy, Amity University , Lucknow, Uttar Pradesh, India., Awasthi R; Laureate Institute of Pharmacy , Kangra, Himachal Pradesh, India., Dua K; School of Pharmacy and Biomedical Sciences, The University of Newcastle , Newcastle, Australia.
Jazyk: angličtina
Zdroj: Interventional medicine & applied science [Interv Med Appl Sci] 2016 Jun 01; Vol. 8 (2), pp. 60-67.
DOI: 10.1556/1646.8.2016.2.6
Abstrakt: Metoprolol tartrate is rapidly absorbed from both gastric and intestinal regions, after oral administration. To retard the release rate of the metoprolol tartrate, microspheres were prepared with varying concentrations of a mixture containing ethylcellulose and polyethylene glycol-6000. The prepared microspheres were evaluated for various physicochemical characteristics and in vitro drug release. The percent yield of microspheres was in the range of 75.2-87.3%. The particle size of microspheres was found to be in the range of 73.2-85.5 μm. Fourier transform-infrared spectral analysis and differential scanning calorimetry concluded the absence of any interaction between the drug and the carriers. The release time profile of metoprolol tartrate from microspheres in 0.1 N hydrochloric acid solution was to the extent of 33.4-60.2%. The complete release of metoprolol tartrate occurred from MPT-3 and MPT-4 in phosphate buffer solution (pH 7.4) within 8 and 7 h, respectively, whereas the incomplete release (72.3%) occurred from MPT-1. Nearly, the complete release (98.5%) of metoprolol occurred from MPT-2 in 10 h. Formulation MPT-2 would be a preferred formulation. The release of metoprolol involves diffusion rate limited ( R 2  = 0.9865) as a mechanism from drug release. The prepared microspheres of metoprolol tartrate eliminate the need for multiple dosing and provide patient compliance.
Databáze: MEDLINE